Ma C

References (45)

Title : Evolution-Based Discovery of Polyketide Acylated Valine from a Cytochalasin-Like Gene Cluster in Simplicillium lamelliciola HDN13430 - Wu_2024_J.Nat.Prod__
Author(s) : Wu Z , Wang W , Li J , Ma C , Chen L , Che Q , Zhang G , Zhu T , Li D
Ref : Journal of Natural Products , : , 2024
Abstract : Utilizing a gene evolution-oriented approach for gene cluster mining, a cryptic cytochalasin-like gene cluster (sla) in Antarctic-derived Simplicillium lamelliciola HDN13430 was identified. Compared with the canonical cytochalasin biosynthetic gene clusters (BGCs), the sla gene cluster lacks the key alpha,beta-hydrolase gene. Heterologous expression of the sla gene cluster led to the discovery of a new compound, slamysin (1), characterized by an N-acylated amino acid structure and demonstrating weak anti-Bacillus cereus activity. These findings underscore the potential of genetic evolution in uncovering novel compounds and indicating specific adaptive evolution within specialized habitats.
ESTHER : Wu_2024_J.Nat.Prod__
PubMedSearch : Wu_2024_J.Nat.Prod__
PubMedID: 38447096

Title : ACE2-using merbecoviruses: Further evidence of convergent evolution of ACE2 recognition by NeoCoV and other MERS-CoV related viruses - Xiong_2024_Cell.Insight_3_100145
Author(s) : Xiong Q , Ma C , Liu C , Tong F , Huang M , Yan H
Ref : Cell Insight , 3 :100145 , 2024
Abstract : Angiotensin-converting enzyme 2 (ACE2) was recognized as an entry receptor shared by coronaviruses from Sarbecovirus and Setracovirus subgenera, including three human coronaviruses: SARS-CoV, SARS-CoV-2, and NL63. We recently disclosed that NeoCoV and three other merbecoviruses (PDF-2180, MOW15-22, PnNL 2018B), which are MERS-CoV relatives found in African and European bats, also utilize ACE2 as their functional receptors through unique receptor binding mechanisms. This unexpected receptor usage assumes significance, particularly in light of the prior recognition of Dipeptidyl peptidase-4 (DPP4) as the only known protein receptor for merbecoviruses. In contrast to other ACE2-using coronaviruses, NeoCoV and PDF-2180 engage a distinct and relatively compact binding surface on ACE2, facilitated by protein-glycan interactions, which is demonstrated by the Cryo-EM structures of the receptor binding domains (RBDs) of these viruses in complex with a bat ACE2 orthologue. These findings further support the hypothesis that phylogenetically distant coronaviruses, characterized by distinct RBD structures, can independently evolve to acquire ACE2 affinity during inter-species transmission and adaptive evolution. To date, these viruses have exhibited limited efficiency in entering human cells, although single mutations like T510F in NeoCoV can overcome the incompatibility with human ACE2. In this review, we present a comprehensive overview of ACE2-using merbecoviruses, summarize our current knowledge regarding receptor usage and host tropism determination, and deliberate on potential strategies for prevention and intervention, with the goal of mitigating potential future outbreaks caused by spillover of these viruses.
ESTHER : Xiong_2024_Cell.Insight_3_100145
PubMedSearch : Xiong_2024_Cell.Insight_3_100145
PubMedID: 38476250

Title : Corrigendum to Design, synthesis and biological evaluation of carbamate derivatives incorporating multifunctional carrier scaffolds as pseudo-irreversible cholinesterase inhibitors for the treatment of Alzheimer's disease [Eur. J. Med. Chem. 265 (2024) 116071] -
Author(s) : Liu Y , Ma C , Li Y , Li M , Cui T , Zhao X , Li Z , Jia H , Wang H , Xiu X , Hu D , Zhang R , Wang N , Liu P , Yang H , Cheng M
Ref : Eur Journal of Medicinal Chemistry , :116169 , 2024
PubMedID: 38290915

Title : A main chain biodegradable polyurethane with anti-protein adsorption and anti-bacterial adhesion performances - Cao_2023_Soft.Matter__
Author(s) : Cao Z , Ma C , Xiang L , Cao L
Ref : Soft Matter , : , 2023
Abstract : Biofilms are initially formed by substances such as proteins secreted by bacteria adhering to a surface. To achieve a durable antibacterial material, biodegradable dihydroxyl-terminated poly[(ethylene oxide)-co-(ethylene carbonate)] (PEOC(OH)(2)) with anti-protein adsorption properties was synthesized in this study. Further polycondensation of PEOC(OH)(2) and isophorone diisocyanate (IPDI) led to biodegradable polyurethane (PEOC-PU) with PEOC as the soft segment. For comparison, polyurethanes with polyethylene glycol (PEG-PU) and polypropylene glycol (PPG-PU) as soft segments were also synthesized. The chemical structures of the polyurethanes were characterized by (1)H NMR and FTIR. The biodegradation behavior of PEOC-PU promoted by lipase due to the presence of ethylene carbonate units was also studied. Their resistance to proteins was studied using quartz crystal microbalance with dissipation (QCM-D) and the results revealed that PEOC-PU exhibited excellent nonspecific resistance to proteins. The colonization of microorganisms on PU in the liquid culture medium was further examined and the results showed that PEOC-PU exhibited excellent antibacterial adhesion performance due to its protein resistance and biodegradation.
ESTHER : Cao_2023_Soft.Matter__
PubMedSearch : Cao_2023_Soft.Matter__
PubMedID: 38073481

Title : Molecular Machinery of Lipid Droplet Degradation and Turnover in Plants - Qin_2023_Int.J.Mol.Sci_24_
Author(s) : Qin Z , Wang T , Zhao Y , Ma C , Shao Q
Ref : Int J Mol Sci , 24 : , 2023
Abstract : Lipid droplets (LDs) are important organelles conserved across eukaryotes with a fascinating biogenesis and consumption cycle. Recent intensive research has focused on uncovering the cellular biology of LDs, with emphasis on their degradation. Briefly, two major pathways for LD degradation have been recognized: (1) lipolysis, in which lipid degradation is catalyzed by lipases on the LD surface, and (2) lipophagy, in which LDs are degraded by autophagy. Both of these pathways require the collective actions of several lipolytic and proteolytic enzymes, some of which have been purified and analyzed for their in vitro activities. Furthermore, several genes encoding these proteins have been cloned and characterized. In seed plants, seed germination is initiated by the hydrolysis of stored lipids in LDs to provide energy and carbon equivalents for the germinating seedling. However, little is known about the mechanism regulating the LD mobilization. In this review, we focus on recent progress toward understanding how lipids are degraded and the specific pathways that coordinate LD mobilization in plants, aiming to provide an accurate and detailed outline of the process. This will set the stage for future studies of LD dynamics and help to utilize LDs to their full potential.
ESTHER : Qin_2023_Int.J.Mol.Sci_24_
PubMedSearch : Qin_2023_Int.J.Mol.Sci_24_
PubMedID: 38003229

Title : Effect of structural stability of lipase in acetonitrile on its catalytic activity in EGCG esterification reaction: FTIR and MD simulation - Wang_2023_Int.J.Biol.Macromol__128266
Author(s) : Wang S , Mo L , Wu B , Ma C , Wang H
Ref : Int J Biol Macromol , :128266 , 2023
Abstract : In this study, (-)-Epigallocatechin-3-O-gallate (EGCG) esterification reaction was catalyzed by Novozym 435, Lipozyme RM, Lipozyme TLIM, and lipase Amano 30SD in acetonitrile. Fourier transform infrared spectroscopy (FTIR) and molecular dynamic (MD) simulations were used to analyze the structural stability of different lipases in acetonitrile and their effect on EGCG esterification reaction. The results showed that conversion rate of EGCG catalyzed by Lipozyme RM was the highest, followed by Lipozyme TLIM. FTIR indicated that the secondary structure of Lipozyme RM was the most stable. MD simulations suggested that whole structural stability of Lipozyme RM in acetonitrile was superior to Novozym 435 and lipase Amano 30SD and similar to Lipozyme TLIM due to their similar conformation, while the active site of Lipozyme RM is more flexible than that of Lipozyme TLIM, which indicated that lipase with stable whole structure and flexible active site may be more conducive to the esterification of EGCG in acetonitrile. This study provided a direction for rapidly screening lipase to synthetize EGCG or other polyphenols esterified derivatives.
ESTHER : Wang_2023_Int.J.Biol.Macromol__128266
PubMedSearch : Wang_2023_Int.J.Biol.Macromol__128266
PubMedID: 37984584

Title : Design, synthesis and biological evaluation of carbamate derivatives incorporating multifunctional carrier scaffolds as pseudo-irreversible cholinesterase inhibitors for the treatment of Alzheimer's disease - Liu_2023_Eur.J.Med.Chem_265_116071
Author(s) : Liu Y , Ma C , Li Y , Li M , Cui T , Zhao X , Li Z , Jia H , Wang H , Xiu X , Hu D , Zhang R , Wang N , Liu P , Yang H , Cheng M
Ref : Eur Journal of Medicinal Chemistry , 265 :116071 , 2023
Abstract : In this study, a series of carbamate derivatives incorporating multifunctional carrier scaffolds were designed, synthesized, and evaluated as potential therapeutic agents for Alzheimer's disease (AD). We used tacrine to modify the aliphatic substituent, and employed rivastigmine, indole and sibiriline fragments as carrier scaffolds. The majority of compounds exhibited good inhibitory activity for cholinesterase. Notably, compound C7 with sibiriline fragment exhibited potent inhibitory activities against human acetylcholinesterase (hAChE, IC(50) = 30.35 +/- 2.07 nM) and human butyrylcholinesterase (hBuChE, IC(50) = 48.03 +/- 6.41 nM) with minimal neurotoxicity. Further investigations have demonstrated that C7 exhibited a remarkable capacity to safeguard PC12 cells against H(2)O(2)-induced apoptosis and effectively suppressed the production of reactive oxygen species (ROS). Moreover, in an inflammation model of BV2 cells induced by lipopolysaccharide (LPS), C7 effectively attenuated the levels of pro-inflammatory cytokines. After 12 h of dialysis, C7 continued to exhibit an inhibitory effect on cholinesterase activity. An acute toxicity test in vivo demonstrated that C7 exhibited a superior safety profile and no hepatotoxicity compared to the parent nucleus tacrine. In the scopolamine-induced AD mouse model, C7 (20 mg/kg) significantly reduced cholinesterase activity in the brain of the mice. C7 was tested in a pharmacological AD mouse model induced by Abeta(1-42) and attenuated memory deficits at doses as low as 5 mg/kg. The pseudo-irreversible cholinesterase inhibitory properties and multifunctional therapeutic attributes of C7 render it a promising candidate for further investigation in the treatment of AD.
ESTHER : Liu_2023_Eur.J.Med.Chem_265_116071
PubMedSearch : Liu_2023_Eur.J.Med.Chem_265_116071
PubMedID: 38157596

Title : Serum cholinesterase as a new nutritional indicator for predicting weaning failure in patients - Liu_2023_Front.Med.(Lausanne)_10_1175089
Author(s) : Liu J , Shao T , Chen H , Ma C , Lu X , Yang X , Song K , Wang L , Lei S , Wang D
Ref : Front Med (Lausanne) , 10 :1175089 , 2023
Abstract : AIM: The objective of this study is to examine the correlation between patient serum cholinesterase (SCHE) concentration and weaning failure in the context of invasive mechanical ventilation (IMV), as well as to identify predictors of ventilator weaning failure. Additionally, this study investigates the potential relationship between SCHE and nutritional risk for developing more effective weaning strategies. METHOD: A retrospective observational study was conducted. The sample was collected from 227 patients with IMV over 48 h who underwent SBT before weaning. Relevant experimental samples and data collection were analyzed at the time of patient admission and before the initiation of the SBT. The correlation between SCHE and weaning failure was determined by multifactorial logistic regression and propensity matching scores. RESULTS: Weaning was successful in 127 patients and failed in 100 patients. Depending on the difficulty of weaning, 55 of these patients had difficulty in weaning and 45 had long-term weaning. In the crude cohort, experimental data collected on the day of SBT showed that SCHE concentrations were higher in patients with successful weaning than in those with failed weaning (4,514 u/l vs. 3,190 u/l p < 0.01). The critical value for predicting weaning failure was SCHE 3,228 u/l (p < 0.01). Ventilator weaning failure was predicted by multifactorial logistic regression analysis of SCHE, heart rate, and PaO(2) before SBT, with SCHE predicting ventilator weaning failure (AUC 0.714; 95% CI 0.647-0.782) better than heart rate (AUC 0.618; 95% CI 0.545-0.690), PaO(2) (AUC 0.59; 95% CI 0.515-0.664). After propensity-matched scores, SCHE remained an independent predictor of weaning failure (p = 0.05). And the SCHE concentration was strongly correlated with the patient's weaning difficulties (p < 0.01). The Nutrition Risk in Critically Ill (NUTRIC) score was also significantly correlated with SCHE according to Spearman's correlation analysis (p < 0.01). CONCLUSION: Our study revealed that the patients who experienced weaning failure exhibited lower SCHE values compared to those who successfully underwent weaning. Before spontaneous breathing trial (SBT), SCHE, heart rate, and PaO(2) were identified as independent predictors of weaning failure. Following propensity score matching (PSM), SCHE and heart rate remained independent predictors. Patients with SCHE levels below 3,228 u/l should undergo careful evaluation before weaning. Our findings suggest that malnutrition may be a contributing factor to weaning failure in patients.
ESTHER : Liu_2023_Front.Med.(Lausanne)_10_1175089
PubMedSearch : Liu_2023_Front.Med.(Lausanne)_10_1175089
PubMedID: 37502364

Title : GR24-mediated enhancement of salt tolerance and roles of H(2)O(2) and Ca(2+) in regulating this enhancement in cucumber - Zhang_2022_J.Plant.Physiol_270_153640
Author(s) : Zhang XH , Ma C , Zhang L , Su M , Wang J , Zheng S , Zhang TG
Ref : J Plant Physiol , 270 :153640 , 2022
Abstract : This study investigated the regulation of the exogenous strigolactone (SL) analog GR24 in enhancing the salt tolerance and the effects of calcium ion (Ca(2+)) and hydrogen peroxide (H(2)O(2)) on GR24's regulation effects in cucumber. The seedlings were sprayed with (1) distilled water (CK), (2) NaCl, (3) GR24, then NaCl, (4) GR24, then H(2)O(2) scavenger, then NaCl, and (5) GR24, then Ca(2+) blocker, then NaCl. The second true leaf was selected for biochemical assays. Under the salt stress, the exogenous GR24 maintained the ion balance, increased the activity of antioxidant enzymes, reduced the membrane lipid peroxidation, and increased the activities of catalase (CAT), superoxide dismutase (SOD), peroxidase (POD), and ascorbate peroxidase (APX), accompanied by a decrease in relative conductivity, an increase in the proline content, and elevated gene expression levels of antioxidant enzymes, nicotinamide adenine dinucleotide phosphate (NADPH) oxidase, calcium-dependent protein kinases (CDPKs), salt overly sensitive SOS1, CBL-interacting protein kinase 2 (CIPK2), and calcineurin B-like protein 3 (CBL3). Such protective effects triggered by GR24 were attenuated or almost abolished by ethylene glycol tetraacetic acid (EGTA), lanthanum chloride (LaCl3, Ca(2+) channel blocker), diphenyleneiodonium (DPI, NADPH oxidase inhibitor), and dimethylthiourea (DMTU, hydroxyl radical scavenger). Our data suggest that exogenous GR24 is highly effective in alleviating salt-induced damages via modulating antioxidant capabilities and improving ionic homeostasis and osmotic balance and that H(2)O(2) and Ca(2+) are required for GR24-mediated enhancement of salt tolerance.
ESTHER : Zhang_2022_J.Plant.Physiol_270_153640
PubMedSearch : Zhang_2022_J.Plant.Physiol_270_153640
PubMedID: 35168135

Title : Improving Effect of the Policosanol from Ericerus pela Wax on Learning and Memory Impairment Caused by Scopolamine in Mice - Sun_2022_Foods_11_
Author(s) : Sun L , Li X , Ma C , He Z , Zhang X , Wang C , Zhao M , Gan J , Feng Y
Ref : Foods , 11 : , 2022
Abstract : Policosanol (PC) is a mixture of long-chain fatty alcohols that exhibits multiple biological activities, such as reducing blood lipid and cholesterol levels, lowering blood pressure, and extenuating liver inflammation. To assess PC's impact on cognitive behavior and function, PC was prepared from Ericerus pela wax using a reduction method and analyzed using gas chromatography (GC). A total of 60 mice were randomly divided into six groups of 10 animals each: control (0.5% CMC-Na solution, i.g.), model (0.5% CMC-Na solution, i.g.), donepezil (3 mg/kg, i.g.), PC low- (2 g/kg, i.g.), medium (4 g/kg, i.g.), and high- (6 g/kg, i.g.) dose groups. All the groups were administered daily for 28 consecutive days. There were four parameters-escape latency, crossings of platform, swimming distance, and time spent in the target quadrant-that were recorded to evaluate the cognitive performance of mice in the Morris Water Maze (MWM). After MWM testing, the levels of acetylcholine (ACh), acetylcholinesterase (AChE), superoxide dismutase (SOD), malondialdehyde (MDA), and glutathione (GSH) that were present in brain tissue were determined using assay kits. The GC data showed that PC consisted of four major components: tetracosanol (14.40%), hexacosanol (48.97%), octacosanol (25.40%), and triacontanol (4.80%). In the MWM test, PC significantly decreased the escape latency (p < 0.05) and increased the crossings of the platform (p < 0.05) and swimming distance (p < 0.05) and time in the target quadrant (p < 0.05) in rodents compared to that in the model group. Moreover, PC increased the levels of ACh, SOD, and GSH; inhibited AChE; and reduced MDA in the brain tissue of the tested animals. This is the first report to evaluate the efficacy of PC for cognitive behavior and function in animals. Our findings demonstrate that PC from E. pela wax is likely to exert an enhancing effect on learning and memory by promoting the cholinergic system and attenuating oxidative stress, which will provide a new insight into the efficacy of PC and expand its application in the food, nutraceutical, and beverage industries.
ESTHER : Sun_2022_Foods_11_
PubMedSearch : Sun_2022_Foods_11_
PubMedID: 35885338

Title : Probiotics and Synbiotics Addition to Bama Mini-Pigs' Diet Improve Carcass Traits and Meat Quality by Altering Plasma Metabolites and Related Gene Expression of Offspring - Zhu_2022_Front.Vet.Sci_9_779745
Author(s) : Zhu Q , Song M , Azad MAK , Ma C , Yin Y , Kong X
Ref : Front Vet Sci , 9 :779745 , 2022
Abstract : This study evaluated the effects of maternal probiotics and synbiotics addition on several traits and parameters in offspring. A total of 64 Bama mini pigs were randomly allocated into the control (basal diet), antibiotic (50 g/t virginiamycin), probiotics (200 mL/day probiotics), or synbiotics (500 g/t xylo-oligosaccharides and 200 mL/day probiotics) group and fed with experimental diets during pregnancy and lactation. After weaning, two piglets per litter and eight piglets per group were selected and fed with a basal diet. Eight pigs per group were selected for analysis at 65, 95, and 125 days of age. The results showed that the addition of probiotics increased the average daily feed intake of the pigs during the 66- to 95-day-old periods and backfat thickness at 65 and 125 days of age, and that the addition of synbiotics increased backfat thickness and decreased muscle percentage and loin-eye area at 125 days of age. The addition of maternal probiotics increased the cooking yield and pH(45min) value at 65 and 95 days of age, respectively, the addition of synbiotics increased the meat color at 95 days of age, and the addition of probiotics and synbiotics decreased drip loss and shear force in 65- and 125-day-old pigs, respectively. However, maternal antibiotic addition increased shear force in 125-day-old pigs. Dietary probiotics and synbiotics addition in sows' diets increased several amino acids (AAs), including total AAs, histidine, methionine, asparagine, arginine, and leucine, and decreased glycine, proline, isoleucine, alpha-aminoadipic acid, alpha-amino-n-butyric acid, beta-alanine, and gamma-amino-n-butyric acid in the plasma and longissimus thoracis (LT) muscle of offspring at different stages. In the LT muscle fatty acid (FA) analysis, saturated FA (including C16:0, C17:0, and C20:0) and C18:1n9t contents were lower, and C18:2n6c, C16:1, C20:1, and unsaturated FA contents were higher in the probiotics group. C10:0, C12:0, and C14:0 contents were higher in 65-day-old pigs, and C20:1 and C18:1n9t contents were lower in the synbiotics group in 95- and 125-day-old pigs, respectively. The plasma biochemical analysis revealed that the addition of maternal probiotics and synbiotics decreased plasma cholinesterase, urea nitrogen, and glucose levels in 95-day-old pigs, and that the addition of synbiotics increased plasma high-density lipoprotein cholesterol, low-density lipoprotein cholesterol, and total cholesterol concentrations in 65-day-old pigs and triglyceride concentration in 125-day-old pigs. The addition of maternal probiotics and synbiotics regulated muscle fiber type, myogenic regulation, and lipid metabolism-related gene expression of LT muscle in offspring. In conclusion, the addition of maternal probiotics and synbiotics improved the piglet feed intake and altered the meat quality parameters, plasma metabolites, and gene expression related to meat quality.
ESTHER : Zhu_2022_Front.Vet.Sci_9_779745
PubMedSearch : Zhu_2022_Front.Vet.Sci_9_779745
PubMedID: 35873696

Title : Pesticide Residues in Commonly Consumed Vegetables in Henan Province of China in 2020 - Ma_2022_Front.Public.Health_10_901485
Author(s) : Ma C , Wei D , Liu P , Fan K , Nie L , Song Y , Wang M , Wang L , Xu Q , Wang J , Shi J , Geng J , Zhao M , Jia Z , Huan C , Huo W , Wang C , Mao Z , Huang S , Zeng X
Ref : Front Public Health , 10 :901485 , 2022
Abstract : BACKGROUND: Pesticides are widely used in agricultural production to control insect pests and regulate plant growth in China, which may result in the presence of some pesticide residues in the vegetables. However, few studies of monitoring pesticides have been conducted in Henan Province. The aim of this study was to evaluate the level of pesticide residues in commonly consumed vegetables in the regions of Henan Province. METHODS: In this study, we collected 5,576 samples of 15 different vegetables in 17 areas from Henan Province during 2020. Eight kinds of pesticides were analyzed by gas chromatography-mass spectrometry (GC-MS), including procymidone, lambda-cyhalothrin, cypermethrin, pendimethalin, isocarbophos, isazophos, fenthion and deltamethrin. The chi-square test was used to compare the detection rates of pesticide residues in different regions. RESULTS: Of all the pesticides above, procymidone, lambda-cyhalothrin, cypermethrin, pendimethalin and isocarbophos were detected in vegetables, the detection rates were 27.0%, 16.2%, 11.4%, 3.5%, and 1.9%, respectively. However, isazophos, fenthion, and deltamethrin were not detected. In addition, procymidone, lambda-cyhalothrin, and cypermethrin were detected in urban areas, while pendimethalin was detected in rural areas. The detection rates of cypermethrin and pendimethalin in rural were 19.8% and 5.4%, respectively, which in urban were at relatively lower levels (13.7% and 1.9%, respectively) (P < 0.05). Compared the differences of pesticide detection rates among five areas of Henan province, we found that there were statistical differences in the detection rates of procymidone, cypermethrin and lambda-cyhalothrin in different regions (all P < 0.05). CONCLUSION: The results have revealed that the pesticide residues are present. Higher detection rates and more types of pesticides were found in rural areas than urban areas. In addition, there were higher detection rates in Eastern Henan. The findings provided valuable information on the current pesticide residues status, which can be a reference of pesticide supervision and management.
ESTHER : Ma_2022_Front.Public.Health_10_901485
PubMedSearch : Ma_2022_Front.Public.Health_10_901485
PubMedID: 35757605

Title : Structural characterization and antioxidant property of enzymatic-transesterification derivatives of (-)-epigallocatechin-3-O-gallate and vinyl laurate - Jiang_2021_J.Food.Sci__
Author(s) : Jiang C , Wang L , Huang X , Zhu S , Ma C , Wang H
Ref : J Food Sci , : , 2021
Abstract : (-)-Epigallocatechin-3-O-gallate(EGCG) was enzymatically modified to enhance the lipophilicity and the antioxidant property. The determination of optimal reaction conditions are as follows: Lipase DF "Amano" 15 and acetone were used as catalyst and solvent, respectively. Equal molar of EGCG and vinyl laurate (1:1); lipase addition of 6.0% (w/w of total substrates); reaction temperature of 50 degreesC and reaction time of 96 h, which obtained the conversion rate of EGCG at 80.1%. The structure of EGCG lauroyl derivatives were 5''-O-lauroyl-EGCG, 3'',5''-2-O-lauroyl-EGCG, and 5',3'',5''-3-O-lauroyl-EGCG, identified by high-performance liquid chromatography-mass spectrometry (HPLC-MS) and nuclear magnetic resonance (NMR). Compared with the logP of precursor EGCG (0.69 +/- 0.03), the logP of EGCG lauroyl derivatives was 1.37 +/- 0.19, 2.27 +/- 0.33, and 3.28 +/- 0.37, increasing by 0.98, 2.28, and 3.75 times, respectively (p < 0.05), suggesting the grafted fatty acid chains make EGCG derivatives more lipophilic, and the lipid solubility gradually increased as the number of substituents increased. Furthermore, EGCG lauroyl derivatives had excellent lipid oxidation than that of EGCG. The POVs (peroxide values) of soybean oil with mono-, di-, tri-lauroyl EGCG were significantly reduced by 42%, 47%, and 57% than that of EGCG at 21 days, respectively, indicating the antioxidative inhibition of these derivatives decreased with the increase in substituents. This indicates that these derivatives have broad prospects of the antioxidant application while improving their solubility properties in lipophilic environments/high-fat food. Practical Application: The lipophilic esterification reaction of EGCG catalyzed by new catalytic lipase DF "Amano" 15 was carried out in a non-aqueous solvent.Various reaction factors on a higher conversion rate of EGCG lauroyl derivatives were evaluated. The lipophilicity and antioxidant properties of EGCG lauroyl derivatives were much excellent than that of parent EGCG.
ESTHER : Jiang_2021_J.Food.Sci__
PubMedSearch : Jiang_2021_J.Food.Sci__
PubMedID: 34553787

Title : Identification and Antioxidant Abilities of Enzymatic-Transesterification (-)-Epigallocatechin-3-O-gallate Stearyl Derivatives in Non-Aqueous Systems - Jiang_2021_Antioxidants.(Basel)_10_
Author(s) : Jiang C , Wang L , Huang X , Zhu S , Ma C , Wang H
Ref : Antioxidants (Basel) , 10 : , 2021
Abstract : Vinyl stearate was added to enzymatic transesterification of (-)-Epigallocatechin-3-O-gallate (EGCG) to enhance its lipophilicity and antioxidant ability in a non-aqueous system. The lipase DF "Amano" 15 was used as the catalyst. The optimal reaction conditions were: acetonitrile as the solvent, the molar ratio of vinyl stearate: EGCG as 3:1, an enzyme amount of 4.0% (ratio of substrate mass), and a reaction temperature and time of 50 degreesC and 96 h, respectively, achieving 65.2% EGCG conversion. HPLC-MS and NMR were used to determine the structure of EGCG stearyl derivative (3'',5''-2-O-stearyl-EGCG). The lipophilicity of EGCG stearyl derivatives (3.49 +/- 0.34) was higher (5.06 times) than that of the parent EGCG (0.69 +/- 0.08). Furthermore, EGCG stearyl derivatives had excellent lipid oxidation compared with BHT, BHA, and parent EGCG. The POVs of soybean oil with EGCG stearyl derivatives (18.17 +/- 0.92 mEq/kg) were significantly reduced (by 62.5%) at 21 d compared with those of EGCG (48.50 +/- 1.23 mEq/kg). These results indicate that EGCG derivatives have broad antioxidant application prospects in lipophilic environments/high-fat food.
ESTHER : Jiang_2021_Antioxidants.(Basel)_10_
PubMedSearch : Jiang_2021_Antioxidants.(Basel)_10_
PubMedID: 34439530

Title : Adipose triglyceride lipase promotes the proliferation of colorectal cancer cells via enhancing the lipolytic pathway - Yin_2021_J.Cell.Mol.Med__
Author(s) : Yin H , Li W , Mo L , Deng S , Lin W , Ma C , Luo Z , Luo C , Hong H
Ref : J Cell Mol Med , : , 2021
Abstract : Abnormal lipid metabolism is the sign of tumour cells. Previous researches have revealed that the lipolytic pathway may contribute to the progression of colorectal cancer (CRC). However, adipose triglyceride lipase (ATGL) role in CRC cells remains unclear. Here, we find that elevated ATGL positively correlates with CRC clinical stages and negatively associates with overall survival. Overexpression of ATGL significantly promotes CRC cell proliferation, while knockdown of ATGL inhibits the proliferation and promotes the apoptosis of CRC cells in vitro. Moreover, in vivo experiments, ATGL promotes the growth of CRC cells. Mechanistically, ATGL enhances the carcinogenic function of CRC cells via promoting sphingolipid metabolism and CoA biosynthesis pathway-related gene levels by degrading triglycerides, which provides adequate nutrition for the progression of CRC. Our researches clarify for the first time that ATGL is a novel oncogene in CRC and may provide an important prognostic factor and therapeutic target for CRC.
ESTHER : Yin_2021_J.Cell.Mol.Med__
PubMedSearch : Yin_2021_J.Cell.Mol.Med__
PubMedID: 33621408

Title : Combined toxicity of micro\/nano scale polystyrene plastics and ciprofloxacin to Corbicula fluminea in freshwater sediments - Guo_2021_Sci.Total.Environ_789_147887
Author(s) : Guo X , Cai Y , Ma C , Han L , Yang Z
Ref : Sci Total Environ , 789 :147887 , 2021
Abstract : Plastic pollution has become a global environmental threat, and its potential to affect the bioavailability and toxicity of pharmaceuticals to aquatic organism are of growing concern. However, little is known regarding the combined toxicity of micro/nano-plastics and pharmaceuticals to benthic organisms in sediments. Thus, we employed a freshwater benthic bivalve, Corbicula fluminea (C. fluminea), to investigate the individual and co-toxicity of model plastics, microscopic fluorescent polystyrene (PS) (PS nano-plastic (PS-NP) and PS micro-plastic (PS-MP), 80 nm and 6 microm, respectively) and the common antibiotic ciprofloxacin (CIP) in formulated sediments. Our results suggest that oxidative damage and neurotoxicity were confirmed to occur in C. fluminea in all the treatments. The oxidative damage in the digestive glands reduced the clam ability to scavenge free radicals, causing severe tissue damage to the digestive glands of C. fluminea. Filtration rates of C. fluminea were significantly decreased in a concentration-dependent manner across all the treatments, which might be due to the inhibition of acetylcholinesterase activities. Interactions between CIP and micro/nano-plastic were observed, whereby the presence of PS decreased the toxicity of CIP in the digestive glands but aggravated the C. fluminea siphoning inhibition rate in the nano-plastic co-treatments group; in addition, the CIP toxicity to C. fluminea decreased because that the concentration of free dissolved CIP was lowered by micro/nano-PS. Taken together, the current study could contribute greatly to evaluating the ecological risk of CIP and PS in aquatic environments and sheds light on potential issues of food safety caused by both emerging pollutants.
ESTHER : Guo_2021_Sci.Total.Environ_789_147887
PubMedSearch : Guo_2021_Sci.Total.Environ_789_147887
PubMedID: 34051493

Title : Detection of Carboxylesterase 1 and Chlorpyrifos with ZIF-8 Metal-Organic Frameworks Using a Red Emission BODIPY-Based Probe - Shen_2021_ACS.Appl.Mater.Interfaces__
Author(s) : Shen B , Ma C , Ji Y , Dai J , Li B , Zhang X , Huang H
Ref : ACS Appl Mater Interfaces , : , 2021
Abstract : In this work, a red emission fluorescent probe CBZ-BOD@zeolitic imidazolate framework-8 (ZIF-8) was fabricated based on metal-organic frameworks (MOFs) for detecting carboxylesterase 1 (CES1). The small molecule probe CBZ-BOD was first synthesized and then used to prepare the functionalized MOF material. ZIF-8 was chosen as an encapsulation shell to improve the detection properties of CBZ-BOD. Using this unique porous materials, ultrasensitive quantification of CES1 and chlorpyrifos was successfully realized. The low detection limit and high fluorescence quantum yield were calculated as 1.15 ng/mL and 0.65 for CBZ-BOD@ZIF-8, respectively. CBZ-BOD@ZIF-8 has good biocompatibility and was successfully applied to monitor the activity of CES1 in living cells. A molecular docking study was used to explore the binding of CES1 and CBZ-BOD, finding that CES1 can bind with the probe before and after hydrolysis. This type of materialized probe can inspire the development of fluorescent tools for further exploration of many pathological processes.
ESTHER : Shen_2021_ACS.Appl.Mater.Interfaces__
PubMedSearch : Shen_2021_ACS.Appl.Mater.Interfaces__
PubMedID: 33569946

Title : Chemical Composition and Biological Activities of Essential Oils from the Leaves, Stems, and Roots of Kadsura coccinea - Zhao_2021_Molecules_26_
Author(s) : Zhao T , Ma C , Zhu G
Ref : Molecules , 26 : , 2021
Abstract : The chemical composition and biological activities of the essential oils from the leaves, stems, and roots of Kadsura coccinea (K. coccinea) were investigated. The essential oils were extracted by hydro distillation and analyzed by gas chromatography mass spectrometry (GC-MS) and gas chromatography with flame ionization detector (GC-FID). Antioxidant activities of the essential oils were examined with DPPH radical scavenging assay, ABTS cation radical scavenging assay, and ferric reducing antioxidant power assay. Antimicrobial activities were evaluated by determining minimum inhibitory concentrations (MIC) and minimum microbiocidal concentrations (MMC). Acetylcholinesterase and butyrylcholinesterase inhibitory activity of the essential oils were also tested. A total of 46, 44, and 47 components were identified in the leaf, stem, and root oils, representing 95.66%, 97.35%, and 92.72% of total composition, respectively. The major compounds of three essential oils were alpha-pinene (16.60-42.02%), beta-pinene (10.03-18.82%), camphene (1.56-10.95%), borneol (0.50-7.71%), delta-cadinene (1.52-7.06%), and beta-elemene (1.86-4.45%). The essential oils were found to have weak antioxidant activities and cholinesterase inhibition activities. The essential oils showed more inhibitory effects against Staphylococcus aureus (S. aureus) than those of other strains. The highest antimicrobial activity was observed in the root oil against S. aureus, with MIC of 0.78 mg/mL. Therefore, K. coccinea essential oils might be considered as a natural antibacterial agent against S. aureus with potential application in food and pharmaceutical industries.
ESTHER : Zhao_2021_Molecules_26_
PubMedSearch : Zhao_2021_Molecules_26_
PubMedID: 34684838

Title : Dynamic changes in chemical compositions and anti-acetylcholinesterase activity associated with steaming process of stem-leaf saponins of Panax notoginseng - Ma_2021_Biomed.Chromatogr__e5077
Author(s) : Ma C , Guan H , Lin Q , Liu C , Ju Z , Xue Y , Cheng X , Wang C
Ref : Biomedical Chromatography , :e5077 , 2021
Abstract : Stem-leaf saponins (SLS), the total saponins from aerial part of P. notoginseng, are by-products of notoginseng, a famous tradition Chinese medicine. SLS have been used as a health functional food in China, but its mild effects limited clinical applications in diseases. Inspired by steaming of notoginseng to enhance pharmacological activity, a steaming protocol was developed to deal SLS. SLS were steamed at 100 degreesC, 120 degreesC, and 140 degreesC for 1, 2, 3, and 4 h, respectively. The UPLC-Q-TOF and UPLC-MS/MS were applied to analyze the dynamic changes in chemical compositions. Anti-acetylcholinesterase activity of steamed SLS were assessed in vitro by directly determining the metabolic product of acetylcholine, choline. The components of SLS were significantly changed by steaming. Total 117 saponins and aglycones were characterized, and 35 of them were newly generated. The anti-acetylcholinesterase activity of steamed SLS gradually increased with the extension of steamed time and the increase of steamed temperature and reached the maximum after 140 degreesC for 3 h. Furthermore, ginsenosides Rk1 and Rg5, the main components of steamed SLS, showed dose-dependent anti-acetylcholinesterase activities with IC(50) values of 26.88 +/- 0.53 microM and 22.41 +/- 1.31 microM that were only 1.8- and 1.5-fold higher than donepezil, respectively.
ESTHER : Ma_2021_Biomed.Chromatogr__e5077
PubMedSearch : Ma_2021_Biomed.Chromatogr__e5077
PubMedID: 33475178

Title : Insecticidal activity of triterpenoids and volatile oil from the stems of Tetraena mongolica - Wu_2020_Pestic.Biochem.Physiol_166_104551
Author(s) : Wu Z , Wei W , Cheng K , Zheng L , Ma C , Wang Y
Ref : Pestic Biochem Physiol , 166 :104551 , 2020
Abstract : Tetraena mongolica Maxim is a species of Zygophyllaceae endemic to China. Because few insect pests affect its growth and flowering, we speculated that this plant produces defensive chemicals that are insect repellents or antifeedants. The effects of different fractions from crude stem and leaf extracts on Pieris rapae were examined. The results confirmed that the ethyl acetate (EtOAc) fraction from the stems had insecticidal potential. Five compounds were isolated from the EtOAc fraction: a volatile oil [bis(2-ethylhexyl) benzene-1,2-dicarboxylate (1)], three triterpenoids 2E-3beta-(3,4-dihydroxycinnamoyl)-erythrodiol (2), 2Z-3beta-(3,4-dihydroxycinnamoyl)-erythrodiol (3), and 2E-3beta-(3,4-dihydroxyphenyl)-2-propenoate (4)], and one steroid [beta-sitosterol (5)]. Compounds 1-5 exhibited different degrees of insecticidal activity, including antifeedant and growth-inhibition effects. Compounds 1-5 inhibited the activity of carboxylesterase (CarE) and acetylcholinesterase (AChE) to different degrees. Compound 1 had the strongest antifeedant and growth-inhibition effects, and significantly inhibited the activity of CarE and AChE. Our results indicate that compounds 1-4 are the major bioactive insecticidal constituents of Tetraena mongolica. This work should facilitate the development and application of plant-derived botanical pesticides.
ESTHER : Wu_2020_Pestic.Biochem.Physiol_166_104551
PubMedSearch : Wu_2020_Pestic.Biochem.Physiol_166_104551
PubMedID: 32448415

Title : Diosgenin alleviates hypercholesterolemia via SRB1\/CES-1\/CYP7A1\/FXR pathway in high-fat diet-fed rats - Yu_2020_Toxicol.Appl.Pharmacol__115388
Author(s) : Yu L , Lu H , Yang X , Li R , Shi J , Yu Y , Ma C , Sun F , Zhang S , Zhang F
Ref : Toxicol Appl Pharmacol , :115388 , 2020
Abstract : Phytosterol diosgenin (DG) exhibits cholesterol-lowering properties. Few studies focused on the underlying mechanism of DG attenuation of hypercholesterolemia by promoting cholesterol metabolism. To investigate the roles of SRB1/CES-1/CYP7A1/FXR pathways in accelerating cholesterol elimination and alleviating hypercholesterolemia, a rat model of hypercholesterolemia was induced by providing a high-fat diet (HFD). Experimental rat models were randomly divided into a normal control (Con) group, HFD group, low-dose DG (LDG) group (150mg/kg/d), high-dose DG (HDG) group (300mg/kg) and Simvastatin (Sim) group (4mg/kg/d). Body weights, serum and hepatic lipid parameters of rats were tested. The expression levels of scavenger receptor class B type I (SRB1), carboxylesterase-1 (CES-1), cholesterol7alpha- hydroxylase (CYP7A1), and farnesoid X receptor (FXR) were determined. The results showed that DG reduced weight and lowered lipid levels in HFD-fed rats. Pathological morphology analyses revealed that DG notably improved hepatic steatosis and intestinal structure. Further studies showed the increased hepatic SRB1, CES-1, CYP7A1 and inhibited FXR-mediated signaling in DG-fed rats, which contributing to the decrease of hepatic cholesterol. DG also increased intestinal SRB1 and CES-1, inhibiting cholesterol absorption and promoting RCT. The expression levels of these receptors in the HDG group were higher than LDG and Sim groups. These data suggested that DG accelerated reverse cholesterol transport (RCT) and enhanced cholesterol elimination via SRB1/CES-1/CYP7A1/FXR pathway, and DG might be a new candidate for the alleviation of hypercholesterolemia.
ESTHER : Yu_2020_Toxicol.Appl.Pharmacol__115388
PubMedSearch : Yu_2020_Toxicol.Appl.Pharmacol__115388
PubMedID: 33383043

Title : Inhibitory mechanisms and interaction of tangeretin, 5-demethyltangeretin, nobiletin, and 5-demethylnobiletin from citrus peels on pancreatic lipase: Kinetics, spectroscopies, and molecular dynamics simulation - Huang_2020_Int.J.Biol.Macromol_164_1927
Author(s) : Huang X , Zhu J , Wang L , Jing H , Ma C , Kou X , Wang H
Ref : Int J Biol Macromol , 164 :1927 , 2020
Abstract : This study aimed to reveal the interaction and inhibitory mechanisms of tangeretin (TAN), nobiletin (NBT), and their acidic hydroxylated forms, 5-demethyltangeretin (5-DT) and 5-demethylnobiletin (5-DN) on porcine pancreatic lipase (PPL) using spectroscopic techniques and molecular dynamics (MD) simulation. PPL inhibition assay showed that the inhibitory activity of NBT (IC(50) value of 3.60 +/- 0.19 microM) was superior to those of three polymethoxylated flavones (PMFs), indicating it may be related to the methoxy groups at the 3'-position in its molecular structure. Inhibition kinetic analyses demonstrated that the inhibition types of the 4 PMFs were consistent with the mixed inhibition model, which agreed well with the results from the ultraviolet-visible (UV-Vis) spectroscopy, Circular dichroism (CD), fluorescence spectroscopy, molecular docking, and MD simulation that PMFs could bind to the PPL catalytic site and non-catalytic site, affecting the normal spatial conformation of PPL and weakening its ability to decompose the substrate. All these findings suggest that PMFs are a kind of natural lipase inhibitors, and NBT has the potential as a lipase inhibition precursor because of its unique flavone skeleton structure.
ESTHER : Huang_2020_Int.J.Biol.Macromol_164_1927
PubMedSearch : Huang_2020_Int.J.Biol.Macromol_164_1927
PubMedID: 32795575

Title : Alterations in the Blood Parameters and Fecal Microbiota and Metabolites during Pregnant and Lactating Stages in Bama Mini Pigs as a Model - Ma_2020_Mediators.Inflamm_2020_8829072
Author(s) : Ma C , Gao Q , Zhang W , Azad MAK , Kong X
Ref : Mediators Inflamm , 2020 :8829072 , 2020
Abstract : This study was conducted to analyze plasma reproductive hormone and biochemical parameter changes, as well as fecal microbiota composition and metabolites in sows, at different pregnancy and lactation stages, using Bama mini pig as an experimental animal model. We found that plasma prolactin (PRL), progesterone, follicle-stimulating hormone (FSH), and estrogen levels decreased from day 45 to day 105 of pregnancy. Plasma total protein and albumin levels were lower in pregnant sows, while glucose, urea nitrogen, total cholesterol, and high-density lipoprotein-cholesterol, as well as fecal acetate, butyrate, valerate, total short-chain fatty acids, skatole, and tyramine levels, were higher in lactating sows. Interestingly, the lactating sows showed lower alpha-diversity and Spirochaetes and Verrucomicrobia relative abundances, while pregnant sows showed a higher Proteobacteria relative abundance. Notably, the Akkermansia relative abundance was highest on day 7 of lactation. Spearman analysis showed a positive correlation between plasma triglyceride and cholinesterase levels and Akkermansia and Streptococcus relative abundances. Moreover, Oscillospira and Desulfovibrio relative abundances were also positively correlated with plasma FSH, LH, and E(2) levels, as well as PRL and LH with Bacteroides. Collectively, plasma reproductive hormones, biochemical parameters, and fecal microbiota composition and metabolite levels could alter along with pregnancy and lactation, which might contribute to the growth and development demands of fetuses and newborns.
ESTHER : Ma_2020_Mediators.Inflamm_2020_8829072
PubMedSearch : Ma_2020_Mediators.Inflamm_2020_8829072
PubMedID: 33162832

Title : In vivo and in vitro metabolism and pharmacokinetics of cholinesterase inhibitor deoxyvasicine from aerial parts of Peganum harmala Linn in rats via UPLC-ESI-QTOF-MS and UPLC-ESI-MS\/MS - Deng_2019_J.Ethnopharmacol_236_288
Author(s) : Deng G , Liu W , Ma C , Rong X , Zhang Y , Wang Y , Wu C , Cao N , Ding W , Guan H , Cheng X , Wang C
Ref : J Ethnopharmacol , 236 :288 , 2019
Abstract : ETHNOPHARMACOLOGICAL RELEVANCE: Aerial parts of Peganum harmala Linn are a Uighur traditional medicinal herb in China used to treat amnesia, bronchial asthma, and cough. Deoxyvasicine (DVAS), a potent cholinesterase inhibitor exhibiting anti-senile dementia activity, is one of the chief active ingredients in aerial parts of P. harmala and plays a key role in mediating the pharmacological effects of P. harmala. However, the metabolic profiling and in vivo pharmacokinetic characteristics of DVAS still remain unknown. AIM OF THE STUDY: The aim of this present study was to investigate the metabolism and pharmacokinetic properties of DVAS in rats by using ultra-performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UPLC-ESI-QTOF-MS) and ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-ESI-MS/MS) method. MATERIALS AND METHODS: The metabolic profiling of DVAS was evaluated in vitro and in vivo by rat liver microsomes (RLMs) incubation and by rat bio-specimens, such as urine, feces, plasma, and bile, after the oral administration of 45mg/kg DVAS. An efficient and sensitive UPLC-ESI-MS/MS method was developed and validated to simultaneously determine DVAS and its major four metabolites, namely, vasicine, deoxyvasicinone, vasicinone, and 1,2,3,9-tetrahydropyrrolo[2,1-b]quinazolin-3-beta-D-glucuronide in rat plasma. For pharmacokinetic studies, 32 Sprague-Dawley rats were randomly divided into four groups, namely, intravenous dosage group (2mg/kg DVAS) and three oral dosage groups (5, 15, and 45mg/kg DVAS). In addition, the activity of the components in plasma after intravenous administration of DVAS was evaluated by in vitro anti-butyrylcholinesterase (BChE) assays. RESULTS: A total of 23 metabolites were found in RLMs, plasma, urine, feces, and bile by UPLC-ESI-QTOF-MS. The metabolic pathway of DVAS in vivo and in vitro mainly involved hydroxylation, dehydrogenation, acetylation, methylation, glucuronidation, and O-sulphate conjugation, and the C-3 and C-9 sites were the main metabolic soft spots. All 23 metabolites were detected in the urine sample, and 13, 8, 22, and 6 metabolites were identified from rat feces, plasma, bile, and RLMs, respectively. The standard curves of DVAS and four metabolites in rat plasma showed good linearity in the concentration range of 0.82-524.00ng/mL with acceptable selectivity, precision, accuracy, recovery, and stability. DVAS exhibited linear dose-proportional pharmacokinetics at doses of 5, 15, and 45mg/kg after oral administration, and the average oral absolute bioavailability of DVAS was 47.46%. The in vitro anti-BChE assays implied that the inhibitive activities were mainly due to the different concentrations of prototype DVAS. CONCLUSIONS: DVAS can be rapidly absorbed and excreted by blood, and it is also extensively metabolized in vivo, and the anti-BChE activity in blood is mainly attributed to DVAS. These findings can lay a foundation for new drug development for DVAS.
ESTHER : Deng_2019_J.Ethnopharmacol_236_288
PubMedSearch : Deng_2019_J.Ethnopharmacol_236_288
PubMedID: 30872168

Title : Ameliorative effect of deoxyvasicine on scopolamine-induced cognitive dysfunction by restoration of cholinergic function in mice - Deng_2019_Phytomedicine_63_153007
Author(s) : Deng G , Wu C , Rong X , Li S , Ju Z , Wang Y , Ma C , Ding W , Guan H , Cheng X , Liu W , Wang C
Ref : Phytomedicine , 63 :153007 , 2019
Abstract : BACKGROUND: Aerial parts of Peganum harmala Linn is used as a traditional medical herb for treatment of amnesia in Uighur medicine in China. Deoxyvasicine (DVAS) is one of the chief active ingredients in P. harmala, it possesses strong acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities in vitro, but the therapeutic effect and mechanisms on amnesia in vivo are unclear. PURPOSE: The objective of this study was to investigate the improvement effect of DVAS from P. harmala in learning and memory deficits of scopolamine-induced mice and elucidate the underlying mechanisms involved. METHODS: Mice were pretreated with DVAS (5, 15 and 45mg/kg) and huperzine-A (0.2mg/kg) by gavage for 7 days, and subsequently were daily intraperitoneally injected with scopolamine (1mg/kg) to induce learning and memory deficits and behavioral performance was assessed by Morris water maze. To further evaluate the potential mechanisms of DVAS in improving learning and memory capabilities, pathological change, levels of various biochemical markers and protein expressions related to cholinergic system, oxidative stress, and neuroinflammation were examined. RESULTS: The results showed that DVAS could alleviate learning and memory deficits in scopolamine-treated mice. DVAS could regulate cholinergic function by inhibiting AChE and activating choline acetyltransferase (ChAT) activities and protein expressions. DVAS could induce brain-derived neurotrophic factor and protect hippocampal pyramidal cells against neuronal damage. DVAS also enhanced antioxidant defense via increasing the antioxidant enzyme level and activity of glutathione peroxidase, and anti-inflammatory function through suppressing tumor necrosis factor-alpha. Additionally, DVAS could regulate the neurotransmitters by elevating acetylcholine, 5-hydroxytryptamine, gamma-aminobutyric acid and reducing 5-hydroxyindole-3-acetic acid and glutamic acid. CONCLUSION: Results illustrated that DVAS may be a promising candidate compound against amnesia via restoration of cholinergic function, regulating neurotransmitters, attenuating neuroinflammation and oxidative stress.
ESTHER : Deng_2019_Phytomedicine_63_153007
PubMedSearch : Deng_2019_Phytomedicine_63_153007
PubMedID: 31301537

Title : Effects of feed intake restriction during late pregnancy on the function, anti-oxidation capability and acute phase protein synthesis of ovine liver - Yang_2019_Asian-Australas.J.Anim.Sci_32_217
Author(s) : Yang H , Wang Y , Ma C , Sun C , Liu Y , Wu K , Li M , Borjigin G , Gao F
Ref : Asian-Australas J Anim Sci , 32 :217 , 2019
Abstract : OBJECTIVE: An experiment was conducted to investigate the effects of feed intake restriction during late pregnancy on the function, anti-oxidation capability and acute phase protein synthesis of ovine liver. METHODS: Eighteen time-mated ewes with singleton fetuses were allocated to three groups: restricted group 1 (RG1, 0.18 MJ ME/kg W0.75 d, n = 6), restricted group 2 (RG2, 0.33 MJ ME/kg W0.75 d), n = 6) and a control group (CG, ad libitum, 0.67 MJ ME/kg W0.75 d, n = 6). The feed restriction period was from 90 days to 140 days of pregnancy. RESULTS: The ewe's body weight, liver weights, water, and protein content of liver in the restricted groups were reduced compared with the CG group (p<0.05), but the liver fat contents in the RG1 group were higher than those of the CG group (p<0.05). The increased hepatic collagen fibers and reticular fibers were observed in the restricted groups with the reduction of energy intake. The concentrations of nonesterified free fatty acids in the RG1 and RG2 groups were higher than those of the CG group with the reduction of energy intake (p<0.05), but there were decreased concentrations of lipoprotein lipase and hepatic lipase in both restricted groups compared with the CG group (p<0.05). In addition, the increased concentrations of beta-hydroxybutyric acid, triglycerides, malondialdehyde, total antioxidant capacity and activities of superoxide dismutase activity and catalase were found in the RG1 group, and the concentrations of cholinesterase in the RG1 group were reduced compared with the CG group (p<0.05). For the concentrations of acute phase proteins, the C-reactive protein (CRP) in the RG1 group were reduced compared with the CG group, but there were no differences in haptoglobin relative to the controls (p>0.05). CONCLUSION: The fat accumulation, increased hepatic fibrosis, antioxidant imbalance and modified synthesis of acute phase proteins were induced in ewe's liver by maternal malnutrition during late pregnancy, which were detrimental for liver function to accommodate pregnancy.
ESTHER : Yang_2019_Asian-Australas.J.Anim.Sci_32_217
PubMedSearch : Yang_2019_Asian-Australas.J.Anim.Sci_32_217
PubMedID: 30056659

Title : Analogous beta-Carboline Alkaloids Harmaline and Harmine Ameliorate Scopolamine-Induced Cognition Dysfunction by Attenuating Acetylcholinesterase Activity, Oxidative Stress, and Inflammation in Mice - Li_2018_Front.Pharmacol_9_346
Author(s) : Li SP , Wang YW , Qi SL , Zhang YP , Deng G , Ding WZ , Ma C , Lin QY , Guan HD , Liu W , Cheng XM , Wang CH
Ref : Front Pharmacol , 9 :346 , 2018
Abstract : The analogous beta-carboline alkaloids, harmaline (HAL) and harmine (HAR), possess a variety of biological properties, including acetylcholinesterase (AChE) inhibitory activity, antioxidant, anti-inflammatory, and many others, and have great potential for treating Alzheimer's disease (AD). However, studies have showed that the two compounds have similar structures and in vitro AChE inhibitory activities but with significant difference in bioavailability. The objective of this study was to comparatively investigate the effects of HAL and HAR in memory deficits of scopolamine-induced mice. In the present study, mice were pretreated with HAL (2, 5, and 10 mg/kg), HAR (10, 20, and 30 mg/kg) and donepezil (5 mg/kg) by intragastrically for 7 days, and were daily intraperitoneal injected with scopolamine (1 mg/kg) to induce memory deficits and then subjected to behavioral evaluation by Morris water maze. To further elucidate the underlying mechanisms of HAL and HAR in improving learning and memory, the levels of various biochemical factors and protein expressions related to cholinergic function, oxidative stress, and inflammation were examined. The results showed that HAL and HAR could effectively ameliorate memory deficits in scopolamine-induced mice. Both of them exhibited an enhancement in cholinergic function by inhibiting AChE and inducing choline acetyltransferase (ChAT) activities, and antioxidant defense via increasing the antioxidant enzymes activities of superoxide dismutase and glutathione peroxidase, and reducing maleic diadehyde production, and anti-inflammatory effects through suppressing myeloperoxidase, tumor necrosis factor alpha, and nitric oxide as well as modulation of critical neurotransmitters such as acetylcholine (ACh), choline (Ch), L-tryptophan (L-Trp), 5-hydroxytryptamine (5-HT), gamma-aminobutyric acid (gamma-GABA), and L-glutamic acid (L-Glu). Furthermore, the regulations of HAL on cholinergic function, inflammation, and neurotransmitters were more striking than those of HAR, and HAL manifested a comparable antioxidant capacity to HAR. Remarkably, the effective dosage of HAL (2 mg/kg) was far lower than that of HAR (20 mg/kg), which probably due to the evidently differences in the bioavailability and metabolic stability of the two analogs. Taken together, all these results revealed that HAL may be a promising candidate compound with better anti-amnesic effects and pharmacokinetic characteristics for the treatments of AD and related diseases.
ESTHER : Li_2018_Front.Pharmacol_9_346
PubMedSearch : Li_2018_Front.Pharmacol_9_346
PubMedID: 29755345

Title : Stereoselective glucuronidation metabolism, pharmacokinetics, anti-amnesic pharmacodynamics, and toxic properties of vasicine enantiomers in vitro and in vivo - Zhu_2018_Eur.J.Pharm.Sci_123_459
Author(s) : Zhu Y , Liu W , Qi S , Wang H , Wang Y , Deng G , Zhang Y , Li S , Ma C , Cheng X , Wang C
Ref : Eur J Pharm Sci , 123 :459 , 2018
Abstract : Vasicine (VAS) is a potential natural cholinesterase inhibitor for treatment of Alzheimer's disease. Due to one chiral centre (C-3) presenting in molecule, VAS has two enantiomers, d-vasicine (d-VAS) and l-vasicine (l-VAS). The study was undertaken to investigate the stereoselective glucuronidation metabolism, pharmacokinetics, anti-amnesic effect and acute toxicity of VAS enantiomers. In results, the glucuronidation metabolic rate of l-VAS was faster than d-VAS in human liver microsomes and isoenzymes tests, and it was proved that the UDP-glucuronosyltransferase (UGT) 1A9 and UGT2B15 were the major metabolic enzymes for glucuronidation of l-VAS, while only UGT1A9 for d-VAS, which take responsibility of the significantly less metabolic affinity of d-VAS than l-VAS in HLM and rhUGT1A9. The plasma exposure of d-VAS in rats was 1.3-fold and 1.6-fold higher than that of l-VAS after intravenous and oral administration of d-VAS and l-VAS, respectively. And the plasma exposure of the major glucuronidation metabolite d-VASG was one of tenth of l-VASG or more less, no matter by intravenous or oral administration. Both d-VAS and l-VAS were exhibited promising acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, and the BChE inhibitory activity of d-VAS with IC50 of 0.03+/-0.001muM was significantly stronger than that of l-VAS with IC50 of 0.98+/-0.19muM. The molecular docking results indicated that d-VAS and l-VAS could bind to the catalytic active site (CAS position) either of human AChE and BChE, and the BChE combing ability of d-VAS (the score of GBI/WAS dG -7.398) was stronger than that of l-VAS (the score of GBI/WAS dG -7.135). Both d-VAS and l-VAS could improving the learning and memory on scopolamine-induced memory deficits in mice. The content of acetylcholine (ACh) after oral administration d-VAS increased more than that of l-VAS in mice cortex, through inhibiting cholinesterase (ChE) and increasing choline acetyltransferase (ChAT). In addition, the LD50 value of d-VAS ( was slight lower than l-VAS ( These results indicated that VAS enantiomers displayed significantly stereoselective metabolic, pharmacokinetics, anti-amnesic effect and toxic properties in vitro and in vivo. The d-VAS might be the dominant configuration for treating Alzheimer's disease.
ESTHER : Zhu_2018_Eur.J.Pharm.Sci_123_459
PubMedSearch : Zhu_2018_Eur.J.Pharm.Sci_123_459
PubMedID: 30077712

Title : Anti-amnesic effect of extract and alkaloid fraction from aerial parts of Peganum harmala on scopolamine-induced memory deficits in mice - Liu_2017_J.Ethnopharmacol_204_95
Author(s) : Liu W , Zhu Y , Wang Y , Qi S , Ma C , Li S , Jiang B , Cheng X , Wang Z , Xuan Z , Wang C
Ref : J Ethnopharmacol , 204 :95 , 2017
Abstract : ETHNOPHARMACOLOGICAL RELEVANCE: Aerial parts of Peganum harmala Linn (APP) is used as traditional medical herb for treatment of forgetfulness in Uighur medicine in China. But, the active ingredients and underlying mechanisms are unclear. AIM OF THE STUDY: The present study was undertaken to investigate the improvement effects of extract and alkaloid fraction from APP on scopolamine-induced cognitive dysfunction and to elucidate their underlying mechanisms of action, and to support its folk use with scientific evidence, and lay a foundation for its further researches. MATERIALS AND
METHODS: The acetylcholinesterase (AChE) inhibitory activities of extract (EXT), alkaloid fraction (ALK) and flavonoid fraction (FLA) from APP were evaluated in normal male C57BL/6 mice. The anti-amnesic effects of EXT and ALK from APP were measured in scopolamine-induced memory deficits mice by the Morris water maze (MWM) tasks. The levels of biomarkers, enzyme activity and protein expression of cholinergic system were determined in brain tissues.
RESULTS: The AChE activity was significantly decreased and the content of neurotransmitter acetylcholine (ACh) was significantly increased in normal mice cortex and hippocampus by treatment with donepezil at dosage of 8mg/kg, EXT at dosages of 183, 550, 1650mg/kg and ALK at dosages of 10, 30, 90mg/kg (P<0.05), and the AChE activity and the content of ACh were not significantly changed in cortex and hippocampus after treatment with FLA at dosages of 10, 30, 90mg/kg (P>0.05). In the MWM task, scopolamine-induced a decrease in both the swimming time within the target zone and the number of crossings where the platform had been placed were significantly reversed by treatment with EXT at dosages of 550, 1650mg/kg and ALK at dosages of 30, 90mg/kg (P<0.05). Moreover, the activity and protein expression of AChE was significantly decreased and the content of neurotransmitter ACh was significantly increased in cerebral cortex of scopolamine-induced mice by treatment with EXT at dosages of 183, 550, 1650mg/kg and ALK at dosages of 10, 30, 90mg/kg (P<0.05), compared with scopolamine-treated group.
CONCLUSIONS: EXT and ALK from APP exert beneficial effect on learning and memory processes in mice with scopolamine-induced memory impairment. APP is an effective traditional folk medicine and the ALK fraction is proved to be the main effective components for the treatment of forgetfulness. The ALK may be valuable source for lead compounds discovery and drug development for treatment of memory impairment such as in Alzheimer's disease.
ESTHER : Liu_2017_J.Ethnopharmacol_204_95
PubMedSearch : Liu_2017_J.Ethnopharmacol_204_95
PubMedID: 28442406

Title : An overview on therapeutics attenuating amyloid beta level in Alzheimer's disease: targeting neurotransmission, inflammation, oxidative stress and enhanced cholesterol levels - Zhou_2016_Am.J.Transl.Res_8_246
Author(s) : Zhou X , Li Y , Shi X , Ma C
Ref : Am J Transl Res , 8 :246 , 2016
Abstract : Alzheimer's disease (AD) is the most common underlying cause of dementia, and novel drugs for its treatment are needed. Of the different theories explaining the development and progression of AD, "amyloid hypothesis" is the most supported by experimental data. This hypothesis states that the cleavage of amyloid precursor protein (APP) leads to the formation of amyloid beta (Abeta) peptides that congregate with formation and deposition of Abeta plaques in the frontal cortex and hippocampus. Risk factors including neurotransmitter modulation, chronic inflammation, metal-induced oxidative stress and elevated cholesterol levels are key contributors to the disease progress. Current therapeutic strategies abating AD progression are primarily based on anti-acetylcholinesterase (AChE) inhibitors as cognitive enhancers. The AChE inhibitor, donepezil, is proven to strengthen cognitive functions and appears effective in treating moderate to severe AD patients. N-Methyl-D-aspartate receptor antagonist, memantine, is also useful, and its combination with donepezil demonstrated a strong stabilizing effect in clinical studies on AD. Nonsteroidal anti-inflammatory drugs delayed the onset and progression of AD and attenuated cognitive dysfunction. Based upon epidemiological evidence and animal studies, antioxidants emerged as potential AD preventive agents; however, clinical trials revealed inconsistencies. Pharmacokinetic and pharmacodynamic profiling demonstrated pleiotropic functions of the hypolipidemic class of drugs, statins, potentially contributing towards the prevention of AD. In addition, targeting the APP processing pathways, stimulating neuroprotective signaling mechanisms, using the amyloid anti-aggregants and Abeta immunotherapy surfaced as well-tested strategies in reducing the AD-like pathology. Overall, this review covers mechanism of inducing the Abeta formation, key risk factors and major therapeutics prevalent in the AD treatment nowadays. It also delineates the need for novel screening approaches towards identifying drugs that may prevent or at least limit the progression of this devastating disease.
ESTHER : Zhou_2016_Am.J.Transl.Res_8_246
PubMedSearch : Zhou_2016_Am.J.Transl.Res_8_246
PubMedID: 27158324

Title : Hypocholesterolaemic mechanism of bitter melon aqueous extracts via inhibition of pancreatic cholesterol esterase and reduction of cholesterol micellar solubility - Su_2016_Int.J.Food.Sci.Nutr_67_20
Author(s) : Su J , Wang H , Ma C , Liu C , Gao C , Nie R , Tanver Rahman MR
Ref : Int J Food Sci Nutr , 67 :20 , 2016
Abstract : This study investigated the hypocholesterolaemic effects of bitter melon aqueous extracts (BMAE) in vitro, the inhibitory effects of BMAE on pancreatic cholesterol esterase (CEase) and incorporation of cholesterol into micelles were investigated. BMAE decreased the in vitro micellar solubility of cholesterol in a dose-dependent manner. The conformation of CEase was investigated by means of circular dichroism (CD) and fluorescence. The result revealed the decrease of alpha-helix contents, increase of beta-sheet and exposure of aromatic amino acid residuals. The incorporation of cholesterol into micelles was inhibited by BMAE. A complex was observed by transmission electron microscopy (TEM), which indicated interaction between cholesterol and BMAE. The result revealed that BMAE can play a role in decreased intestinal cholesterol absorption via inhibition of CEase, and of micelle formation.
ESTHER : Su_2016_Int.J.Food.Sci.Nutr_67_20
PubMedSearch : Su_2016_Int.J.Food.Sci.Nutr_67_20
PubMedID: 26653879

Title : Associations of Rs3744841 and Rs3744843 Polymorphisms in Endothelial Lipase Gene with Risk of Coronary Artery Disease and Lipid Levels in a Chinese Population - Cai_2016_PLoS.One_11_e0162727
Author(s) : Cai G , Zhang B , Ma C , Shi G , Weng W , Xue S
Ref : PLoS ONE , 11 :e0162727 , 2016
Abstract : OBJECTIVE: The aim of the present study was to assess the association between the 2037T/C and 2237G/A polymorphisms in the EL gene and the risk of CAD and lipid levels in a Chinese population.
METHODS: A case-control study including 706 patients with CAD and 315 controls was performed. The polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) method was used to identify the genotypes.
RESULTS: The EL 2037 T/C polymorphism was associated with CAD risk and HDL-C levels. No significant differences were found between the EL 2237 G/A genotypes and CAD risk and lipid levels in the whole population. However, carriers of the 2237 A allele had higher Apo A1 levels than those with the 2237 GG genotype and in the CAD subgroup (P = 0.044). The CAD cases have a significantly lower frequency of the C-G haplotypes than the controls, and the T-A haplotype was significantly more common in the CAD patients than in the controls.
CONCLUSIONS: Our study concluded that the EL 2037 T/C polymorphism was associated with CAD risk and HDL-C levels, and that the C allele might be a protective factor against CAD in the Chinese Han population. In addition, the EL 2237 A allele might be associated with an increased Apo A1 level in CAD subjects.
ESTHER : Cai_2016_PLoS.One_11_e0162727
PubMedSearch : Cai_2016_PLoS.One_11_e0162727
PubMedID: 27612170

Title : Receptor usage and cell entry of bat coronavirus HKU4 provide insight into bat-to-human transmission of MERS coronavirus - Yang_2014_Proc.Natl.Acad.Sci.U.S.A_111_12516
Author(s) : Yang Y , Du L , Liu C , Wang L , Ma C , Tang J , Baric RS , Jiang S , Li F
Ref : Proc Natl Acad Sci U S A , 111 :12516 , 2014
Abstract : Middle East respiratory syndrome coronavirus (MERS-CoV) currently spreads in humans and causes approximately 36% fatality in infected patients. Believed to have originated from bats, MERS-CoV is genetically related to bat coronaviruses HKU4 and HKU5. To understand how bat coronaviruses transmit to humans, we investigated the receptor usage and cell entry activity of the virus-surface spike proteins of HKU4 and HKU5. We found that dipeptidyl peptidase 4 (DPP4), the receptor for MERS-CoV, is also the receptor for HKU4, but not HKU5. Despite sharing a common receptor, MERS-CoV and HKU4 spikes demonstrated functional differences. First, whereas MERS-CoV prefers human DPP4 over bat DPP4 as its receptor, HKU4 shows the opposite trend. Second, in the absence of exogenous proteases, both MERS-CoV and HKU4 spikes mediate pseudovirus entry into bat cells, whereas only MERS-CoV spike, but not HKU4 spike, mediates pseudovirus entry into human cells. Thus, MERS-CoV, but not HKU4, has adapted to use human DPP4 and human cellular proteases for efficient human cell entry, contributing to the enhanced pathogenesis of MERS-CoV in humans. These results establish DPP4 as a functional receptor for HKU4 and host cellular proteases as a host range determinant for HKU4. They also suggest that DPP4-recognizing bat coronaviruses threaten human health because of their spikes' capability to adapt to human cells for cross-species transmissions.
ESTHER : Yang_2014_Proc.Natl.Acad.Sci.U.S.A_111_12516
PubMedSearch : Yang_2014_Proc.Natl.Acad.Sci.U.S.A_111_12516
PubMedID: 25114257

Title : A truncated receptor-binding domain of MERS-CoV spike protein potently inhibits MERS-CoV infection and induces strong neutralizing antibody responses: implication for developing therapeutics and vaccines - Du_2013_PLoS.One_8_e81587
Author(s) : Du L , Kou Z , Ma C , Tao X , Wang L , Zhao G , Chen Y , Yu F , Tseng CT , Zhou Y , Jiang S
Ref : PLoS ONE , 8 :e81587 , 2013
Abstract : An emerging respiratory infectious disease with high mortality, Middle East respiratory syndrome (MERS), is caused by a novel coronavirus (MERS-CoV). It was first reported in 2012 in Saudi Arabia and has now spread to eight countries. Development of effective therapeutics and vaccines is crucial to save lives and halt the spread of MERS-CoV. Here, we show that a recombinant protein containing a 212-amino acid fragment (residues 377-588) in the truncated receptor-binding domain (RBD: residues 367-606) of MERS-CoV spike (S) protein fused with human IgG Fc fragment (S377-588-Fc) is highly expressed in the culture supernatant of transfected 293T cells. The purified S377-588-Fc protein efficiently binds to dipeptidyl peptidase 4 (DPP4), the receptor of MERS-CoV, and potently inhibited MERS-CoV infection, suggesting its potential to be further developed as a therapeutic modality for treating MERS-CoV infection and saving the patients' lives. The recombinant S377-588-Fc is able to induce in the vaccinated mice strong MERS-CoV S-specific antibodies, which blocks the binding of RBD to DPP4 receptor and effectively neutralizes MERS-CoV infection. These findings indicate that this truncated RBD protein shows promise for further development as an effective and safe vaccine for the prevention of MERS-CoV infection.
ESTHER : Du_2013_PLoS.One_8_e81587
PubMedSearch : Du_2013_PLoS.One_8_e81587
PubMedID: 24324708

Title : The Reference Genome of the Halophytic Plant Eutrema salsugineum - Yang_2013_Front.Plant.Sci_4_46
Author(s) : Yang R , Jarvis DE , Chen H , Beilstein MA , Grimwood J , Jenkins J , Shu S , Prochnik S , Xin M , Ma C , Schmutz J , Wing RA , Mitchell-Olds T , Schumaker KS , Wang X
Ref : Front Plant Sci , 4 :46 , 2013
Abstract : Halophytes are plants that can naturally tolerate high concentrations of salt in the soil, and their tolerance to salt stress may occur through various evolutionary and molecular mechanisms. Eutrema salsugineum is a halophytic species in the Brassicaceae that can naturally tolerate multiple types of abiotic stresses that typically limit crop productivity, including extreme salinity and cold. It has been widely used as a laboratorial model for stress biology research in plants. Here, we present the reference genome sequence (241 Mb) of E. salsugineum at 8x coverage sequenced using the traditional Sanger sequencing-based approach with comparison to its close relative Arabidopsis thaliana. The E. salsugineum genome contains 26,531 protein-coding genes and 51.4% of its genome is composed of repetitive sequences that mostly reside in pericentromeric regions. Comparative analyses of the genome structures, protein-coding genes, microRNAs, stress-related pathways, and estimated translation efficiency of proteins between E. salsugineum and A. thaliana suggest that halophyte adaptation to environmental stresses may occur via a global network adjustment of multiple regulatory mechanisms. The E. salsugineum genome provides a resource to identify naturally occurring genetic alterations contributing to the adaptation of halophytic plants to salinity and that might be bioengineered in related crop species.
ESTHER : Yang_2013_Front.Plant.Sci_4_46
PubMedSearch : Yang_2013_Front.Plant.Sci_4_46
PubMedID: 23518688
Gene_locus related to this paper: theha-e4mxu0 , thesl-v4nk72 , eutsa-v4l4z1 , eutsa-v4kk46 , eutsa-v4mej3 , eutsa-v4ns11 , eutsa-v4mg02 , eutsa-v4mqm9 , eutsa-v4k1y6 , eutsa-v4lad0 , eutsa-v4nr92 , eutsa-v4kqc3 , eutsa-v4l0s2 , eutsa-v4lip3 , eutsa-v4kkg2 , eutsa-v4kvd3 , eutsa-v4m9g4 , eutsa-v4lqg2 , eutsa-v4lp36 , eutsa-v4km66 , eutsa-v4nhr8 , eutsa-v4kqx9 , eutsa-v4lv73

Title : Identification of a receptor-binding domain in the S protein of the novel human coronavirus Middle East respiratory syndrome coronavirus as an essential target for vaccine development - Du_2013_J.Virol_87_9939
Author(s) : Du L , Zhao G , Kou Z , Ma C , Sun S , Poon VK , Lu L , Wang L , Debnath AK , Zheng BJ , Zhou Y , Jiang S
Ref : J Virol , 87 :9939 , 2013
Abstract : A novel human Middle East respiratory syndrome coronavirus (MERS-CoV) caused outbreaks of severe acute respiratory syndrome (SARS)-like illness with a high mortality rate, raising concerns of its pandemic potential. Dipeptidyl peptidase-4 (DPP4) was recently identified as its receptor. Here we showed that residues 377 to 662 in the S protein of MERS-CoV specifically bound to DPP4-expressing cells and soluble DPP4 protein and induced significant neutralizing antibody responses, suggesting that this region contains the receptor-binding domain (RBD), which has a potential to be developed as a MERS-CoV vaccine.
ESTHER : Du_2013_J.Virol_87_9939
PubMedSearch : Du_2013_J.Virol_87_9939
PubMedID: 23824801

Title : Genome sequence of Enterobacter cloacae subsp. dissolvens SDM, an efficient biomass-utilizing producer of platform chemical 2,3-butanediol - Xu_2012_J.Bacteriol_194_897
Author(s) : Xu Y , Wang A , Tao F , Su F , Tang H , Ma C , Xu P
Ref : Journal of Bacteriology , 194 :897 , 2012
Abstract : Enterobacter cloacae subsp. dissolvens SDM has an extraordinary characteristic of biomass utilization for 2,3-butanediol production. Here we present a 4.9-Mb assembly of its genome. The key genes for regulation and metabolism of 2,3-butanediol production were annotated, which could provide further insights into the molecular mechanism of high-yield production of 2,3-butanediol.
ESTHER : Xu_2012_J.Bacteriol_194_897
PubMedSearch : Xu_2012_J.Bacteriol_194_897
PubMedID: 22275097
Gene_locus related to this paper: entcl-i6s5g2 , entcl-y1bd05 , entcl-g8lek8

Title : Genome sequence of the thermophilic strain Bacillus coagulans 2-6, an efficient producer of high-optical-purity L-lactic acid - Su_2011_J.Bacteriol_193_4563
Author(s) : Su F , Yu B , Sun J , Ou HY , Zhao B , Wang L , Qin J , Tang H , Tao F , Jarek M , Scharfe M , Ma C , Ma Y , Xu P
Ref : Journal of Bacteriology , 193 :4563 , 2011
Abstract : Bacillus coagulans 2-6 is an efficient producer of lactic acid. The genome of B. coagulans 2-6 has the smallest genome among the members of the genus Bacillus known to date. The frameshift mutation at the start of the d-lactate dehydrogenase sequence might be responsible for the production of high-optical-purity l-lactic acid.
ESTHER : Su_2011_J.Bacteriol_193_4563
PubMedSearch : Su_2011_J.Bacteriol_193_4563
PubMedID: 21705584
Gene_locus related to this paper: bacc6-f7z0w1 , bacco-c1p801 , bacco-g2tqg6

Title : Cytochrome P450-specific human PBPK\/PD models for the organophosphorus pesticides: chlorpyrifos and parathion - Foxenberg_2011_Toxicology_285_57
Author(s) : Foxenberg RJ , Ellison CA , Knaak JB , Ma C , Olson JR
Ref : Toxicology , 285 :57 , 2011
Abstract : Organophosphorus pesticides (OPs) remain a potential concern to human health because of their continuing use worldwide. Phosphororthioate OPs like chlorpyrifos and parathion are directly activated and detoxified by various cytochrome P450s (CYPs), with the primary CYPs involved being CYP2B6 and CYP2C19. The goal of the current study was to convert a previously reported human pharmacokinetic and pharmacodynamic (PBPK/PD) model for chlorpyrifos, that used chlorpyrifos metabolism parameters from rat liver, into a human CYP based/age-specific model using recombinant human CYP kinetic parameters (V(max), K(m)), hepatic CYP content and plasma binding measurements to estimate new values for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition and to use the model as a template for the development of a comparable parathion PBPK/PD model. The human CYP based/age-specific PBPK/PD models were used to simulate single oral exposures of adults (19 year old) and infants (1 year) to chlorpyrifos (10,000, 1000 and 100 mug/kg) or parathion (100, 25 and 5 mug/kg). Model simulations showed that there is an age dependency in the amount of blood cholinesterase inhibition observed, however additional age-dependent data are needed to further optimize age-specific human PBPK/PD modeling for these OP compounds. PBPK/PD model simulations estimated that a 4-fold increase or decrease in relative CYP2B6 and CYP2C19 content would produce a 9-22% inhibition in blood AChE activity following exposure of an adult to chlorpyrifos (1000 mug/kg). Similar model simulation produced an 18-22% inhibition in blood AChE activity following exposure of an adult to parathion (25 mug/kg). Individuals with greater CYP2B6 content and lower CYP2C19 content were predicted to be most sensitive to both OPs. Changes in hepatic CYP2B6 and CYP2C19 content had more of an influence on cholinesterase inhibition for exposures to chlorpyrifos than parathion, which agrees with previously reported literature that these CYPs are more reaction biased for desulfurization (activation) and dearylation (detoxification) of chlorpyrifos compared to parathion. The data presented here illustrate how PBPK/PD models with human enzyme-specific parameters can assist ongoing risk assessment efforts and aid in the identification of sensitive individuals and populations.
ESTHER : Foxenberg_2011_Toxicology_285_57
PubMedSearch : Foxenberg_2011_Toxicology_285_57
PubMedID: 21514354

Title : Ablation of ligament of Marshall attenuates atrial vulnerability to fibrillation induced by inferior left atrial fat pad stimulation in dogs - Liu_2010_J.Cardiovasc.Electrophysiol_21_1024
Author(s) : Liu X , Yan Q , Li H , Tian Y , Su J , Tang R , Lu C , Dong J , Ma C
Ref : J Cardiovasc Electrophysiol , 21 :1024 , 2010
Abstract : BACKGROUND: The role of ligament of Marshall (LOM) in the mechanism of "vagal" atrial fibrillation (AF) is still unknown. OBJECTIVE: To investigate the impact of LOM ablation on atrial vulnerability to AF induced by inferior left atrial fat pad (ILAFP) stimulation in dogs. METHODS: AF inducibility and atrial effective refractory period (ERP) were elevated before and after LOM ablation in 8 of 14 dogs (the ablation group). Same protocol but without LOM ablation was conducted in the remaining 6 dogs (the control group). The activation patterns of LOM and left pulmonary veins (LPVs) during sustained AF were analyzed. The distribution of epicardial cholinergic nerve fibers between LOM and ILAFP was investigated in the control group. RESULTS: Ablation of LOM significantly attenuated AF inducibility (87.5% vs 33.3%, P < 0.001) and prolonged ERPs of the structures in contiguity with LOM (P < 0.05) in the ablation group. In contrast, there was no significant change in ERPs and AF inducibility in the control group. During sustained AF, fractionated atrial electrograms were more common in the LOM area than the LPVs (84% vs 18% of the analyzed episodes, P < 0.001). In 46.7% of the episodes with identifiable LOM spikes, atrial potentials, and LOM spikes were related in 2:1 or 3:2 pattern during the intermittent organized activity. Acetylcholinesterase staining revealed a close cholinergic nerved relationship between LOM and ILAFP. CONCLUSIONS: LOM plays a critical role in maintaining AF induced by stimulation of ILAFP. Ablation of LOM can markedly attenuate AF inducibility in this model.
ESTHER : Liu_2010_J.Cardiovasc.Electrophysiol_21_1024
PubMedSearch : Liu_2010_J.Cardiovasc.Electrophysiol_21_1024
PubMedID: 20367662

Title : [Susceptibility and related physiological and biochemical mechanisms of Carposina niponensis Walsingham larvae on six insecticides before and after overwintering] - Zhang_2007_Ying.Yong.Sheng.Tai.Xue.Bao_18_1913
Author(s) : Zhang YL , Mu W , Chen ZL , Han ZR , Ma C , Zhai RH
Ref : Ying Yong Sheng Tai Xue Bao , 18 :1913 , 2007
Abstract : The study with impregnating method showed that after overwintering, the susceptibility of Carposina niponensis larvae on triazophos, phoxim, chlorpyrifos, malathion, lambda-cyhalothrin and abamectin was 34.50, 16.71, 3.89, 3.28, 5.90 and 2.73 times as much as that before overwintering, the total protein, glycogen and fat contents and carboxylesterase, acid phosphatase, alkaline phosphatase, glutathione-S-transferase, superoxide dismutase, catalase and peroxidase activities in C. niponensis larvae were decreased by 17.10%, 41.76% and 30.08%, 62.36%, 53.47%, 76.19%, 80.60%, 18.77%, 14.16% and 64.02%, respectively, and the activity of acetylcholinesterase, the target enzyme of many insecticides, was 1.41 times as much as that before overwintering. It was suggested that the difference of the susceptibility was resulted from the changes in the contents of biochemical substances and the activities of metabolic enzymes, protective enzymes and target enzyme.
ESTHER : Zhang_2007_Ying.Yong.Sheng.Tai.Xue.Bao_18_1913
PubMedSearch : Zhang_2007_Ying.Yong.Sheng.Tai.Xue.Bao_18_1913
PubMedID: 17974266

Title : Acute effects of oral pyridostigmine bromide on conditioned operant performance in rats - Shih_1991_Pharmacol.Biochem.Behav_38_549
Author(s) : Shih JH , Liu WF , Lee SF , Lee JD , Ma C , Lin CH
Ref : Pharmacol Biochem Behav , 38 :549 , 1991
Abstract : Pyridostigmine bromide (Pyr), the current drug of choice in the management of myasthenia gravis, has been suggested for use in Alzheimer's dementia, and as a prophylactic treatment for intoxication with organophosphate cholinesterase inhibitors. The present study was undertaken to evaluate the dose-response and time-course effects of acute oral administration of Pyr over a broad dose range (3-40 mg/kg) on the lever pressing of rats maintained under a multiple fixed-ratio (FR-20) time-out schedule of reinforcement for water reward. The drug produced a dose-dependent biphasic response depression in the overall rate of FR responding. Low doses of Pyr (less than or equal to 12 mg/kg) that caused no gross signs of toxicity only moderately decreased rates of responding, primarily due to a decrease in response rates. Whereas high doses of Pyr (greater than 24 mg/kg) which produced overt signs of peripheral cholinergic intoxication markedly suppressed overall responding, primarily due to cessation of responding. The lowest effective dose of performance disruption was 6 mg/kg, and the ED50 was calculated as 23.3 (17.9-28.7) mg/kg. The time-course data of performance disruption showed that low doses of Pyr (less than or equal to 12 mg/kg) had an onset latency within 40-80 min and a duration of 20-80 min, whereas high doses (greater than or equal to 24 mg/kg) had an onset latency of 20-40 min and a duration greater than 80 min. These results suggest the recommended human therapeutic or prophylactic regimen of Pyr, orally taken each 8 hours, might adversely affect behavioral performance.
ESTHER : Shih_1991_Pharmacol.Biochem.Behav_38_549
PubMedSearch : Shih_1991_Pharmacol.Biochem.Behav_38_549
PubMedID: 2068191

Title : Ortho-iodosobenzoic acid: its acute toxicity and neurobehavioral effects in mice - Liu_1989_Toxicol.Lett_45_289
Author(s) : Liu WF , Wei YC , Lee JD , Ma C , Lin CH
Ref : Toxicol Lett , 45 :289 , 1989
Abstract : o-Iodosobenzoic acid (IBA), in a surfactant micellar medium, is a rapid and efficient catalyst for the hydrolysis of organophosphate (OP) esters. Since little is known about the toxicity of IBA, a primary screen of neurobehavioral toxicity was evaluated in male ICR mice. IBA was administered intraperitoneally in a pH 7.4 phosphate buffer solution containing 8% dimethylformamide. The predominant overt signs of toxicity included an immediate and transient writhing reflex and/or persistent spasmodic myotwitching of the abdomen, and conspicuous suppression of orienting/exploratory behavior and emotional defecation. The dose ranges for ED50 of writhing response, suppression of rearing and spontaneous motor activity overlapped at levels of about one-tenth the acute LD50, 742 (633-856) mumol/kg, being 94.9 (74.5-122.5), 69.8 (47.9-105.4) and 71.1 (49.9-101.3) mumol/kg, respectively; the dose ranges for ED50 of abdominal myotwitching and depression of emotional defecation in a novel environment also overlapped but at levels of about one-fifth the acute LD50, being 138.4 (115.3-167.2) and 146.2 (110.7-196.3) mumol/kg, respectively. Morphine (1.25-10 mg/kg s.c.) antagonized the IBA-induced writhing response and abdominal myotwitching in a dose-dependent manner, with a PD50 of 4.2 and 4.9 mg/kg, respectively. The present report demonstrates that acute intraperitoneal administration of IBA produces an intriguing, non-specific behavioral syndrome, probably resulting from nociceptive stimulation. This implies that IBA might be irritating to the skin and mucosa.
ESTHER : Liu_1989_Toxicol.Lett_45_289
PubMedSearch : Liu_1989_Toxicol.Lett_45_289
PubMedID: 2919407

Title : Kinetic studies and structure-activity relationships of bispyridinium oximes as reactivators of acetylcholinesterase inhibited by organophosphorus compounds - Su_1986_Fundam.Appl.Toxicol_6_506
Author(s) : Su CT , Wang PH , Liu RF , Shih JH , Ma C , Lin CH , Liu CY , Wu MT
Ref : Fundamental & Applied Toxicology , 6 :506 , 1986
Abstract : The kinetics of the reactivation of acetylcholinesterase inhibited by isopropyl methylphosphonofluoridate was studied. The reactivators used include nine bispyridinium monooximes and three bispyridinium dioximes. The dissociation constant (Kd) and the rate constant (k2) of dephosphorylation of the complex formed from the organophosphorus acetylcholinesterase (OP-AChE) and the oxime were measured. The reactivation parameters obtained from the in vitro kinetic studies were used to elucidate the structure-activity relationships. The hydrophobic property of a nonoxime substituent at the 3-position on the pyridinium ring can exert a positive effect on their binding affinity to OP-AChE. However, the rate constants (k2) of the nucleophilic displacement of OP-AChE by oximes depend negatively on these physical and structural factors of the oximes. The correlations of the in vivo antidotal efficacy (ED50) of these bispyridinium oximes have been analyzed with their pharmacological properties, e.g., reactivation potency, antimuscarinic activities, and antinicotinic activities. However, no satisfactory correlations were observed. It may be concluded that the detoxication mechanism of poisoning by isopropyl methylphosphonofluoridate is different from those of pinacolyl methylphosphonofluoridate and paraoxon.
ESTHER : Su_1986_Fundam.Appl.Toxicol_6_506
PubMedSearch : Su_1986_Fundam.Appl.Toxicol_6_506
PubMedID: 3699334

Title : Quantitative structure-activity relationships and possible mechanisms of action of bispyridinium oximes as antidotes against pinacolyl methylphosphonofluoridate - Su_1983_Fundam.Appl.Toxicol_3_271
Author(s) : Su CT , Tang CP , Ma C , Shih YS , Liu CY , Wu MT
Ref : Fundamental & Applied Toxicology , 3 :271 , 1983
Abstract : The antidotal efficacy of bispyridinium oximes against the poisoning by pinacolyl methylphosphonofluoridate can be correlated well with their physicochemical parameters. Good correlation was observed between the efficacy of antagonism against pinacolyl methylphosphonofluoridate and antinicotinic action of these oximes. X-ray structural analysis showed that these oximes possessed structural similarity to nicotine and acetylcholine of nicotinic conformation. A new model of antidotal action, other than reactivation, against the poisoning by pinacolyl methylphosphonofluoridate was proposed for these bispyridinium oximes through nicotinic receptor binding. The antagonistic efficacy of these antidotes against pinacolyl methylphosphonofluoridate may be attributed to their direct antagonism at nicotinic receptor as well as reactivation of inhibited acetylcholinesterase.
ESTHER : Su_1983_Fundam.Appl.Toxicol_3_271
PubMedSearch : Su_1983_Fundam.Appl.Toxicol_3_271
PubMedID: 6628889