Song Q

References (34)

Title : Ganshuang granule plays a pharmacological role in anti-alcoholic and anti-hangover via regulating alcohol metabolism and affecting neurotransmitters - Li_2024_Int.J.Neurosci__1
Author(s) : Li Q , Lu Y , Shang J , Song Q , Jiao J , Bi L , Jiang T , Liu X
Ref : International Journal of Neuroscience , :1 , 2024
Abstract : Background: To explore the effect of Ganshuang granule on anti-alcoholic and anti-hangover and its potential mechanism.Methods: SPF SD rats' drunken model and SPF Kunming mice's hangover model were used as models.Results: Ganshuang granule could significantly reduce sleep time, the time to climb in mice, and significantly prolong the tolerance time and shorten sleep time in rats (P < 0.05). The blood ethanol concentration of rats in each administration group was lower than that in the model group at each time point (P < 0.05). Compared with the control group, the activities of ADH and ALDH in the liver of the model group were significantly decreased (P < 0.05); the content of DA and 5-HT in the striatum of the model group was significantly increased (P < 0.05); and the activity of AchE in the hippocampus was significantly decreased (P < 0.05). The above processes could be improved and regulated in the drug administration group. Compared with the control group, there was no significant difference between ADH and ALDH in the serum of the model group (P > 0.05). However, the activities of ADH and ALDH in the liver of drunk rats could be upregulated by Ganshuang granule (P < 0.05).Conclusion: Ganshuang granule has the pharmacological effects of anti-alcoholic and anti-hangover, which is related to regulating the activities of ADH and ALDH in the liver, the contents of DA and 5-HT in striatum, and the activity of AchE in the hippocampus.
ESTHER : Li_2024_Int.J.Neurosci__1
PubMedSearch : Li_2024_Int.J.Neurosci__1
PubMedID: 38197183

Title : Cobalt oxyhydroxide nanosheet-modulated ratiometric fluorescence platform for the selective detection of malachite green in fish - Zhang_2024_Mikrochim.Acta_191_119
Author(s) : Zhang Y , Shi YE , Wang S , Song Q , Li W , Wang Z
Ref : Mikrochim Acta , 191 :119 , 2024
Abstract : A ratiometric fluorescence platform was developed based on the cobalt oxyhydroxide (CoOOH) nanosheet-modulated fluorescence response of blue emissive copper nanoclusters (Cu NCs) and yellow emissive o-phenylenediamine (OPD). CoOOH nanosheets showed dual function of strong absorption and oxidation ability, which can effectively quench the blue fluorescence of Cu NCs, with an excitation and emission peak maximum at 390 and 450 nm, respectively , and transfer the OPD into yellow fluorescence products, with an excitation and emission peak maximum at 390 and 560 nm, respectively. Upon introducing butyrylcholinesterase (BChE) and its substrates, CoOOH nanosheets were decomposed into Co(2+), and malachite green (MG) showed strong inhibition ability to this process. This resulted in the obvious difference on the ratio of blue and yellow fluorescence recorded on the system in the presence and absence of MG, which was utilized for the quantitative detection of MG, with a limit of detection of 0.140 microM and a coefficient of variation of 3.5%. The fluorescence ratiometric assay showed excellent detection performances in practical sample analysis.
ESTHER : Zhang_2024_Mikrochim.Acta_191_119
PubMedSearch : Zhang_2024_Mikrochim.Acta_191_119
PubMedID: 38300297

Title : Isolation of four new monoterpenes from Ailanthus altissima (mill.) Swingle and their enzyme inhibitory effects - Song_2024_Fitoterapia_176_105984
Author(s) : Song Q , Duan ZK , Tan YN , Gao ZH , Liu D , Hao JL , Lin B , Huang XX , Song SJ
Ref : Fitoterapia , 176 :105984 , 2024
Abstract : A phytochemical study of the ethanol extract from Ailanthus altissima (Mill.) Swingle leaves resulted in the isolation of four new monoterpenoids (1-3, 5). The structures were elucidated using HRESIMS data, NMR spectroscopic data, quantum chemical calculations for NMR and ECD, and custom DP4+ probability analysis. Additionally, the absolute configuration of sugar was determined by acid hydrolysis. Compounds 1-4 are cyclogeraniane monocyclic monoterpenes, while compound 5 contains an acyclic mycrane monoterpenes skeleton. Anti-tyrosinase, anti-acetylcholinesterase, and anti-butyrylcholinesterase activities were tested. Compound 1 showed notable anti-acetylcholinesterase activity, and compound 3 exhibited significant inhibitory effects on anti-tyrosinase activity. Furthermore, the potential binding sites of compounds 1 and 3 were predicted by molecular docking.
ESTHER : Song_2024_Fitoterapia_176_105984
PubMedSearch : Song_2024_Fitoterapia_176_105984
PubMedID: 38701870

Title : Efficacy and Safety of Plasma Exchange Combined with Hemoperfusion in the Treatment of Organophosphorus Poisoning: A Meta-Analysis - Yao_2023_Blood.Purif__1
Author(s) : Yao Z , Wang P , Fu Q , Song Q , Wang W , Liu A , Zhang P
Ref : Blood Purif , :1 , 2023
Abstract : INTRODUCTION: The aim of the study was to systematically evaluate the efficacy and safety of plasma exchange combined with hemoperfusion in the treatment of organophosphorus poisoning. METHODS: PubMed, Embase, the Cochrane Library, China National Knowledge Internet, Wanfang database, and Weipu database were searched for articles about this subject. Literature screening and selection were conducted in strict accordance with the inclusion and exclusion criteria. RESULTS: 14 randomized controlled trials with 1,034 participants were included in this meta-analysis study, including 518 cases in plasma exchange combined with hemoperfusion group (the combination treatment group) and 516 cases in hemoperfusion group (the control group). Compared with the control group, the combination treatment group was associated with a higher effective rate (relative risk [RR] = 1.20, 95% confidence interval [CI] [1.11, 1.30], p < 0.00001) and lower fatality rate (RR = 0.28, 95% CI [0.15, 0.52], p< 0.0001); reduced TNF-alpha (standardized mean difference [SMD] = -1.95, 95% CI [-2.42, -1.48], p < 0.00001), IL-6 (SMD = -1.94, 95% CI [-3.08, -0.80], p = 0.0009), and C-reactive protein (CRP) (SMD = -1.94, 95% CI [-2.86, -1.03], p < 0.0001); shorten coma time (SMD = -1.99, 95% CI [-2.75, -1.24], p < 0.00001), recovery time of cholinesterase activity (SMD = -1.71, 95% CI [-1.90, -1.53], p < 0.00001), and hospital stay (SMD = -1.29, 95% CI [-1.59, -0.98], p < 0.00001). The incidence of complications in the combination treatment group such as liver and kidney damage (RR = 0.30, 95% CI [0.18, 0.50], p < 0.00001), pulmonary infection (RR = 0.29, 95% CI [0.18, 0.47], p < 0.00001), and intermediate syndrome (RR = 0.32, 95% CI [0.21, 0.49], p < 0.00001) was lower than that in the control group. CONCLUSIONS: The current evidence suggests that the combination of plasma exchange with hemoperfusion therapy can reduce the mortality of patients with organophosphorus poisoning, shorten the recovery time of cholinesterase activity and the time of coma, reduce the average length of hospital stay, and reduce the levels of IL-6, TNF-alpha, and CRP, but high-quality randomized double-blind controlled trials are still required to confirm the current findings in the future.
ESTHER : Yao_2023_Blood.Purif__1
PubMedSearch : Yao_2023_Blood.Purif__1
PubMedID: 37302392

Title : Novel miR-108 and miR-234 target juvenile hormone esterase to regulate the response of Plutella xylostella to Cry1Ac protoxin - Yang_2023_Ecotoxicol.Environ.Saf_254_114761
Author(s) : Yang J , Chen S , Xu X , Lin S , Wu J , Lin G , Bai J , Song Q , You M , Xie M
Ref : Ecotoxicology & Environmental Safety , 254 :114761 , 2023
Abstract : Insect hormones, such as juvenile hormone (JH), precisely regulate insect life-history traits. The regulation of JH is tightly associated with the tolerance or resistance to Bacillus thuringiensis (Bt). JH esterase (JHE) is a primary JH-specific metabolic enzyme which plays a key role in regulating JH titer. Here, we characterized a JHE gene from Plutella xylostella (PxJHE), and found it was differentially expressed in the Bt Cry1Ac resistant and susceptible strains. Suppression of PxJHE expression with RNAi increased the tolerance of P. xylostella to Cry1Ac protoxin. To investigate the regulatory mechanism of PxJHE, two target site prediction algorithms were applied to predict the putative miRNAs targeting PxJHE, and the resulting putative miRNAs were subsequently verified for their function targeting PxJHE using luciferase reporter assay and RNA immunoprecipitation. MiR-108 or miR-234 agomir delivery dramatically reduced PxJHE expression in vivo, whilst only miR-108 overexpression consequently increased the tolerance of P. xylostella larvae to Cry1Ac protoxin. By contrast, reduction of miR-108 or miR-234 dramatically increased PxJHE expression, accompanied by the decreased tolerance to Cry1Ac protoxin. Furthermore, injection of miR-108 or miR-234 led to developmental defects in P. xylostella, whilst injection of antagomir did not cause any obvious abnormal phenotypes. Our results indicated that miR-108 or miR-234 can be applied as potential molecular targets to combat P. xylostella and perhaps other lepidopteran pests, providing novel insights into miRNA-based integrated pest management.
ESTHER : Yang_2023_Ecotoxicol.Environ.Saf_254_114761
PubMedSearch : Yang_2023_Ecotoxicol.Environ.Saf_254_114761
PubMedID: 36907089

Title : Elucidation of Carboxylesterase Mediated Pharmacokinetic Interactions between Irinotecan and Oroxylin A in Rats via Physiologically Based Pharmacokinetic Modeling - Zhang_2023_Pharm.Res__
Author(s) : Zhang J , Zhang Y , Lai YS , Song Q , Xiao M , Ji X , Yan X , Zuo Z
Ref : Pharm Res , : , 2023
Abstract : PURPOSE: Our previous screening studies identified Oroxylin A (OXA) as a strong inhibitor on the carboxyolesterase mediated hydrolysis of irinotecan to SN-38. The current study employed a whole-body physiologically based pharmacokinetic (PBPK) modeling approach to investigate the underlying mechanisms of the carboxylesterase-mediated pharmacokinetics interactions between irinotecan and OXA in rats. METHODS: Firstly, rats received irinotecan intravenous treatment at 35 micromol/kg without or with oral OXA pretreatment (2800 micromol/kg) daily for 5 days. On day 5, blood and tissues were collected for analyses of irinotecan/SN-38 concentrations and carboxylesterase expression. In addition, effects of OXA on the enzyme kinetics of irinotecan hydrolysis and unbound fractions of irinotecan and SN-38 in rat plasma, liver and intestine were also determined. Finally, a PBPK model that integrated the physiological parameters, enzyme kinetics, and physicochemical properties of irinotecan and OXA was developed. RESULTS: Our PBPK model could accurately predict the pharmacokinetic profiles of irinotecan/SN-38, with AUC(0-6h) and C(max) values within +/-27% of observed values. When OXA was included as a carboxylesterase inhibitor, the model could also predict the irinotecan/SN-38 plasma concentrations within twofold of those observed. In addition, the PBPK model indicated inhibition of carboxylesterase-mediated hydrolysis of irinotecan in the intestinal mucosa as the major underlying mechanism for the pharmacokinetics interactions between irinotecan and OXA. CONCLUSION: A whole-body PBPK model was successfully developed to not only predict the impact of oral OXA pretreatment on the pharmacokinetics profiles of irinotecan but also reveal its inhibition on the intestinal carboxylesterase as the major underlying mechanism.
ESTHER : Zhang_2023_Pharm.Res__
PubMedSearch : Zhang_2023_Pharm.Res__
PubMedID: 37667147

Title : Sensitive detection of butyrylcholinesterase activity based on a stimuli-responsive fluorescence reaction - Pang_2023_Spectrochim.Acta.A.Mol.Biomol.Spectrosc_299_122886
Author(s) : Pang Y , Ma Z , Song Q , Wang Z , Shi YE
Ref : Spectrochim Acta A Mol Biomol Spectrosc , 299 :122886 , 2023
Abstract : A fluorogenic reaction between the chelate of Mn(II)-citric acid and terephthalic acid (PTA) was discovered, which was carried out through heating the aqueous mixture of Mn(2+), citric acid and PTA. Detailed investigations indicated the reaction products were 2-hydroxyterephthalic acid (PTA-OH), which was attributed to the reaction between PTA and OH, formed by the triggering of Mn(II)-citric acid in the presence of dissolved O(2). PTA-OH showed a strong blue fluorescence, peaked at 420 nm, and the fluorescence intensity presented a sensitive response to pH of the reaction system. Based on these mechanisms, the fluorogenic reaction was used for the detection of butyrylcholinesterase activity, achieving a detection limit of 0.15 U/L. The detection strategy was successfully applied in human serum samples, and it was also extended for the detection of organophosphorus pesticides and radical scavengers. Such a facile fluorogenic reaction and its stimuli-responsive properties offered an effective tool for designing detection pathways in the fields of clinical diagnosis, environmental monitoring and bioimaging.
ESTHER : Pang_2023_Spectrochim.Acta.A.Mol.Biomol.Spectrosc_299_122886
PubMedSearch : Pang_2023_Spectrochim.Acta.A.Mol.Biomol.Spectrosc_299_122886
PubMedID: 37210854

Title : Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease - Shi_2022_Eur.J.Med.Chem_230_114098
Author(s) : Shi Y , Zhang H , Song Q , Yu G , Liu Z , Zhong F , Tan Z , Liu X , Deng Y
Ref : Eur Journal of Medicinal Chemistry , 230 :114098 , 2022
Abstract : Based on multitarget-directed ligands approach, through two rounds of screening, a series of 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives were designed, synthesized and evaluated as innovative multifunctional agents against Alzheimer's disease. In vitro biological assays indicated that most of the hybrids were endowed with great AChE inhibitory activity, excellent antioxidant activity and moderate Abeta(1-42) aggregation inhibition. Taken both efficacy and balance into account, 12a was identified as the optimal multifunctional ligand with significant inhibition of AChE (EeAChE, IC(50) = 0.20 microM; HuAChE, IC(50) = 37.02 nM) and anti-Abeta activity (IC(50) = 1.92 microM for self-induced Abeta(1-42) aggregation; IC(50) = 1.80 microM for disaggregation of Abeta(1-42) fibrils; IC(50) = 2.18 microM for Cu(2+)-induced Abeta(1-42) aggregation; IC(50) = 1.17 microM for disaggregation of Cu(2+)-induced Abeta(1-42) fibrils; 81.7% for HuAChE-induced Abeta(1-40) aggregation). Moreover, it was equipped with the potential to serve as antioxidant (3.03 Trolox equivalents), metals chelator and anti-neuroinflammation agent for synergetic treatment. Finally, in vivo study demonstrated that 12a, with suitable BBB permeability (log BB = -0.61), could efficaciously ameliorate cognitive dysfunction on scopolamine-treated mice by regulating cholinergic system and oxidative stress simultaneously. Altogether, these results highlight the potential of 12a as an innovative balanced multifunctional candidate for Alzheimer's disease treatment.
ESTHER : Shi_2022_Eur.J.Med.Chem_230_114098
PubMedSearch : Shi_2022_Eur.J.Med.Chem_230_114098
PubMedID: 35026532

Title : Inhibition of Radix Scutellariae flavones on carboxylesterase mediated activations of prodrugs - Zhang_2022_Life.Sci_305_120743
Author(s) : Zhang J , Xiao M , Ji X , Lai YS , Song Q , Zhang Y , Ip CM , Ng WL , Zuo Z
Ref : Life Sciences , 305 :120743 , 2022
Abstract : AIMS: Carboxylesterase (CES) plays an essential role in the hydrolysis of ester prodrugs. Our study explored the inhibitions of Radix Scutellariae flavones, including baicalein (B), baicalin (BG), wogonin (W), wogonoside (WG), oroxylin A (OXA) and oroxylin A-7-O-glucuronide (OAG), on CES-mediated hydrolysis of seven prodrugs (capecitabine, clopidogrel, mycophenolate mofetil, dabigatran etexilate, acetylsalicylic acid, prasugrel and irinotecan). MAIN METHODS: In vitro screenings were developed by incubating the flavones with prodrugs in rat plasma, intestine S9 and liver S9. Docking simulations were conducted using AMDock v1.5.2. In vivo evaluations were performed in rats co-administered with the selected flavone and prodrug via oral gavage/intravenous administration for five consecutive days. KEY FINDINGS: The in vitro investigation showed that B and OXA demonstrated strongest inhibitions on the hydrolysis of irinotecan followed by dabigatran in rat plasma, intestine S9 and liver S9. Consistent results showed in the molecular docking analyses. Additionally, in rats receiving irinotecan, B/OXA intravenous and oral pre-treatments both led to reduction trends on the active metabolite SN-38 formation in plasma. Besides, significant decreases of SN-38/irinotecan plasma concentration ratios were found in the B/OXA oral pre-treatment group with quicker and stronger inhibition potential in OXA pre-treatment than that from B pre-treatment. OXA oral pre-treatment was also found to be able to significantly inhibit intestinal CES2 activities at 0.5 h and 5 h after irinotecan administration. SIGNIFICANCE: Our current findings for the first time alert on potential CES-mediated HDIs between RS flavones and prodrugs, which provide a constructive information referring to rational drug combinations in clinical practice.
ESTHER : Zhang_2022_Life.Sci_305_120743
PubMedSearch : Zhang_2022_Life.Sci_305_120743
PubMedID: 35780840

Title : Phthalimide-(N-alkylbenzylamine) cysteamide hybrids as multifunctional agents against Alzheimer's disease: Design, synthesis and biological evaluation - Zhang_2021_Chem.Biol.Drug.Des__
Author(s) : Zhang H , Song Q , Yu G , Cao Z , Qiang X , Liu X , Deng Y
Ref : Chemical Biology Drug Des , : , 2021
Abstract : The complex pathogenesis of Alzheimer's disease (AD) calls for multi-target approach for disease treatment. Herein, based on the MTDLs strategy, a series of phthalimide-(N-alkylbenzylamine) cysteamide hybrids were designed, synthesized and investigated in vitro for the purpose. Most of the target compounds were found to be potential multi-target agents. In vitro results showed that compound 9e was the representative compound in this series, endowed with high EeAChE and HuAChE inhibitory potency (IC(50) = 1.55microM and 2.23 microM, respectively), good inhibitory activity against self-induced Abeta(1-42) aggregation (36.08% at 25 microM) and moderate antioxidant capacity (ORAC-FL value was 0.68 Trolox equivalents). Molecular docking studies rationalized the binding mode of 9e in both PAS and CAS of AChE. Moreover, 9e displayed excellent ability to against H(2) O(2) -induced PC12 cell injury and penetrate BBB. Overall, these results highlighted that compound 9e was an effective and promising multi-target agent for further anti-AD drug development.
ESTHER : Zhang_2021_Chem.Biol.Drug.Des__
PubMedSearch : Zhang_2021_Chem.Biol.Drug.Des__
PubMedID: 34143938

Title : Novel 3-benzylidene\/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease - Cao_2021_Bioorg.Med.Chem_35_116074
Author(s) : Cao Z , Song Q , Yu G , Liu Z , Cong S , Tan Z , Deng Y
Ref : Bioorganic & Medicinal Chemistry , 35 :116074 , 2021
Abstract : To discover novel multifunctional agents for the treatment of Alzheimer's disease, a series of 3-benzylidene/benzylphthalide Mannich base derivatives were designed, synthesized and evaluated. The biological screening results indicated that most of these derivatives exhibited good multifunctional activities. Among them, compound (Z)-13c raised particular interest because of its excellent multifunctional bioactivities. It displayed excellent EeAChE and HuAChE inhibition (IC(50) = 9.18 x 10(-5) and 6.16 x 10(-4) microM, respectively), good MAO-B inhibitory activity (IC(50) = 5.88 microM) and high antioxidant activity (ORAC =2.05 Trolox equivalents). Additionally, it also exhibited good antiplatelet aggregation activity, moderate self- and Cu(2+)-induced Abeta(1-42) aggregation inhibitory potency, disaggregation ability on Abeta(1-42) fibrils, biometal chelating ability, appropriate BBB permeability and significant neuroprotective effect. Furthermore, (Z)-13c can also ameliorate the learning and memory impairment induced by scopolamine in mice. These multifunctional properties highlight compound (Z)-13c as a promising candidate for further development of multifunctional drug against AD.
ESTHER : Cao_2021_Bioorg.Med.Chem_35_116074
PubMedSearch : Cao_2021_Bioorg.Med.Chem_35_116074
PubMedID: 33640707

Title : Design, synthesis, and in vitro evaluation of 4-aminoalkyl-1(2H)-phthalazinones as potential multifunctional anti-Alzheimer's disease agents - Ye_2021_Bioorg.Chem_111_104895
Author(s) : Ye C , Xu R , Cao Z , Song Q , Yu G , Shi Y , Liu Z , Liu X , Deng Y
Ref : Bioorg Chem , 111 :104895 , 2021
Abstract : A series of 4-aminoalkyl-1(2H)-phthalazinone derivatives was designed and synthesized as potential multifunctional agents for Alzheimer's disease (AD) treatment. In vitro biological assay results demonstrated that most synthesized compounds exhibited significant AChE inhibition, moderate to high MAOs inhibitory potencies and good anti-platelet aggregation abilities. Among them, compound 15b exhibited the highest inhibitory potencies towards MAO-B and MAO-A (IC(50) = 0.7 microM and 6.4 microM respectively), moderate inhibition towards AChE (IC(50) = 8.2 microM), and good activities against self- and Cu(2+)-induced Abeta(1-42) aggregation and platelet aggregation. Moreover, 15b also displayed antioxidant capacity, neuroprotective potency, anti-neuroinflammation and BBB permeability. These excellent results indicated that compound 15b could be worthy of further studies to be considered as a promising multifunctional candidate for the treatment of AD.
ESTHER : Ye_2021_Bioorg.Chem_111_104895
PubMedSearch : Ye_2021_Bioorg.Chem_111_104895
PubMedID: 33887586

Title : Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease - Luo_2020_Bioorg.Med.Chem__115400
Author(s) : Luo L , Song Q , Li Y , Cao Z , Qiang X , Tan Z , Deng Y
Ref : Bioorganic & Medicinal Chemistry , :115400 , 2020
Abstract : A series of phthalide alkyl tertiary amine derivatives were designed, synthesized and evaluated as potential multi-target agents against Alzheimer's disease (AD). The results indicated that almost all the compounds displayed significant AChE inhibitory and selective activities. Besides, most of the derivatives exhibited increased self-induced Abeta1-42 aggregation inhibitory activity compared to the lead compound dl-NBP, and some compounds also exerted good antioxidant activity. Specifically, compound I-8 showed the highest inhibitory potency toward AChE (IC50=2.66nM), which was significantly better than Donepezil (IC50=26.4nM). Moreover, molecular docking studies revealed that compound I-8 could bind to both the catalytic active site and peripheral anionic site of AChE. Furthermore, compound I-8 displayed excellent BBB permeability in vitro. Importantly, the step-down passive avoidance test indicated that I-8 significantly reversed scopolamine-induced memory deficit in mice. Collectively, these results suggested that I-8 might be a potent and selective AChE inhibitor for further anti-AD drug development.
ESTHER : Luo_2020_Bioorg.Med.Chem__115400
PubMedSearch : Luo_2020_Bioorg.Med.Chem__115400
PubMedID: 32146060

Title : Preparation of a Sensor Based on Biomass Porous Carbon\/Covalent-Organic Frame Composites for Pesticide Residues Detection - Liu_2020_Front.Chem_8_643
Author(s) : Liu Y , Zhou M , Jin C , Zeng J , Huang C , Song Q , Song Y
Ref : Front Chem , 8 :643 , 2020
Abstract : In this work, a covalent-organic framework with high carbon and nitrogen content microstructures (named COF-LZU1), assisted by 3D nitrogen-containing kenaf stem composites (represented as COF-LZU1/3D-KSCs), was constructed. Moreover, it was utilized for immobilizing acetylcholinesterase (AChE) for identifying trichlorfon, a commonly applied organophosphorus (OP) pesticide. The development of COF-LZU1/3D-KSC was affirmed by SEM, PXRD, and EDXS. The findings confirmed that COF-LZU1 microstructures were uniformly developed on 3D-KSC holes using a one-step synthesis approach, which can substantially enhance the effective surface area. Also, the COF-LZU1/3D-KSC composite contains not only the nitrogen element in COF-LZU1 but also the nitrogen element in 3D-KSC, which will greatly improve the biocompatibility of the material. The AChE/COF-LZU1/3D-KSC integrated electrode was fabricated by directly fixing a large amount of AChE on the composite. At the same time, the integrated electrode had good detection efficiency for trichlorfon. Improved stabilization, a wide-linear-range (0.2-19 ng/mL), and a lower detection limit (0.067 ng/mL) have been displayed by the sensor. Therefore, this sensor can be used as an important platform for the on-site detection of OP residue.
ESTHER : Liu_2020_Front.Chem_8_643
PubMedSearch : Liu_2020_Front.Chem_8_643
PubMedID: 33005599

Title : Insight into the Functional Diversification of Lipases in the Endoparasitoid Pteromalus puparum (Hymenoptera: Pteromalidae) by Genome-scale Annotation and Expression Analysis - Wang_2020_Insects_11_
Author(s) : Wang J , Song J , Fang Q , Yao H , Wang F , Song Q , Ye G
Ref : Insects , 11 : , 2020
Abstract : Lipases play essential roles in digestion, transport, and processing of dietary lipids in insects. For parasitoid wasps with a unique life cycle, lipase functions could be multitudinous in particular. Pteromalus puparum is a pupal endoparasitoid of butterflies. The female adult deposits eggs into its host, along with multifunctional venom, and the developing larvae consume host as its main nutrition source. Parasitoid lipases are known to participate in the food digestion process, but the mechanism remains unclear. P. puparum genome and transcriptome data were interrogated. Multiple alignments and phylogenetic trees were constructed. We annotated a total of 64 predicted lipase genes belonging to five lipase families and suggested that eight venom and four salivary lipases could determine host nutrition environment post-parasitization. Many putative venom lipases were found with incomplete catalytic triads, relatively long beta9 loops, and short lids. Data analysis reveals the loss of catalytic activities and weak triacylglycerol (TAG) hydrolytic activities of lipases in venom. Phylogenetic trees indicate various predicted functions of lipases in P. puparum. Our information enriches the database of parasitoid lipases and the knowledge of their functional diversification, providing novel insight into how parasitoid wasps manipulate host lipid storage by using venom lipases.
ESTHER : Wang_2020_Insects_11_
PubMedSearch : Wang_2020_Insects_11_
PubMedID: 32260574

Title : Flurbiprofen-chalcone hybrid Mannich base derivatives as balanced multifunctional agents against Alzheimer's disease: Design, synthesis and biological evaluation - Tian_2019_Bioorg.Chem__103477
Author(s) : Tian C , Qiang X , Song Q , Cao Z , Ye C , He Y , Deng Y , Zhang L
Ref : Bioorg Chem , :103477 , 2019
Abstract : The complex pathogenesis of Alzheimer's disease (AD) calls for multitarget approach for disease management. Herein, a series of novel flurbiprofen-chalcone hybrid Mannich base derivatives were designed and synthesized. The biological screening results indicated that most of the derivatives exhibited potent multi-target effects involved in AD. In particular, compound 6c bearing a pyrrolidine group showed the highest activities against self- and Cu(2+)-induced Abeta1-42 aggregation (70.65% and 54.89% at 25.0 microM, respectively), highly selective inhibition towards AChE and MAO-B (IC50 = 7.15 muM and 0.43 muM respectively), good antioxidant ability and metal-chelating property. Moreover, 6c displayed excellent anti-neuroinflammatory activity and appropriate BBB permeability in vitro. These outstanding results qualified compound 6c as a promising multifunctional agent for further development of disease-modifying treatment of AD.
ESTHER : Tian_2019_Bioorg.Chem__103477
PubMedSearch : Tian_2019_Bioorg.Chem__103477
PubMedID: 31818478

Title : Design, synthesis and evaluation of chalcone Mannich base derivatives as multifunctional agents for the potential treatment of Alzheimer's disease - Zhang_2019_Bioorg.Chem_87_395
Author(s) : Zhang X , Song Q , Cao Z , Li Y , Tian C , Yang Z , Zhang H , Deng Y
Ref : Bioorg Chem , 87 :395 , 2019
Abstract : A series of chalcone Mannich base derivatives were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease based on the multi-target directed ligands design strategy. In vitro assays demonstrated that most of the derivatives exerted potent selective inhibitory potency on AChE with good multifunctional properties. Among them, representative compound 7c exhibited moderate inhibitory potency for EeAChE (IC50=0.44muM) and MAO-B inhibition (IC50=1.21muM), good inhibitory effect on self-induced Abeta1-42 aggregation (55.0%, at 25muM), biometal chelating property, moderate antioxidant activity with a value 1.93-fold of Trolox. Moreover, both kinetic analysis of AChE inhibition and molecular modeling study revealed that 7c showed a mixed-type inhibition, binding simultaneously to CAS and PAS of AChE. In addition, 7c also displayed high BBB permeability. These properties indicated 7c may be a promising multifunctional agent for the treatment of AD.
ESTHER : Zhang_2019_Bioorg.Chem_87_395
PubMedSearch : Zhang_2019_Bioorg.Chem_87_395
PubMedID: 30921741

Title : Design, synthesis and evaluation of pterostilbene beta-amino alcohol derivatives as multifunctional agents for Alzheimer's disease treatment - Zheng_2018_Bioorg.Chem_78_298
Author(s) : Zheng Y , Qiang X , Xu R , Song Q , Tian C , Liu H , Li W , Tan Z , Deng Y
Ref : Bioorg Chem , 78 :298 , 2018
Abstract : A series of pterostilbene beta-amino alcohol derivatives were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease (AD). In vitro assays demonstrated that most of the derivatives were selective acetylacholinesterase (AChE) inhibitors with moderate multifunctional properties. Among them, compound 5f exhibited the best inhibitory activity for EeAChE (IC50=24.04muM), that was better than pterostilbene under our experimental condition. In addition, compound 5f displayed reasonable antioxidant activity and could confer significant neuroprotective effect against H2O2-induced PC-12 cell injury. Moreover, 5f also showed self-induced Abeta1-42 aggregation inhibitory potency and displayed high BBB permeability in vitro. These multifunctional properties highlight 5f as a promising candidate for further studies directed to the development of novel drugs against AD.
ESTHER : Zheng_2018_Bioorg.Chem_78_298
PubMedSearch : Zheng_2018_Bioorg.Chem_78_298
PubMedID: 29625269

Title : Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease - Song_2018_Bioorg.Med.Chem_26_6115
Author(s) : Song Q , Li Y , Cao Z , Liu H , Tian C , Yang Z , Qiang X , Tan Z , Deng Y
Ref : Bioorganic & Medicinal Chemistry , 26 :6115 , 2018
Abstract : A series of 2,5-dihydroxyterephthalamide derivatives were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease. In vitro assays demonstrated that most of the derivatives exhibited good multifunctional activities. Among them, compound 9d showed the best inhibitory activity against both RatAChE and EeAChE (IC50=0.56muM and 5.12muM, respectively). Moreover, 9d exhibited excellent inhibitory effects on self-induced Abeta1-42 aggregation (IC50=3.05muM) and Cu(2+)-induced Abeta1-42 aggregation (71.7% at 25.0muM), and displayed significant disaggregation ability to self- and Cu(2+)-induced Abeta1-42 aggregation fibrils (75.2% and 77.2% at 25.0muM, respectively). Furthermore, 9d also showed biometal chelating abilities, antioxidant activity, anti-neuroinflammatory activities and appropriate BBB permeability. These multifunctional properties highlight 9d as promising candidate for further studies directed to the development of novel drugs against AD.
ESTHER : Song_2018_Bioorg.Med.Chem_26_6115
PubMedSearch : Song_2018_Bioorg.Med.Chem_26_6115
PubMedID: 30470598

Title : Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and beta-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease - Xu_2018_Bioorg.Med.Chem_26_1885
Author(s) : Xu R , Xiao G , Li Y , Liu H , Song Q , Zhang X , Yang Z , Zheng Y , Tan Z , Deng Y
Ref : Bioorganic & Medicinal Chemistry , 26 :1885 , 2018
Abstract : A series of 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives were designed, synthesized and evaluated as potential multifunctional agents for the treatment of Alzheimer's disease (AD). The in vitro assays indicated that most of these derivatives were selective AChE inhibitors with good multifunctional properties. Among them, compounds 11b and 11d displayed comprehensive advantages, with good AChE (IC50=0.29+/-0.01muM and 0.46+/-0.02muM, respectively), MAO-A (IC50=8.2+/-0.08muM and 7.9+/-0.07muM, respectively) and MAO-B (IC50=20.1+/-0.16muM and 43.8+/-2.0% at 10muM, respectively) inhibitory activities, moderate self-induced Abeta1-42 aggregation inhibitory potency (35.4+/-0.42% and 48.0+/-1.53% at 25muM, respectively) and potential antioxidant activity. In addition, the two representative compounds displayed high BBB permeability in vitro. Taken together, these multifunctional properties make 11b and 11d as a promising candidate for the development of efficient drugs against AD.
ESTHER : Xu_2018_Bioorg.Med.Chem_26_1885
PubMedSearch : Xu_2018_Bioorg.Med.Chem_26_1885
PubMedID: 29500132

Title : Novel salicylamide derivatives as potent multifunctional agents for the treatment of Alzheimer's disease: Design, synthesis and biological evaluation - Song_2018_Bioorg.Chem_84_137
Author(s) : Song Q , Li Y , Cao Z , Qiang X , Tan Z , Deng Y
Ref : Bioorg Chem , 84 :137 , 2018
Abstract : A series of salicylamide derivatives were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease. In vitro assays demonstrated that most of the derivatives were selective AChE inhibitors. They showed good inhibitory activities of self- and Cu(2+)-induced Abeta1-42 aggregation, and significant antioxidant activities. Among them, compound 15b exhibited good inhibitory activity toward RatAChE and EeAChE with IC50 value of 10.4muM and 15.2muM, respectively. Moreover, 15b displayed high antioxidant activity (2.46 Trolox equivalents), good self- and Cu(2+)-induced Abeta1-42 aggregation inhibitory potency (42.5% and 31.4% at 25.0muM, respectively) and moderate disaggregation ability to self- and Cu(2+)-induced Abeta1-42 aggregation fibrils (23.4% and 27.0% at 25muM, respectively). Furthermore, 15b also showed biometal chelating abilities, anti-neuroinflammatory ability and BBB permeability. These multifunctional properties indicated compound 15b was worthy of being chosen for further pharmacokinetics, toxicity and behavioral researches to test its potential for AD treatment.
ESTHER : Song_2018_Bioorg.Chem_84_137
PubMedSearch : Song_2018_Bioorg.Chem_84_137
PubMedID: 30500523

Title : Prognostic value of immunoscore to identify mortality outcomes in adults with HBV-related primary hepatocellular carcinoma - Yao_2017_Medicine.(Baltimore)_96_e6735
Author(s) : Yao Q , Bao X , Xue R , Liu H , Li J , Dong J , Duan Z , Ren M , Zhao J , Song Q , Yu H , Zhu Y , Lu J , Meng Q
Ref : Medicine (Baltimore) , 96 :e6735 , 2017
Abstract : This study aimed to determine if the immunoscore (IS) staging system would be a potential prognostic factor in hepatitis B virus-related hepatocellular carcinoma (HBV-HCC) in China.IS was performed in a consecutive cohort of HBV-HCC patients (n= 92). CD3+, CD8+, and CD45RO+ T cells were quantified by immunohistochemical analyses. The patients were stratified into 5 IS groups: I0, I1, I2, I3, I4 for every 2 cell phenotypes (IS1 (CD8/CD45RO, IS2 (CD3/CD8), and IS3 (CD3/CD45RO), respectively. ImagePro Plus software was used in the calculation of the paraffin-embedded tumor sections.The staining of CD3+, CD8+, and CD45RO+ cells in the HBV-HCC tissue demonstrated that there were higher density and larger area of lymphocytes in the invasive margins (IM) region than in the center (CT). Univariate analysis showed that preoperative TNM staging (P = .01), serum gamma-glutamyl transpeptidase (GGT) level (P = .03), vascular invasion (P = .00), and density of CD3+T (CT) (P = 0.01) were correlated significantly with disease-free survival (DFS); serum alpha-fetoprotein (AFP) level (P = .02), tumor size (P = .00), serum cholinesterase (CHE) (P = .04), and GGT level (P = .01), density of CD3+T(CT) (P = .00), CD8+T(CT)(P = .00), CD45RO+T(CT) (P = .00), and CD45RO+T (IM) (P = .02) were correlated with overall survival (OS). Multivariate analysis showed that TNM staging was not an independent prognostic factor of DFS and OS. Our results showed ISs did not have a significantly correlation with DFS (P = .35, .19, and .07, respectively), but it was correlated significantly with OS (P = .00, .00, and .00, respectively). There were statistical differences among the OS of every ISs subgroup except I0 and I1 by the Cox regressions analysis.The IS staging was closely related to the outcome of patients. It can compensate the TNM tumor classification system in predicting the prognosis of HBV-HCC patients.
ESTHER : Yao_2017_Medicine.(Baltimore)_96_e6735
PubMedSearch : Yao_2017_Medicine.(Baltimore)_96_e6735
PubMedID: 28445292

Title : Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease - Sang_2017_Eur.J.Med.Chem_135_307
Author(s) : Sang Z , Qiang X , Li Y , Xu R , Cao Z , Song Q , Wang T , Zhang X , Liu H , Tan Z , Deng Y
Ref : Eur Journal of Medicinal Chemistry , 135 :307 , 2017
Abstract : A series of scutellarein-O-acetamidoalkylbenzylamines derivatives were designed based on a multitarget-directed ligands strategy for the treatment of Alzheimer's disease. Among these compounds, compound T-22 demonstrated excellent acetylcholinesterase inhibitory, moderate inhibitory effects on self-induced Abeta1-42 aggregation, Cu2+-induced Abeta1-42 aggregation, human AChE-induced Abeta1-40 aggregation and disassembled Cu2+-induced aggregation of the well-structured Abeta1-42 fibrils, and also acted as potential antioxidant and biometals chelator. Both kinetic analysis of AChE inhibition and molecular modeling study suggested that T-22 interacted with both the catalytic active site and peripheral anionic site of AChE. Moreover, compound T-22 showed a good neuroprotective effect against H2O2-induced PC12 cell injury and low toxicity in SH-SY5Y cells. Furthermore, the step-down passive avoidance test indicated T-22 significantly reversed scopolamine-induced memory deficit in mice. Taken together, the data showed that T-22 was an interesting multifunctional lead compound worthy of further study for AD.
ESTHER : Sang_2017_Eur.J.Med.Chem_135_307
PubMedSearch : Sang_2017_Eur.J.Med.Chem_135_307
PubMedID: 28458136

Title : Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and beta-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease - Luo_2017_Bioorg.Med.Chem_25_1997
Author(s) : Luo L , Li Y , Qiang X , Cao Z , Xu R , Yang X , Xiao G , Song Q , Tan Z , Deng Y
Ref : Bioorganic & Medicinal Chemistry , 25 :1997 , 2017
Abstract : A series of 1-hydroxyl-3-aminoalkoxy-thioxanthone derivatives were designed, synthesized and evaluated as potential multifunctional agents against Alzheimer's disease (AD). The results indicated that most of these compounds exhibited good AChE and MAOs inhibitory activities, significant inhibition of self- and Cu2+-induced Abeta1-42 aggregation, and moderate to good antioxidant activities. Specifically, compound 9e displayed high inhibitory potency toward AChE (IC50=0.59+/-0.02muM), MAO-A and MAO-B (IC50=1.01+/-0.02muM and 0.90+/-0.01muM respectively), excellent efficiency to block both self- and Cu2+-induced Abeta1-42 aggregation (74.8+/-1.2% and 87.7+/-1.9% at 25muM, respectively), good metal-chelating property and a low toxicity in SH-SY5Y cells. Furthermore, kinetic and molecular modeling studies revealed that compound 9e binds simultaneously to the catalytic active site and peripheral anionic site of AChE, and could penetrate the BBB. Collectively, these results suggested that 9e might be a potential multifunctional agent for further development in the treatment of AD.
ESTHER : Luo_2017_Bioorg.Med.Chem_25_1997
PubMedSearch : Luo_2017_Bioorg.Med.Chem_25_1997
PubMedID: 28237559

Title : Crystal Structure of StnA for the Biosynthesis of Antitumor Drug Streptonigrin Reveals a Unique Substrate Binding Mode - Qian_2017_Sci.Rep_7_40254
Author(s) : Qian T , Wo J , Zhang Y , Song Q , Feng G , Luo R , Lin S , Wu G , Chen HF
Ref : Sci Rep , 7 :40254 , 2017
Abstract : Streptonigrin methylesterase A (StnA) is one of the tailoring enzymes that modify the aminoquinone skeleton in the biosynthesis pathway of Streptomyces species. Although StnA has no significant sequence homology with the reported alpha/beta-fold hydrolases, it shows typical hydrolytic activity in vivo and in vitro. In order to reveal its functional characteristics, the crystal structures of the selenomethionine substituted StnA (SeMet-StnA) and the complex (S185A mutant) with its substrate were resolved to the resolution of 2.71 A and 2.90 A, respectively. The overall structure of StnA can be described as an alpha-helix cap domain on top of a common alpha/beta hydrolase domain. The substrate methyl ester of 10'-demethoxystreptonigrin binds in a hydrophobic pocket that mainly consists of cap domain residues and is close to the catalytic triad Ser185-His349-Asp308. The transition state is stabilized by an oxyanion hole formed by the backbone amides of Ala102 and Leu186. The substrate binding appears to be dominated by interactions with several specific hydrophobic contacts and hydrogen bonds in the cap domain. The molecular dynamics simulation and site-directed mutagenesis confirmed the important roles of the key interacting residues in the cap domain. Structural alignment and phylogenetic tree analysis indicate that StnA represents a new subfamily of lipolytic enzymes with the specific binding pocket located at the cap domain instead of the interface between the two domains.
ESTHER : Qian_2017_Sci.Rep_7_40254
PubMedSearch : Qian_2017_Sci.Rep_7_40254
PubMedID: 28074848
Gene_locus related to this paper: 9actn-l7pij2

Title : Effect of the R92H and A379V genotypes of platelet-activating factor acetylhydrolase on its enzyme activity, oxidative stress and metabolic profile in Chinese women with polycystic ovary syndrome - Zhang_2017_Lipids.Health.Dis_16_57
Author(s) : Zhang R , Song Q , Liu H , Bai H , Zhang Y , Liu Q , Guan L , Fan P
Ref : Lipids Health Dis , 16 :57 , 2017
Abstract : BACKGROUND: The G994T polymorphism in platelet-activating factor acetylhydrolase (PAF-AH) gene is associated with the risk of polycystic ovary syndrome (PCOS). The aim of this study was to investigate the relationship between R92H and A379V variants of the PAF-AH gene and the risk of PCOS and to evaluate the effects of the genotypes on PAF-AH activities and clinical, metabolic and oxidative stress indexes in Chinese women.
METHODS: A total of 862 patients with PCOS based on the Rotterdam consensus criteria and 750 control women from a population of Chinese Han nationality in the Chengdu area were studied from 2006-2015. PAF-AH genotypes were determined by PCR and restriction fragment length polymorphism analysis. Plasma PAF-AH, high-density lipoprotein (HDL)-associated PAF-AH (H-PAF-AH) and apolipoprotein (apo) B-containing lipoprotein-associated PAF-AH (apoB-PAF-AH) activities were measured using the trichloroacetic acid precipitation procedure with PAF C-16 as a substrate. Circulating markers of oxidative stress, including serum total oxidant status, total antioxidant capacity, oxidative stress index and malondialdehyde levels, and clinical and metabolic parameters were also analyzed.
RESULTS: No significant differences were observed in the frequencies of R92H and A379V genotypes and alleles of the PAF-AH gene between PCOS and control groups (P > 0.05). Compared with patients with the 92RR genotype, patients with H allele of R92H (RH + HH genotype) had significantly higher plasma PAF-AH and apoB-PAF-AH activities (P < 0.05) and tended to exhibit increased H-PAF-AH activity (P = 0.063) after adjusted for age and BMI. However, when serum LDL-C, HDL-C, TG and HOMA index were added as covariates, the comparisons no longer remained statistical significance (P > 0.05). There were no significant differences in clinical, hormonal, metabolic and circulating oxidative stress parameters and the frequencies of PAF-AH G449T genotype according to PAF-AH R92H or A379V genotyping in patients with PCOS and control women.
CONCLUSIONS: There were no significant associations between R92H and A379V variants of PAF-AH gene and risk of PCOS in Chinese women. The increased plasma PAF-AH and apoB-PAF-AH activities in patients with H allele of R92H are related to the R92 --> H variation, changes in plasma lipoprotein levels, insulin resistance, aging, and gaining weight and thus may be involved in the pathogenesis of PCOS and the increased risks of future cardiovascular diseases.
ESTHER : Zhang_2017_Lipids.Health.Dis_16_57
PubMedSearch : Zhang_2017_Lipids.Health.Dis_16_57
PubMedID: 28320416

Title : A reference genome for common bean and genome-wide analysis of dual domestications - Schmutz_2014_Nat.Genet_46_707
Author(s) : Schmutz J , McClean PE , Mamidi S , Wu GA , Cannon SB , Grimwood J , Jenkins J , Shu S , Song Q , Chavarro C , Torres-Torres M , Geffroy V , Moghaddam SM , Gao D , Abernathy B , Barry K , Blair M , Brick MA , Chovatia M , Gepts P , Goodstein DM , Gonzales M , Hellsten U , Hyten DL , Jia G , Kelly JD , Kudrna D , Lee R , Richard MM , Miklas PN , Osorno JM , Rodrigues J , Thareau V , Urrea CA , Wang M , Yu Y , Zhang M , Wing RA , Cregan PB , Rokhsar DS , Jackson SA
Ref : Nat Genet , 46 :707 , 2014
Abstract : Common bean (Phaseolus vulgaris L.) is the most important grain legume for human consumption and has a role in sustainable agriculture owing to its ability to fix atmospheric nitrogen. We assembled 473 Mb of the 587-Mb genome and genetically anchored 98% of this sequence in 11 chromosome-scale pseudomolecules. We compared the genome for the common bean against the soybean genome to find changes in soybean resulting from polyploidy. Using resequencing of 60 wild individuals and 100 landraces from the genetically differentiated Mesoamerican and Andean gene pools, we confirmed 2 independent domestications from genetic pools that diverged before human colonization. Less than 10% of the 74 Mb of sequence putatively involved in domestication was shared by the two domestication events. We identified a set of genes linked with increased leaf and seed size and combined these results with quantitative trait locus data from Mesoamerican cultivars. Genes affected by domestication may be useful for genomics-enabled crop improvement.
ESTHER : Schmutz_2014_Nat.Genet_46_707
PubMedSearch : Schmutz_2014_Nat.Genet_46_707
PubMedID: 24908249
Gene_locus related to this paper: phavu-v7azs2 , phavu-v7awu7 , phavu-v7bpt6 , phavu-v7b6k3 , phavu-v7cry4

Title : miR-124 represses ROCK1 expression to promote neurite elongation through activation of the PI3K\/Akt signal pathway - Gu_2014_J.Mol.Neurosci_52_156
Author(s) : Gu X , Meng S , Liu S , Jia C , Fang Y , Li S , Fu C , Song Q , Lin L , Wang X
Ref : Journal of Molecular Neuroscience , 52 :156 , 2014
Abstract : Recent studies have demonstrated an important role for miR-124, the most abundant and well-conserved brain-specific microRNA(miRNA), in promoting neurite outgrowth and elongation during neuronal differentiation. This miRNA's target genes and the mechanisms that execute this role remain unclear. In this study, we identified ROCK1, a small GTPase Rho kinase, as a direct target of miR-124 for regulating neurite elongation. miR-124 significantly inhibited ROCK1 expression in M17 cells. Inhibiting ROCK1 promoted neurite elongation, and the overexpression of ROCK1 strongly repressed the neurite elongation-enhancing effect of miR-124 in M17 cells. We determined that Akt functions as a novel ROCK1 downstream effector in regulating neurite outgrowth and elongation.
ESTHER : Gu_2014_J.Mol.Neurosci_52_156
PubMedSearch : Gu_2014_J.Mol.Neurosci_52_156
PubMedID: 24338057

Title : Lactoferrin-modified PEG-co-PCL nanoparticles for enhanced brain delivery of NAP peptide following intranasal administration - Liu_2013_Biomaterials_34_3870
Author(s) : Liu Z , Jiang M , Kang T , Miao D , Gu G , Song Q , Yao L , Hu Q , Tu Y , Pang Z , Chen H , Jiang X , Gao X , Chen J
Ref : Biomaterials , 34 :3870 , 2013
Abstract : Development of effective non-invasive drug delivery systems is of great importance to the treatment of Alzheimer's diseases and has made great progress in recent years. In this work, lactoferrin (Lf), a natural iron binding protein, whose receptor is highly expressed in both respiratory epithelial cells and neurons is here utilized to facilitate the nose-to-brain drug delivery of neuroprotection peptides. The Lf-conjugated PEG-PCL nanoparticle (Lf-NP) was constructed via a maleimide-thiol reaction with the Lf conjugation confirmed by CBQCA Protein Quantitation and XPS analysis. Other important parameters such as particle size distribution, zeta potential and in vitro release of fluorescent probes were also characterized. Compared with unmodified nanoparticles (NP), Lf-NP exhibited a significantly enhanced cellular accumulation in 16HBE14o-cells through both caveolae-/clathrin-mediated endocytosis and direct translocation. Following intranasal administration, Lf-NP facilitated the brain distribution of the coumarin-6 incorporated with the AUC0-8h in rat cerebrum (with hippocampus removed), cerebellum, olfactory tract, olfactory bulb and hippocampus 1.36, 1.53, 1.70, 1.57 and 1.23 times higher than that of coumarin-6 carried by NP, respectively. Using a neuroprotective peptide - NAPVSIPQ (NAP) as the model drug, the neuroprotective and memory improvement effect of Lf-NP was observed even at lower dose than that of NP in a Morris water maze experiment, which was also confirmed by the evaluation of acetylcholinesterase, choline acetyltransferase activity and neuronal degeneration in the mice hippocampus. In conclusion, Lf-NP may serve as a promising nose-to-brain drug delivery carrier especially for peptides and proteins.
ESTHER : Liu_2013_Biomaterials_34_3870
PubMedSearch : Liu_2013_Biomaterials_34_3870
PubMedID: 23453061

Title : Identification of lipases involved in PBAN stimulated pheromone production in Bombyx mori using the DGE and RNAi approaches - Du_2012_PLoS.One_7_e31045
Author(s) : Du M , Yin X , Zhang S , Zhu B , Song Q , An S
Ref : PLoS ONE , 7 :e31045 , 2012
Abstract : BACKGROUND: Pheromone biosynthesis activating neuropeptide (PBAN) is a neurohormone that regulates sex pheromone synthesis in female moths. Bombyx mori is a model organism that has been used to explore the signal transduction pattern of PBAN, which is mediated by a G-protein coupled receptor (GPCR). Although significant progress has been made in elucidating PBAN-regulated lipolysis that releases the precursor of the sex pheromone, little is known about the molecular components involved in this step. To better elucidate the molecular mechanisms of PBAN-stimulated lipolysis of cytoplasmic lipid droplets (LDs), the associated lipase genes involved in PBAN- regulated sex pheromone biosynthesis were identified using digital gene expression (DGE) and subsequent RNA interference (RNAi). RESULTS: Three DGE libraries were constructed from pheromone glands (PGs) at different developed stages, namely, 72 hours before eclosion (-72 h), new emergence (0 h) and 72 h after eclosion (72 h), to investigate the gene expression profiles during PG development. The DGE evaluated over 5.6 million clean tags in each PG sample and revealed numerous genes that were differentially expressed at these stages. Most importantly, seven lipases were found to be richly expressed during the key stage of sex pheromone synthesis and release (new emergence). RNAi-mediated knockdown confirmed for the first time that four of these seven lipases play important roles in sex pheromone synthesis. CONCLUSION: This study has identified four lipases directly involved in PBAN-stimulated sex pheromone biosynthesis, which improve our understanding of the lipases involved in releasing bombykol precursors from triacylglycerols (TAGs) within the cytoplasmic LDs.
ESTHER : Du_2012_PLoS.One_7_e31045
PubMedSearch : Du_2012_PLoS.One_7_e31045
PubMedID: 22359564

Title : Identification of the G994T polymorphism in exon 9 of plasma platelet-activating factor acetylhydrolase gene as a risk factor for polycystic ovary syndrome - Fan_2010_Hum.Reprod_25_1288
Author(s) : Fan P , Liu Hw , Wang XS , Zhang F , Song Q , Li Q , Wu HM , Bai H
Ref : Hum Reprod , 25 :1288 , 2010
Abstract : BACKGROUND: Low-grade chronic inflammation and greater risks of cardiovascular diseases are often present in patients with polycystic ovary syndrome (PCOS). Platelet-activating factor (PAF) acetylhydrolase (PAF-AH) hydrolyzes and inactivates PAF and PAF-like oxidized phospholipids that are potent lipid mediators involved in inflammation and atherosclerosis. Deficiency of this enzyme is caused by a missense mutation (G994 --> T) in exon 9 of the plasma PAF-AH gene. The aim of the study was to investigate a possible association of this polymorphism with the risk of PCOS and to evaluate the effects of the genotype on the activity and distribution of PAFAH in Chinese patients.
METHODS: A total of 661 subjects (346 patients with PCOS and 315 healthy control women) from a population of Chinese Han nationality in Chengdu area were included in this study. PAFAH G994T genotype was studied using PCR and restriction fragment length polymorphism analysis. Total plasma PAF-AH, high-density lipoprotein (HDL)-associated PAF-AH (H-PAF-AH) and low-density lipoprotein (LDL)-associated PAF-AH (L-PAF-AH) activities were measured by the trichloroacetic acid precipitation procedure using [(3)H-acetyl] PAF and PAF C-16 as a substrate.
RESULTS: The prevalence of the mutant genotype (GT + TT) was significantly more frequent in patients with PCOS than in control subjects (12.7 versus 6.0%, P = 0.003). Genotype (GT + TT) remained a significant predictor for PCOS (P = 0.020) in prognostic models including age, body mass index, insulin resistance index, triglyceride, HDL and LDL as covariates. There was a significant difference in plasma PAF-AH, L-PAF-AH and H-PAF-AH activities between GG and GT genotypes in both the patient and control groups. The ratio of L-PAF-AH to H-PAF-AH activities was significantly higher after adjustment for multiple variables in patients with GT genotype compared with patients with GG genotype (P = 0.003). There were no significant differences in clinical, biochemical and metabolic parameters according to PAFAH G994T genotyping in patients with PCOS and control women.
CONCLUSIONS: The G994T polymorphism in PAFAH gene may be one of the genetic determinants for PCOS in Chinese Han women.
ESTHER : Fan_2010_Hum.Reprod_25_1288
PubMedSearch : Fan_2010_Hum.Reprod_25_1288
PubMedID: 20185515
Gene_locus related to this paper: human-PLA2G7

Title : Genome sequence of the palaeopolyploid soybean - Schmutz_2010_Nature_463_178
Author(s) : Schmutz J , Cannon SB , Schlueter J , Ma J , Mitros T , Nelson W , Hyten DL , Song Q , Thelen JJ , Cheng J , Xu D , Hellsten U , May GD , Yu Y , Sakurai T , Umezawa T , Bhattacharyya MK , Sandhu D , Valliyodan B , Lindquist E , Peto M , Grant D , Shu S , Goodstein D , Barry K , Futrell-Griggs M , Abernathy B , Du J , Tian Z , Zhu L , Gill N , Joshi T , Libault M , Sethuraman A , Zhang XC , Shinozaki K , Nguyen HT , Wing RA , Cregan P , Specht J , Grimwood J , Rokhsar D , Stacey G , Shoemaker RC , Jackson SA
Ref : Nature , 463 :178 , 2010
Abstract : Soybean (Glycine max) is one of the most important crop plants for seed protein and oil content, and for its capacity to fix atmospheric nitrogen through symbioses with soil-borne microorganisms. We sequenced the 1.1-gigabase genome by a whole-genome shotgun approach and integrated it with physical and high-density genetic maps to create a chromosome-scale draft sequence assembly. We predict 46,430 protein-coding genes, 70% more than Arabidopsis and similar to the poplar genome which, like soybean, is an ancient polyploid (palaeopolyploid). About 78% of the predicted genes occur in chromosome ends, which comprise less than one-half of the genome but account for nearly all of the genetic recombination. Genome duplications occurred at approximately 59 and 13 million years ago, resulting in a highly duplicated genome with nearly 75% of the genes present in multiple copies. The two duplication events were followed by gene diversification and loss, and numerous chromosome rearrangements. An accurate soybean genome sequence will facilitate the identification of the genetic basis of many soybean traits, and accelerate the creation of improved soybean varieties.
ESTHER : Schmutz_2010_Nature_463_178
PubMedSearch : Schmutz_2010_Nature_463_178
PubMedID: 20075913
Gene_locus related to this paper: soybn-c6t4m5 , soybn-c6t4p4 , soybn-c6tav4 , soybn-c6tdf9 , soybn-c6tiz7 , soybn-c6tmg3 , soybn-i1jgq5 , soybn-i1kpj2 , soybn-i1kwe7 , soybn-i1l7e3 , soybn-i1l497 , soybn-i1ll09 , soybn-i1lpi4 , soybn-i1jcw2 , soybn-i1jcw3 , soybn-i1jcw4 , soybn-i1jcw7 , soybn-i1k217 , soybn-i1kfz3 , soybn-i1lhi0 , soybn-k7k6s4 , soybn-i1jtw1 , soybn-c6tas4 , soybn-i1m910 , soybn-c6t7k8 , soybn-i1k636 , soybn-i1kju7 , soybn-i1j4c6 , soybn-i1lbk2 , soybn-i1jqy5 , soybn-i1nbj8 , soybn-i1j855 , soybn-i1l5a3 , soybn-k7mt28 , soybn-i1lau7 , soybn-i1lay0 , soybn-i1net3 , soybn-i1jr09 , soybn-i1ms08 , soybn-i1mmh5 , soybn-i1mly5 , soybn-i1mmh3 , soybn-i1mmh4 , soybn-i1ngu7 , soybn-k7ll20 , soybn-i1mly4 , soybn-a0a0r0i9y7 , soybn-a0a0r0j241 , soybn-i1les8 , soybn-k7n313 , soybn-i1kfj1 , soybn-a0a0r0k7x4 , soybn-i1ly30 , soybn-i1mwr8 , soybn-i1kfg5 , soybn-i1kly2 , soybn-a0a0r0ixi2 , soybn-i1jew0 , glyso-a0a445l5n1 , soybn-i1kfz9 , soybn-i1jqs1 , soybn-i1nbc7 , soybn-k7mm57 , soybn-a0a0r0fec7 , soybn-a0a0r0hcn9 , soybn-i1jx17 , soybn-k7kvv2 , soybn-i1kcl6 , soybn-i1kcl7 , soybn-i1jrc3 , soybn-i1nbz1 , soybn-a0a0r0euk2 , soybn-a0a0r0fx16 , soybn-a0a0r0k3t3 , soybn-i1kuc7 , soybn-i1lvy4

Title : Studies on a novel carbon source and cosolvent for lipase production by Candida rugosa - Wei_2004_J.Ind.Microbiol.Biotechnol_31_133
Author(s) : Wei D , Zhang LY , Song Q
Ref : J Ind Microbiol Biotechnol , 31 :133 , 2004
Abstract : Oleic acid esters were shown to be the best carbon source for both cell growth and lipase production by Candida rugosa. Use of a cosolvent, dodecane, in fermentations improved the solubility of solid substrates and increased oxygen solubility. This resulted in the highest lipase activity in batch fermentation with glycerol trioleate and dodecane. Lipase activity reached 77.1 units ml(-1).
ESTHER : Wei_2004_J.Ind.Microbiol.Biotechnol_31_133
PubMedSearch : Wei_2004_J.Ind.Microbiol.Biotechnol_31_133
PubMedID: 15069604

Title : Cloning and characterization of a human protein phosphatase 1-encoding cDNA - Song_1993_Gene_129_291
Author(s) : Song Q , Khanna KK , Lu H , Lavin MF
Ref : Gene , 129 :291 , 1993
Abstract : While sequence information is available for a number of eukaryotic protein phosphatase 1 (PP1)-encoding genes, the cloning and characterization of a complete human pp1 gene has not been reported. We have used two conserved regions within the pp1 family of genes to synthesize oligodeoxyribonucleotide primers for the amplification of a 438-bp sequence from human mRNA. This DNA fragment was sequenced to verify that it corresponded to a pp1 cDNA and it was used to screen a human cDNA library to isolate a full-length clone. The deduced amino acid (aa) sequence identified a protein of 330 aa in length. Comparison with the rabbit pp1 cDNA sequence showed some nucleotide differences, largely at the third position of the codon, with complete concordance at the aa level. Northern blot analysis revealed an mRNA of approximately 1.6 kb.
ESTHER : Song_1993_Gene_129_291
PubMedSearch : Song_1993_Gene_129_291
PubMedID: 8392016