Ahemad N

References (18)

Title : Nutritional and medicinal plants as potential sources of enzyme inhibitors toward the bioactive functional foods: an updated review - Saleem_2023_Crit.Rev.Food.Sci.Nutr__1
Author(s) : Saleem H , Yaqub A , Rafique R , Ali Chohan T , Malik DE , Tousif MI , Khurshid U , Ahemad N , Ramasubburayan R , Rengasamy KR
Ref : Crit Rev Food Sci Nutr , :1 , 2023
Abstract : Enzymes are biologically active complex protein molecules that catalyze most chemical reactions in living organisms, and their inhibitors accelerate biological processes. This review emphasizes medicinal food plants and their isolated chemicals inhibiting clinically important enzymes in common diseases. A mechanistic overview was investigated to explain the mechanism of these food bases enzyme inhibitors. The enzyme inhibition potential of medicinal food plants and their isolated substances was searched in Ovid, PubMed, Science Direct, Scopus, and Google Scholar. Cholinesterase, amylase, glucosidase, xanthine oxidase, tyrosinase, urease, lipoxygenase, and others were inhibited by crude extracts, solvent fractions, or isolated pure chemicals from medicinal food plants. Several natural compounds have shown tyrosinase inhibition potential, including quercetin, glabridin, phloretin-4-O-beta-D-glucopyranoside, lupinalbin, and others. Some of these compounds' inhibitory kinetics and molecular mechanisms are also discussed. Phenolics and flavonoids inhibit enzyme activity best among the secondary metabolites investigated. Several studies showed flavonoids' significant antioxidant and anti-inflammatory activities, highlighting their medicinal potential. Overall, many medicinal food plants, their crude extracts/fractions, and isolated compounds have been studied, and some promising compounds depending on the enzyme have been found. Still, more studies are recommended to derive potential pharmacologically active functional foods.
ESTHER : Saleem_2023_Crit.Rev.Food.Sci.Nutr__1
PubMedSearch : Saleem_2023_Crit.Rev.Food.Sci.Nutr__1
PubMedID: 37255100

Title : Development of substituted benzylidene derivatives as novel dual cholinesterase inhibitors for Alzheimer's treatment - Gupta_2023_RSC.Adv_13_26344
Author(s) : Gupta SM , Behera A , Jain NK , Tripathi A , Rishipathak D , Singh S , Ahemad N , Erol M , Kumar D
Ref : RSC Adv , 13 :26344 , 2023
Abstract : Leading pathological markers of Alzheimer's disease (AD) include Acetylcholinesterase (AChE), Butyrylcholinesterase (BuChE), Amyloid beta (Abeta) and reactive oxygen species (ROS). Indole derivatives were identified and optimized to improve the potency against AChE, BuChE, Abeta and ROS. The lead molecule IND-30 was found to be selective for AChE (selectivity ratio: 22.92) in comparison to BuChE and showed maximum inhibition potential for human AChE (IC(50): 4.16 +/- 0.063 microM). IND-30 was found to be safe on the SH-SY5Y cell line until the dose of 30 mM. Further, molecule IND-30 was evaluated for its ability to inhibit AChE-induced Abeta aggregation at 0.5, 10 and 20 microM doses. Approximately, 50% of AChE-induced Abeta aggregation was inhibited by IND-30. Thus, IND-30 was found to be multitargeting for AD.
ESTHER : Gupta_2023_RSC.Adv_13_26344
PubMedSearch : Gupta_2023_RSC.Adv_13_26344
PubMedID: 37671344

Title : A comprehensive phytochemical, biological, and toxicological studies of roots and aerial parts of Crotalaria burhia Buch.-Ham: An important medicinal plant - Anwar_2022_Front.Plant.Sci_13_988352
Author(s) : Anwar S , Faisal Nadeem M , Pervaiz I , Khurshid U , Akmal N , Aamir K , Haseeb Ur Rehman M , Almansour K , Alshammari F , Shaikh MF , Locatelli M , Ahemad N , Saleem H
Ref : Front Plant Sci , 13 :988352 , 2022
Abstract : This study was designed to seek the phytochemical analysis, antioxidant, enzyme inhibition, and toxicity potentials of methanol and dichloromethane (DCM) extracts of aerial and root parts of Crotalaria burhia. Total bioactive content, high-performance liquid chromatography-photodiode array detector (HPLC-PDA) polyphenolic quantification, and ultra-high performance liquid chromatography-mass spectrometry (UHPLC-MS) analysis were utilized to evaluate the phytochemical composition. Antioxidant [including 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH)], 2,2'-azino-bis[3-ethylbenzothiazoline-6-sulfonic acid (ABTS), ferric reducing antioxidant power assay (FRAP), cupric reducing antioxidant capacity CUPRAC, phosphomolybdenum, and metal chelation assays] and enzyme inhibition [against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), alpha-glucosidase, alpha-amylase, and tyrosinase] assays were carried out for biological evaluation. The cytotoxicity was tested against MCF-7 and MDA-MB-231 breast cell lines. The root-methanol extract contained the highest levels of phenolics (37.69 mg gallic acid equivalent/g extract) and flavonoids (83.0 mg quercetin equivalent/g extract) contents, and was also the most active for DPPH (50.04 mg Trolox equivalent/g extract) and CUPRAC (139.96 mg Trolox equivalent /g extract) antioxidant assays. Likewise, the aerial-methanol extract exhibited maximum activity for ABTS (94.05 mg Trolox equivalent/g extract) and FRAP (64.23 mg Trolox equivalent/g extract) assays. The aerial-DCM extract was noted to be a convincing cholinesterase (AChE; 4.01 and BChE; 4.28 mg galantamine equivalent/g extract), and alpha-glucosidase inhibitor (1.92 mmol acarbose equivalent/g extract). All of the extracts exhibited weak to modest toxicity against the tested cell lines. A considerable quantities of gallic acid, catechin, 4-OH benzoic acid, syringic acid, vanillic acid, 3-OH-4-MeO benzaldehyde, epicatechin, p-coumaric acid, rutin, naringenin, and carvacrol were quantified via HPLC-PDA analysis. UHPLC-MS analysis of methanolic extracts from roots and aerial parts revealed the tentative identification of important phytoconstituents such as polyphenols, saponins, flavonoids, and glycoside derivatives. To conclude, this plant could be considered a promising source of origin for bioactive compounds with several therapeutic uses.
ESTHER : Anwar_2022_Front.Plant.Sci_13_988352
PubMedSearch : Anwar_2022_Front.Plant.Sci_13_988352
PubMedID: 36212347

Title : New insights into the phytochemical composition, enzyme inhibition and antioxidant properties of desert cotton (Aerva javanica (Bum.f) Shult. -Amaranthaceae) - Saleem_2021_Nat.Prod.Res_35_664
Author(s) : Saleem H , Zengin G , Khan KU , Ahmad I , Waqas M , Mahomoodally FM , Rengasamy KRR , Zainol N , Abidin SAZ , Ahemad N
Ref : Nat Prod Res , 35 :664 , 2021
Abstract : This study sets out to probe into total bioactive contents, UHPLC-MS secondary metabolites profiling, antioxidant (DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum and metal chelating) and enzyme inhibitory (acetylcholinesterase- AChE, butyrylcholinesterase- BChE, alpha-amylase, alpha glucosidase, and tyrosinase) activities of methanol extract of Aerva javanica, also known as desert cotton or Kapok bush. Aerva javanica contains considerable phenolic (44.79 +/- 3.12 mg GAE/g) and flavonoid (28.86 +/- 0.12 mg QE/g) contents which tends to correlate with its significant antioxidant potential for ABTS, FRAP and CUPRAC assays with values of 101.41 +/- 1.18, 124.10 +/- 1.71 and 190.22 +/- 5.70 mg TE/g, respectively. The UHPLC-MS analysis identified the presence of 45 phytochemicals belonging to six major groups: phenolic, flavonoids, lignin, terpenes, glycoside and alkaloid. Moreover, the plant extract also showed potent inhibitory action against AChE (3.73 +/- 0.22 mg GALAE/g), BChE (3.31 +/- 0.19 mg GALAE/g) and tyrosinase (126.05 +/- 1.77 mg KAE/g). The observed results suggest A. javanica could be further explored as a natural source of bioactive compounds.
ESTHER : Saleem_2021_Nat.Prod.Res_35_664
PubMedSearch : Saleem_2021_Nat.Prod.Res_35_664
PubMedID: 30919661

Title : A comprehensive phytochemical, biological, toxicological and molecular docking evaluation of Suaeda fruticosa (L.) Forssk.: An edible halophyte medicinal plant - Saleem_2021_Food.Chem.Toxicol__112348
Author(s) : Saleem H , Khurshid U , Sarfraz M , Tousif MI , Alamri A , Anwar S , Ahmad I , Abdallah HH , Mahomoodally FM , Ahemad N
Ref : Food & Chemical Toxicology , :112348 , 2021
Abstract : Suaeda fruticosa is an edible medicinal halophyte known for its traditional uses. In this study, methanol and dichloromethane extracts of S. fruticosa were explored for phytochemical, biological and toxicological parameters. Total phenolic and flavonoid constituents were determined by using standard aluminum chloride and Folin-Ciocalteu methods, and UHPLC-MS analysis of methanol extract was performed for tentative identification of secondary metabolites. Different standard methods like DPPH, ABTS, FRAP, CUPRAC, total antioxidant capacity (TAC), and metal chelation assays were utilized to find out the antioxidant potential of extracts. Enzyme inhibition studies of extracts against acetylcholinesterase, butyrylcholinesterase, tyrosinase, alpha-amylase and, alpha-glucosidase enzymes were also studied. Likewise, the cytotoxicity was also assessed against MCF-7, MDA-MB-231, and DU-145 cell lines. The higher phenolic and flavonoids contents were observed in methanol extracts which can be correlated to its higher radical scavenging potential. Similarly, 11 different secondary metabolites were tentatively identified by UHPLC profiling. Both the extract showed significant inhibition against all the enzymes except for alpha-glucosidase. Moreover, docking studies were also performed against the tested enzymes. In the case of cytotoxicity, both the samples were found moderately toxic against the tested cell lines. This plant can be explored further for its potential therapeutic and edible uses.
ESTHER : Saleem_2021_Food.Chem.Toxicol__112348
PubMedSearch : Saleem_2021_Food.Chem.Toxicol__112348
PubMedID: 34144099

Title : Investigation into the biological properties, secondary metabolites composition, and toxicity of aerial and root parts of Capparis spinosa L.: An important medicinal food plant - Saleem_2021_Food.Chem.Toxicol__112404
Author(s) : Saleem H , Khurshid U , Sarfraz M , Ahmad I , Alamri A , Anwar S , Alamri AS , Locatelli M , Tartaglia A , Mahomoodally MF , Zainal Abidin SA , Ahemad N
Ref : Food & Chemical Toxicology , :112404 , 2021
Abstract : Capparis spinose L. also known as Caper is of great significance as a traditional medicinal food plant. The present work was targeted on the determination of chemical composition, pharmacological properties, and in-vitro toxicity of methanol and dichloromethane (DCM) extracts of different parts of C. spinosa. Chemical composition was established by determining total bioactive contents and via UHPLC-MS secondary metabolites profiling. For determination of biological activities, antioxidant capacity was determined through DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelating assays while enzyme inhibition against cholinesterase, tyrosinase, alpha-amylase and alpha-glucosidase were also tested. All the extracts were also tested for toxicity against two breast cell lines. The methanolic extracts were found to contain highest total phenolic and flavonoids which is correlated with their significant radical scavenging, cholinesterase, tyrosinase and glucosidase inhibition potential. Whereas DCM extracts showed significant activity for reducing power, phosphomolybdenum, metal chelation, tyrosinase, and alpha-amylase inhibition activities. The secondary metabolites profiling of both methanolic extracts exposed the presence of 21 different secondary metabolites belonging to glucosinolate, alkaloid, flavonoid, phenol, triterpene, and alkaloid derivatives. The present results tend to validate folklore uses of C. spinose and indicate this plant to be used as a potent source of designing novel bioactive compounds.
ESTHER : Saleem_2021_Food.Chem.Toxicol__112404
PubMedSearch : Saleem_2021_Food.Chem.Toxicol__112404
PubMedID: 34246708

Title : RP-UHPLC-MS Chemical Profiling, Biological and In Silico Docking Studies to Unravel the Therapeutic Potential of Heliotropium crispum Desf. as a Novel Source of Neuroprotective Bioactive Compounds - Arshad_2021_Biomolecules_11_
Author(s) : Arshad A , Ahemad S , Saleem H , Saleem M , Zengin G , Abdallah HH , Tousif MI , Ahemad N , Fawzi Mahomoodally M
Ref : Biomolecules , 11 : , 2021
Abstract : Heliotropium is one of the most important plant genera to have conventional folklore importance, and hence is a potential source of bioactive compounds. Thus, the present study was designed to explore the therapeutic potential of Heliotropium crispum Desf., a relatively under-explored medicinal plant species. Methanolic extracts prepared from a whole plant of H. crispum were studied for phytochemical composition and possible in vitro and in silico biological properties. Antioxidant potential was assessed via six different assays, and enzyme inhibition potential against key clinical enzymes involved in neurodegenerative diseases (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)), diabetes (alpha-amylase and alpha-glucosidase), and skin problems (tyrosinase) was assayed. Phytochemical composition was established via determination of the total bioactive contents and reverse phase ultra-high performance liquid chromatography mass spectrometry (RP-UHPLC-MS) analysis. Chemical profiling revealed the tentative presence of 50 secondary metabolites. The plant extract exhibited significant inhibition against AChE and BChE enzymes, with values of 3.80 and 3.44 mg GALAE/g extract, respectively. Further, the extract displayed considerable free radical scavenging activity against DPPH and ABTS radicals, with potential values of 43.19 and 41.80 mg TE/g extract, respectively. In addition, the selected compounds were then docked against the tested enzymes, which have shown high inhibition affinity. To conclude, H. crispum was found to harbor bioactive compounds and showed potent biological activities which could be further explored for potential uses in nutraceutical and pharmaceutical industries, particularly as a neuroprotective agent.
ESTHER : Arshad_2021_Biomolecules_11_
PubMedSearch : Arshad_2021_Biomolecules_11_
PubMedID: 33406643

Title : Metabolic fingerprinting, antioxidant characterization, and enzyme-inhibitory response of Monotheca buxifolia (Falc.) A. DC. extracts - Ali_2020_BMC.Complement.Med.Ther_20_313
Author(s) : Ali JS , Saleem H , Mannan A , Zengin G , Mahomoodally MF , Locatelli M , Abidin SAZ , Ahemad N , Zia M
Ref : BMC Complement Med Ther , 20 :313 , 2020
Abstract : BACKGROUND: Ethnobotanical and plant-based products allow for the isolation of active constituents against a number of maladies. Monotheca buxifolia is used by local communities due to its digestive and laxative properties, as well as its ability to cure liver, kidney, and urinary diseases. There is a need to explore the biological activities and chemical constituents of this medicinal plant. METHODS: In this work, the biochemical potential of M. buxifolia (Falc.) A. DC was explored and linked with its biological activities. Methanol and chloroform extracts from leaves and stems were investigated for total phenolic and flavonoid contents. Ultrahigh-performance liquid chromatography coupled with mass spectrometry (UHPLC-MS) was used to determine secondary-metabolite composition, while high-performance liquid chromatography coupled with photodiode array detection (HPLC-PDA) was used for polyphenolic quantification. In addition, we carried out in vitro assays to determine antioxidant potential and the enzyme-inhibitory response of M. buxifolia extracts. RESULTS: Phenolics (91 mg gallic-acid equivalent (GAE)/g) and flavonoids (48.86 mg quercetin equivalent (QE)/g) exhibited their highest concentration in the methanol extract of stems and the chloroform extract of leaves, respectively. UHPLC-MS analysis identified a number of important phytochemicals, belonging to the flavonoid, phenolic, alkaloid, and terpenoid classes of secondary metabolites. The methanol extract of leaves contained a diosgenin derivative and polygalacin D, while kaempferol and robinin were most abundant in the chloroform extract. The methanol extract of stems contained a greater peak area for diosgenin and kaempferol, whereas this was true for lucidumol A and 3-O-cis-coumaroyl maslinic acid in the chloroform extract. Rutin, epicatechin, and catechin were the main phenolics identified by HPLC-PDA analysis. The methanol extract of stems exhibited significant 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical-scavenging activities (145.18 and 279.04 mmol Trolox equivalent (TE)/g, respectively). The maximum cupric reducing antioxidant capacity (CUPRAC) (361.4 mg TE/g), ferric-reducing antioxidant power (FRAP) (247.19 mg TE/g), and total antioxidant potential (2.75 mmol TE/g) were depicted by the methanol extract of stems. The methanol extract of leaves exhibited stronger inhibition against acetylcholinesterase (AChE) and glucosidase, while the chloroform extract of stems was most active against butyrylcholinesterase (BChE) (4.27 mg galantamine equivalent (GALAE)/g). Similarly, the highest tyrosinase (140 mg kojic-acid equivalent (KAE)/g) and amylase (0.67 mmol acarbose equivalent (ACAE)/g) inhibition was observed for the methanol extract of stems. CONCLUSIONS: UHPLC-MS analysis and HPLC-PDA quantification identified a number of bioactive secondary metabolites of M. buxifolia, which may be responsible for its antioxidant potential and enzyme-inhibitory response. M. buxifolia can be further explored for the isolation of its active components to be used as a drug.
ESTHER : Ali_2020_BMC.Complement.Med.Ther_20_313
PubMedSearch : Ali_2020_BMC.Complement.Med.Ther_20_313
PubMedID: 33066787

Title : Phytochemical profiling, antioxidant, enzyme inhibition and cytotoxic potential of Bougainvillea glabra flowers - Saleem_2020_Nat.Prod.Res_34_2602
Author(s) : Saleem H , Htar TT , Naidu R , Zengin G , Ahmad I , Ahemad N
Ref : Nat Prod Res , 34 :2602 , 2020
Abstract : In this study, phytochemical composition, antioxidant, enzyme inhibition and cytotoxic activities of methanol and dichloromethane (DCM) extracts of Bougainvillea glabra (B. glabra) flowers were investigated. Methanol extract was found to have higher total bioactive contents and UHPLC-MS analysis of methanol extract revealed the presence of well-known phenolic and flavonoid compounds. Antioxidant activities were performed by radical scavenging (DPPH and ABTS), reducing power (FRAP and CUPRAC), phosphomolybdenum (TAC) and metal chelating assays. From our result, we observed that methanol extract had many antioxidant compounds. The DCM extract exhibited higher cholinesterases and alpha-glucosidase enzyme inhibition, while methanol extract showed significant urease inhibition. Both extracts exhibited strong to moderate cytotoxicity against MCF-7, MDA-MB-231, CaSki, DU-145 and SW-480 cancer cells with IC50 values ranging from 88.49 to 304.7 microg/mL. The findings showed the B. glabra to possess considerable antioxidant, enzyme inhibition and cytotoxic potentials and therefore has potential to discover novel bioactive molecules.
ESTHER : Saleem_2020_Nat.Prod.Res_34_2602
PubMedSearch : Saleem_2020_Nat.Prod.Res_34_2602
PubMedID: 30600720

Title : Multidirectional insights into the phytochemical, biological, and multivariate analysis of the famine food plant (Calligonum polygonoides L).: A novel source of bioactive phytocompounds - Pervaiz_2020_Food.Res.Int_137_109606
Author(s) : Pervaiz I , Saleem H , Sarfraz M , Imran Tousif M , Khurshid U , Ahmad S , Zengin G , Ibrahime Sinan K , Locatelli M , Mahomoodally FM , Asnawi Zainal Abidin S , Ahemad N
Ref : Food Res Int , 137 :109606 , 2020
Abstract : Calligonum polygonoides L. also known as famine food plant, is normally consumed in times of food scarcity in India and Pakistan and also used traditionally in the management of common diseases. The present design aims to provide an insight into the medicinal potential of four solvent extracts of C. polygonoides via an assessment of its phytochemical profile, antioxidant and enzyme inhibitory potential. Phytochemical composition was estimated by deducing total bioactive constituents, UHPLC-MS secondary metabolites profile, and HPLC phenolic quantification. Antioxidant potential was determined via six methods (radical scavenging (DPPH and ABTS), reducing power (FRAP and CUPRAC), phosphomolybdenum total antioxidant capacity and metal chelation activity). Enzyme inhibitory potential was assessed against clinical enzymes (acetylcholinesterase -AChE, butyrylcholinesterase -BChE, tyrosinase, and alpha-amylase). The highest amounts of phenolic contents were found in chloroform extract (76.59 mg GAE/g extract) which may be attributed to its higher radical scavenging, reducing power and tyrosinase inhibition potential. The n-butanol extract containing the maximum amount of flavonoids (55.84 mg RE/g extract) exhibited highest metal chelating capacity. Similarly, the n-hexane extract was found to be most active against AChE (4.65 mg GALAE/g extract), BChE (6.59 mg GALAE/g extract), and alpha-amylase (0.70 mmol ACAE/g extract) enzymes. Secondary metabolite assessment of the crude methanol extract as determined by UHPLC-MS analysis revealed the presence of 24 (negative ionization mode) and 15 (positive ionization mode) secondary metabolites, with most of them belonging to phenolic, flavonoids, terpene, and alkaloid groups. Moreover, gallic acid and naringenin were the main phenolics quantified by HPLC-PDA analysis in all the tested extracts (except n-butanol extract). PCA statistical analysis was also conducted to establish any possible relationship amongst bioactive contents and biological activities. Overall, the C. polygonoides extracts could be further considered to isolate bioactive enzyme inhibitory and antioxidant natural phytocompounds.
ESTHER : Pervaiz_2020_Food.Res.Int_137_109606
PubMedSearch : Pervaiz_2020_Food.Res.Int_137_109606
PubMedID: 33233202

Title : Therapeutic propensities, phytochemical composition, and toxicological evaluation of Anagallis arvensis (L.): A wild edible medicinal food plant - Saleem_2020_Food.Res.Int_137_109651
Author(s) : Saleem H , Zengin G , Ahmad I , Htar TT , Naidu R , Mahomoodally MF , Ahemad N
Ref : Food Res Int , 137 :109651 , 2020
Abstract : Anagallis arvensis (L.) is a wild edible food plant that has been used in folklore as a natural remedy for treating common ailments. This study aimed to explore the biochemical properties and toxicity of methanol (MeOH) and dichloromethane (DCM) extracts of A. arvensis (aerial and root parts). Bioactive contents were assessed spectrophotometrically, and the secondary metabolites were identified by UHPLC-MS analysis. DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum, and metal chelating assays were employed to assess antioxidant activity. Inhibitory potential against key enzymes (alpha-glucosidase, urease, lipoxygenase (LOX), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE)) were also assessed. MTT assay was employed to test toxicity against SW-480, MDA-MB-231, CaSki, MCF-7, and DU-145 cancer cell lines. Methanolic extracts showed highest phenolic (aerial-MeOH: 27.5 mg GAE/g extract; root-MeOH: 21.17 mg GAE/g extract) and flavonoid (aerial-MeOH: 26.15 mg QE/g extract; root-MeOH: 19.07 mg QE/g extract) contents, and potent antioxidant activities. The aerial-MeOH extract was most potent for DPPH (IC(50): 231 ug/mL), ABTS (131.12 mg TE/g extract), FRAP (82.97 mg TE/g extract), and CUPRAC (137.15 mg TE/g extract) antioxidant assays. All extracts were cytotoxic towards tested cancer cells with IC(50) values ranging from 12.57 to 294.5 microg/mL and conferred a comparatively strong inhibition against alpha-glucosidase (aerial-DCM extract showed the highest inhibition against alpha-glucosidase with IC(50) value of 20.97 microg /mL), while aerial extracts were also considerably active against BChE (aerial-MeOH IC(50): 224.63 microg /mL), LOX (aerial-DCM IC(50): 385.7 microg /mL). Likewise, aerial-MeOH extract was most active against urease enzyme (IC(50): 129.72 microg /mL). UHPLC-MS investigation of methanolic extracts showed the existence of important phenolics, flavonoids, and saponins, including methyl gallte, quercetin, lanceoletin, and balanitesin, amongst others. Moreover, principal component analysis (PCA) highlighted the correlation amongst bioactive contents and observed biological activities. A. arvensis extracts could be regarded as a natural source of bioactive antioxidants, enzyme inhibitors and anticancer agents and can be further investigated as a lead source for food and pharmaceutical products. However, further studies to isolate, purify, and to characterize its bioactive phytochemicals are needed.
ESTHER : Saleem_2020_Food.Res.Int_137_109651
PubMedSearch : Saleem_2020_Food.Res.Int_137_109651
PubMedID: 33233230

Title : UHPLC-MS Phytochemical profiling, biological propensities and in-silico studies of Alhagi maurorum roots: A medicinal herb with multifunctional properties - Saleem_2020_Drug.Dev.Ind.Pharm__1
Author(s) : Saleem H , Sarfaraz M , Khan KM , Anwar MI , Zengin G , Ahmad I , Khan SU , Mahomoodally FM , Ahemad N
Ref : Drug Dev Ind Pharm , :1 , 2020
Abstract : The biological, chemical, and in silico properties of methanol and dichloromethane (DCM) extracts of Alhagi maurorum roots with respect to the antioxidant, enzyme inhibition, and phytochemical composition were evaluated. Total bioactive contents were determined spectrophotometrically, and the individual secondary metabolites composition was assessed via ultra-high-performance liquid chromatography mass spectrometry (UHPLC-MS) analysis. Antioxidant capacities were evaluated using a panoply of assays (2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radical scavenging, ferric reducing antioxidant power (FRAP), cupric reducing antioxidant power (CUPRAC), phosphomolybdenum total antioxidant capacity (TAC), and metal chelating activity (MCA)). The enzyme inhibition potential was studied against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), alpha-amylase, alpha-glucosidase, tyrosinase, urease and lipoxygenase (LOX) enzymes. The methanol extract was found to contain higher total phenolic (105.91 mg GAE/g extract) and flavonoid (2.27 mg RE/g extract) contents which can be correlated to its more substantial antioxidant potential as well as AChE, BChE, tyrosinase and alpha-glucosidase inhibition. However, the DCM extract was the most effective against alpha-amylase (1.86 mmol ACAE/g extract) enzyme inhibition. The UHPLC-MS analysis of methanol extract identified the tentative presence of a total of 18 secondary metabolites, including flavonoids, saponins, phenolic and terpenoid derivatives. Three compounds named emmotin A, luteolin 5,3'-dimethyl ether, and preferrugone were further investigated for their in silico molecular docking studies against the tested enzymes. The selected compounds were found to have higher binding interaction with AChE followed by BChE, alpha -glucosidase, alpha-amylase, and tyrosinase. The results of the present study have demonstrated A. mauroram to be considered as a lead source of natural antioxidant and enzyme inhibitor compounds.
ESTHER : Saleem_2020_Drug.Dev.Ind.Pharm__1
PubMedSearch : Saleem_2020_Drug.Dev.Ind.Pharm__1
PubMedID: 32352878

Title : Chemical characterization, antioxidant, enzyme inhibitory and cytotoxic properties of two geophytes: Crocus pallasii and Cyclamen cilicium - Zengin_2020_Food.Res.Int_133_109129
Author(s) : Zengin G , Mahomoodally MF , Sinan KI , Picot-Allain MCN , Yildiztugay E , Cziaky Z , Jeko J , Saleem H , Ahemad N
Ref : Food Res Int , 133 :109129 , 2020
Abstract : The Crocus and Cyclamen genus have been reported to possess diverse biological properties. In the present investigation, two geophytes from these genus, namely Crocus pallasi and Cyclamen cilicium have been studied. The in vitro antioxidant, enzyme inhibitory, and cytotoxic effects of the methanol extracts of Crocus pallasii and Cyclamen cilicium aerial and underground parts were investigated. Antioxidant abilities of the extracts were investigated via different antioxidant assays (metal chelating, radical quenching (ABTS and DPPH), reducing power (CUPRAC and FRAP) and phosphomolybdenum). Cholinesterases, amylase, tyrosinase, and glucosidase were used as target enzymes for detecting enzyme inhibitory abilities of the samples. Regarding the cytotoxic abilities, breast cancer cell lines (MDA-MB 231 and MCF-7) and prostate cancer cell lines (DU-145) were used. The flowers extracts of Crocus pallasii and C. cilicium possessed the highest flavonoid content. The highest phenolic content was recorded from C. cilicium root extract (47.62 mg gallic acid equivalent/g extract). Cyclamen cilicium root extract showed significantly (p < 0.05) high radical scavenging (94.28 and 139.60 mg trolox equivalent [TE]/g extract, against DPPH and ABTS radicals, respectively) and reducing potential (173.30 and 109.53 mg TE/g extract, against CUPRAC and FRAP, respectively). The best acetylcholinesterase, glucosidase and tyrosinase inhibition was observed in C. cilicium root (4.46 mg GALAE/g; 15.75 mmol ACAE/g; 136.99 mg KAE/g, respectively). Methanolic extracts of C. pallasii and C. cilicium showed toxicity against breast cancer cell lines. In light of the above findings, C. cilicium might be considered as an interesting candidate in the development of anti-cancer agent coupled with antioxidant properties.
ESTHER : Zengin_2020_Food.Res.Int_133_109129
PubMedSearch : Zengin_2020_Food.Res.Int_133_109129
PubMedID: 32466933

Title : Multidirectional insights into the biochemical and toxicological properties of Bougainvillea glabra (Choisy.) aerial parts: A functional approach for bioactive compounds - Saleem_2019_J.Pharm.Biomed.Anal_170_132
Author(s) : Saleem H , Zengin G , Ahmad I , Lee JTB , Htar TT , Mahomoodally FM , Naidu R , Ahemad N
Ref : J Pharm Biomed Anal , 170 :132 , 2019
Abstract : The current research work was conducted in order to probe into the biochemical and toxicological characterisation of methanol and dichloromethane (DCM) extracts of Bougainvillea glabra (Choisy.) aerial parts. Biological fingerprints were assessed for in vitro antioxidant, key enzyme inhibitory and cytotoxicity potential. Total bioactive contents were determined spectrophotometrically and the secondary metabolite components of methanol extract was assessed by UHPLC mass spectrometric analysis. The antioxidant capabilities were evaluated via six different in vitro antioxidant assays namely DPPH, ABTS (free radical scavenging), FRAP, CUPRAC (reducing antioxidant power), phosphomolybdenum (total antioxidant capacity) and ferrous chelating activity. Inhibition potential against key enzymes urease, alpha-glucosidase and cholinesterases were also determined. Methanol extract exhibited higher phenolic (24.01 mg GAE/g extract) as well as flavonoid (41.51mg QE/g extract) contents. Phytochemical profiling of methanol extract identified a total of twenty secondary metabolites and the major compounds belonged to flavonoids, phenolics and alkaloid derivatives. The findings of antioxidant assays revealed the methanol extract to exhibit stronger antioxidant (except phosphomolybdenum) activities. Similarly, the methanol extract showed highest butyrylcholinesterase and urease inhibition. The DCM extract was most active for phosphomolybdenum and alpha-glucosidase inhibition assays. Moreover, both extracts exhibited significant cytotoxic potential against five (MCF-7, MDA-MB-231, CaSki, DU-145, and SW-480) human carcinoma cell lines with half maximal inhibitory concentration values of 22.09 to 257.2 mug/mL. Results from the present study highlighted the potential of B. glabra aerial extracts to be further explored in an endeavour to discover novel phytotherapeutics as well as functional ingredients.
ESTHER : Saleem_2019_J.Pharm.Biomed.Anal_170_132
PubMedSearch : Saleem_2019_J.Pharm.Biomed.Anal_170_132
PubMedID: 30921647

Title : Biological, chemical and toxicological perspectives on aerial and roots of Filago germanica (L.) huds: Functional approaches for novel phyto-pharmaceuticals - Saleem_2019_Food.Chem.Toxicol_123_363
Author(s) : Saleem H , Htar TT , Naidu R , Nawawi NS , Ahmad I , Ashraf M , Ahemad N
Ref : Food & Chemical Toxicology , 123 :363 , 2019
Abstract : We investigated into the effects of methanol and dichloromethane extracts from aerial and roots of Filago germanica (L.) Huds (Astearaceae) on key enzymes (cholinesterases, alpha-glucosidase and urease), antioxidant capabilities, cytotoxic potential and secondary metabolomics profile. Total phenolic and flavonoids were determined by spectrophotometric technique and secondary metabolites composition by UHPLC-MS. Antioxidant activities were assessed employing free radical scavenging, ferric reducing power and phosphomolybdenum assays. The cell-toxicity was evaluated by MTT assay against breast (MCF-7, MDA-MB-231), cervix (CaSki) and prostate (DU-145) cancers. Overall, methanol extracts were found to have higher total bioactive contents and antioxidant potential. UHPLC-MS analysis revealed significant variation in the secondary metabolites in the methanol extracts. The most common derivatives belong to seven groups i.e. alkaloids, benzoic acids, flavones, flavonols, flavan-3-ols, terpenoids and saponins. The major polyphenolic compounds were found to be kampferol, robinin, luteolin, ferulic acid, benzoic acid and salicylic acid. All the extracts showed moderate cholinesterases inhibition, whereas methanol extracts exhibited highest urease inhibition and all extracts presented a relatively high inhibition against alpha-glucosidase. Similarly, all extracts showed strong to moderate cytotoxicity with IC50 values ranging from 53.02 to 382.7mug/mL. Overall, results have suggested F. germanica to be a lead source for novel natural products.
ESTHER : Saleem_2019_Food.Chem.Toxicol_123_363
PubMedSearch : Saleem_2019_Food.Chem.Toxicol_123_363
PubMedID: 30419323

Title : Embelin, a Potent Molecule for Alzheimer's Disease: A Proof of Concept From Blood-Brain Barrier Permeability, Acetylcholinesterase Inhibition and Molecular Docking Studies - Bhuvanendran_2019_Front.Neurosci_13_495
Author(s) : Bhuvanendran S , Hanapi NA , Ahemad N , Othman I , Yusof SR , Shaikh MF
Ref : Front Neurosci , 13 :495 , 2019
Abstract : Embelin is well-known in ethnomedicine and reported to have central nervous system activities. However, there is no report on blood-brain barrier (BBB) permeability of embelin. Here the BBB permeability of embelin was evaluated using in vitro primary porcine brain endothelial cell (PBEC) model of the BBB. Embelin was also evaluated for acetylcholinesterase (AChE) inhibitory activity and docking prediction for interaction with AChE and amyloid beta (Abeta) binding sites. Embelin was found to be non-toxic to the PBECs and did not disturb the PBEC barrier function. The PBECs showed restrictive tight junctions with average transendothelial electrical resistance of 365.37 +/- 113.00 Omega.cm(2), for monolayers used for permeability assays. Permeability assays were conducted from apical-to-basolateral direction (blood-to-brain side). Embelin showed apparent permeability (P app) value of 35.46 +/- 20.33 x 10(-6) cm/s with 85.53% recovery. In vitro AChE inhibitory assay demonstrated that embelin could inhibit the enzyme. Molecular docking study showed that embelin binds well to active site of AChE with CDOCKER interaction energy of -65.75 kcal/mol which correlates with the in vitro results. Docking of embelin with Abeta peptides also revealed the promising binding with low CDOCKER interaction energy. Thus, findings from this study indicate that embelin could be a suitable molecule to be further developed as therapeutic molecule to treat neurological disorders particularly Alzheimer's disease.
ESTHER : Bhuvanendran_2019_Front.Neurosci_13_495
PubMedSearch : Bhuvanendran_2019_Front.Neurosci_13_495
PubMedID: 31156375

Title : Pharmacological, phytochemical and in-vivo toxicological perspectives of a xero-halophyte medicinal plant: Zaleya pentandra (L.) Jeffrey - Saleem_2019_Food.Chem.Toxicol_131_110535
Author(s) : Saleem H , Zengin G , Locatelli M , Ahmad I , Khaliq S , Mahomoodally MF , Hussain R , Rengasamy KRR , Mollica A , Zainal Abidin SA , Ahemad N
Ref : Food & Chemical Toxicology , 131 :110535 , 2019
Abstract : This study endeavours to investigate the phytochemical composition, biological properties and in vivo toxicity of methanol and dichloromethane extracts of Zaleya pentandra (L.) Jeffrey. Total bioactive contents, antioxidant (phosphomolybdenum and metal chelating, DPPH, ABTS, FRAP and CUPRAC) and enzyme inhibition (cholinesterases, tyrosinase alpha-amylase, and alpha-glucosidase) potential were assessed utilizing in vitro bioassays. UHPLC-MS phytochemical profiling was carried out to identify the essential compounds. The methanol extract was found to contain highest phenolic (22.60mg GAE/g) and flavonoid (31.49mg QE/g) contents which correlate with its most significant radical scavenging, reducing potential and tyrosinase inhibition. The dichloromethane extract was most potent for phosphomolybdenum, ferrous chelation, alpha-amylase, alpha-glucosidase, and cholinesterase inhibition assays. UHPLC-MS analysis of methanol extract unveiled to identify 11 secondary metabolites belonging to five sub-groups, i.e., phenolic, alkaloid, carbohydrate, terpenoid, and fatty acid derivatives. Additionally, in vivo toxicity was conducted for 21 days and the methanol extract at different doses (150, 200, 250 and 300mg/kg) was administered in experimental chicks divided into five groups each containing five individuals. Different physical, haematological and biochemical parameters along with the absolute and relative weight of visceral body organs were studied. Overall, no toxic effect was noted for the extract at tested doses.
ESTHER : Saleem_2019_Food.Chem.Toxicol_131_110535
PubMedSearch : Saleem_2019_Food.Chem.Toxicol_131_110535
PubMedID: 31154083

Title : Investigations into the therapeutic effects of aerial and stem parts of Buxus papillosa C.K. Schneid.: In vitro chemical, biological and toxicological perspectives - Saleem_2019_J.Pharm.Biomed.Anal_166_128
Author(s) : Saleem H , Htar TT , Naidu R , Ahmad I , Zengin G , Ahmad M , Ahemad N
Ref : J Pharm Biomed Anal , 166 :128 , 2019
Abstract : In this study, different solvent extracts (methanol, dichloromethane and n-hexane) from aerial and stem parts of Buxus papillosa C.K. Schneid (Buxaceae) were investigated for a panoply of bioassays. Biological profiles were established by determining antioxidant and enzyme inhibition profiles. Toxicity was tested using MTT cell viability assay on five different human cancer cell lines i.e, MCF-7, MDA-MB-231, CaSki, DU-145 and SW-480. For chemical fingerprinting, total bioactive contents and UHPLC-MS secondary metabolites profile were determined. Generally, both aerial and stem methanol extracts had highest total bioactive contents, radical scavenging and reducing power potential. DCM and n-hexane extracts were found to be most active for total antioxidant and metal chelating activity. The UHPLC-MS analysis of methanol extracts revealed the presence of several phenolic, flavonoid, alkaloid, saponin and depsipeptide derivatives. All the extracts were significantly active against butyrylcholinesterase, whereas moderate inhibition was observed for acetylcholinesterase, alpha-glucosidase and urease. Similarly, a considerable level of cytotoxicity was observed against all the tested cell lines with IC50 values ranging from 26 to 225.9 mug/mL. Aerial methanol and stem n-hexane extracts were found to be most cytotoxic. Principal component analysis was also performed to find any possible correlation between biological activities and total bioactive contents. On the basis of our findings, B. papillosa may be considered as promising source of bioactive molecules.
ESTHER : Saleem_2019_J.Pharm.Biomed.Anal_166_128
PubMedSearch : Saleem_2019_J.Pharm.Biomed.Anal_166_128
PubMedID: 30640043