Screening chemical inhibitors for alpha-amylase from leaves extracts of Murraya koenigii (Linn.) and Aegle marmelos L.

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Alagar Yadav Sangilimuthu ◽  
Thirunavukkarasu Sivaraman ◽  
Rajkuberan Chandrasekaran ◽  
Karpagavalli Meenatchi Sundaram ◽  
Gayathiri Ekambaram
Keyword(s):  
Docking Studies ◽  
Alpha Amylase ◽  
Antidiabetic Activity ◽  
Gas Chromatography Mass Spectrometry ◽  
Murraya Koenigii ◽  
Aegle Marmelos ◽  
High Concentration ◽  
Low Concentrations ◽  
Chemical Inhibitors

AbstractObjectivesAqueous leaves extracts of Murraya koenigii (M. koenigii) and Aegle marmelos (A. marmelos) were prepared and effect of the extracts on inhibiting alpha-amylase playing essential roles on converting starch into glucose have been examined using in vitro assays.MethodsAlpha amylase inhibitory assay was used to asses the in vitro antidiabetic activity of the extracts. Gas chromatography-mass spectrometry (GC-MS) analysis was performed to identify the volatile molecules of the extracts. Identified molecule were converted as ligand and docked against human pancreatic α-amylase (0.95 Å; PDB ID: 5U3A) using Autodock tool.ResultsThe data analyzes suggested that the alpha-amylase inhibition potential of the extract obtained from M. koenigii was stronger than that of the A. marmelos at low concentrations (<1 mg/mL), whereas both the extracts depicted similar inhibition effects on the enzyme at high concentration (>1 mg/mL). The phytochemicals present in both the plant extracts were identified by using their respective GC-MS data and the data analyzes revealed that the extracts of M. koenigii and A. Marmelos seemed to consist of about 20 and 24 diverse chemical molecules, respectively. Through the molecular docking studies, azulene of M. koenigii and hydroxycyclodecadiene of A. marmelos showed higher binding affinity on alpha-amylase.ConclusionsConcentration-dependent alpha-amylase inhibition effects of the extracts were observed and M. koenigii contains more alpha-amylase inhibitory effects due to the presence of azulene. This is primary lead to find out the better anti diabetic natural based drug to the society after clinical trial.

scholarly journals Investigation of α-Glucosidase Inhibitory Metabolites from Tetracera scandens Leaves by GC–MS Metabolite Profiling and Docking Studies

Biomolecules ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 287 ◽  
Author(s):  
Ahmed Nokhala ◽  
Mohammad Jamshed Siddiqui ◽  
Qamar Uddin Ahmed ◽  
Muhammad Safwan Ahamad Bustamam ◽  
Zainul Amiruddin Zakaria
Keyword(s):  
Metabolite Profiling ◽  
Docking Studies ◽  
Binding Energies ◽  
Antidiabetic Activity ◽  
Gas Chromatography Mass Spectrometry ◽  
Mass Spectral ◽  
Ic50 Values ◽  
Inhibitory Potential ◽  
Underlying Mechanisms

Stone leaf (Tetracera scandens) is a Southeast Asian medicinal plant that has been traditionally used for the management of diabetes mellitus. The underlying mechanisms of the antidiabetic activity have not been fully explored yet. Hence, this study aimed to evaluate the α-glucosidase inhibitory potential of the hydromethanolic extracts of T. scandens leaves and to characterize the metabolites responsible for such activity through gas chromatography–mass spectrometry (GC–MS) metabolomics. Crude hydromethanolic extracts of different strengths were prepared and in vitro assayed for α-glucosidase inhibition. GC–MS analysis was further carried out and the mass spectral data were correlated to the corresponding α-glucosidase inhibitory IC50 values via an orthogonal partial least squares (OPLS) model. The 100%, 80%, 60% and 40% methanol extracts displayed potent α-glucosidase inhibitory potentials. Moreover, the established model identified 16 metabolites to be responsible for the α-glucosidase inhibitory activity of T. scandens. The putative α-glucosidase inhibitory metabolites showed moderate to high affinities (binding energies of −5.9 to −9.8 kcal/mol) upon docking into the active site of Saccharomyces cerevisiae isomaltase. To sum up, an OPLS model was developed as a rapid method to characterize the α-glucosidase inhibitory metabolites existing in the hydromethanolic extracts of T. scandens leaves based on GC–MS metabolite profiling.

scholarly journals Characterization of Possible α-Glucosidase Inhibitors from Trigonella stellata Extract Using LC–MS and In Silico Molecular Docking

Plants ◽  
2022 ◽  
Vol 11 (2) ◽  
pp. 208
Author(s):  
Ahlam Elwekeel ◽  
Dalia El Amir ◽  
Enas I. A. Mohamed ◽  
Elham Amin ◽  
Marwa H. A. Hassan ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Docking Study ◽  
Docking Studies ◽  
Antidiabetic Activity ◽  
Flavonoid Glycosides ◽  
Total Phenolic ◽  
Cytotoxic Activities ◽  
Alcoholic Extract ◽  
Molecular Docking Study

The current study accentuates the significance of performing the multiplex approach of LC-HRESIMS, biological activity, and docking studies in drug discovery, taking into consideration a review of the literature. In this regard, the investigation of antioxidant and cytotoxic activities of Trigonella stellata collected from the Egyptian desert revealed a significant antioxidant capacity using DPPH with IC50 = 656.9 µg/mL and a moderate cytotoxicity against HepG2, MCF7, and CACO2, with IC50 values of 53.3, 48.3, and 55.8 µg/mL, respectively. The evaluation of total phenolic and flavonoid contents resulted in 32.8 mg GAE/g calculated as gallic acid equivalent and 5.6 mg RE/g calculated as rutin equivalent, respectively. Chemical profiling of T. stellata extract, using LC-HRESIMS analysis, revealed the presence of 15 metabolites, among which eleven compounds were detected for the first time in this species. Interestingly, in vitro testing of the antidiabetic activity of the alcoholic extract noted an α-glucosidase enzyme inhibitory activity (IC50 = 559.4 µg/mL) better than that of the standard Acarbose (IC50 = 799.9 µg/mL), in addition to a moderate inhibition of the α-amylase enzyme (IC50 = 0.77 µg/mL) compared to Acarbose (IC50 = 0.21 µg/mL). α-Glucosidase inhibition was also virtualized by binding interactions through the molecular docking study, presenting a high binding activity of six flavonoid glycosides, as well as the diterpenoid compound graecumoside A and the alkaloid fenugreekine. Taken together, the conglomeration of LC-HRESIMS, antidiabetic activity, and molecular docking studies shed light on T. stellata as a promising antidiabetic herb.

Effect of two bio-polysaccharides on organogenesis of protocorm-like bodies in Phalaenopsis cultured in vitro

2020 ◽  
Vol 26 (1) ◽  
pp. 2137-2142
Author(s):  
A. M. Meskatul ◽  
K. Shimasaki ◽  
S. U. Habiba
Keyword(s):  
Shoot Formation ◽  
Vital Role ◽  
White Led ◽  
Fresh Weight ◽  
High Concentration ◽  
Low Concentrations ◽  
Different Types ◽  
Modified Ms Medium ◽  
Led Lights

Different types of bio-polysaccharide play a vital role in the growth of PLBs cultured in vitro. In this study, to we investigated the potential impacts of two bio-polymers,: hyaluronic acid (HA9) and sodium alginate (ALG) on the organogenesis of protocorm-like bodies (PLBs) in Phalaenopsis under white LED lights. PLBs of Phalaenopsis ‘Fmk02010’ were explanted on modified MS medium with different concentrations of HA and (ALG). The highest average number of PLBs per explant (24.6) was recorded for ALG alone at a concentration of 0.01mg/L, and the fresh weight was also highest at the same concentration. The combination of 0.01mg/L ALG and 0.01mg/L HA also resulted in a large number of PLBs (23.8) and high fresh weight. As opposed to, the highest number of shoots /explant (3.6) was observed at the treatment of the combination of 1mg/L ALG and 10mg/L HA. This study shows that the application of ALG and HA alone, and in combination, at low concentrations, increased the average number of PLBs and the amount of fresh weight, but shoot formation was higher at a high concentration compared with control.

scholarly journals EFFECT OF ACTINOMYCIN D ON RNA SYNTHESIS AND ANTIBODY FORMATION IN THE ANAMNESTIC RESPONSE IN VITRO

1964 ◽  
Vol 119 (6) ◽  
pp. 881-893 ◽  
Author(s):  
J. Donald Smiley ◽  
John G. Heard ◽  
Morris Ziff
Keyword(s):  
Messenger Rna ◽  
Rna Synthesis ◽  
Actinomycin D ◽  
Lymphoid Cells ◽  
Limiting Factor ◽  
High Concentration ◽  
Antibody Synthesis ◽  
Anamnestic Response ◽  
Low Concentrations

Antibody synthesis in anamnestic lymphoid cells, measured by incorporation of leucine-C14 into specific antibody, was inhibited at moderate concentrations of actinomycin D. This was accompanied by marked inhibition of synthesis of RNA as measured by incorporation of H3-cytidine monophosphate. However, at low concentrations of actinomycin D, antibody synthesis was unaffected or even increased while RNA synthesis continued to be inhibited. The results obtained suggest that messenger RNA for antibody synthesis, either because it is relatively stable or present in excess, does not become a limiting factor until its synthesis is maximally inhibited. Puromycin, an inhibitor of amino acid coupling, abolished antibody synthesis in low concentration. 6-Mercaptopurine had no effect on the synthesis of antibody or RNA even at high concentration. The data obtained support the view that antibody synthesis follows pathways similar to those utilized for the formation of other types of proteins.

scholarly journals Assessment of In Vitro Antidiabetic Potential of Purified Anthocyanin Extract from Floral Petals of Wild Balsam Species

2020 ◽  
Vol 10 (3) ◽  
pp. 31-35
Author(s):  
R ARATHY ◽  
K MURUGAN ◽  
KV DINESH BABU ◽  
GS MANOJ
Keyword(s):  
International Diabetes Federation ◽  
Inhibitory Effect ◽  
Alpha Amylase ◽  
Herbal Remedies ◽  
Antidiabetic Activity ◽  
Public Health Issue ◽  
Impatiens Balsamina ◽  
Alpha Glucosidase

Diabetes is a notorious and growing clinical and public health issue. The International Diabetes Federation assumes that 592 million had diabetes by 2035 and that by 2040 the number will increase to 642 million. Cardiovascular corollary accounts for four million deaths annually attributable to diabetes. Evidence reveals that certain glucose-lowering phytochemicals can improve vascular outcomes with type 2 diabetes, which, together with better understanding of using multiple therapies concurrently, offers opportunities for beneficial personalization of medication regimens. Anthocyanins are coloured pigments and are natural antioxidants. Keeping this in focus, this study was undertaken to evaluate the in vitro antidiabetic activity in the petals of wild Impatiens balsamina L. The anthocyanin was extracted from floral petals of wild balsam species and purified to homogeneity using chromatographic techniques. Evaluation of in vitro antidiabetic properties of anthocyanin extract revealed a dose-dependent increase in the inhibitory effect on the alpha-glucosidase (200 μg/ml) and alpha-amylase enzymes (500 μg/ml) and was comparable with the standard acarbose drug (189 μg/ml and 50 μg/ml). These results indicated that anthocyanin could be used as a source of functional food and nutraceuticals. This information from wild species will be useful in finding more potent antidiabetic principle from the natural resources for the clinical development of antidiabetic therapeutics. Future studies are planned to substantiate the antidiabetic power of anthocyanin using in vivo animal models. Keywords: Alpha amylase, alpha glucosidase, diabetes, herbal remedies, Impatiens balsamina L.

scholarly journals Biphasic Effect of Pirfenidone on Angiogenesis

2022 ◽  
Vol 12 ◽  
Author(s):  
Donghao Gan ◽  
Wenxiang Cheng ◽  
Liqing Ke ◽  
Antonia RuJia Sun ◽  
Qingyun Jia ◽  
...  
Keyword(s):  
Vascular Endothelial Cells ◽  
Tube Formation ◽  
Endothelial Cell Migration ◽  
High Concentration ◽  
Low Concentrations ◽  
Biphasic Effect ◽  
High Concentrations ◽  
And Migration ◽  
The Impact

Pirfenidone (PFD), a synthetic arsenic compound, has been found to inhibit angiogenesis at high concentrations. However, the biphasic effects of different PFD concentrations on angiogenesis have not yet been elucidated, and the present study used an in vitro model to explore the mechanisms underlying this biphasic response. The effect of PFD on the initial angiogenesis of vascular endothelial cells was investigated through a Matrigel tube formation assay, and the impact of PFD on endothelial cell migration was evaluated through scratch and transwell migration experiments. Moreover, the expression of key migration cytokines, matrix metalloproteinase (MMP)-2 and MMP-9, was examined. Finally, the biphasic mechanism of PFD on angiogenesis was explored through cell signaling and apoptosis analyses. The results showed that 10–100 μM PFD has a significant and dose-dependent inhibitory effect on tube formation and migration, while 10 nM–1 μM PFD significantly promoted tube formation and migration, with 100 nM PFD having the strongest effect. Additionally, we found that a high concentration of PFD could significantly inhibit MMP-2 and MMP-9 expression, while low concentrations of PFD significantly promoted their expression. Finally, we found that high concentrations of PFD inhibited EA.hy926 cell tube formation by promoting apoptosis, while low concentrations of PFD promoted tube formation by increasing MMP-2 and MMP-9 protein expression predominantly via the EGFR/p-p38 pathway. Overall, PFD elicits a biphasic effect on angiogenesis through different mechanisms, could be used as a new potential drug for the treatment of vascular diseases.

scholarly journals INHIBITORY EFFECT OF A STANDARDIZED HYDROETHANOLIC EXTRACT OF TERMINALIA ARJUNA BARK ON ALPHA-AMYLASE ENZYMEINHIBITORY EFFECT OF A STANDARDIZED HYDROETHANOLIC EXTRACT OF TERMINALIA ARJUNA BARK ON ALPHA-AMYLASE ENZYME

2018 ◽  
Vol 11 (4) ◽  
pp. 366 ◽  
Author(s):  
Sushant A Shengule ◽  
Sanjay Mishra ◽  
Shweta Bodhale
Keyword(s):  
Inhibitory Activity ◽  
High Performance ◽  
Soxhlet Extraction ◽  
Inhibitory Effect ◽  
Alpha Amylase ◽  
Antidiabetic Activity ◽  
Bark Extract ◽  
Terminalia Arjuna ◽  
Hydroethanolic Extract

 Objective: The present study was initiated to screen the hydroethanolic bark extract for α-amylase inhibitory activity and standardization of the Terminalia arjuna for polyphenolic phytochemicals using high-performance liquid chromatography-photo diode array (HPLC-PDA) method.Methods: The T. arjuna bark sample was extracted with ethanol: water (70:30 v/v) using Soxhlet extraction. A Dionex P680 HPLC system was used to acquire chromatograms. The screening of extract of T. arjuna bark has performed for in vitro α-amylase inhibitory assay. Each experiment was repeated 3 times. All values were expressed mean ± standard deviation.Results: The content of arjunetin, arjungenin, gallic acid, ellagic acid, and quercetin was 0.47, 8.22, 2.443, 7.901, and 3.20 mg/g, respectively, in a hydroethanolic extract of T. arjuna. The hydroethanolic extract of T. arjuna bark and acarbose has shown an inhibitory activity with an IC50 value 145.90 and 62.35 μg/mL, respectively.Conclusion: The hydroethanolic extract T. arjuna bark demonstrates α-amylase inhibitory activity due to a synergistic effect of the phytochemical constituents present in it. This study suggests that one of the mechanisms of this plant for antidiabetic activity is through the inhibition of α-amylase enzyme.

Mechanochemical Synthesis, in vitro Evaluation and Molecular Docking Studies of 4-Amino-2-arylamino-5-(benzofuran-2-oyl)thiazoles as Antidiabetic Agents

2019 ◽  
Vol 16 (7) ◽  
pp. 560-568
Author(s):  
Vijayan R. Akhila ◽  
Maheswari R. Priya ◽  
Daisy R. Sherin ◽  
Girija K. Krishnapriya ◽  
Sreerekha V. Keerthi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Mechanochemical Synthesis ◽  
Active Sites ◽  
Docking Studies ◽  
Binding Energies ◽  
Antidiabetic Activity ◽  
Antidiabetic Agents ◽  
Molecular Docking Studies ◽  
Ic50 Value

The synthesis of 4-amino-2-arylamino-5-(benzofuran-2-oyl)thiazoles 4a-h, as example of 2,4-diaminothiazole-benzofuran hybrids and an evaluation of their antidiabetic activity, by in vitro and computational methods, are reported. The synthesis of these diaminothiazoles was achieved mechano chemically by a rapid solvent-less method. Their antidiabetic activity was assessed by &#945;-glucosidase and &#945;-amylase inhibition assays. The, IC50 value for &#945;-glucosidase inhibition by 4-amino-5- (benzofuran-2-oyl)-2-(4-methoxyphenylamino)thiazole (4d) was found to be 20.04 &#181;M and the IC50 value for &#945;-amylase inhibition, 195.03 &#181;M, whereas the corresponding values for reference acarbose were 53.38 &#181;M and 502.03 &#181;M, respectively. Molecular docking studies at the active sites of &#945;- glucosidase and α-amylase showed that among the diaminothiazoles 4a-h now studied, 4-amino-5- (benzofuran-2-oyl)-2-(4-methoxyphenylamino)thiazole (4d) has the highest D-scores of -8.63 and -8.08 for &#945;-glucosidase and for α-amylase, with binding energies -47.76 and -19.73 kcal/mol, respectively.

Exploration of Diosmin to control diabitis and its complications-an in vitro and in silico approach

2020 ◽  
Vol 16 ◽  
Author(s):  
Kushagra Dubey ◽  
Raghvendra Dubey ◽  
Revathi Gupta ◽  
Arun Gupta
Keyword(s):  
Molecular Docking ◽  
Aldose Reductase ◽  
Inhibitory Activity ◽  
Blood Lipid ◽  
Docking Studies ◽  
Alpha Amylase ◽  
Lipid Lowering ◽  
Molecular Docking Studies ◽  
Alpha Glucosidase

Background: Diosmin is a flavonoid obtained from the citrus fruits of the plants. Diosmin has blood lipid lowering activities, antioxidant activity, enhances venous tone and microcirculation, protects capillaries, mainly by reducing systemic oxidative stress. Objective: The present study demonstrates the potential of Diosmin against the enzymes aldose reductase, α-glucosidase, and α-amylase involved in diabetes and its complications by in vitro evaluation and reverse molecular docking studies. Method: The assay of aldose reductase was performed by using NADPH as starting material and DL-Glyceraldehyde as a substrate. DNS method was used for alpha amylase inhibition and in alpha glucosidase inhibitory activity p-nitrophenyl glucopyranoside (pNPG) was used as substrate. The reverse molecular docking studies was performed by using Molegro software (MVD) with grid resolution of 30 Å. Result: Diosmin shows potent inhibitory effect against aldose reductase (IC50:333.88±0.04 µg/mL), α-glucosidase (IC50:410.3±0.01 µg/mL) and α-amylase (IC50: 404.22±0.02 µg/mL) respectively. The standard drugs shows moderate inhibitory activity for enzymes. The MolDock Score of Diosmin was -224.127 against aldose reductase, -168.17 against α-glucosidase and -176.013 against α-amylase respectively, which was much higher than standard drugs. Conclusion: From the result it was concluded that diosmin was a potentially inhibitor of aldose reductase, alpha amylase and alpha glucosidase enzymes then the standard drugs and it will be helpful in the management of diabetes and its complications. This will also be benevolent to decrease the socio economical burden on the middle class family of the society.

scholarly journals BIOASSAY-GUIDED EVALUATION OF FICUS SEMICORDATA FOR ANTIDIABETIC ACTIVITY

2017 ◽  
Vol 9 (3) ◽  
pp. 71 ◽  
Author(s):  
Virender Kaur ◽  
Kumud Upadhyaya ◽  
Milind Pande
Keyword(s):  
Diabetes Mellitus ◽  
Early Stage ◽  
Ethanol Extract ◽  
Postprandial Hyperglycemia ◽  
Alpha Amylase ◽  
Antidiabetic Activity ◽  
Biological Studies

Objective: The early stage of diabetes mellitus type 2 is associated with postprandial hyperglycemia. The therapeutic approach involved in the treatment of type 2 diabetes mellitus is the use of agents that can decrease postprandial hyperglycemia by inhibiting carbohydrate digesting enzymes. In an effort of identifying herbal drugs which may become useful in the prevention or mitigation of diabetes, the antidiabetic activity of Ficus semicordata (FS) and its constituents were studied. The present study was undertaken in part to identify the potent antihyperglycemic fraction from the ethanol extract of the plant, using bioassay guided evaluation.Methods: The ethanol extract of Ficus semicordata were fractionated to obtain chloroform, ethyl acetate, n-butanol and ethanol extracts which were tested for alpha-amylase, alpha-glucosidase inhibitory, properties. Further fractionation of the more active ethanol fraction yielded isolates FS-1 and FS-2 which were tested for in vivo antidiabetic activity using Streptozotocin (STZ)-induced diabetic rats.Results: Ethanol extract from leaves of the plant showed notable alpha-amylase (IC50 = 3.352µg/ml and alpha-glycosidase inhibitory activity (IC50= 3.448µg/ml) as compared to standard acarbose (IC50 = 3.175µg/ml. Subfraction FS-1 and FS-2 which were tested for in vivo antidiabetic activity using acute STZ-induced diabetic rats significantly (*p<0.05, **p<0.01, *** p<0.001) reduced blood glucose level.Conclusion: The Ficus semicordata plant extracts and the fractionated components could be used as a natural antidiabetic after comprehensive in vitro and in vivo biological studies.

Sign in / Sign up

Export Citation Format

Share Document