Dataset Information

Smilax aristolochiifolia Root Extract and Its Compounds Chlorogenic Acid and Astilbin Inhibit the Activity of ?-Amylase and ?-Glucosidase Enzymes.

ABSTRACT: Regulating activities of ?-amylase and ?-glucosidase through the use of specific inhibitors is a main strategy for controlling type 2 diabetes. Smilax aristolochiifolia root decoctions are traditionally used in Mexico as hypoglycemic and for weight loss, but the active principles and mechanisms underlying such putative metabolic effects are yet unknown. Here, we isolated the major bioactive compounds from a hydroethanolic extract of S. aristolochiifolia root by fast centrifugal partition chromatography and evaluated their effects against pancreatic ?-amylase and yeast ?-glucosidase. A chlorogenic acid-rich fraction (CAF) inhibited ?-amylase activity with an IC50 value of 59.28??g/mL in an uncompetitive manner and ?-glucosidase activity with an IC50 value of 9.27??g/mL in a noncompetitive mode. Also, an astilbin-rich fraction (ABF) inhibited ?-glucosidase activity with an IC50 value of 12.30??g/mL, in a noncompetitive manner. CAF inhibition ?-amylase was as active as acarbose while both CAF and ABF were 50-fold more potent inhibitors of ?-glucosidase than acarbose. The molecular docking results of chlorogenic acid and astilbin with ?-amylase and ?-glucosidase enzymes correlated with the inhibition mechanisms suggested by enzymatic assays. Our results prove that S. aristolochiifolia roots contain chlorogenic acid and astilbin, which inhibit carbohydrates-hydrolyzing enzymes, suggesting a new mechanism for the hypoglycemic effect reported for this plant.

SUBMITTER: Perez-Najera VC

PROVIDER: S-EPMC6036819 | biostudies-literature | 2018

REPOSITORIES: biostudies-literature

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Smilax aristolochiifolia Root Extract and Its Compounds Chlorogenic Acid and Astilbin Inhibit the Activity of α-Amylase and α-Glucosidase Enzymes.

Pérez-Nájera Viridiana Candelaria VC Gutiérrez-Uribe Janet Alejandra JA Antunes-Ricardo Marilena M Hidalgo-Figueroa Sergio S Del-Toro-Sánchez Carmen Lizette CL Salazar-Olivo Luis A LA Lugo-Cervantes Eugenia E

Evidence-based complementary and alternative medicine : eCAM 20180625

Regulating activities of α-amylase and α-glucosidase through the use of specific inhibitors is a main strategy for controlling type 2 diabetes. Smilax aristolochiifolia root decoctions are traditionally used in Mexico as hypoglycemic and for weight loss, but the active principles and mechanisms underlying such putative metabolic effects are yet unknown. Here, we isolated the major bioactive compounds from a hydroethanolic extract of S. aristolochiifolia root by fast c ...[more]

PMID: 30046343

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Project description:BackgroundAs a traditional herbal medicine, Dracaena angustifolia Roxb has been used as an anti-inflammatory agent by the Li people in Hainan, China. In preliminary phytochemical studies conducted in our lab, its fractions were found to inhibit α-glucosidase in vitro, indicating a potential for alleviating glucose dysregulation.MethodsThrough in vitro enzymatic assays, the abilities of the separated components to affect α-glucosidase and α-amylase were evaluated. By establishing concentration gradients and generating Lineweaver-Burk plots, the corresponding inhibition modes together with kinetic parameters were assessed. Following the evaluation of the outcomes of their combination with acarbose, computational docking and molecular dynamic simulations were carried out to analyse the interaction mechanisms and perform virtual screening against human enzymes.ResultsCompared with acarbose, 7 compounds, including flavonoid derivatives, amides and aromatic derivatives, with higher α-glucosidase inhibitory efficiencies were confirmed. It was found that those competitive/mixed candidates and acarbose interacted synergistically or additively on α-glucosidase. Moreover, 3 of them were able to inhibit α-amylase in mixed mode, and additive effects were observed in combination with acarbose. Through in silico docking, it was found that the active site residues as well as adjacent residues were involved in α-glucosidase and α-amylase binding, which were mainly achieved through hydrogen bonding. Among those dual-function flavonoids, Compound 9 was predicted to be a considerable inhibitor of human enzymes, as the formation of ligand-enzyme complexes was mediated by the residues responsible for substrate recognition and catalysis, the stabilities of which were reiterated by molecular dynamics simulations.ConclusionDespite their mild effects on α-amylase, considerable α-glucosidase inhibitory efficiencies and potential synergy with acarbose were exhibited by these natural candidates. Furthermore, a stable ligand, human α-glucosidase, was predicted by the performed simulations, which provided useful information for the application of Dracaena angustifolia Roxb in diabetes treatment.

Project description:Diabetes mellitus is a chronic disease that is becoming a serious global health problem. Diabetes has been considered to be one of the major risks of cataract and retinopathy. Synthetic and natural product inhibitors of carbohydrate degrading enzymes are able to reduce type 2 diabetes and its complications. For a long time, potatoes have been portrayed as unhealthy for diabetic patients by some nutritionist due to their high starch content. However, purple and red potato cultivars have received considerable attention from consumers because they have high levels of polyphenolic compounds that have potent antioxidant activities. In this study, we screened the total phenolics (TP) and total anthocyanins (TA) and analyzed the phenolic and anthocyanin compounds in selected potato cultivars and advanced selections with distinct flesh colors (purple, red, yellow and white). Purple and red potato cultivars had higher levels of TP and TA than tubers with other flesh colors. Chlorogenic acid is the predominant phenolic acid, and major anthocyanin is composed of the derivatives of petunidin, peonidin, malvidin and pelargonidin. We tested the potential inhibitory effect of potato extracts on the activities of ?-amylase and ?-glucosidase, which were targeted to develop antidiabetic therapeutic agents. We also measured inhibitory effect of potato extracts on aldose reductase (AR) which is a key enzyme that has been a major drug target for the development of therapies to treat diabetic complications. Purple flesh tubers extract showed the most effective inhibition of ?-amylase, ?-glucosidase, and aldose reductase with IC50 values 25, 42, and 32 ?g/ml, respectively. Kinetic studies showed that anthocyanins are noncompetitive inhibitors of these enzymes, whereas phenolic acids behaved as mixed inhibitors for ?-amylase and ?-glucosidase and noncompetitive inhibitors for AR. This study supports the development of a positive and healthful image of potatoes, which is an important issue for consumers.

Dataset Information

Smilax aristolochiifolia Root Extract and Its Compounds Chlorogenic Acid and Astilbin Inhibit the Activity of ?-Amylase and ?-Glucosidase Enzymes.

Publications

<i>Smilax aristolochiifolia</i> Root Extract and Its Compounds Chlorogenic Acid and Astilbin Inhibit the Activity of <i>α</i>-Amylase and <i>α</i>-Glucosidase Enzymes.

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