Plant alpha-amylase inhibitors: steady kinetic study, Bidens odorata aqueous infusion toxicity and stability in digestive tract simulation

Q4 Pharmacology, Toxicology and Pharmaceutics

Current Enzyme Inhibition Pub Date : 2022-09-29 DOI:10.2174/1573408018666220929154758

R. Valdés, E. P. S. Ceniceros, A. Iliná, J. L. Hernández, Sonia Yesenia Silva Belmares, Rodolfo Ramos González, Raihana Kunakova, R. Zaynullin

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引用次数: 0

Abstract

α-Amylase inhibitors are considered an important therapeutic target to control type 2 diabetes mellitus, reducing postprandial hyperglycemia. Medicinal plants are an important source with inhibitory activities of this enzyme, but little studied. The present study explored the α-amylase inhibition with extracts of 11 medicinal plants available in Saltillo, Mexico; the kinetic mechanism of inhibition of selected extracts and their phytochemical screening; evaluation of the toxicity of Bidens odorata extract in Artemia salina model, as well as estimation of its inhibitory effect under in vitro digestive tract conditions. The inhibitory assays were carried out spectrophotometrically with aqueous suspensions of the extracts obtained after evaporation of solvent from aqueous and ethanolic infusions. Eleven plants showed an inhibitory effect of α-amylase above 10% of the initial activity at 666.7 ppm. Four plants were selected for kinetic assay due to inhibitory effect near or higher than 20 %. The IC50 for the aqueous suspension of the ethanolic extract of Bidens odorata was 851 ppm similar to that detected with the drug acarbose. The inhibition mechanism for Bidens odorata, Cinchona succirub, and Opuntia ficus-indicata was competitive, and for Cnidoscolus chayamansa it was uncompetitive. All selected extracts presented flavonoids, the majority contained terpenoids, 3 contained tannins and phenols. The aqueous infusion of Bidens odorata - model of a functional drink, showed no toxicity and was characterized by resistance for 60 min to simulated stomach and intestinal conditions in vitro. The findings of this study revealed the species of medicinal plants, which were not previously considered as sources of α-amylase inhibitors, and their kinetic mechanisms of inhibition, which can be used for functional hypoglycemic food preparation.

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植物α-淀粉酶抑制剂：稳定动力学研究，鬼针草水溶液输注毒性和消化道稳定性模拟

α-淀粉酶抑制剂被认为是控制2型糖尿病，降低餐后高血糖的重要治疗靶点。药用植物是该酶抑制活性的重要来源，但研究较少。研究了墨西哥Saltillo地区11种药用植物提取物对α-淀粉酶的抑制作用;所选提取物的抑制动力学机制及其植物化学筛选对臭草提取物在盐蒿模型中的毒性进行评价，并对其体外消化道条件下的抑制作用进行评价。采用分光光度法对水浸液和乙醇浸液蒸发后得到的提取物进行水悬浮液的抑制试验。在666.7 ppm条件下，有11株α-淀粉酶的抑制作用超过初始活性的10%。选择4株抑制率接近或高于20%的植物进行动力学试验。气味Bidens odorata乙醇提取物水溶液悬浮液的IC50为851 ppm，与药物阿卡波糖检测的IC50相似。对花蔷薇、金鸡纳和无花果的抑制机制为竞争性抑制机制，对刺毛线虫的抑制机制为非竞争性抑制机制。所有提取物均含有黄酮类化合物，大部分含有萜类化合物，3种含有单宁和酚类化合物。功能饮料模型的水输注无毒性，对体外模拟胃肠条件具有60 min的耐药性。本研究结果揭示了以往未被认为是α-淀粉酶抑制剂来源的药用植物种类及其抑制α-淀粉酶抑制剂的动力学机制，可用于功能性降糖食品的制备。

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来源期刊

Current Enzyme Inhibition Pharmacology, Toxicology and Pharmaceutics-Drug Discovery

CiteScore

1.30

自引率

0.00%

发文量

期刊介绍： Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.