Machine Learning and In Vitro Chemical Screening of Potential α-Amylase and α-Glucosidase Inhibitors from Thai Indigenous Plants.

Tarapong Srisongkram,Thaweesak Thitimetharoch,Natthida Weerapreeyakul,Sasisom Waithong

doi:10.3390/nu14020267

Abstract

Diabetes mellitus is a major predisposing factor for cardiovascular disease and mortality. α-Amylase and α-glucosidase enzymes are the rate-limiting steps for carbohydrate digestion. The inhibition of these two enzymes is clinically used for the treatment of diabetes mellitus. Here, in vitro study and machine learning models were employed for the chemical screening of inhibiting the activity of 31 plant samples on α-amylase and α-glucosidase enzymes. The results showed that the ethanolic twig extract of Pinus kesiya had the highest inhibitory activity against the α-amylase enzyme. The respective ethanolic extract of Croton oblongifolius stem, Parinari anamense twig, and Polyalthia evecta leaf showed high inhibitory activity against the α-glucosidase enzyme. The classification analysis revealed that the α-glucosidase inhibitory activity of Thai indigenous plants was more predictive based on phytochemical constituents, compared with the α-amylase inhibitory activity (1.00 versus 0.97 accuracy score). The correlation loading plot revealed that flavonoids and alkaloids contributed to the α-amylase inhibitory activity, while flavonoids, tannins, and reducing sugars contributed to the α-glucosidase inhibitory activity. In conclusion, the ethanolic extracts of P. kesiya, C. oblongifolius, P. anamense, and P. evecta have the potential for further chemical characterization and the development of anti-diabetic recipes.

Highlights

IntroductionDiabetes mellitus (DM) has become one of the prevalent issues with the rising obesity crisis, leading to cardiovascular complications and mortality [1]
Introduction published maps and institutional affilDiabetes mellitus (DM) has become one of the prevalent issues with the rising obesity crisis, leading to cardiovascular complications and mortality [1]
We found that five plants exhibited inhibition against both α-amylase and α-glucosidase, which were P. evecta, P. kesiya, G. cowa, C. formosum, and P. debilis

Summary

Introduction

Diabetes mellitus (DM) has become one of the prevalent issues with the rising obesity crisis, leading to cardiovascular complications and mortality [1]. Type II DM is the most common form of DM, accounting for 90–95% percent of DM diagnoses [1,3], caused by the impairment of insulin secretion by pancreatic β cells and the incapacity of tissues to use insulin [4]. The inability to produce or use insulin in the cells results in a high sudden surge of glucose levels in the bloodstream, called postprandial hyperglycemia. Long-term postprandial hyperglycemia leads to oxidative stress, produced by reactive oxygen species (ROS) [5]. The ROS can destroy the microvascular tissues, and increase the risk of micro-and macro-vascular complications, resulting in hypertension, myocardial infarction, diabetes retinopathy, dyslipidemia, and diabetes nephropathy [6]

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