Comparative In Vitro analysis and inhibition kinetics of Vernonia amygdalina chloroform extract as a potent dual inhibitor of α-Amylase and α-Glucosidase for the management of diabetes and obesity

Background: The global burden of diabetes and obesity requires new treatments. This study investigated the chloroform extract of Vernonia amygdalina as a natural alternative to acarbose, a standard drug for managing post-meal blood sugar that often causes side effects. Objectives: We measured the extract's ability to inhibit key carbohydrate-digesting enzymes (α-amylase and α-glucosidase) in vitro, determined its potency (IC₅₀), and analyzed its mechanism of action compared to acarbose.Methods: This study evaluated the in vitro inhibitory activity of a chloroform extract of V. amygdalina leaves against α-amylase and α-glucosidase using spectrophotometric assays. The inhibitory potency was quantified by IC₅₀ values and compared to acarbose. Enzyme kinetics were analyzed via Lineweaver-Burk plots to determine the mechanism of inhibition.Results: The chloroform extract exhibited significantly stronger inhibition of both enzymes compared to acarbose. At ۱ mg/mL, it inhibited α-amylase by ۷۶.۴% (acarbose: ۶۲.۸%) and α-glucosidase by ۶۲.۵% (acarbose: ۴۶.۹%). The IC₅₀ values further confirmed its superior potency, with values of ۰.۲۴ mg/mL for α-amylase (acarbose: ۰.۴۹ mg/mL) and ۰.۵۰ mg/mL for α-glucosidase (acarbose: ۱.۰۱ mg/mL). Kinetic analysis revealed a competitive inhibition mechanism for α-glucosidase, characterized by an increased Michaelis constant (Kₘ) and unchanged maximum velocity (Vₘₐₓ), indicating direct binding of bioactive compounds to the enzyme’s active site.Conclusions: The chloroform extract of V. amygdalina is a highly potent, competitive dual inhibitor of α-amylase and α-glucosidase, outperforming acarbose. Its efficacy, coupled with a defined mechanism of action, supports its traditional use and highlights its potential as a natural therapeutic agent for managing postprandial hyperglycemia in diabetes and obesity. Future studies should focus on isolating active compounds and validating these findings in in vivo models.

کلیدواژه ها:

Vernonia amygdalina ، &alpha ، -glucosidase ، &alpha ، -amylase ، Diabetes ، Obesity