Mechanism & inhibition kinetics of bioassay-guided fractions of Indian medicinal plants and foods as ACE inhibitors

摘要

Hypertension is a becoming a major threat to the world. Angiotensin converting enzyme (ACE) is a key part in the renin angiotensin aldosterone system (RAAS) which control blood pressure. Over expression of RAAS is related with vascular hypertension, ACE inhibition has turned into a noteworthy target for controlling hypertension. In the search of lead molecules from plant origin as a substitute for toxic synthetic drugs, 25 Indian medicinal plants and foods were screened for their ACE inhibitory activity. IC50(50% inhibition of ACE) values of hydroalcoholic crude extracts and fraction were determined by a colorimetric method. Active fractions were further screened to determine the enzyme kinetics, mode, specificity and mechanism of inhibition. Standardization was done by determining total phenolics and flavonoids as gallic acid and quercetin equivalents/mg of extract respectively. Among 25 crude extracts,Cynara scolymusextract showed the best activity, IC50value 356.62?μg/mL. ACE inhibition resulting from protein precipitation was highest inCoscinium fenestratum. Lineweaver-Burk plots revealed a competitive mode of inhibition forPunica granatumethyl acetate fraction. Fractions ofCassia occidentalis,Cynara scolymusandEmbelia ribeswere found to be non-specific inhibitors of ACE.Embelia ribes, Cassia occidentalisandCoscinium fenestratumfractions inhibited the ACE by Zn2+ion chelation. Research revealed the potential of tested plants fractions as ACE inhibitors along with their inhibition kinetics and mechanism of inhibition. These active plant fractions might find importance in the development of potential antihypertensive agents after further investigations using preclinical and clinical trials.