高血压正在成为世界的主要威胁。血管紧张素转换酶(ACE)是肾素血管紧张素醛固酮系统(RAAS)中控制血压的关键部分。RAAS的过度表达与血管性高血压有关,ACE抑制已成为控制高血压的值得注意的目标。在寻找植物来源的铅分子作为有毒合成药物的替代品时,筛选了25种印度药用植物和食品的ACE抑制活性。通过比色法测定水醇粗提物和级分的IC50(ACE的50%抑制)值。进一步筛选活性组分以确定酶动力学,mode,特异性和抑制机制。通过分别测定没食子酸和槲皮素当量/mg提取物的总酚和黄酮来进行标准化。在25种粗提物中,Cynarascolymus提取物显示出最好的活性,IC50值356.62μg/mL。蛋白沉淀引起的ACE抑制作用在开窗草中最高。Lineweaver-Burk图揭示了对Punicagranatus乙酸乙酯部分的竞争性抑制模式。西花决明子的部分,发现Cynarascolymus和Enbeliaribes是ACE的非特异性抑制剂。恩贝丽亚里布,西花决明和开窗决明部分通过Zn2离子螯合抑制ACE。研究揭示了测试植物部分作为ACE抑制剂的潜力,以及它们的抑制动力学和抑制机制。在使用临床前和临床试验进行进一步研究后,这些活性植物部分可能在潜在抗高血压药的开发中很重要。
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 scolymus extract showed the best activity, IC50 value 356.62 μg/mL. ACE inhibition resulting from protein precipitation was highest in Coscinium fenestratum. Lineweaver-Burk plots revealed a competitive mode of inhibition for Punica granatum ethyl acetate fraction. Fractions of Cassia occidentalis, Cynara scolymus and Embelia ribes were found to be non-specific inhibitors of ACE. Embelia ribes, Cassia occidentalis and Coscinium fenestratum fractions 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.