Repurposing of pharmaceutical drugs by high-throughput approach for antihypertensive activity as inhibitors of angiotensin-converting enzyme (ACE) using HPLC-ESI-MS/MS method

Arabian Journal of Chemistry

Syed Ghulam Musharraf¹  Jalal Uddin²  Yahya Ibrahim Asiri³  Muhammad Salman Bhatti⁴  Hesham R. El-Seedi⁵ 

[1]International Research Center for Food Nutrition and Safety, Jiangsu University, Zhenjiang 212013, China

[2]Department of Pharmaceutical Chemistry, College of Pharmacy, King Khalid University, Abha 62529, Saudi Arabia

[3]Department of Pharmacology and Toxicology, College of Pharmacy, King Khalid University, Abha 625629, Saudi Arabia

[4]H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan

[5]Pharmacognosy Group, Department of Pharmaceutical Biosciences, BMC, Uppsala University, SE-751 23 Uppsala, Sweden

关键词: Angiotensin-converting enzyme;    Antihypertensive activity;    Inhibitory activity;    Drugs &;    natural products;    LC-QqQ-MS;    Repurposing of drugs;   

DOI  :  

来源: DOAJ

【 摘 要 】

Angiotensin-converting enzyme (ACE) plays an important role in regulating blood pressure in the body by converting angiotensin-I into angiotensin-II. It is the basic component of Renin angiotensin aldosterone system (RAAS), imbalance of RAAS may leads to many cardiovascular and renal diseases. There are many marketed available drugs for the inhibition of ACE, but prolonged use of some drugs may cause the progressive side effects. Repurposing of existing drugs can be a way to find new inhibitors of ACE. In this study, a high-throughput and sensitive method of HPLC-ESI-QqQ-MS with good reproducibility (%RSD < 9.98) and linearity (R2 = 0.999) was used to investigate the 77 commercial drugs for their inhibitory potential as antihypertensive drugs. Among these drugs, 41 drugs were found active and 36 of them showed moderate to good inhibition with lowest IC50 = 272 µM. This study showed that different pharmaceutical drugs can also be used as ACE inhibitor after necessary clinical trials or validation.

【 授权许可】

Unknown