Synthesis and Anti-hypertensive Effects of the Twin Drug of Nicotinic Acid and Quercetin Tetramethyl Ether

Molecules

Zhonglei Wang¹  Liyan Yang²  Shuai Cui¹  Yingxi Liang¹ 

[1] School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China; E-Mails:;College of Science, China University of Petroleum, Beijing 102249, China; E-Mail:

关键词: rutin;    nicotinic acid;    synthesis;    twin drug;    VB3-QTME;    SHR rats;    anti-hypertensive effects;   

DOI  :  10.3390/molecules19044791

来源: mdpi

【 摘 要 】

A novel twin drug consisting of nicotinic acid (VB3) and quercetin tetramethyl ether (QTME) has been synthesized as an antihypertensive in a total yield of 79.2% through methylation, hydrolysis, acylation and esterification starting from rutin. The structures of synthesized compounds were elucidated by ¹H-NMR, ¹³C-NMR and elemental analysis. The anti-hypertensive effects of an oral daily dose (15 mg/kg) of the synthesized compounds in spontaneously hypertensive (SHR) rats and normotensive Wistar Kyoto (WKY) rats were analysed. The data demonstrate that the twin drug VB3-QTME both reduces the elevated blood pressure and prolongs the action time in SHR rats without effect on WKY rats. However, definitive evidence of a precise mechanism of action by which VB3-QTME might decrease blood pressure remains elusive. Based on the results, the therapeutic potential of this twin drug is discussed.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.