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

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...

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Bibliographic Details
Main Authors: Zhonglei Wang, Liyan Yang, Shuai Cui, Yingxi Liang, Xiaohua Zhang
Format: Article
Language:English
Published: MDPI AG 2014-04-01
Series:Molecules
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Online Access:http://www.mdpi.com/1420-3049/19/4/4791
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Summary: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.
ISSN:1420-3049