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Molecules 2014, 19(4), 4791-4801; doi:10.3390/molecules19044791

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

1
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China
2
College of Science, China University of Petroleum, Beijing 102249, China
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 10 March 2014 / Revised: 8 April 2014 / Accepted: 9 April 2014 / Published: 16 April 2014
(This article belongs to the Section Medicinal Chemistry)
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Abstract

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.
Keywords: rutin; nicotinic acid; synthesis; twin drug; VB3-QTME; SHR rats; anti-hypertensive effects rutin; nicotinic acid; synthesis; twin drug; VB3-QTME; SHR rats; anti-hypertensive effects
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Wang, Z.; Yang, L.; Cui, S.; Liang, Y.; Zhang, X. Synthesis and Anti-hypertensive Effects of the Twin Drug of Nicotinic Acid and Quercetin Tetramethyl Ether. Molecules 2014, 19, 4791-4801.

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