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

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

1,†
, 2,†
, 1
, 1
 and 1,*
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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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