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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Autores principales: Wang, Zhonglei, Yang, Liyan, Cui, Shuai, Liang, Yingxi, Zhang, Xiaohua
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271710/
https://www.ncbi.nlm.nih.gov/pubmed/24743936
http://dx.doi.org/10.3390/molecules19044791
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author Wang, Zhonglei
Yang, Liyan
Cui, Shuai
Liang, Yingxi
Zhang, Xiaohua
author_facet Wang, Zhonglei
Yang, Liyan
Cui, Shuai
Liang, Yingxi
Zhang, Xiaohua
author_sort Wang, Zhonglei
collection PubMed
description 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 (1)H-NMR, (13)C-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.
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spelling pubmed-62717102019-01-02 Synthesis and Anti-hypertensive Effects of the Twin Drug of Nicotinic Acid and Quercetin Tetramethyl Ether Wang, Zhonglei Yang, Liyan Cui, Shuai Liang, Yingxi Zhang, Xiaohua Molecules Article 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 (1)H-NMR, (13)C-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. MDPI 2014-04-16 /pmc/articles/PMC6271710/ /pubmed/24743936 http://dx.doi.org/10.3390/molecules19044791 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Wang, Zhonglei
Yang, Liyan
Cui, Shuai
Liang, Yingxi
Zhang, Xiaohua
Synthesis and Anti-hypertensive Effects of the Twin Drug of Nicotinic Acid and Quercetin Tetramethyl Ether
title Synthesis and Anti-hypertensive Effects of the Twin Drug of Nicotinic Acid and Quercetin Tetramethyl Ether
title_full Synthesis and Anti-hypertensive Effects of the Twin Drug of Nicotinic Acid and Quercetin Tetramethyl Ether
title_fullStr Synthesis and Anti-hypertensive Effects of the Twin Drug of Nicotinic Acid and Quercetin Tetramethyl Ether
title_full_unstemmed Synthesis and Anti-hypertensive Effects of the Twin Drug of Nicotinic Acid and Quercetin Tetramethyl Ether
title_short Synthesis and Anti-hypertensive Effects of the Twin Drug of Nicotinic Acid and Quercetin Tetramethyl Ether
title_sort synthesis and anti-hypertensive effects of the twin drug of nicotinic acid and quercetin tetramethyl ether
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271710/
https://www.ncbi.nlm.nih.gov/pubmed/24743936
http://dx.doi.org/10.3390/molecules19044791
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