title: Synthesis and anti-hypertensive effects of the twin drug of nicotinic acid and quercetin tetramethyl ether.
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.
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. wzlei2011bzy@sina.com.
authors.forename: Zhonglei
authors.initials: Z
authors.lastname: Wang
authors.affiliation: College of Science, China University of Petroleum, Beijing 102249, China. ylyan2011cup@163.com.
authors.forename: Liyan
authors.initials: L
authors.lastname: Yang
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. cuishuaistrive@163.com.
authors.forename: Shuai
authors.initials: S
authors.lastname: Cui
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. yxx.liang@163.com.
authors.forename: Yingxi
authors.initials: Y
authors.lastname: Liang
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. xhua_zhang@sina.com.
authors.forename: Xiaohua
authors.initials: X
authors.lastname: Zhang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D004987:Ethers; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D008297:Male; D009525:Niacin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D011794:Quercetin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D011918:Rats, Inbred SHR; D011921:Rats, Inbred WKY; D012431:Rutin / Q000737:chemistry; D013997:Time Factors
chemical_list: D000959:Antihypertensive Agents; D004987:Ethers; D009525:Niacin; D012431:Rutin; D011794:Quercetin
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