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
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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.
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(4):4791-4801.
Wang, Zhonglei; Yang, Liyan; Cui, Shuai; Liang, Yingxi; Zhang, Xiaohua. 2014. "Synthesis and Anti-hypertensive Effects of the Twin Drug of Nicotinic Acid and Quercetin Tetramethyl Ether." Molecules 19, no. 4: 4791-4801.