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Dual-targeting Rutaecarpine-NO donor hybrids as novel anti-hypertensive agents by promoting release of CGRP.

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成果类型:
期刊论文
作者:
Ma, Jinjin;Chen, Lan;Fan, Jinbao;Cao, Wei;Zeng, Guangyao;...
通讯作者:
Zhou, Yingjun;Deng, Xu
作者机构:
[Zeng, Guangyao; Deng, Xu; Zhou, YJ; Deng, X; Zhou, Yingjun; Cao, Wei; Fan, Jinbao; Li, Yuanjian; Ma, Jinjin; Chen, Lan] Cent S Univ, Xiangya Sch Pharmaceut Sci, Changsha 410013, Hunan, Peoples R China.
[Wang, Yajing] Hunan Univ Chinese Med, Changsha 410028, Hunan, Peoples R China.
通讯机构:
[Zhou, YJ; Deng, X] C
Cent S Univ, Xiangya Sch Pharmaceut Sci, Changsha 410013, Hunan, Peoples R China.
语种:
英文
关键词:
Anti-hypertensive agents;CGRP;Dual-targeting;Rutaecarpine-NO donor hybrids
期刊:
European Journal of Medicinal Chemistry
ISSN:
0223-5234
年:
2019
卷:
168
页码:
146-153
基金类别:
National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21302193, 81573314]; Nature Science Foundation of Hunan ProvinceNatural Science Foundation of Hunan Province [2018113707]; Changsha Science and Technology Projects [kq1701088]; Start-up funds of Central South University
机构署名:
本校为其他机构
摘要:
CGRP, known as the most potent vasodilator substance, plays an important role in hypertension initiation and development. TRPV1 and TRPA1 are critical in promoting the synthesis and release of CGRP, thereby regulating the cardiovascular tone. Rutaecarpine exhibits potent vasodilator and hypertensive effects by stimulating CGRP synthesis and release via activation of TRPV1. And NO has been shown to react with H2S in vivo to form HNO, thereby activating HNO-TRPA1-CGRP pathway. Inspired by combination therapy, 11 rutaecarpine-furoxan hybrids were designed, synthesized and evaluated. The results d...

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