Department of Preventive Medicine, School of Public Health, Zunyi Medical University, Zunyi, Guizhou, China.
Key Laboratory of Basic Pharmacology of Ministry of Education and Joint International Research Laboratory of Ethnomedicine of Ministry of Education, Zunyi Medical University, Zunyi, Guizhou, 563003, China.
Pharmacol Res. 2019 Mar;141:541-550. doi: 10.1016/j.phrs.2018.12.019. Epub 2019 Jan 4.
Rutaecarpine is a bioactive alkaloid isolated from Evodia rutaecarpa (Wu Zhu Yu, Family: Rutaceae), a versatile medicinal herb which is clinically used to treat headache, abdominal pain, postpartum hemorrhage, dysentery, and amenorrhea in China. As one of the most representative indolopyridoquinazoline alkaloids of Evodia rutaecarpa, rutaecarpine has broad pharmacological actions in treating various cardiovascular, cerebrovascular, and metabolic diseases. The cardiovascular actions of rutaecarpine have aroused intense research interest due to its purported inotropic and chronotropic, vasodilatory, anti-platelet activation, anti-oxidant, anti-inflammatory, and lipid-lowering effects. Biochemical and pharmacological studies have illustrated the molecular targets of rutaecarpine, such as TRPV1, CGRP, AMPK, ABCA1, and β1-AR. Furthermore, several rutaecarpine derivatives (such as bromorutaecarpine and fluororutaecarpine) have been shown to possess cardioprotective and vasculoprotective effects with improved safety profile. Hereby, we provide a systematic overview of pharmacological actions, toxicological effects, and molecular targets of rutaecarpine in cardiovascular disease prevention/treatment, aiming to exploit the therapeutic potential of rutaecarpine and its derivatives in treating cardiovascular diseases.
吴茱萸碱是从吴茱萸（芸香科）中分离得到的一种生物活性生物碱，吴茱萸是一种用途广泛的药用植物，在中国临床上用于治疗头痛、腹痛、产后出血、痢疾和闭经。作为吴茱萸中最具代表性的吲哚并吡啶喹嗪生物碱之一，吴茱萸碱在治疗各种心血管、脑血管和代谢性疾病方面具有广泛的药理作用。由于吴茱萸碱具有变力性和变时性、血管扩张、抗血小板活化、抗氧化、抗炎和降血脂作用，其心血管作用引起了强烈的研究兴趣。生化和药理学研究阐明了吴茱萸碱的分子靶点，如 TRPV1、CGRP、AMPK、ABCA1 和β1-AR。此外，一些吴茱萸碱衍生物（如溴吴茱萸碱和氟吴茱萸碱）已被证明具有心脏保护和血管保护作用，且安全性更好。因此，我们系统地综述了吴茱萸碱在预防/治疗心血管疾病方面的药理作用、毒理学作用和分子靶点，旨在开发吴茱萸碱及其衍生物治疗心血管疾病的治疗潜力。
