Celastrol ameliorates energy metabolism dysfunction of hypertensive rats by dilating vessels to improve hemodynamics

作者全名："Zou, Gang; Yu, Ruihong; Zhao, Dezhang; Duan, Zhaohui; Guo, Shimin; Wang, Tingting; Ma, Limei; Yuan, Zhiyi; Yu, Chao"

作者地址："[Zou, Gang; Yu, Ruihong; Zhao, Dezhang; Duan, Zhaohui; Guo, Shimin; Wang, Tingting; Ma, Limei; Yuan, Zhiyi; Yu, Chao] Chongqing Med Univ, Coll Pharm, Chongqing 400016, Peoples R China; [Zou, Gang; Yu, Ruihong; Duan, Zhaohui; Guo, Shimin; Wang, Tingting; Ma, Limei; Yuan, Zhiyi; Yu, Chao] Chongqing Med Univ, Coll Pharm, Chongqing Key Lab Pharmaceut Metab Res, 1 Yixueyuan Rd, Chongqing 400016, Peoples R China; [Zhao, Dezhang] Res Ctr Innovat Pharmaceut & Expt Anal Technol, Chongqing 400016, Peoples R China"

通信作者："Yu, C (通讯作者)，Chongqing Med Univ, Coll Pharm, Chongqing 400016, Peoples R China.; Yu, C (通讯作者)，Chongqing Med Univ, Coll Pharm, Chongqing Key Lab Pharmaceut Metab Res, 1 Yixueyuan Rd, Chongqing 400016, Peoples R China."

来源：JOURNAL OF NATURAL MEDICINES

ESI学科分类：PHARMACOLOGY & TOXICOLOGY

WOS号：WOS:001111236800001

JCR分区：Q2

影响因子：3.3

年份：2024

卷号：78

期号：1

开始页：191

结束页：207

文献类型：Article

关键词：Celastrol; Blood flow; Energy metabolism; Hypertension; Vasodilation

摘要："The impact of hypertension on tissue and organ damage is mediated through its influence on the structure and function of blood vessels. This study aimed to examine the potential of celastrol, a bioactive compound derived from Tripterygium wilfordiiHook F, in mitigating hypertension-induced energy metabolism disorder and enhancing blood perfusion and vasodilation. In order to investigate this phenomenon, we conducted in vivo experiments on renovascular hypertensive rats, employing indirect calorimetry to measure energy metabolism and laser speckle contrast imaging to evaluate hemodynamics. In vitro, we assessed the vasodilatory effects of celastrol on the basilar artery and superior mesenteric artery of rats using the Multi Wires Myograph System. Furthermore, we conducted preliminary investigations to elucidate the underlying mechanism. Moreover, administration of celastrol at doses of 1 and 2 mg/kg yielded a notable enhancement in blood flow ranging from 6 to 31% across different cerebral and mesenteric vessels in hypertensive rats. Furthermore, celastrol demonstrated a concentration-dependent (1 x 10-7 to 1 x 10-5 M) arterial dilation, independent of endothelial function. This vasodilatory effect could potentially be attributed to the inhibition of Ca2+ channels on vascular smooth muscle cells induced by celastrol. These findings imply that celastrol has the potential to ameliorate hemodynamics through vasodilation, thereby alleviating energy metabolism dysfunctions in hypertensive rats. Consequently, celastrol may hold promise as a novel therapeutic agent for the treatment of hypertension. [GRAPHICS] ."

基金机构：National Natural Science Foundation of China

基金资助正文：Not applicable.