《生命科学》 2023, 35(10): 1337-1347

脂联素受体激动剂研究进展

孔燕明 , 刘　聪 , 邢晓钰 , 李嘉鑫 , 魏诗音 , 姚泽龙 , 曹中赞^* , 栾新红^*

沈阳农业大学动物科学与医学学院，沈阳 110161

摘　要：

脂联素是人和动物体内重要的内源性生物活性激素，具有改善胰岛素抵抗、调控脂类代谢、抗动脉粥样硬化、保护心脏、抗炎、抗氧化应激、抗纤维化以及调控细胞凋亡等作用。脂联素需要与其受体结合才能发挥生物学功能，但因其结构和浓度的影响，脂联素在临床上的应用受到一定程度限制。研究发现，多种脂联素受体激动剂通过激活脂联素受体发挥与脂联素相似的生物学功能，且脂联素受体激动剂多为人工合成的小分子或筛选的多肽，作用效果更加明确。本文整理了目前已经报道的脂联素受体激动剂及其研究进展，概述了脂联素受体激动剂对肝脏、肾脏、心脏、血管、眼和皮肤等相关器官或组织疾病的作用或影响，为开发以脂联素及其受体为靶点的治疗药物提供理论依据。

通讯作者：曹中赞 , Email:caozhongzan@syau.edu.cn 栾新红 , Email:xhluan@syau.edu.cn

Research progress of adiponectin receptor agonists

KONG Yan-Ming , LIU Cong , XING Xiao-Yu , LI Jia-Xin , WEI Shi-Yin , YAO Ze-Long , CAO Zhong-Zan^* , LUAN Xin-Hong^*

College of Animal Science and Veterinary Medicine, Shenyang Agricultural University, Shenyang 110161, China

Abstract:

Adiponectin is an important endogenous bioactive hormone in human and animals, which has the functions of improving insulin resistance, regulating lipid metabolism, anti-atherosclerosis, protecting the heart, antiinflammation, anti-oxidative stress, anti-fibrosis and regulating apoptosis. Adiponectin needs to bind to its receptor to exert its biological function, but its clinical application is limited to some extent due to its structure and concentration. It has been found that many adiponectin receptor agonists play similar biological functions to adiponectin by activating adiponectin receptor, and adiponectin receptor agonists are mostly synthetic small molecules or screened polypeptides, with more clear effect. This review summarizes the adiponectin receptor agonists and their reported research progress, and outlines their effects on liver, kidney, heart, blood vessel, eye, skin and other related organs or tissue diseases, whereby provides a theoretical basis for the development of therapeutic drugs based on adiponectin and its receptors.

Communication Author：CAO Zhong-Zan , Email:caozhongzan@syau.edu.cn LUAN Xin-Hong , Email:xhluan@syau.edu.cn