摘要
甲状腺激素具有促进机体的生长发育、调节基础代谢率、影响人体的心血管系统和体温的稳态等作用,并且随着激素水平的增加可以改善血脂谱并降低体质量。但因其同时又会对人体产生心功能受损和骨质疏松等不良反应,因此在很大程度上限制了它们的使用。近期通过研究发现,甲状腺激素代谢物包括3,5-T2、3-T1AM、Triac、Tetrac以及rT3和Dio3等,不仅可以很好地避免甲状腺激素的不良反应,而且可以通过不同的作用机制来产生降低血脂,减轻胰岛素抵抗,营养心肌,调节神经病变以及抗肿瘤增殖等作用。新近研发的GC-1、KB-141、KB-2115、MGL-3196、VK-2809(MB-07811)等甲状腺激素类似物,可以更特异性地作用于THR-α和THR-β,甚至可以和突变的THR-β相结合,将对人体心脏的保护作用和机体的代谢作用发挥到最大,并在此基础上,开发出新型拟甲状腺素化合物IS-25及其前药TG-68,在促进肝脏的再生和抑制肝癌的增殖等方面,有了更进一步的探索。本文通过查阅近些年的文献,对甲状腺激素代谢物和类似物的作用机制以及临床实验研究进行论述。
Thyroid hormone can promote the growth and development of the body,regulate the basal metabolic rate,affect the body’s cardiovascular system and body temperature homeostasis,and can improve blood lipid profile and reduce body mass with the increase of hormone level.However,their use has been limited to a great extent because of their adverse reactions to the human body such as impaired heart function and osteoporosis.Recent studies have found that thyroid hormone metabolites,including 3,5-T2,3-T1AM,Triac,Tetrac,rT3 and Dio 3,can not only avoid the adverse reactions of thyroid hormone,but also reduce blood lipid,alleviate insulin resistance,nourish myocardium through different mechanisms of action and regulate neuropathy and anti-tumor proliferation.Newly developed thyroid hormone analogues such as GC-1,KB-141,KB-2115,MGL-3196,VK-2809(MB-07811)can act more specifically on THR-αand THR-β,and even combine with mutant THR-βto maximize the protective effect on the human heart and the metabolic effect of the body.On this basis,a new thyroxine compound IS-25 and its prodrug TG-68 were developed,which provides further exploration in promoting liver regeneration and inhibiting the proliferation of liver cancer.This paper discussed the mechanism of action and clinical experiments of thyroid hormone metabolites and analogues by reviewing recent literature.
作者
周哲
徐洪涛
郅扶旻
杜丽坤
李舒梅
于洪宇
ZHOU Zhe;XU Hongtao;ZHI Fumin;DU Likun;LI Shumei;YU Hongyu(Graduate School,Heilongjiang University of Traditional Chinese Medicine,Harbin 150040,China;Department of Endocrine,the First Affiliated Hospital of Heilongjiang University of Traditional Chinese Medicine,Harbin 150040,China;Endoscopy Room,the First Affiliated Hospital of Heilongjiang University of Chinese Medicine,Harbin 150040,China)
出处
《温州医科大学学报》
2025年第2期153-160,共8页
Journal of Wenzhou Medical University
基金
黑龙江省中医药管理局基金项目(ZHY2022-154,ZHY2023-113,ZYW2024-122)
黑龙江中医药大学科研基金项目(201216)
第七批全国老中医药专家学术经验继承工作项目(国中医药人教函[2022]76号)
黑龙江省自然科学基金项目(PL2024H216)
黑龙江中医药大学附属第一医院国家自然科学基金培育支持计划项目([2024]286号)。
