单味中药及其有效成分组织蛋白酶K抑制剂研究进展  

Study advance in cathepsin K inhibitors derived from single Chinese herb and its effective components

作　　者：薛黎明[1] 董志敏 金玉娥[1] 蒋益萍 Dieter Br mme XUE Liming;DONG Zhimin;JIN Yu′e;JIANG Yiping;DIETER Br mme(Shanghai Municipal Center for Disease Control and Prevention,Shanghai 200336;Shanghai Normal University,Shanghai 200234;The Second Military Medical University,Shanghai 200433,China;The University of British Columbia,Vancouver V6T1Z3,Canada)

机构地区：[1]上海市疾病预防控制中心,上海200336 [2]上海师范大学,上海200234 [3]中国人民解放军海军军医大学,上海200433 [4]不列颠哥伦比亚大学,加拿大温哥华V6T1Z3

出　　处：《中国骨质疏松杂志》2023年第1期95-98,103,共5页Chinese Journal of Osteoporosis

基　　金：上海市卫生健康委员会中医药重点项目(2020YZ001);国家自然科学基金项目(81503493);上海市“医苑新星”青年医学人才-公共卫生领导者项目资助计划(沪卫人事〔2021〕99号)。

摘　　要：组织蛋白酶K(Cathepsin K,CTSK)属于半胱氨酸蛋白酶,是抗骨质疏松药物研发的重要靶点,在破骨细胞中特异性高表达,对降解骨胶原基质至关重要。与临床常用的抑制骨吸收药物相比,CTSK抑制剂具有在不影响骨形成的情况下有效减少骨吸收的优点。迄今为止,CTSK抑制剂的研发均因安全性不足而失败,原因是对皮肤和血管系统等非骨组织造成副作用。传统中药富含抑制骨吸收的活性物质,一些文献表明中药来源的CTSK抑制剂抗骨质疏松作用明显,且没有明显的不良反应。笔者拟综述近10年中药来源的CTSK抑制剂的研究进展,资料主要来源于中国知网、万方和Web of Science数据库,为开发中药CTSK抑制剂和治疗CTSK相关疾病提供参考。Cathepsin K(CTSK)is a cysteine protease and an important target for the development of anti-osteoporosis drugs.CTSK is highly expressed in osteoclasts and essential for degrading the bone matrix.Compared with common clinical drugs for inhibiting bone resorption,CTSK inhibitors have the advantage of effectively reducing bone resorption without effecting bone formation.Until now,CTSK inhibitors have failed due to insufficient safety,causing side effects on non-bone tissues such as skin and the vascular system.Traditional Chinese medicine(TCM)is rich in active substances that inhibit bone resorption.To date,several publications have demonstrated that TCM-derived CTSK inhibitors are effective in skeletal diseases without obvious side effects.This review intends to summarize the research progress on CTSK inhibitors in TCM and provides some advises for the development of TCM-derived CTSK inhibitors and the treatment of related CTSK-associated diseases.

关 键 词：组织蛋白酶K 骨质疏松 中药 活性位点抑制剂 非活性位点抑制剂 

分 类 号：R285[医药卫生—中药学]