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作 者:郑瑞蓉 欧阳倩兮 刘子瑶 李林楠 杨莉[1] 王峥涛[1] ZHENG Rui-rong;OUYANG Qian-xi;LIU Zi-yao;LI Lin-nan;YANG Li;WANG Zheng-tao(Shanghai Key Laboratory of Compound Chinese Medicines,MOE Key Laboratory of Standardization of Chinese Medicines,SATCM Key Laboratory of New Resources and Quality Evaluation of Chinese Medicines,Institute of Chinese Materia Medica,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China;School of Pharmacy and Pharmaceutical Sciences,Xiamen Medical College,Xiamen 361023,China)
机构地区:[1]上海中医药大学中药研究所,中药标准化教育部重点实验室,国家中医药管理局中药新资源与质量评价重点实验室,上海市复方中药重点实验室,上海201203 [2]厦门医学院药学系,福建厦门361023
出 处:《中国中药杂志》2024年第4期858-867,共10页China Journal of Chinese Materia Medica
基 金:国家自然科学基金项目(82130115,82274223);国家中医药管理局高水平中医药重点学科建设项目(zyyzdxk-2023058);上海市晨光计划项目(20CG51);上海中医药大学“杏林百人”计划项目(20QN012)。
摘 要:良性前列腺增生是一种常见的男性泌尿系统疾病,其发病率在我国呈逐年上升的趋势。目前针对该疾病的发病机制尚未十分明确,有研究认为其发病机制与类固醇激素水平变化有关。当体内二氢睾酮的含量过高,会引起前列腺增生等相关疾病。二氢睾酮由睾酮在5α-还原酶的作用下转化而成,因而通过抑制该酶活性,可减少二氢睾酮的生成量,进而达到减轻前列腺增生的效果。从天然药物中筛选和发现新的、有效和安全的5α-还原酶抑制剂,应用于防治前列腺增生,但又不影响男性的生理功能,成为该领域研究的热点话题。该文总结了5α-还原酶的作用特点及组织分布,临床常用的5α-还原酶抑制剂及其副作用,并整理了中药和天然药物中5α-还原酶抑制剂的筛选和发现,概括了前列腺增生实验动物模型和常用检测指标,为良性前列腺增生发病机制及防治药物的研发提供参考依据。Benign prostatic hyperplasia(BPH) is a common disease of the male urinary system,and its incidence rate in China is increasing.However,the mechanism underlying the pathogenesis of BPH remains unclear.Some studies demonstrated that the incidence of BPH was related to the change in the levels of steroid hormones.Too high content of dihydrotestosterone(DHT) in the body may cause BPH and other related diseases.Testosterone(T) is converted to DHT by 5α-reductase(SRD5A).By inhibiting the activity of this enzyme,the production of DHT can be reduced,and then the incidence of BPH can be lowered.Therefore,it has drawn great attention to screen and discover safer and more effective 5α-reductase inhibitors from natural medicines to treat prostatic hyperplasia without affecting the physiological function of men.This review summarizes the characteristics and tissue distribution of 5α-reductase,the discovery of 5α-reductase inhibitors in traditional Chinese medicine and natural medicines,5α-reductase inhibitors commonly used in clinical practice and their side effects,as well as the animal models of prostatic hyperplasia and common detection indicators,aiming to provide a reference for more in-depth understanding and research about BPH and development of drugs.
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