单位：[1]Department of Urology, Tianjin Institute of Urology, The Second Hospital of Tianjin Medical University, Tianjin, China[2]China-Korea Joint Research Center for Male Reproductive and Sexual Medicine, Institute of Urology, Tianjin, China[3]Knuppe Molecular Urology Laboratory, Department of Urology, School of Medicine, University of California, San Francisco, CA, USA[4]Department of Urology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China华中科技大学同济医学院附属同济医院[5]Institute of Urology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China华中科技大学同济医学院附属同济医院[6]Department of Urology, Beijing Friendship Hospital, Capital Medical University, Beijing, China临床科室泌尿外科泌尿外科首都医科大学附属北京友谊医院[7]Department of Urology, Seoul St. Mary’s Hospital, the Catholic University of Korea, Seoul, Korea[8]Andrology Center, Peking University First Hospital, Peking University, Beijing, China
Background and Objective: Although epimedium herb (EH) has been widely used in ancient Chinese medicine to enhance sexual activity, its pharmacological mechanism is not clear. Modern studies have shown that epimedium herb is rich in icariin (ICA, a flavonoid compound), and 91.2% of icariin is converted to icariside II (ICA II) by hydrolytic enzymes in intestinal bacteria after oral administration. YS-10 is a synthetic derivative of icariside II. The aim of this review was to summarize the contemporary evidence regarding the pharmacokinetics, therapeutic properties, and molecular biological mechanisms of ICA and some ICA derivatives for erectile dysfunction therapy. Methods: A detailed search was conducted in the PubMed database using keywords and phrases, such as "icariin" AND "erectile dysfunction", "icariside II" AND "erectile dysfunction". The publication time is limited to last 20 years. Articles had to be published in peer reviewed journals. Key Content and Findings: ICA and its some derivatives showed the specific inhibition on phosphodiesterase type 5 (PDE5) and the promotion of testosterone synthesis. In addition, by regulating various reliable evidence of signaling pathways such as PI3K/AKT, TGF beta 1/Smad2, p38/MAPK, Wnt and secretion of various cytokines, ICA and ICA derivatives can activate endogenous stem cells (ESCs) leading to endothelial cell and smooth muscle cell proliferation, nerve regeneration and fibrosis inhibition, repair pathological changes in penile tissue and improve erectile function. Conclusions: ICA and some of its derivatives could be a potential treatment for restoring spontaneous erections. In addition ICA and his derivatives may also be valuable as a regenerative medicine approach for other diseases, but more clinical and basic researches with high quality and large samples are recommended.
基金：
National Natural Science Foundation of China [81971379]
第一作者单位：[1]Department of Urology, Tianjin Institute of Urology, The Second Hospital of Tianjin Medical University, Tianjin, China[2]China-Korea Joint Research Center for Male Reproductive and Sexual Medicine, Institute of Urology, Tianjin, China
共同第一作者：
通讯作者：
通讯机构：[1]Department of Urology, Tianjin Institute of Urology, The Second Hospital of Tianjin Medical University, Tianjin, China[2]China-Korea Joint Research Center for Male Reproductive and Sexual Medicine, Institute of Urology, Tianjin, China[8]Andrology Center, Peking University First Hospital, Peking University, Beijing, China[*1]Molecular Biology Laboratory of Andrology Center, Peking University First Hospital, Peking University, Beijing, China[*2]Male reproductive and sexual medicine, department of urology, the second hospital of tianjin medical university, Tianjin, China[*3]China-Korea Joint Research Center for Male Reproductive and Sexual Medicine, Institute of Urology, Tianjin, China[*4]Molecular Biology Laboratory of Andrology Center, Peking University First Hospital, Peking University, Beijing, China
推荐引用方式(GB/T 7714)：
Niu Yuanjie,Lin Guiting,Pan Jiancheng,et al.Deciphering the myth of icariin and synthetic derivatives in improving erectile function from a molecular biology perspective: a narrative review[J].TRANSLATIONAL ANDROLOGY and UROLOGY.2022,doi:10.21037/tau-22-232.
APA：
Niu, Yuanjie,Lin, Guiting,Pan, Jiancheng,Liu, Jihong,Xu, Yongde...&Xin, Zhongcheng.(2022).Deciphering the myth of icariin and synthetic derivatives in improving erectile function from a molecular biology perspective: a narrative review.TRANSLATIONAL ANDROLOGY and UROLOGY,,
MLA：
Niu, Yuanjie,et al."Deciphering the myth of icariin and synthetic derivatives in improving erectile function from a molecular biology perspective: a narrative review".TRANSLATIONAL ANDROLOGY and UROLOGY .(2022)
