Niu Yuanjie, Lin Guiting, Pan Jiancheng, Liu Jihong, Xu Yongde, Cai Qiliang, Wang Tao, Luan Yang, Chen Yegang, Feng Yuhong, Yang Xiaoqing, Tian Wenjie, Bae Wong Jin, Guan Ruili, Xin Zhongcheng
Department of Urology, Tianjin Institute of Urology, The Second Hospital of Tianjin Medical University, Tianjin, China.
China-Korea Joint Research Center for Male Reproductive and Sexual Medicine, Institute of Urology, Tianjin, China.
Transl Androl Urol. 2022 Jul;11(7):1007-1022. doi: 10.21037/tau-22-232.
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.
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.
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, TGFβ1/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.
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.
尽管淫羊藿在中国古代医学中已被广泛用于增强性功能，但其药理机制尚不清楚。现代研究表明，淫羊藿富含淫羊藿苷（ICA，一种黄酮类化合物），口服后，肠道细菌中的水解酶可将91.2%的淫羊藿苷转化为淫羊藿次苷II（ICA II）。YS-10是淫羊藿次苷II的合成衍生物。本综述的目的是总结关于ICA及其一些衍生物用于勃起功能障碍治疗的药代动力学、治疗特性和分子生物学机制的当代证据。
在PubMed数据库中使用关键词和短语进行详细检索，如“淫羊藿苷”和“勃起功能障碍”、“淫羊藿次苷II”和“勃起功能障碍”。发表时间限制在过去20年。文章必须发表在同行评审期刊上。
ICA及其一些衍生物对5型磷酸二酯酶（PDE5）有特异性抑制作用，并能促进睾酮合成。此外，通过调节PI3K/AKT、TGFβ1/Smad2、p38/MAPK、Wnt等各种信号通路以及多种细胞因子的分泌等可靠证据，ICA和ICA衍生物可激活内源性干细胞（ESCs），导致内皮细胞和平滑肌细胞增殖、神经再生和纤维化抑制，修复阴茎组织的病理变化并改善勃起功能。
ICA及其一些衍生物可能是恢复自发性勃起的潜在治疗方法。此外，ICA及其衍生物作为其他疾病的再生医学方法可能也有价值，但建议进行更多高质量、大样本的临床和基础研究。
