裁决——一种具有其他生物活性的男性避孕药。

Yan-Ho Cheng, Weiliang Xia, Elissa W P Wong, Qian R Xie, Jiaxiang Shao, Tengyuan Liu, Yizhou Quan, Tingting Zhang, Xiao Yang, Keyi Geng, Bruno Silvestrini, Chuen-Yan Cheng
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引用次数: 9

摘要

背景:自20世纪90年代末首次合成以来,rulin作为男性避孕药已被探索了15年。已有50多篇论文发表在PubMed上,其中描述了其诱导生殖细胞从精系上皮脱落的机制,例如其对顶端ES(外质特化,睾丸特异性的富含肌动蛋白的锚定连接)的肌动蛋白微丝的影响。目的:近年来的研究表明,除能诱导雄性啮齿动物精系上皮生殖细胞脱落引起可逆性不育外,还具有抗肿瘤、抗脑炎症、抗庆大霉素所致啮齿动物耳毒性等生物活性。这些发现的结果可能激发研究人员的兴趣,探索这种和其他以吲唑为基础的化合物的其他医学用途,可能是由哺乳动物细胞线粒体中的信号通路介导的。在这篇综述中,我们仔细评估了这些最近的发现。方法:检索www.pubmed.org网站上已发表和收录的有关裁决素及其相关化合物的论文和专利。对研究结果进行了回顾和批判性评价,并在此进行了总结。结果:裁决素是一种具有抗精子发生活性的新化合物。此外,根据不同体外和体内模型的研究,它具有抗癌、抗炎症、抗神经变性和抗耳毒性活性。结论:应扩大对裁决素的研究,进一步了解其生物学活性,使裁决素除作为男性避孕药外,还可作为治疗其他疾病的有效药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Adjudin--A Male Contraceptive with Other Biological Activities.

Adjudin--A Male Contraceptive with Other Biological Activities.

Adjudin--A Male Contraceptive with Other Biological Activities.

Background: Adjudin has been explored as a male contraceptive for the last 15 years since its initial synthesis in the late 1990s. More than 50 papers have been published and listed in PubMed in which its mechanism that induces exfoliation of germ cells from the seminiferous epithelium, such as its effects on actin microfilaments at the apical ES (ectoplasmic specialization, a testis-specific actin-rich anchoring junction) has been delineated.

Objective: Recent studies have demonstrated that, besides its activity to induce germ cell exfoliation from the seminiferous epithelium to cause reversible infertility in male rodents, adjudin possesses other biological activities, which include anti-cancer, anti-inflammation in the brain, and anti-ototoxicity induced by gentamicin in rodents. Results of these findings likely spark the interest of investigators to explore other medical use of this and other indazole-based compounds, possibly mediated by the signaling pathway(s) in the mitochondria of mammalian cells following treatment with adjudin. In this review, we carefully evaluate these recent findings.

Methods: Papers published and listed at www.pubmed.org and patents pertinent to adjudin and its related compounds were searched. Findings were reviewed and critically evaluated, and summarized herein.

Results: Adjudin is a novel compound that possesses anti-spermatogenetic activity. Furthermore, it possesses anti-cancer, anti-inflammation, anti-neurodegeneration, and anti-ototoxicity activities based on studies using different in vitro and in vivo models.

Conclusion: Studies on adjudin should be expanded to better understand its biological activities so that it can become a useful drug for treatment of other ailments besides serving as a male contraceptive.

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