Adjudin, a potential male contraceptive, exerts its effects locally in the seminiferous epithelium of mammalian testes.
Adjudin, a potential male contraceptive, exerts its effects locally in the seminiferous epithelium of mammalian testes.
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DOI：
10.1530/rep-10-0464
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发表时间：
2011-05
期刊：
影响因子：
--
通讯作者：
Cheng CY
中科院分区：
文献类型：
--
作者：
Mok KW;Mruk DD;Lie PP;Lui WY;Cheng CY
Adjudin是1H-吲唑-3-羧酸的衍生物，在大鼠、兔和犬中显示出强效抗精子生成活性。它通过破坏生殖细胞（最明显的是精子细胞）与支持细胞的粘附，从而诱导未成熟精子细胞从上皮释放，导致不育，在生精上皮的顶端隔室（血-睾丸屏障后面）局部发挥其作用。在adjudin被代谢后，剩余的精原干细胞和精原细胞通过精原细胞的自我更新和分化逐渐重新填充生精上皮，随后进行减数分裂和精子发生，从而生育力反弹。最近在大鼠中的研究已经明确地表明，睾丸中的初级和初始的细胞靶向的adjudin是顶端外质特化，睾丸特异性锚定连接类型限制于支持细胞和伸长精子细胞之间的界面（从步骤8到19精子细胞）。在这次审查中，我们强调了一些最近的进展和障碍，可能使用的adjudin作为男性避孕药。
Adjudin is a derivative of 1H-indazole-3-carboxylic acid that was shown to have potent anti-spermatogenic activity in rats, rabbits, and dogs. It exerts its effects most notably locally in the apical compartment of the seminiferous epithelium, behind the blood–testis barrier, by disrupting adhesion of germ cells, most notably spermatids to the Sertoli cells, thereby inducing release of immature spermatids from the epithelium that leads to infertility. After adjudin is metabolized, the remaining spermatogonial stem cells and spermatogonia repopulate the seminiferous epithelium gradually via spermatogonial self-renewal and differentiation, to be followed by meiosis and spermiogenesis, and thus fertility rebounds. Recent studies in rats have demonstrated unequivocally that the primary and initial cellular target of adjudin in the testis is the apical ectoplasmic specialization, a testis-specific anchoring junction type restricted to the interface between Sertoli cells and elongating spermatids (from step 8 to 19 spermatids). In this review, we highlight some of the recent advances and obstacles regarding the possible use of adjudin as a male contraceptive.