Kumar V S Kiran, Sharma Vishnu Lal, Tiwari Pratibha, Singh Divya, Maikhuri Jagdamba Prasad, Gupta Gopal, Singh Man Mohan
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow-226001, India.
Bioorg Med Chem Lett. 2006 May 1;16(9):2509-12. doi: 10.1016/j.bmcl.2006.01.078. Epub 2006 Feb 7.
The study investigated spermicidal and antitrichomonas activities of selective serotonin reuptake inhibitor (SSRI) antidepressants with a view to generate new lead for development of dual-function spermicidal microbicides, which is an urgent global need. Fluoxetine, Sertraline, and Fluvoxamine exhibited both spermicidal and anti-STI (antitrichomonas) activities in vitro, whereas Paroxetine and Citalopram showed only the spermicidal activity. Fluoxetine exhibited better activity profile than the other antidepressant drugs with its spermicidal and antitrichomonas activities being comparable to that of the OTC contraceptive Nonoxynol-9. The non-detergent nature of Fluoxetine and a much lower spermicidal ED50 value (than N-9) may add considerably to its merit as a candidate for microbicidal contraceptive. Thus, the antidepressants exhibiting both spermicidal and antitrichomonas activities might provide useful lead for the development of novel, dual-function spermicidal contraceptives.
该研究调查了选择性5-羟色胺再摄取抑制剂（SSRI）类抗抑郁药的杀精和抗滴虫活性，以期为开发双功能杀精杀菌剂找到新的先导物，这是全球迫切的需求。氟西汀、舍曲林和氟伏沙明在体外均表现出杀精和抗性传播感染（抗滴虫）活性，而帕罗西汀和西酞普兰仅表现出杀精活性。氟西汀比其他抗抑郁药具有更好的活性，其杀精和抗滴虫活性与非处方避孕药壬苯醇醚-9相当。氟西汀的非去污剂性质以及低得多的杀精半数有效剂量值（比壬苯醇醚-9低）可能大大增加其作为杀微生物避孕药候选物的优势。因此，兼具杀精和抗滴虫活性的抗抑郁药可能为新型双功能杀精避孕药的开发提供有用的先导物。
