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皮肤防御素的杀精活性。

Spermicidal activity of dermaseptins.

作者信息

Zairi Amira, Belaïd Afifa, Gahbiche Amina, Hani Khaled

机构信息

Laboratory of Biochemistry (UR/08-45), Faculty of Medicine, 4002 Sousse, Tunisia.

出版信息

Contraception. 2005 Dec;72(6):447-53. doi: 10.1016/j.contraception.2005.06.055. Epub 2005 Aug 26.

Abstract

OBJECTIVE

The present study was undertaken to elucidate the spermicidal efficacy of two synthetic antimicrobial peptides, dermaseptin (DS1 and DS4).

METHODS

Twenty samples of fresh semen were obtained from patients aged between 23 and 35 years. The ability of DS to kill sperm was evaluated by the Sander-Cramer test under in vitro conditions.

RESULTS

The data showed that sperm motility was inhibited with various concentrations of DS at different intervals ranging from 2 to 240 min. The effective 100% inhibitory concentration (EC(100)) of DS4 in 2 min during the sperm immobilization assay was 100 microg/mL whereas the sperm immobilization of EC(100) of DS1 was 200 microg/mL. The presence of 0.1% chelating agent ethylenediaminetetraacetic acid (EDTA) reduced the EC(100) of DS4 to 10 microg/mL whereas less than a two-time enhancement in DS1 activity was observed upon combination with EDTA. The action of DSs on sperm motility was observed to be dose dependent. Supplementation with pentoxifylline and that with calcium are known to enhance the motility of sperm but they did not prevent the spermicidal action of DSs.

CONCLUSION

This present study indicates that DS is an effective agent to kill sperm. In view of this fact, it is suggested that DS4 has antibacterial, antiviral, antifungal and potentially spermicidal activities and could be a potent vaginal contraceptive.

摘要

目的

本研究旨在阐明两种合成抗菌肽——皮肤抗菌肽(DS1和DS4)的杀精效果。

方法

从23至35岁的患者中获取20份新鲜精液样本。在体外条件下,通过桑德 - 克拉默试验评估皮肤抗菌肽杀死精子的能力。

结果

数据显示,在2至240分钟的不同时间间隔内,不同浓度的皮肤抗菌肽均可抑制精子活力。在精子固定试验中,DS4在2分钟内达到100%抑制效果的有效浓度(EC(100))为100微克/毫升,而DS1的EC(100)为200微克/毫升。添加0.1%的螯合剂乙二胺四乙酸(EDTA)可使DS4的EC(100)降至10微克/毫升,而DS1与EDTA联合使用时活性增强不到两倍。观察到皮肤抗菌肽对精子活力的作用呈剂量依赖性。已知补充己酮可可碱和钙可增强精子活力,但它们并不能阻止皮肤抗菌肽的杀精作用。

结论

本研究表明皮肤抗菌肽是一种有效的杀精剂。鉴于此,建议DS4具有抗菌、抗病毒、抗真菌和潜在的杀精活性,可能是一种有效的阴道避孕药。

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