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关于硫咪唑对一些敏感及耐甲硝唑阴道毛滴虫菌株化疗活性的“体外”研究。

'In vitro' study of chemotherapeutic activity of sulphimidazole on some sensitive and metronidazole-resistant Trichomonas vaginalis strains.

作者信息

Malagoli Monica, Rossi Tiziana, Baggio Andrea, Zandomeneghi Ginevra, Zanca Andrea, Casolari Chiara, Castelli Mario

机构信息

Section of Pharmacology, Department of Biomedical Sciences, Via G. Campi 287, 41100 Modena, Italy.

出版信息

Pharmacol Res. 2002 Nov;46(5):469-72. doi: 10.1016/s1043661802002074.

Abstract

Trichomonacidal treatment based on 5-nitroimidazoles is problematic both when Metronidazole, the drug of choice, is ineffective owing to the presence of resistant strains and when bacterial aerobic infections are present. Sulphimidazole (SIZ) possesses two distinct functional groups: one sulphonamide, the other 5-nitroimidazole. Since SIZ is active against aerobic and anaerobic bacteria, we set out to discover whether, in view of the presence of the 5-nitroimidazole group, it could also be effective against Trichomonas vaginalis. Twelve strains of T. vaginalis were cultured in Modified Thioglycate Medium in anaerobic conditions; subsequently, their growth was monitored in the presence of Metronidazole (MZ), SIZ, Sulphamethoxazole (SMX), Trimethoprim (TMP) and their associations. Eight strains proved to be sensitive to Metronidazole (minimum lethal concentration=0.5 microgml(-1)) and four to be resistant (minimum lethal concentration=40-60 microgml(-1)). SIZ was active against both the sensitive and the Metronidazole-resistant strains (minimum lethal concentrations=0.5-1 and 10 microgml(-1), respectively), thus showing that the chemotherapeutic activities of the two functional groups coexisting in SIZ remain unimpaired.

摘要

基于5-硝基咪唑的滴虫病治疗存在问题,无论是首选药物甲硝唑因耐药菌株的存在而无效,还是存在需氧菌感染的情况。磺胺咪唑(SIZ)具有两个不同的官能团:一个是磺酰胺,另一个是5-硝基咪唑。由于SIZ对需氧菌和厌氧菌均有活性,我们着手探究鉴于其5-硝基咪唑基团的存在,它是否也能有效对抗阴道毛滴虫。将12株阴道毛滴虫在改良硫乙醇酸盐培养基中于厌氧条件下培养;随后,在甲硝唑(MZ)、SIZ、磺胺甲恶唑(SMX)、甲氧苄啶(TMP)及其组合存在的情况下监测其生长情况。8株菌株被证明对甲硝唑敏感(最低致死浓度=0.5μg/ml(-1)),4株耐药(最低致死浓度=40 - 60μg/ml(-1))。SIZ对敏感菌株和耐甲硝唑菌株均有活性(最低致死浓度分别为0.5 - 1μg/ml(-1)和10μg/ml(-1)),这表明SIZ中两个共存官能团的化疗活性未受影响。

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