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采用微量稀释法体外实验评价功能化羧酸酯的有机锡化合物的抗真菌活性。

Antifungal activity of organotin compounds with functionalized carboxylates evaluated by the microdilution bioassay in vitro.

机构信息

Institute of Genetics and Microbiology, University of Wroclaw, Wroclaw, Poland.

出版信息

Med Mycol. 2010 Mar;48(2):373-83. doi: 10.1080/13693780903188680.

Abstract

We investigated the susceptibility of 96 well-characterized strains of yeast-like and filamentous fungi towards new organotin compounds: (1) [Sn(C4H9)3(OOCC6H4SO3H-2)], (2) Sn(C4H9)3{OOC(CH2)3P(C6H5)3}]Br, and (3) [Sn(C6H5)3[OOC(CH2)3N(CH3)3}]Cl. In the case of yeast-like fungi, the in vitro susceptibility tests were carried out according to the Clinical Laboratory Standards Institute (CLSI, formerly NCCLS) reference method M27-A2, while for filamentous fungi the investigations were conducted according to the M38-A and M38-P methods. The organotin complexes 1, 2 and 3 are active antifungal agents. Minimal inhibitory concentrations (MIC) were in the range of 0.25-4.68 microg/ml for all tested fungal strains. Considerably larger differences were found for minimal fungicidal concentrations (MFC). In the case of yeast-like fungi, the fungicidal effect was generally observed at organotin compounds concentrations of 2.34-9.37 microg/ml. The MFC values for filamentous fungi were considerably higher and were in the range of 18.74-50 microg/ml. In conclusion, organotin compounds 1, 2 and 3 showed high fungistatic and fungicidal activities against different species of pathogenic and nonpathogenic fungi. However, they were also highly cytotoxic towards two mammalian cell lines.

摘要

我们研究了 96 种经过充分鉴定的酵母样真菌和丝状真菌对新型有机锡化合物的敏感性:(1)[Sn(C4H9)3(OOCC6H4SO3H-2)],(2)Sn(C4H9)3{OOC(CH2)3P(C6H5)3}]Br,和(3)[Sn(C6H5)3[OOC(CH2)3N(CH3)3}]Cl。对于酵母样真菌,体外药敏试验按照临床实验室标准协会(CLSI,前身为 NCCLS)参考方法 M27-A2 进行,而对于丝状真菌,则按照 M38-A 和 M38-P 方法进行。有机锡配合物 1、2 和 3 是有效的抗真菌剂。所有测试真菌菌株的最小抑菌浓度(MIC)在 0.25-4.68 μg/ml 范围内。对于最小杀菌浓度(MFC),发现了相当大的差异。对于酵母样真菌,一般在真菌化合物浓度为 2.34-9.37 μg/ml 时观察到杀菌作用。丝状真菌的 MFC 值要高得多,范围在 18.74-50 μg/ml 之间。总之,有机锡化合物 1、2 和 3 对不同种类的致病性和非致病性真菌表现出高的抑菌和杀菌活性。然而,它们对两种哺乳动物细胞系也具有高度的细胞毒性。

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