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水黄皮中的水黄皮素和一个新的联苯化合物对巴西副球孢子菌的抗真菌活性。

Antifungal activity of schinol and a new biphenyl compound isolated from Schinus terebinthifolius against the pathogenic fungus Paracoccidioides brasiliensis.

机构信息

Laboratório de Química de Produtos Naturais, Centro de Pesquisas René Rachou, Belo Horizonte, MG, Brazil.

出版信息

Ann Clin Microbiol Antimicrob. 2010 Oct 12;9:30. doi: 10.1186/1476-0711-9-30.

Abstract

BACKGROUND

The aim of this study was to isolate and identify the antifungal compounds from the extracts of Schinus terebinthifolius (Anacardiaceae) against clinical isolates of the pathogenic fungus Paracoccidioides brasiliensis.

METHODS

The hexane and dichlomethane fractions from leaves and stems of S. terebinthifolius were fractionated using several chromatography techniques to afford four compounds.

RESULTS

The compounds isolated from S. terebinthifolius were identified as schinol (1), a new biphenyl compound, namely, 4'-ethyl-4-methyl-2,2',6,6'-tetrahydroxy[1,1'-biphenyl]-4,4'-dicarboxylate (2), quercetin (3), and kaempferol (4). Compounds 1 and 2 were active against different strains of P. brasiliensis, showing a minimal inhibitory concentration value against the isolate Pb B339 of 15.6 μg/ml. The isolate Pb 1578 was more sensitive to compound 1 with a MIC value of 7.5 μg/ml. Schinol presented synergistic effect only when combined with itraconazole. The compounds isolated from S. terebinthifolius were not able to inhibit cell wall synthesis or assembly using the sorbitol assay.

CONCLUSION

This work reveals for the first time the occurrence of compound 2 and discloses activity of compounds 1 and 2 against several clinical isolates of P. brasiliensis. These results justify further studies to clarify the mechanisms of action of these compounds.

摘要

背景

本研究的目的是从 Schinus terebinthifolius(漆树科)提取物中分离和鉴定抗真菌化合物,以对抗致病性真菌巴西副球孢子菌的临床分离株。

方法

采用多种色谱技术对 S. terebinthifolius 的叶和茎的正己烷和二氯甲烷馏分进行分离,得到四种化合物。

结果

从 S. terebinthifolius 中分离得到的化合物被鉴定为 schinol(1),一种新的联苯化合物,即 4'-乙基-4-甲基-2,2',6,6'-四羟基[1,1'-联苯]-4,4'-二羧酸酯(2)、槲皮素(3)和山奈酚(4)。化合物 1 和 2 对不同株的巴西副球孢子菌表现出活性,对分离株 Pb B339 的最小抑菌浓度值为 15.6 μg/ml。分离株 Pb 1578 对化合物 1 更敏感,MIC 值为 7.5 μg/ml。当与伊曲康唑联合使用时,schinol 仅表现出协同作用。从 S. terebinthifolius 中分离得到的化合物在山梨醇测定中不能抑制细胞壁的合成或组装。

结论

本研究首次揭示了化合物 2 的存在,并揭示了化合物 1 和 2 对几种巴西副球孢子菌临床分离株的活性。这些结果证明了进一步研究这些化合物作用机制的合理性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e69/2964558/1a4357abf214/1476-0711-9-30-1.jpg

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