Heptaketides from an Endolichenic Fungus Biatriospora sp and Their Antifungal Activity
Heptaketides from an Endolichenic Fungus Biatriospora sp and Their Antifungal Activity
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内生真菌 Biatriospora sp 的七肽及其抗真菌活性
DOI：
10.1021/acs.jnatprod.5b00998
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发表时间：
2016-09-01
影响因子：
5.1
通讯作者：
Lou, Hong-Xiang
中科院分区：
文献类型：
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作者：
Zhou, Yan-Hui;Zhang, Ming;Lou, Hong-Xiang
从地衣内生真菌Biatriospora sp.（8331 C）中分离得到12个新的七肽类化合物，biatriospora A-L（1-12），biatriosporin M（13）（一种多枝菌素衍生物）和19个已知化合物（14-32）。通过MS和NMR数据分析确定了这些化合物的结构。化合物1，2，7和9的绝对构型由单晶X-射线衍射分析确定，化合物10的绝对构型由Mosher方法推测。四种化合物在抗真菌试验中具有活性。最有效的化合物化合物4也使临床衍生的唑类耐药白色念珠菌菌株对氟康唑（FLC）敏感。一个机制的调查显示，4抑制外排泵的功能，并减少外排泵相关基因CDR 1和CDR 2的转录表达。
Twelve new heptaketides, biatriospOrifis A-L (1-12), biatriosporin M (13) (a ramulosin derivative), and 19 known compounds (14-32) were isolated from the endolichenic fungus Biatriospora sp. (8331C). The structures of these compounds were determined by analyzing MS and NMR data. The absolute configurations of compounds 1, 2, 7, and 9 were determined by single-crystal X-ray diffraction analysis, whereas compound 10 was deduced with Mosher's method. Four of the compounds were active in an antifungal assay. The most potent compound, compound 4, also sensitized clinically derived azole-resistant Candida albicans strains to fluconazole (FLC). A mechanistic investigation revealed that 4 inhibited the function of efflux pumps and reduced the transcriptional expression of the efflux-pump-related genes CDR1 and CDR2.