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土壤来源的短密青霉中的杂色曲菌素。

Trichothecenes from a Soil-Derived Trichoderma brevicompactum.

机构信息

Faculty of Science and Industrial Technology , Prince of Songkla University , Surat Thani Campus, Muang Surat Thani, Surat Thani 84000 , Thailand.

Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science , Prince of Songkla University , Hat Yai, Songkhla 90112 , Thailand.

出版信息

J Nat Prod. 2019 Apr 26;82(4):687-693. doi: 10.1021/acs.jnatprod.8b00205. Epub 2019 Mar 12.

DOI:10.1021/acs.jnatprod.8b00205
PMID:30860372
Abstract

Six new (1-6), together with seven known (7-13), trichothecenes were isolated from the soil-derived Trichoderma brevicompactum PSU-RSPG27. Their structures were established using spectroscopic data. The structure of 1 was confirmed by X-ray data. Trichodermin (7) exhibited the most potent activity against Plasmodium falciparum (K1 strain) with an IC value of 0.1 μM, while other trichothecenes (1, 8, 9, and 12) were much less active, with IC values in the range of 7.1-9.6 μM. Compound 7 displayed activity against noncancerous Vero cells with an IC value of 0.4 μM. The remaining compounds showed moderate to weak activity, with IC values in the range of 6.9-15.3 μM. Compounds 7 and 12 were active against human oral carcinoma (KB) cells with IC values of 2.4 and 3.7 μM, respectively. Additionally, compounds 7 and 12 displayed antifungal activity against Candida albicans with the respective MIC values of 1 and 2 μg/mL and were active against Cryptococcus neoformans with equal MIC values of 4 μg/mL.

摘要

从土壤来源的 Trichoderma brevicompactum PSU-RSPG27 中分离得到了 6 种新的(1-6)和 7 种已知的(7-13)曲古霉素。通过光谱数据确定了它们的结构。1 的结构通过 X 射线数据得到了证实。曲古霉素(7)对恶性疟原虫(K1 株)表现出最强的活性,IC 值为 0.1 μM,而其他曲古霉素(1、8、9 和 12)则活性较弱,IC 值在 7.1-9.6 μM 范围内。化合物 7 对非癌细胞 Vero 的 IC 值为 0.4 μM。其余化合物表现出中等至较弱的活性,IC 值在 6.9-15.3 μM 范围内。化合物 7 和 12 对人口腔癌细胞(KB)的活性分别为 2.4 和 3.7 μM。此外,化合物 7 和 12 对白色念珠菌的 MIC 值分别为 1 和 2 μg/mL,对新型隐球菌的 MIC 值相同,均为 4 μg/mL。

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