Graduate School of Bioagricultural Sciences , Nagoya University , Chikusa-ku, Nagoya 464-8601 , Japan.
Department of Chemistry , University of Yangon , Yangon 11041 , Myanmar.
J Nat Prod. 2019 Jul 26;82(7):1971-1978. doi: 10.1021/acs.jnatprod.9b00366. Epub 2019 Jun 20.
Seven new cyclic depsipeptides, clavariopsins C-I (-), together with two known congeners, clavariopsins A and B ( and ), were isolated from the aquatic hyphomycete . Their planar structures, which consist of nine amino acids and one α-hydroxy acid, were elucidated by NMR spectroscopy and HRESIMS. The absolute configurations were established by the advanced Marfey's method and chiral-phase HPLC analysis. Their antifungal and cytotoxic activities were evaluated against six plant pathogenic fungi (, , , , , and ) and a cancer cell line (HeLa-S3), respectively. The majority of the compounds exhibited potent antifungal activity against the fungi tested (minimum inhibition dose = 0.01-10 μg/disk) and induced hyphal swelling in (minimum effective dose = 0.3-3 μg/disk), whereas the compounds exhibited no cytotoxicity toward the cancer cell line. The results suggest that the clavariopsins could be a promising class of antifungal agents.
从水生丝孢菌中分离得到了 7 种新的环二肽，克拉瓦里菌素 C-I(-)，以及两种已知的同系物，克拉瓦里菌素 A 和 B（和）。通过 NMR 光谱和 HRESIMS 阐明了它们由九个氨基酸和一个α-羟基酸组成的平面结构。通过先进的 Marfey 法和手性相 HPLC 分析确定了它们的绝对构型。分别评估了它们对六种植物病原真菌（、、、、和）和一个癌细胞系（HeLa-S3）的抗真菌和细胞毒性活性。大多数化合物对测试的真菌表现出很强的抗真菌活性（最小抑制剂量=0.01-10 μg/disk），并在（最小有效剂量=0.3-3 μg/disk）中诱导菌丝肿胀，而化合物对癌细胞系没有细胞毒性。结果表明，克拉瓦里菌素可能是一类有前途的抗真菌药物。
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