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A New Cyclic Hexapeptide and a New Isocoumarin Derivative from the Marine Sponge-Associated Fungus Aspergillus similanensis KUFA 0013

机译:海洋海绵伴生真菌曲霉曲霉KUFA 0013的一种新的六环肽和一种新的异香豆素衍生物

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摘要

A new isocoumarin derivative, similanpyrone C (>1), a new cyclohexapeptide, similanamide (>2), and a new pyripyropene derivative, named pyripyropene T (>3) were isolated from the ethyl acetate extract of the culture of the marine sponge-associated fungus Aspergillus similanensis KUFA 0013. The structures of the compounds were established based on 1D and 2D NMR spectral analysis, and in the case of compound >2 the stereochemistry of its amino acid constituents was determined by chiral HPLC analysis of the hydrolysate by co-injection with the d and l amino acids standards. Compounds >2 and >3 were evaluated for their in vitro growth inhibitory activity against MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and A373 (melanoma) cell lines, as well as antibacterial activity against reference strains and the environmental multidrug-resistant isolates (MRS and VRE). Only compound >2 exhibited weak activity against the three cancer cell lines, and neither of them showed antibacterial activity.
机译:一个新的异香豆素衍生物,similanpyrone C(> 1 ),一个新的环六肽,similanamide(> 2 ),和一个新的吡啶并戊二烯衍生物,命名为pyripyropene T(> 3 2 通过与d和l氨基酸标准品共进样,通过水解物的手性HPLC分析确定其氨基酸组成的立体化学。评价化合物> 2 和> 3 对MCF-7(乳腺腺癌),NCI-H460(非小细胞肺癌)和A373(黑色素瘤)细胞系,以及对参考菌株和环境多重耐药菌株(MRS和VRE)的抗菌活性。只有化合物> 2 显示出对这三种癌细胞的弱活性,并且它们都不显示出抗菌活性。

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