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Dichloroisocoumarins with Potential Anti-Inflammatory Activity from the Mangrove Endophytic Fungus Ascomycota sp. CYSK-4

机译:具有来自红树林内生真菌Ascomycota sp。的潜在抗炎活性的二氯异香豆素。 CYSK-4

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摘要

Three new isocoumarins—dichlorodiaportintone (>1), desmethyldichlorodiaportintone (>2) and desmethyldichlorodiaportinol (>3)—as well as six known analogues (>4–9) were isolated from the culture of the mangrove endophytic fungus Ascomycota sp. CYSK-4 from Pluchea indica. Their structures were elucidated by analysis of spectroscopic data. The absolute configuration of compounds >1 and >2 were determined by the modified Mosher’s method. Compound >2 showed significant anti-inflammatory activity by inhibiting the production of NO in LPS-induced RAW 264.7 cells with IC50 value of 15.8 μM, while compounds >1, >5, and >6 exhibited weak activities with IC50 values of 41.5, 33.6, and 67.2 μM, respectively. In addition, compounds >1, >5, and >6 showed antibacterial effects against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae, and Acinetobacter calcoaceticus with the MIC values in the range of 25–50 μg·mL−1.
机译:三种新的异香豆素-二氯二苯丙酮(> 1 ),去甲基二氯二苯甲酮(> 2 )和去甲基二氯二苯甲酚(> 3 )-以及六个已知的类似物(> 4–9 )是从红树林内生真菌Ascomycota sp。的培养物中分离得到的。来自印度Pluchea的CYSK-4。通过光谱数据分析阐明了它们的结构。化合物> 1 和> 2 的绝对构型是通过改良的Mosher方法确定的。化合物> 2 通过抑制LPS诱导的RAW 264.7细胞中NO的产生而具有显着的抗炎活性,IC50值为15.8μM,而化合物> 1 ,> 5 和> 6 表现出较弱的活性,IC50值分别为41.5、33.6和67.2μM。此外,化合物> 1 ,> 5 和> 6 显示出对金黄色葡萄球菌,枯草芽孢杆菌,大肠杆菌,肺炎克雷伯菌和钙乙酸不动杆菌的抗菌作用。 MIC值在25–50μg·mL -1 范围内。

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