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Neuraminidase Inhibitors from the Fermentation Broth of Phellinus linteus

机译:桑黄发酵液中神经氨酸酶抑制剂

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摘要

During a search for neuraminidase inhibitors derived from medicinal fungi, we found that the fermentation broth of Phellinus linteus exhibited potent neuraminidase inhibitory activity. Through bioassay-guided fractionation, two active compounds were purified from the ethyl acetate-soluble portion of the fermentation broth of P. linteus. These structures were identified as inotilone (>1) and 4-(3,4-dihydroxyphenyl)-3-buten-2-one (>2) by spectroscopic methods. Compounds >1 and >2 inhibited H1N1 neuraminidase activity with IC50 values of 29.1 and 125.6 µM, respectively, in a dose-dependent manner. They also exhibited an antiviral effect in a viral cytopathic effect reduction assay using MDCK cells. These results suggest that compounds >1 and >2 from the culture broth of P. linteus would be good candidates for the prevention and therapeutic strategies towards viral infections.
机译:在搜寻源自药用真菌的神经氨酸酶抑制剂时,我们发现桑黄的发酵液具有强大的神经氨酸酶抑制活性。通过生物测定指导的分级分离,从亚麻假单胞菌发酵液的乙酸乙酯可溶部分中纯化了两种活性化合物。通过光谱法将这些结构鉴定为因替尼(> 1 )和4-(3,4-二羟基苯基)-3-丁烯-2-一(> 2 )。化合物> 1 和> 2 以剂量依赖性方式抑制H1N1神经氨酸酶活性,IC50值分别为29.1和125.6 µM。在使用MDCK细胞的病毒细胞病变效应降低测定中,它们还表现出抗病毒作用。这些结果表明,来自P. linteus培养液中的化合物> 1 和> 2 将是预防和治疗病毒感染策略的良好候选者。

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