Kim Ji-Yul, Woo E-Eum, Ha Lee Su, Ki Dae-Won, Lee In-Kyoung, Yun Bong-Sik
Division of Biotechnology and Advanced Institute of Environment and Bioscience, College of Environmental and Bioresource Sciences, Chonbuk National University, Iksan-si, Korea.
Mycobiology. 2019 Jun 5;47(2):256-260. doi: 10.1080/12298093.2019.1616377. eCollection 2019.
Neuraminidase (NA) cleaves the glycosidic bond linkages of sialic acids to release the mature virions from infected cells and has been an attractive therapeutic target for anti-influenza agents. In our ongoing investigation of NA inhibitors in mushroom extracts, we found that the extract the fruiting body of potently inhibited neuraminidase. The fruiting bodies of . were extracted and partitioned successively with hexane, ethyl acetate, and butanol. The ethyl acetate soluble-layer was subjected to silica gel and Sephadex LH-20 column chromatographies, and MPLC to obtain five compounds (-). Their structures were determined by spectroscopic methods. NA inhibitory activity of these compounds was evaluated using NAs from recombinant rvH1N1, H3N2, and H5N1 influenza A viruses. One compound () was elucidated as a new azaphilone derivative, and four compounds (-) were identified as entonaemin A, comazaphilone D, rubiginosin A, and entonaemin B, respectively. Compounds and showed considerable inhibitory activity against three types of neuraminidases with the IC values of 30.9, 41.8, and 35.7 µM for and 46.5, 50.4, and 29.9 µM for , respectively. This study reveals that the fruiting bodies of . possess azaphilone derivatives with the NA inhibitory activity. This is the first report on the isolation of neuraminidase inhibitors from the fruiting bodies of . .
神经氨酸酶（NA）可裂解唾液酸的糖苷键连接，从而使成熟病毒粒子从受感染细胞中释放出来，一直是抗流感药物颇具吸引力的治疗靶点。在我们对蘑菇提取物中NA抑制剂的持续研究中，我们发现[具体蘑菇名称]子实体的提取物能有效抑制神经氨酸酶。对[具体蘑菇名称]的子实体进行提取，并依次用己烷、乙酸乙酯和丁醇进行分配。将乙酸乙酯可溶层进行硅胶柱色谱、葡聚糖凝胶LH - 20柱色谱和中压液相色谱，得到5种化合物（-）。通过光谱方法确定了它们的结构。使用重组rvH1N1、H3N2和H5N1甲型流感病毒的NA评估了这些化合物的NA抑制活性。一种化合物（）被鉴定为一种新的氮杂蒽酮衍生物，另外四种化合物（-）分别被鉴定为内托纳明A、科马扎菲隆D、红菌素A和内托纳明B。化合物[具体化合物编号1]和[具体化合物编号2]对三种类型的神经氨酸酶均表现出显著的抑制活性，[具体化合物编号1]的IC值分别为30.9、41.8和35.7 μM，[具体化合物编号2]的IC值分别为46.5、50.4和29.9 μM。本研究表明，[具体蘑菇名称]的子实体含有具有NA抑制活性的氮杂蒽酮衍生物。这是首次关于从[具体蘑菇名称]子实体中分离神经氨酸酶抑制剂的报道。
