属于最重要和广泛研究的真菌属青霉属(Penicillium)已被广泛认知为次生代谢物的丰富来源。本研究旨在分析和调查来自属于 P. levitum 的一株海洋来源真菌代谢物的生物活性，包括体外抗癌、抗炎和抗糖尿病的特性。使用乙酸乙酯提取了 P. levitum N33.2 株的培养基中的化合物。随后，对提取物进行化学分析，成功分离得到了三种麦角甾醇类类固醇成分，分别为梭曲菌素(1)、麦角固醇过氧化物(2)和(3β,5α,22E)-麦角甾-6,8(14),22-三烯-3,5-二醇(3)。其中，(3)对人类肝癌细胞系Hep-G2，肺癌细胞系A549和乳腺癌细胞系MCF-7的半数抑制浓度(IC50)分别为2.89、18.51和16.47 µg/mL，是最具细胞毒性的成分，而化合物(1)对所测试的癌细胞没有显著效果。通过在LPS诱导的小鼠RAW264.7巨噬细胞中基于NO产生评估纯化化合物的抗炎特性。结果显示，经过测试的化合物对巨噬细胞的NO生成产生了不同的抑制效果，其中化合物(2)在25 µg/mL的浓度下表现出最显著的抑制率为81.37 ± 1.35%。有趣的是，化合物(2)和(3)在体外实验中表现出对胰脂肪酶和α-葡萄糖苷酶的抑制活性。本研究为从 P. levitum 真菌中分离出的类固醇的化学特性和生物活性提供了新数据。© 2023 作者。由韩国真菌学会的 Informa UK Limited 代表 Taylor & Francis 集团出版。

Genus Penicillium comprising the most important and extensively studied fungi has been well-known as a rich source of secondary metabolites. Our study aimed to analyze and investigate biological activities, including in vitro anti-cancer, anti-inflammatory and anti-diabetic properties, of metabolites from a marine-derived fungus belonging to P. levitum. The chemical compounds in the culture broth of P. levitum strain N33.2 were extracted with ethyl acetate. Followingly, chemical analysis of the extract leaded to the isolation of three ergostane-type steroid components, namely cerevisterol (1), ergosterol peroxide (2), and (3β,5α,22E)-ergosta-6,8(14),22-triene-3,5-diol (3). Among these, (3) was the most potent cytotoxic against human cancer cell lines Hep-G2, A549 and MCF-7 with IC50 values of 2.89, 18.51, and 16.47 µg/mL, respectively, while the compound (1) showed no significant effect against tested cancer cells. Anti-inflammatory properties of purified compounds were evaluated based on NO-production in LPS-induced murine RAW264.7 macrophages. As a result, tested compounds performed diverse inhibitory effects on NO production by the macrophages, with the most significant inhibition rate of 81.37 ± 1.35% at 25 µg/mL by the compound (2). Interestingly, compounds (2) and (3) exhibited inhibitory activities against pancreatic lipase and α-glucosidase enzymes in vitro assays. Our study brought out new data concerning the chemical properties and biological activities of isolated steroids from a P. levitum fungus.© 2023 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group on behalf of the Korean Society of Mycology.