作者：雷辉¹, 夏童², 王佳女², 熊霞², 刘利²

作者单位：1. 西南医科大学药学院，四川 泸州 646000;
2. 西南医科大学附属医院，四川 泸州 646000

关键词：拟盘多毛孢属;甾体;结构鉴定;抗肿瘤活性

摘要：

为了从海洋真菌次生代谢产物中获得抗肿瘤药物，该文对海洋真菌Pestalotiopsis sp.中的甾体化合物进行分离纯化、结构鉴定和抗肿瘤活性研究。利用硅胶柱色谱，Sephadex LH-20 柱色谱等技术，从固体大米培养基发酵产物中分离纯化得到甾体化合物，鉴定为：4,4-dimethyl-5α-ergosta-8,24(28)-dien-3β-ol，该化合物为首次从该属种分离获得，命名为：LH-1。采用MTT方法对该化合物进行体外细胞毒性测试，发现其可以选择性抑制肿瘤细胞的生长（IC₅₀：8.3 μmol/L），而对正常细胞没有明显的杀伤作用。该研究可为微生物来源的抗肿瘤先导化合物的发现提供实验基础。

Separation and purification of sterols from marine fungus Pestalotiopsis sp. and study on its anti-tumor activity
LEI Hui¹, XIA Tong², WANG Jianü², XIONG Xia², LIU Li²
1. School of Pharmacy, Southwest Medical University, Luzhou 646000, China;
2. the Affiliated Hospital of Southwest Medical University, Luzhou 646000, China
Abstract: To obtain antitumor drugs from secondary metabolites of marine fungi, the sterol constituents of marine fungus Pestalotiopsis sp. and its antimelanoma activity were studied. One compound was isolated from the extracts of solid rice medium by means of chromatographic techniques, including silica gel column and Sephadex LH-20 column chromatography. The structure was identified as 4, 4-dimethyl-5α-ergosta-8, 24 (28)-dien-3β-ol, which was isolated from the marine fungus Pestalotiopsis sp. for the first time and was named LH-1. The anti-tumor activities of LH-1 was screened by using the MTT. The result showed that compound LH-1 exhibited selective inhibitor activities against anti-tumor cells and not toxicity to normal cells, with IC₅₀ value of 8.3 μmol/L. This study provides an experimental basis for the discovery of antitumor lead compounds from microorganisms.
Keywords: Pestalotiopsis sp.;sterols;structure elucidation;anti-tumor activity
2023, 49(3):60-64  收稿日期: 2021-12-27;收到修改稿日期: 2022-02-20
基金项目: 四川省科技厅项目（2020YJ0191）；国家自然科学基金青年项目（82003716）
作者简介: 雷辉(1979-),男,河南信阳市人,讲师,硕士生导师,博士,研究方向天然产物分离、纯化及活性筛选
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