从深海沉积物中分离得到的真菌 Penicillium sp. 的生物碱及其抗肿瘤活性。

Alkaloids from a deep ocean sediment-derived fungus Penicillium sp. and their antitumor activities.

机构信息

Key Laboratory of Marine Drugs, Chinese Ministry of Education School of Medicine and Pharmacy, Institute of Marine Drugs and Food, Ocean University of China, Qingdao, PR China.

出版信息

J Antibiot (Tokyo). 2010 Apr;63(4):165-70. doi: 10.1038/ja.2010.11. Epub 2010 Feb 26.

DOI:10.1038/ja.2010.11

PMID:20186171

Abstract

Four new alkaloids, including two new meleagrin analogs, meleagrin D (1) and E (2), and two new diketopiperazines, roquefortine H (3) and I (4), were isolated from a deep ocean sediment-derived fungus Penicillium sp. Meleagrin D (1) and E (2) possess unprecedented acetate-mevalonate-derived side chains on the imidazole moiety. These new meleagrins showed weak cytotoxicity against the A-549 cell line, whereas meleagrin B (5) and meleagrin (6), which were isolated previously from the same strain, induced HL-60 cell apoptosis or arrested the cell cycle through G(2)/M phase, respectively. The results indicate that the distinct substitutions on the imidazole ring significantly influence the cytotoxicity of the meleagrin alkaloids.

摘要

从深海沉积物来源的真菌青霉（Penicillium）中分离得到四个新的生物碱，包括两个新的麦角灵类似物，麦角灵 D（1）和 E（2），以及两个新的二酮哌嗪，罗奎福汀 H（3）和 I（4）。麦角灵 D（1）和 E（2）在咪唑部分具有前所未有的醋酸甲羟戊酸衍生侧链。这些新的麦角灵对 A-549 细胞系表现出较弱的细胞毒性，而先前从同一菌株中分离得到的麦角灵 B（5）和麦角灵（6）则分别通过诱导 HL-60 细胞凋亡或使细胞周期停滞在 G2/M 期来发挥作用。结果表明，咪唑环上的不同取代基显著影响麦角灵生物碱的细胞毒性。