青霉酸 E-G，三种新型麦考酚酸衍生物，来自海洋来源真菌青霉 parvum HDN17-478。

Penicacids E-G, three new mycophenolic acid derivatives from the marine-derived fungus Penicillium parvum HDN17-478.

机构信息

Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.

Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Laboratory for Marine Drugs and Bioproducts of Qingdao Pilot National Laboratory for Marine Science and Technology, Qingdao, 266237, China.

出版信息

Chin J Nat Med. 2020 Nov;18(11):850-854. doi: 10.1016/S1875-5364(20)60027-9.

DOI:10.1016/S1875-5364(20)60027-9

PMID:33308607

Abstract

Three new mycophenolic acid derivatives, penicacids E-G (1-3), together with three known analogues, mycophenolic acid (4), 4'-hydroxy-mycophenolic acid (5) and mycophenolic methyl ester (6), were isolated from a marine-derived fungus Penicillium parvum HDN17-478 from a South China Sea marine sediment sample. The structures of compounds 1-3 were elucidated by HRMS, NMR, and Mosher's method. Among them, compounds 1 and 2 were the first examples of mycophenolic acid analogs with a double bond at C-3'/C-4' position. The cytotoxicity of 1-6 was evaluated against the HCT-116, BEL-7402, MGC-803, SH-SY5Y, HO-8910 and HL-60 cell lines, and compounds 4 and 6 showed potent cytotoxicity with IC values ranging from 1.69 to 12.98 μmol·L.

摘要

从南海海洋沉积物样品中分离到一株海洋来源真菌青霉（Penicillium parvum）HDN17-478，从中得到三个新的麦考酚酸衍生物，penicacids E-G（1-3），以及三个已知类似物，麦考酚酸（4）、4'-羟基麦考酚酸（5）和麦考酚酸甲酯（6）。通过高分辨质谱、核磁共振和 Mosher 方法确定了化合物 1-3 的结构。其中，化合物 1 和 2 是 C-3'/C-4' 位置双键的麦考酚酸类似物的首例。对 HCT-116、BEL-7402、MGC-803、SH-SY5Y、HO-8910 和 HL-60 细胞系进行了 1-6 的细胞毒性评价，化合物 4 和 6 表现出较强的细胞毒性，IC 值范围为 1.69-12.98 μmol·L。