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茯苓中的三萜酸及其抗肿瘤促进作用。

Triterpene acids from Poria cocos and their anti-tumor-promoting effects.

作者信息

Akihisa Toshihiro, Nakamura Yuji, Tokuda Harukuni, Uchiyama Emiko, Suzuki Takashi, Kimura Yumiko, Uchikura Kazuo, Nishino Hoyoku

机构信息

College of Science and Technology, Nihon University, 1-8 Kanda Surugadai, Chiyoda-ku, Tokyo 101-8308, Japan.

出版信息

J Nat Prod. 2007 Jun;70(6):948-53. doi: 10.1021/np0780001. Epub 2007 May 9.

DOI:10.1021/np0780001
PMID:17488130
Abstract

The structures of six new lanostane-type triterpene acids isolated from the epidermis of the sclerotia of Poria cocos were established to be 15alpha-hydroxydehydrotumulosic acid (5), 16alpha,25-dihydroxydehydroeburicoic acid (9), 5alpha,8alpha-peroxydehydrotumulosic acid (10), 25-hydroxyporicoic acid H (11), 16-deoxyporicoic acid B (12), and poricoic acid CM (16) on the basis of spectroscopic methods. On evaluation of these six and 11 other known triterpene acids isolated from the sclerotium, 1-4, 6-8, 13-15, and 17, against the Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells, all of the compounds except for 1, 3, 4, and 8 exhibited inhibitory effects with IC50 values of 195-340 mol ratio/32 pmol TPA. Compound 12 and poricoic acid C (13) exhibited inhibitory effects on skin tumor promotion in an in vivo two-stage carcinogenesis test using 7,12-dimethylbenz[a]anthracene (DMBA) as an initiator and TPA as a promoter.

摘要

从茯苓菌核表皮分离得到的6种新羊毛甾烷型三萜酸的结构经光谱方法确定为15α-羟基脱氢块苓酸(5)、16α,25-二羟基脱氢齿孔酸(9)、5α,8α-过氧脱氢块苓酸(10)、25-羟基茯苓酸H(11)、16-脱氧茯苓酸B(12)和茯苓酸CM(16)。在对从菌核中分离得到的这6种以及其他11种已知三萜酸(1 - 4、6 - 8、13 - 15和17)针对由12 - O - 十四烷酰佛波醇 - 13 - 乙酸酯(TPA)诱导的Raji细胞中爱泼斯坦 - 巴尔病毒早期抗原(EBV - EA)激活进行评估时,除1、3、4和8外,所有化合物均表现出抑制作用,IC50值为195 - 340摩尔比/32 pmol TPA。化合物12和茯苓酸C(13)在以7,12 - 二甲基苯并[a]蒽(DMBA)作为引发剂、TPA作为促进剂的体内两阶段致癌试验中对皮肤肿瘤促进表现出抑制作用。

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