Anti-inflammatory and anti-tumor-promoting effects of triterpene acids and sterols from the fungus Ganoderma lucidum
Anti-inflammatory and anti-tumor-promoting effects of triterpene acids and sterols from the fungus Ganoderma lucidum
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DOI：
10.1002/cbdv.200790027
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发表时间：
2007-01-01
影响因子：
2.9
通讯作者：
Kimura, Yumiko
中科院分区：
文献类型：
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作者：
Akihisa, Toshihiro;Nakamura, Yuji;Kimura, Yumiko
一系列羊毛甾烷型三萜酸，包括十一种葡糖酸（3，4，9，10，13-19）和六种灵芝酸（20-22，24，26，27），以及六种甾醇（28-33），均分离自真菌灵芝的子实体，检测了它们对Raji细胞中12-O-十四烷酰基佛波醇-13-乙酸酯（TPA）诱导EB病毒早期抗原（EBV-EA）的抑制作用，这是一种已知的抗肿瘤启动子的初步筛选试验。除了灵芝内酯（27）和三种甾醇（29-31）之外，所有测试的化合物都显示出对EBV-EA诱导的有效抑制作用，IC 50值为235-370摩尔比/32 pmol TPA。此外，发现9种葡糖酸（1，2，5 - 8，11，12，18）和4种灵芝酸（20，23-25）抑制TPA诱导的小鼠炎症（1 μ g/耳），ID 50值为0.07-0.39 mg/耳。此外，在以7，12-二甲基苯并[a]蒽（DMBA）为引发剂、以TPA为促进剂的体内两阶段小鼠皮肤致癌试验中，20-羟基琥珀酸N（18）对皮肤肿瘤促进具有抑制作用。
A series of lanostane-type triterpene acids, including eleven lucidenic acids (3, 4, 9, 10, 13-19) and six ganoderic acids (20-22, 24, 26,27), as well as six sterols (28-33), all isolated from the fruiting bodies of the fungus Ganoderma lucidum, were examined for their inhibitory effects on the induction of Epstein-Barr virus early antigen (EBV-EA) by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells, a known primary screening test for anti-tumor promoters. All of the compounds tested, except for ganolactone (27) and three sterols (29-31), showed potent inhibitory effects on EBV-EA induction, with IC50 values of 235-370 mol ratio/32 pmol TPA. In addition, nine lucidenic acids (1,2,5-8,11,12,18) and four ganoderic acids (20, 23-25) were found to inhibit TPA-induced inflammation (1 mu g/ear) in mice, with ID50 values of 0.07-0.39 mg per ear. Further, 20-hydroxylucidenic acid N (18) exhibited inhibitory effects on skin-tumor promotion in an in vivo two-stage mouse-skin carcinogenesis test based on 7,12-dimethylbenz[a]anthracene (DMBA) as initiator, and with TPA as promoter.