State Key Laboratory of Mycology, Institute of Microbiology, Chinese Academy of Sciences, Beijing, PR China; Savaid Medical School, University of Chinese Academy of Sciences, Beijing, PR China.
Institute of Vegetable Research, Tibet Academy of Agriculture and Animal Science, PR China.
Fitoterapia. 2018 Oct;130:79-88. doi: 10.1016/j.fitote.2018.08.009. Epub 2018 Aug 24.
Eight new triterpenoids, ganoleucoins T-Z(1-3, 5-8), and AA (9), together with eleven known triterpenes were isolated and identified from the wild fruiting bodies of the medicinal mushroom Ganoderma leucocontextum. The structures of new compounds were determined on the basis of NMR and MS spectral analysis. The inhibitory effects of 1-9 on HMG-CoA reductase were tested in vitro. Compounds 1, 7 and 8 showed significant HMG-CoA reductase inhibition with IC values of 10.2, 9.72 and 8.68 μM, respectively. The other isolated compounds presented relatively weak inhibitory activity with IC values >100 μM. Preliminary structure-activity relationship analysis showed that the HMG moiety in 7 and 8 contributed greatly to their inhibitory activity against HMG-CoA reductase. This work further demonstrates the mushroom G. leucocontextum to be valuable herbal medicine that deserves deep investigation.
从药用真菌灵芝(Ganoderma leucocontextum)的野生子实体中分离并鉴定了 8 个新的三萜类化合物，即 ganoleucoins T-Z(1-3, 5-8)和 AA(9)，以及 11 个已知的三萜类化合物。新化合物的结构是基于 NMR 和 MS 光谱分析确定的。在体外测试了 1-9 对 HMG-CoA 还原酶的抑制作用。化合物 1、7 和 8 对 HMG-CoA 还原酶表现出显著的抑制作用，IC 值分别为 10.2、9.72 和 8.68 μM。其他分离得到的化合物的抑制活性相对较弱，IC 值>100 μM。初步的构效关系分析表明，7 和 8 中的 HMG 部分对其抑制 HMG-CoA 还原酶的活性有很大贡献。这项工作进一步证明了灵芝(Ganoderma leucocontextum)是一种有价值的草药，值得深入研究。
