Yang Li, Kong De-Xian, Xiao Na, Ma Qing-Yun, Xie Qing-Yi, Guo Jiao-Cen, Ying Deng Chun, Ma Hai-Xia, Hua Yan, Dai Hao-Fu, Zhao You-Xing
Hainan Academy of Tropical Agricultural Resource, Haikou Key Laboratory for Research and Utilization of Tropical Natural Products, Institute of Tropical Bioscience and Biotechnology, CATAS, Haikou 571101, China.
Hainan Academy of Tropical Agricultural Resource, Haikou Key Laboratory for Research and Utilization of Tropical Natural Products, Institute of Tropical Bioscience and Biotechnology, CATAS, Haikou 571101, China; Key Laboratory for Forest Resources Conservation and Utilization in the Southwest Mountains of China, Ministry of Education, Southwest Forestry University, Kunming 650224, China.
Bioorg Chem. 2022 Oct;127:106025. doi: 10.1016/j.bioorg.2022.106025. Epub 2022 Jul 13.
Eight previously undescribed lanostane triterpenoids, ganodeweberiols A ∼ H (1-8), together with eighteen known compounds (9-26), were isolated from the fruiting bodies of Ganoderma weberianum. The structures and absolute configurations of the new compounds were determined by extensive spectroscopic analysis, as well as NMR chemical shifts and electronic circular dichroism (ECD) calculations. Compounds 2, 7, 12, and 14 showed significant α-glucosidase inhibitory activity with IC values ranging from 35.3 μM ∼ 223.4 μM compared to the positive control acarbose (IC, 304.6 μM). Kinetic study indicated that the most potent compound 12 was a mixed type inhibitor for α-glucosidase. Molecular docking simulation revealed the interactions of 12 with α-glucosidase. Additionally, Compounds 3 and 6 inhibited glucagon-induced hepatic glucose production in HepG2 cells with EC values of 42.0 and 85.9 μM, respectively. Further study revealed that compounds 3 and 6 inhibited hepatic glucose production by suppression glucagon-induced cAMP accumulation. Moreover, compounds 3 and 26 were active against HeLa cell line with IC values of 17.0 and 6.8 μM, respectively.
从韦氏灵芝子实体中分离得到8个新的羊毛甾烷型三萜类化合物，即ganodeweberiols A ∼ H（1-8），以及18个已知化合物（9-26）。通过广泛的光谱分析以及核磁共振化学位移和电子圆二色光谱（ECD）计算确定了新化合物的结构和绝对构型。与阳性对照阿卡波糖（IC，304.6 μM）相比，化合物2、7、12和14表现出显著的α-葡萄糖苷酶抑制活性，IC值范围为35.3 μM ∼ 223.4 μM。动力学研究表明，最有效的化合物12是α-葡萄糖苷酶的混合型抑制剂。分子对接模拟揭示了化合物12与α-葡萄糖苷酶的相互作用。此外，化合物3和6在HepG2细胞中抑制胰高血糖素诱导的肝葡萄糖生成，EC值分别为42.0和85.9 μM。进一步研究表明，化合物3和6通过抑制胰高血糖素诱导的cAMP积累来抑制肝葡萄糖生成。此外，化合物3和26对HeLa细胞系有活性，IC值分别为17.0和6.8 μM。
