201. Antidiabetic lanostane triterpenoids from the fruiting bodies of Ganoderma weberianum.
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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, and Zhao, You-Xing
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FRUITING bodies (Fungi) , *ALPHA-glucosidases , *TRITERPENOIDS , *GANODERMA , *MOLECULAR docking , *HYPOGLYCEMIC agents - Abstract
[Display omitted] • Eight new lanostane triterpenoids and eighteen known ones were isolated from Ganoderma weberianum. • Two compounds inhibited glucagon-induced hepatic glucose production in HepG2 cells. • Four compounds showed significant inhibitory activities against α-glucosidase. 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 50 values ranging from 35.3 μM ∼ 223.4 μM compared to the positive control acarbose (IC 50 , 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 50 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 50 values of 17.0 and 6.8 μM, respectively. [ABSTRACT FROM AUTHOR]
- Published
- 2022
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