甘草伞菌木质部提取物中具有抗增殖和PTP1B/α-葡萄糖苷酶抑制活性的蓝纯脂类三萜化合物。
Lanostane triterpenoids with anti-proliferative and PTP1B/α-glucosidase inhibitory activities from the fruiting bodies of Ganoderma calidophilum.
发表日期:2023 Sep 15
作者:
Li Yang, Ting-Ting Zhang, Qing-Yun Ma, Qing-Yi Xie, Jiao-Cen Guo, Jia-Ju Lu, Zhi-Fang Yu, Hao-Fu Dai, You-Xing Zhao
来源:
PHYTOCHEMISTRY
摘要:
从温带灵芝(Ganoderma calidophilum)的子实体中分离出12种前未报道的和4种已知的蓝灵萜类三萜化合物。通过广泛的光谱分析、ECD和NMR计算,阐明了前未报道的化合物ganodecalones H-S (1-12) 的结构。化合物4对人白血病细胞系K562、胃癌细胞系SGC-7901和宫颈癌细胞系HeLa表现出显著的抑制活性,IC50值分别为13.10±0.19、17.26±4.75和4.36±0.58μM。化合物16对蛋白酪氨酸磷酸酶1B(PTP1B)和α-葡萄糖苷酶表现出抑制活性,IC50值分别为30.2±0.13μM和120.6±0.14μM。通过分子对接模拟揭示了16与PTP1B和α-葡萄糖苷酶的结合位点和相互作用。版权所有 © 2023 Elsevier Ltd.
Twelve previously undescribed and four known lanostane triterpenoids were isolated from the fruiting bodies of Ganoderma calidophilum. The structures of undescribed compounds, ganodecalones H-S (1-12), were elucidated by extensive spectroscopic analysis as well as ECD and NMR calculations. Compound 4 showed significant inhibitory activity against human leukaemia cell line K562, gastric cancer cell line SGC-7901, and cervical cancer cell line HeLa with IC50 values of 13.10 ± 0.19, 17.26 ± 4.75, and 4.36 ± 0.58 μM, respectively. Compound 16 exhibited inhibitory potency against protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase with IC50 values of 30.2 ± 0.13 μM and 120.6 ± 0.14 μM, respectively. The binding sites and interactions of 16 with PTP1B and α-glucosidase were revealed using molecular docking simulations.Copyright © 2023. Published by Elsevier Ltd.