来源于高温灵芝子实体的羊毛甾烷型三萜具有抗增殖和 PTP1B/α-葡萄糖苷酶抑制活性。
Lanostane triterpenoids with anti-proliferative and PTP1B/α-glucosidase inhibitory activities from the fruiting bodies of Ganoderma calidophilum.
机构信息
Key Laboratory of Research and Development of Natural Product from Li Folk Medicine of Hainan Province & National Key Laboratory for Tropical Crop Breeding, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou, 571101, China.
College of Food Science and Technology, Nanjing Agricultural University, Nanjing, 210095, China.
出版信息
Phytochemistry. 2023 Nov;215:113856. doi: 10.1016/j.phytochem.2023.113856. Epub 2023 Sep 15.
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 IC 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 IC 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.
从灵芝（Ganoderma calidophilum）的子实体中分离得到 12 个先前未描述的和 4 个已知的羊毛甾烷三萜。通过广泛的光谱分析以及 ECD 和 NMR 计算，阐明了未描述化合物 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 显示出显著的抑制活性，IC 值分别为 13.10±0.19、17.26±4.75 和 4.36±0.58 μM。化合物 16 对蛋白酪氨酸磷酸酶 1B（PTP1B）和 α-葡萄糖苷酶具有抑制活性，IC 值分别为 30.2±0.13 μM 和 120.6±0.14 μM。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。
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