College of Chinese Medicinal Materials, Jilin Agricultural University, Changchun, China.
Department of Pharmacy, The First Affiliated Hospital of Soochow University, Suzhou, China.
Nat Prod Res. 2022 Feb;36(4):1062-1066. doi: 10.1080/14786419.2020.1844698. Epub 2020 Nov 13.
A rich of 3,4--lupane triterpenoids (3,4-SLT), including chiisanoside (CSS), divaroside (DVS), sessiloside-A1 (SSA), chiisanogenin (CSG), sessiligenin (SSG), were isolated from the ethanol extract of the leaves of (LES). The present study was performed to explore the cytotoxic and anti-tumor effects of the isolated five ones, as well as potential molecular mechanisms. The results of a CCK-8 assay demonstrated that these 3,4-SLT can inhibit the growth of HepG2 cells, and SSG showed the most significant cytotoxicity. Hoechst 33258 fluorescence staining and Annexin V-FITC/PI staining indicated that 3,4-SLT in LES can induce HepG2 cell apoptosis effectively. The AutoDock Vina program was used to simulate molecular docking of drugs and targets to discuss possible pharmacological mechanisms. Besides, western blot and qRT-PCR results indicated that SSG can inhibit PI3K/AKT signaling pathway through controlling multi-targets. This study suggested that 3,4-SLT might become a new research hotspot for antineoplastic drugs.
从 (LES)的叶乙醇提取物中分离出丰富的 3,4-齐墩果烷三萜(3,4-SLT),包括柴胡皂苷(CSS)、柴胡皂苷 D(DVS)、柴胡皂苷 A1(SSA)、柴胡皂苷元(CSG)和柴胡皂苷元(SSG)。本研究旨在探讨分离得到的这五种化合物的细胞毒性和抗肿瘤作用及其潜在的分子机制。CCK-8 检测结果表明,这些 3,4-SLT 能抑制 HepG2 细胞的生长,其中 SSG 表现出最显著的细胞毒性。Hoechst 33258 荧光染色和 Annexin V-FITC/PI 染色表明,LES 中的 3,4-SLT 能有效诱导 HepG2 细胞凋亡。AutoDock Vina 程序用于模拟药物和靶点的分子对接,以讨论可能的药理学机制。此外,Western blot 和 qRT-PCR 结果表明,SSG 可通过控制多个靶点抑制 PI3K/AKT 信号通路。本研究表明,3,4-SLT 可能成为抗肿瘤药物的一个新的研究热点。