Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2021-05-07 , DOI: 10.1007/s00044-021-02732-7 ZiLi Feng , ZhiBin Zhu , Wang Chen , JiaYuan Xu , Yu Bai , DaiHua Hu , ZhengDong Zhao
The natural product Ginkgolide B was used as a raw material and modified by esterification on C10-OH or C1-OH to obtain 11 derivatives (1–11), which were structurally characterized with nuclear magnetic resonance spectroscopy. An MTT assay-based in vitro tumor proliferation inhibitory activity test showed that compounds 2, 3, 6, 7, 10, and 11 exhibited strong inhibitory activity against the human ovarian cancer cells SKOV3, with IC50 values of 16.05 µmol/L, 15.65 µmol/L, 32.00 µmol/L, 63.30 µmol/L, 23.20 µmol/L, and 31.10 µmol/L, respectively. Annexin V/PI double staining assay showed that compound 2 induced apoptosis in SKOV3 cells to a slightly greater extent than GB and compounds 5 and 9, with an apoptosis rate of 31.68%.
中文翻译:
银杏内酯B衍生物的合成及其对SKOV3细胞活力的影响
天然产物银杏内酯B被用作原料并通过在C10-OH或C1-OH酯化改性,以获得11个衍生物(1 - 11),其在结构上表征核磁共振谱。基于测定的体外肿瘤细胞增殖抑制活性试验的MTT结果显示化合物2,3,6,7,10,和11显示出强抑制活性对人卵巢癌细胞SKOV3,用IC 50倍16.05微摩尔/ L的值,15.65 µmol / L,32.00 µmol / L,63.30 µmol / L,23.20 µmol / L和31.10 µmol / L。Annexin V / PI双重染色试验表明该化合物2诱导SKOV3细胞凋亡的程度略高于GB和化合物5和9,凋亡率为31.68%。