[关键词]
[摘要]
目的 研究留萼木Blachia pentzii叶中的化学成分及其体外抗肿瘤活性。方法 利用硅胶柱色谱、MCI柱色谱、ODS柱色谱和半制备HPLC等柱色谱分离技术进行分离纯化,并综合应用HR-ESI-MS、NMR和ECD等多种波谱方法鉴定化合物结构,采用CCK-8或MTT法筛选了部位浸膏和新化合物对几种肿瘤细胞的增殖抑制作用。结果 从留萼木叶的95%乙醇提取物中分离得到2个萜类化合物,分别鉴定为(R)-5-methyl-5-((S)-4-methyl-2-oxocyclohex-3-en-1-yl)dihydrofuran-2(3H)-one(1)和3β-乙酰基多花独尾草-8-烯-17-酸(2);醋酸乙酯萃取部位对人肺癌A549细胞、人宫颈癌HeLa细胞、人肝癌HepG2细胞3种肿瘤细胞系的半数抑制浓度(half inhibitory concentration,IC50)分别为(21.37±1.98)、(22.91±0.33)、(22.14±4.95)μg/mL。化合物2在80 μmol/L对2种胃癌细胞HGC-27、AGS抑制率分别达到81.9%和89.2%。结论 化合物1为降倍半萜类,2为三萜类,1和2均为新化合物,分别命名为留萼木素A和3β-乙酰基多花独尾草-8-烯-17-酸;化合物2对胃癌细胞具有一定的增殖抑制作用。
[Key word]
[Abstract]
Objective To study the chemical constituents from the leaves of Blachia pentzii and antitumor activity in vitro. Methods The chemical constituents were separated and purified by silica gel, MCI, ODS column chromatography, and the semi-preparative HPLC. Their structures were elucidated by analysis of HR-ESI-MS, NMR and ECD spectroscopic data. The anti-inflammatory activity of new compounds were screened by MTT method. Results Two terpenoids were isolated from the 95% ethanol extract of the leaves of B. pentzii, and identified as blapenin A (1) and 3β-acetylmultiflora-8-en-17-oic acid (2), respectively. The IC50 of ethyl acetate extracts against A549, HeLa and HepG2 cell lines was (21.37 ±1.98), (22.91 ±0.33) and (22.14 ±4.95) μg/mL, respectively. Conclusion Compound 1 is a norsesquiterpenoid, 2 is a triterpenoid, 1 and 2 are both new compounds, and compound 2 exhibited a certain inhibitory effect on the proliferation of gastric cancer cells.
[中图分类号]
R284.1
[基金项目]
国家自然科学基金资助项目(32070384)