Xing Shao-Fang, Jang Moonhee, Wang Yu-Rong, Piao Xiang-Lan
Institute of Chinese Minority Traditional Medicine, Minzu University of China, Beijing 100081, PR China; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China.
National Forensic Service, 139 Jiyang-ro, Yangcheon-gu, Seoul 158-707, Republic of Korea.
Bioorg Med Chem Lett. 2016 Apr 1;26(7):1754-9. doi: 10.1016/j.bmcl.2016.02.046. Epub 2016 Feb 17.
Gynostemma pentaphyllum has been widely used as a traditional herb for its antioxidant and immunostimulatory activities. We have previously reported several useful dammarane-type saponins with cytotoxicity against A549 human lung cancer cells from heat-processed G. pentaphyllum. In this study, a new dammarane-type saponin, 20(S)-2α,3β,12β-tetrahydroxydammar-3-O-β-d-glucopyranoside (namely gypenoside Jh1), was isolated from the ethanol extract of heat-processed G. pentaphyllum using column chromatography and semi-preparative HPLC. Gypenoside Jh1 exhibited strong cytotoxicity against A549 cells in a concentration-dependent manner, which was associated with apoptotic cell death characterized by morphological changes, Hoechst 33258 nuclear staining, Annexin V and propidium iodide binding and mitochondrial potentials assay. Quantitative analysis using flow cytometry also showed that the proportion of apoptotic cells was increased after gypenoside Jh1 treatment. These findings indicated that gypenoside Jh1 showed antiproliferative effects on A549 cells and mitochondrial-dependent pathway is involved in gypenoside Jh1-induced apoptosis.
绞股蓝因其抗氧化和免疫刺激活性而被广泛用作传统草药。我们之前报道过几种来自炮制绞股蓝的对A549人肺癌细胞具有细胞毒性的达玛烷型皂苷。在本研究中,使用柱色谱和半制备型高效液相色谱从炮制绞股蓝的乙醇提取物中分离出一种新的达玛烷型皂苷,20(S)-2α,3β,12β-四羟基达玛烷-3-O-β-D-吡喃葡萄糖苷(即绞股蓝皂苷Jh1)。绞股蓝皂苷Jh1对A549细胞表现出浓度依赖性的强细胞毒性,这与以形态变化、Hoechst 33258核染色、膜联蛋白V和碘化丙啶结合以及线粒体电位测定为特征的凋亡细胞死亡有关。使用流式细胞术进行的定量分析还表明,绞股蓝皂苷Jh1处理后凋亡细胞的比例增加。这些发现表明绞股蓝皂苷Jh1对A549细胞具有抗增殖作用,并且线粒体依赖性途径参与了绞股蓝皂苷Jh1诱导的凋亡。