Ooi Kheng Leong, Tengku Muhammad Tengku Sifzizul, Lam Lee Yein, Sulaiman Shaida Fariza
School of Biological Sciences, Universiti Sains Malaysia, Pulau Pinang, Malaysia.
Malaysian Institute of Pharmaceuticals and Nutraceuticals, Jalan Bukit Gambir, Pulau Pinang, Malaysia Department of Biological Sciences, Faculty of Science and Technology, Universiti Malaysia Terengganu, Terengganu, Malaysia.
Integr Cancer Ther. 2014 May;13(3):NP1-9. doi: 10.1177/1534735411433203. Epub 2012 Feb 15.
Previous cytotoxic (anticancer) evaluations ofElephantopus molliswere mainly focused on its elephantopin derivatives neglecting the combined effect of the phytochemicals in its traditionally used extracts. In this study, the cytotoxic mechanism of its extracts was investigated using methylene blue assay. The cytotoxic screening results revealed the ethyl acetate extract as the most potent extract by displaying prominent dose-dependent and time-dependent growth inhibitions in human liver carcinoma HepG2 cells with the lowest EC50value of 9.38 ± 0.43 µg/mL after 72 hours of treatment. Acute exposure of the HepG2 cells to the ethyl acetate extract produced a significant regulation of caspase-3 with the peak expression at 8 hours of treatment (P< .05). DNA fragmentation indicated by DeadEnd Apoptosis Detection System-labeled nuclei cells confirmed that the extract induced apoptotic cell death through caspase-3-dependent pathway in HepG2 cells.
先前对软叶地胆草的细胞毒性（抗癌）评估主要集中在其地胆草苦素衍生物上，而忽略了其传统使用提取物中植物化学成分的联合作用。在本研究中，使用亚甲蓝测定法研究了其提取物的细胞毒性机制。细胞毒性筛选结果显示，乙酸乙酯提取物是最有效的提取物，在人肝癌HepG2细胞中表现出显著的剂量依赖性和时间依赖性生长抑制，处理72小时后最低EC50值为9.38±0.43μg/mL。将HepG2细胞急性暴露于乙酸乙酯提取物中，可显著调节caspase-3，在处理8小时时表达达到峰值（P<0.05）。DeadEnd凋亡检测系统标记的细胞核细胞显示的DNA片段化证实，该提取物通过caspase-3依赖性途径诱导HepG2细胞凋亡性细胞死亡。
