Department of Biochemistry, Indian Institute of Science, Bangalore, 560 012, India.
Invest New Drugs. 2011 Aug;29(4):583-92. doi: 10.1007/s10637-010-9393-7. Epub 2010 Feb 20.
Natural products discovered from medicinal plants have played an important role in the treatment of cancer. In an effort to identify novel small molecules which can affect the proliferation of lymphoma cells, we tested methyl angolensate (MA), a plant derived tetranortriterpenoid, purified from the crude extract of the root callus of Soymida febrifuga commonly known as Indian red wood tree. We have tested MA for its cytotoxic properties on Burkitt's lymphoma cell lines, using various cellular assays. We observed that MA induces cytotoxicity in Daudi cells in a dose-dependent manner using trypan blue, MTT and LDH assays. We find that the treatment with MA led to activation of DNA double-strand break repair proteins including KU70 and KU80, suggesting the activation of nonhomologous DNA end joining pathway in surviving cells. Further, we find that methyl angolensate could induce apoptosis by cell cycle analysis, annexin V-FITC staining, DNA fragmentation and PARP cleavage. Besides, MA treatment led to reactive oxygen species generation and loss of mitochondrial transmembrane potential. These results suggest the activation of mitochondrial pathway of apoptosis. Hence, we identify MA as a potential chemotherapeutic agent against Daudi cells.
从药用植物中发现的天然产物在癌症治疗中发挥了重要作用。为了寻找能影响淋巴瘤细胞增殖的新型小分子,我们测试了甲基安哥拉酸(MA),这是一种从印度红木树(俗称印度红木树)根愈伤组织粗提取物中分离出的植物衍生的四环三萜。我们已经使用各种细胞测定法测试了 MA 对伯基特淋巴瘤细胞系的细胞毒性。我们观察到 MA 在使用台盼蓝、MTT 和 LDH 测定法时,以剂量依赖的方式诱导 Daudi 细胞的细胞毒性。我们发现 MA 的处理导致包括 KU70 和 KU80 在内的 DNA 双链断裂修复蛋白的激活,这表明在存活细胞中激活了非同源 DNA 末端连接途径。此外,我们发现甲基安哥拉酸可以通过细胞周期分析、膜联蛋白 V-FITC 染色、DNA 片段化和 PARP 切割诱导细胞凋亡。此外,MA 处理会导致活性氧的产生和线粒体跨膜电位的丧失。这些结果表明凋亡的线粒体途径被激活。因此,我们将 MA 鉴定为针对 Daudi 细胞的潜在化疗药物。