Geethangili Madamanchi, Rao Yerra Koteswara, Fang Shih-Hua, Tzeng Yew-Min
Institute of Biochemical Sciences and Technology, Chaoyang University of Technology, Wufeng, Taiwan, ROC.
Phytother Res. 2008 Oct;22(10):1336-41. doi: 10.1002/ptr.2493.
Herbal medicines are now attracting attention as potential sources of anticancer agents. Andrographis paniculata is a traditionally used anticancer herb in Indian and Chinese herbal medicine. Phytochemical investigation of the ethanol extract of the aerial parts of this herb resulted in the isolation of 14 compounds including flavonoids and labdane diterpenoids. This is the first isolation of compound 6 from a natural source, and the aerial parts of A. paniculata are a rich source for the molecule andrographolide (9, 1.375%, w/w). The structures of the isolated compounds were established by means of spectral data. The cytotoxic activities of these isolates were evaluated against Jurkat, PC-3, HepG2 and Colon 205 tumor cells, and normal cells PBMCs. The bioactivity assays showed that metabolites 1-4 and 6-8 exhibited moderate cytotoxic activity against Jurkat, PC-3 and Colon 205 cell lines, where compound 6 had IC(50) values of 0.05, 0.07 and 0.05 mm, respectively. Further, among these effective compounds, 3 and 6 selectively blocked the cell cycle progression at G0/G1, while 1, 2, 4, 7 and 8 blocked the same at G2/M phase of the Jurkat cell line. This is the first cell cycle analysis for the above mentioned isolates on the Jurkat cells. Therefore, these plant-derived compounds may play a role in the prevention and/or management of cancer.
草药作为抗癌剂的潜在来源正引起关注。穿心莲是印度和中国传统医学中使用的一种抗癌草药。对该草药地上部分的乙醇提取物进行植物化学研究，分离出14种化合物，包括黄酮类化合物和半日花烷二萜类化合物。这是首次从天然来源分离出化合物6，穿心莲地上部分是穿心莲内酯（9，1.375%，w/w）这种分子的丰富来源。通过光谱数据确定了分离出的化合物的结构。评估了这些分离物对Jurkat、PC-3、HepG2和结肠205肿瘤细胞以及正常细胞PBMCs的细胞毒性活性。生物活性测定表明，代谢物1-4和6-8对Jurkat、PC-3和结肠205细胞系表现出中等细胞毒性活性，其中化合物6的IC(50)值分别为0.05、0.07和0.05mm。此外，在这些有效化合物中，3和6在G0/G1期选择性地阻断细胞周期进程，而1、2、4、7和8在Jurkat细胞系的G2/M期阻断细胞周期进程。这是上述分离物对Jurkat细胞的首次细胞周期分析。因此，这些植物来源的化合物可能在癌症的预防和/或治疗中发挥作用。
