Department of Molecular Reproduction, Development and Genetics, Indian Institute of Science, Bangalore 560012, India.
J Biosci. 2011 Jun;36(2):297-307. doi: 10.1007/s12038-011-9056-7.
Triterpenoids are pentacyclic secondary metabolites present in many terrestrial plants. Natural triterpenoids have been reported to exhibit anti-inflammatory and anti-carcinogenic activities. Here, we show that modifications of ring A of boswellic acid (2 cyano, 3 enone) resulted in a highly active growth inhibitory, anti-inflammatory, prodifferentiative and anti-tumour triterpenoid compound called cyano enone of methyl boswellates (CEMB). This compound showed cytotoxic activity on a number of cancer cell lines with IC₅₀ ranging from 0.2 to 0.6 μM. CEMB inhibits DNA synthesis and induces apoptosis in A549 cell line at 0.25 μM and 1 μM concentrations, respectively. CEMB induces adipogenic differentiation in 3T3-L1 cells at a concentration of 0.1 μM. Finally, administration of CEMB intra-tumourally significantly inhibited the growth of C6 glioma tumour xenograft in immuno-compromised mice. Collectively, these results suggest that CEMB is a very potent anti-tumour compound.
三萜类化合物是存在于许多陆生植物中的五环次生代谢物。天然三萜类化合物已被报道具有抗炎和抗癌活性。在这里，我们展示了对乳香酸（2 氰基，3 烯酮）的 A 环进行修饰，得到了一种高度活跃的生长抑制、抗炎、促分化和抗肿瘤三萜化合物，称为甲基乳香酸的氰基烯酮（CEMB）。该化合物对多种癌细胞系表现出细胞毒性活性，IC₅₀值范围为 0.2 至 0.6 μM。CEMB 在 0.25 μM 和 1 μM 浓度下分别抑制 A549 细胞系的 DNA 合成并诱导细胞凋亡。CEMB 在 0.1 μM 浓度下诱导 3T3-L1 细胞的脂肪生成分化。最后，CEMB 的肿瘤内给药显著抑制了免疫缺陷小鼠 C6 神经胶质瘤肿瘤异种移植物的生长。总之，这些结果表明 CEMB 是一种非常有效的抗肿瘤化合物。
