Growth inhibitory, apoptotic and anti-inflammatory activities displayed by a novel modified triterpenoid, cyano enone of methyl boswellates

Journal of biosciences

Palaniyandi Ravanan¹  G S R Subba Rao²  Sanjay K Singh²  Paturu Kondaiah1¹ 

[1] Department of Molecular Reproduction, Development and Genetics, Indian Institute of Science, Bangalore 560 012, India$$;Department of Organic Chemistry, Indian Institute of Science, Bangalore 560 012, India$$

关键词: Cancer therapeutics;    cytotoxicity;    differentiation;    natural products;   

DOI  :  

来源: Indian Academy of Sciences

【 摘 要 】

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.

【 授权许可】

Unknown