Growth inhibitory,apoptotic and anti-inflammatory activities displayed by a novel modified triterpenoid,cyano enone of methyl boswellates |
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Authors: | Palaniyandi Ravanan Sanjay K Singh G S R Subba Rao Paturu Kondaiah |
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Institution: | (1) Department of Molecular Reproduction, Development and Genetics, Bangalore, 560 012, India;(2) Department of Organic Chemistry, Indian Institute of Science, Bangalore, 560 012, India;(3) Present address: Centre for Biomedical Research, School of Biosciences and Technology, Vellore Institute of Technology University, Vellore, 632 014, India; |
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Abstract: | 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, pro-differentiative 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. |
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