Cardiospermum halicacabum ethanol extract inhibits LPS induced COX-2, TNF-alpha and iNOS expression, which is mediated by NF-kappaB regulation, in RAW264.7 cells.

AIM OF THIS STUDY: Cardiospermum halicacabum L. is well known for its anti-inflammatory, analgesic and antipyretic activities. It has been used in Ayurveda and folk medicine for the treatment of rheumatism, fever and earache. But its mechanism of anti-inflammatory and analgesic action is still unclear, hence in this context, the objective of our study is to reveal the mechanism of anti-inflammatory and analgesic activity of Cardiospermum halicacabum L. which would form an additional proof to the traditional knowledge of Cardiospermum halicacabum L. MATERIALS AND METHODS: In this study the ethanolic extract of the whole plant was used to evaluate the anti-inflammatory action in mouse macrophage cell line RAW264.7 cells. The expression levels of cyclooxygenase (COX)-1, COX-2, tumor necrosis factor-alpha (TNF-alpha), inducible nitric oxide synthase (iNOS) and COX-2 protein expression by semi-quantitative reverse transcriptase-polymerase chain reaction (RT-PCR) and western blot and nuclear factor kappa-B (NF-kappaB) binding activity by electrophoretic mobility shift assay (EMSA). RESULTS: We found that the ethanol extract dose dependently inhibit mRNA expression of COX-2, TNF-alpha, iNOS and COX-2 protein expression. But the extract did not affect the expression of COX-1 mRNA expression. Furthermore, Cardiospermum halicacabum L. ethanol extract inhibited the TNF-alpha induced DNA binding activity of NF-kappaB, which was associated with decreased p65 protein level in the nucleus in Jurkat cells. CONCLUSION: These results enabled to understand the mechanisms behind the anti-inflammatory and analgesic activity of Cardiospermum halicacabum L.