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Eur J Med Chem. 2015 Jun 15;98:170-8. doi: 10.1016/j.ejmech.2015.05.001. Epub 2015 May 5.

Synthesis and biological evaluation of boswellic acid-NSAID hybrid molecules as anti-inflammatory and anti-arthritic agents.

Author information

1
Chemical Sciences Division, Vittal Mallya Scientific Research Foundation, BTM II Stage, Bangalore 560076, India.
2
Department of Biological Sciences, Vittal Mallya Scientific Research Foundation, BTM II Stage, Bangalore 560076, India.
3
Chemical Sciences Division, Vittal Mallya Scientific Research Foundation, BTM II Stage, Bangalore 560076, India. Electronic address: gcreddy@vmsrf.org.

Abstract

Methyl esters of the β-boswellic acid (BA) and 11-keto-β-boswellic acid (KBA) obtained from Boswellia serrata resin were subjected to Steglich esterification with the different non-steroidal anti-inflammatory drugs (NSAID) viz., ibuprofen, naproxen, diclophenac and indomethacin. The novel hybrids of methyl boswellate (5-8) and that of methyl 11-keto boswellate (9-12) were evaluated for anti-inflammatory activity by carrageenan-induced rat hind paw edema model and anti-arthritic activity by Complete Freund's Adjuvant (CFA) induced arthritis in Wister albino rat. Significant inhibition on carrageenan-induced paw edema has been observed with 5, 6 and 10 where as in CFA induced rats, hybrids 5, 8, 9 and 12 exhibited pronounced antiarthritic activity. Hybrid molecules 5 and 9 have been found to be more effective in inhibiting in-vivo COX-2 than ibuprofen by itself, thus showing the synergistic effect. Hybrid 5 and 9 tested for in-vitro lipoxygenase and cyclooxygenase-2 (LOX/COX-2) inhibitory activity. The studies revealed that both 5 and 9 inhibited COX-2 relatively better than LOX enzyme.

KEYWORDS:

Anti-arthritic; Anti-inflammatory; Boswellia serrata; Boswellic acids; NSAIDs

PMID:
26010018
DOI:
10.1016/j.ejmech.2015.05.001
[Indexed for MEDLINE]

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