Background: Several clinically used COX-1 and COX-2 inhibitor drugs were reported
to possess severe side effects like GI ulcers and cardiovascular disturbances, respectively.
Natural products being structurally diverse always attracted the attention of chemists/
medicinal chemists as a potential source of lead molecules in the drug discovery process.
COX-2 inhibitory natural products also possess potential cancer chemopreventive property
against various cancers including that of colon, breast and prostate.
Methods: Various in vitro, in vivo and in silico standardized methods were used to evaluate
COX inhibition property of different secondary metabolites isolated from plant, microbial and
Results: We had earlier reported a detailed account of natural product inhibitors of COX reported
during 1995-2005, in 2006. In the proposed review, we report 158 natural product inhibitors
of COX during 2006 to 2019 belonging to various secondary metabolite classes such
as alkaloids, terpenoids, polyphenols as flavonoids, chromones, coumarins, lignans, anthraquinones,
naphthalenes, curcuminoids, diarylheptanoids and miscellaneous compounds of
plant and marine origin. Further Structure Activity Relationship (SAR) studies of possible
leads are also included in the article.
Conclusion: COX inhibitors served as a potential source of lead molecules for the discovery
and development of anti-inflammatory drugs. Compilation of natural product and semisynthetic
inhibitors of COX may serve as valuable information to the researchers who are
looking for possible lead molecules from a natural source to conduct further preclinical and