A hexane extract of Plantago major was investigated by bioactivity-directed fractionation, using an in vitro cyclooxygenase-2 (COX-2) catalyzed prostaglandin biosynthesis inhibition assay, and resulted in the isolation of ursolic acid (1). This triterpenoid showed a significant COX-2 inhibitory effect, directly on the enzyme activity, with an IC50 value of 130 microM and a COX-2/COX-1 selectivi...

INTRODUCTION The enzyme cyclooxygenase (COX) is an enzyme that catalyzes the formation of one of the mediators of inflammation, the prostaglandins. Inhibition of COX allegedly can improve inflammation-induced pathological conditions. AIM The purpose of the present study was to evaluate the potential of Sargassum sp. components, Fucoidan and alginate, as COX inhibitors. MATERIAL AND METHODS ...

a new group of 4-(imidazolylmethyl) quinoline derivatives possessing a methylsulfonyl cox-2 pharmacophore at the para position of the c-2 phenyl ring were designed and synthesized as selective cox-2 inhibitors and in-vitro anti breast cancer agents. in-vitro cox-1 and cox-2 inhibition studies showed that all the compounds were potent and selective inhibitors of the cox-2 isozyme with ic50 value...

BACKGROUND Placebo-controlled trials of nonsteroidal anti-inflammatory drugs selective for inhibition of cyclooxygenase-2 (COX-2) reveal an emergent cardiovascular hazard in patients selected for low risk of heart disease. Postnatal global deletion of COX-2 accelerates atherogenesis in hyperlipidemic mice, a process delayed by selective enzyme deletion in macrophages. METHODS AND RESULTS In t...

Decreased expression of peroxisome proliferator activated receptor-gamma (PPARgamma) and high levels of the proinflammatory enzyme cyclooxygenase-2 (COX-2) have been observed in many tumor types. Both reduced (PPARgamma) expression and elevated COX-2 within the tumor are associated with poor prognosis in lung cancer patients, and recent work has indicated that these signaling pathways may be in...

Background: Aberrant glycosylation is a common feature of breast cancer. Results: Cyclooxygenase-2 (COX-2) an enzyme associated with tumorigenesis in breast cancer upregulated the sialyltransferase ST3Gal-I. Conclusion: COX-2 can regulate the expression of ST3Gal-I in breast cancer Significance: Some of the tumorigenic properties associated with COX-2 may be the result of upregulating ST3Gal-I ...

Because across-the-board data indicate that renin and cyclooxygenase-2 (COX-2) expression in the kidney cortex are regulated in parallel and because ANG II can inhibit COX-2 expression, the purpose of our study was to characterize a potential general inhibitory feedback of the renin-angiotensin system on renocortical COX-2 expression in vivo. Rats were fed a high-, normal-, or low-salt diet or ...

Studies have conjectured that nonsteroidal anti-inflammatory drugs (NSAID) inhibit growth of various malignancies by inhibiting cyclooxygenase-2 (COX-2) enzyme activity. Yet, several lines of evidence indicate that a COX-2-independent mechanism may also be involved in their antitumor effects. Here, we report that NSAIDs may inhibit the growth of glioblastoma multiforme (GBM) cells through COX-2...