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PubMed1976

The influence of coumarin on blood levels of radio labelled protein and radio labelled poly-vinyl-pyrrolidone in thermally injured rats.

The evidence presented in this paper suggests that coumarin is a RES stimulator. An enhanced removal of both RPP and radio RPVP was observed beginning at or before 30 minutes and lasting up to 6 hours. Over this time, RPP removal was enhanced by an average of 40%, while RPVP removal was enhanced by 60%. Since RPVP is non-metbabolizable, its levels may be a more accurate estimate of the stimulatory effect of coumarin. This evidence fits in well previous results which have suggested that coumarin may increase the number of phagocytic cells. Other results have shown enhancement of protein lysis by 74% over similar periods, while enhanced protease activity levels of 50% have been observed to accompany this.

Animals↗
PubMed1987

In vitro effect of N-methoxy-3-(3,5-ditert-butyl-4-hydroxybenzylidene)-2-pyrrolidon e (E-5110), a novel nonsteroidal antiinflammatory agent, on generation of some inflammatory mediators.

Cultured rat synovial cells generate PGE2 upon stimulation with a factor derived from rate polymorphonuclear cells (Prostaglandins 27, 697, 1984). E-5110 inhibited PGE2 generation by the synovial cells. The IC50 values (microM) for inhibition of PGE2 generation were 0.026 for E-5110, 0.008 for indomethacin, 0.112 for piroxicam, 0.003 for R-830, 0.667 for BW-755C and 2.05 for benoxaprofen. Calcium ionophore A-23187-stimulated LTB4 generation by human neutrophils was inhibited by E-5110 with an IC50 value of 0.20 microM, which was similar to NDGA. The inhibition of LTB4 by E-5110 was more potent than that of R-830, BW-755C or benoxaprofen. E-5110 also inhibited superoxide generation by human neutrophils stimulated with opsonized zymosan, f-Met-Leu-Phe and phorbol myristate acetate. These results indicate that E-5110 is a potent dual inhibitor that suppresses superoxide generation.

Animals↗