PGS-IN-1

PGS-IN-1 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM.

Signaling Pathways >> Metabolic Enzyme/Protease >> 5-Lipoxygenase

Signaling Pathways >> Immunology/Inflammation >> PGE synthase

Research Areas >> Inflammation/Immunology

IC50: 0.28 μM (PGS), 1.05 μM (5-lipoxygenase)[1]

The synthesized α-benzulidene-γ-butyrolactones are pure isomers (either cis or trans). PGS-IN-1 is the trans isomer. PGS-IN-1 exhibits potent antiinflammatrory and PGS inhibitory activity (IC50=0.28 μM). PGS-IN-1 also shows potent inhibitory activity against 5-lipoxygenase (IC50=1.05 μM)[1].

PGS-IN-1 is dissolved in ethanol and the final concentration of ethanol is kept at 2% in each assay. The reaction mixture includes reaction buffer, enzyme (20 μg protein), and PGS-IN-1 in a total volume of 0.2 mL. The mixture is incubated for 15 min at 37°C with shaking and terminated by the addition of 2.5 mL ethyl acetate and 25 μL 1 N formic acid[1].

Rats: PGS-IN-1 is administered orally to groups of 4-6 male Wistar rats weighting 160-220 g. One hour later, 1 % carrageenin in 0.9 % NaCl is injected subcutaneously into a hind paw. Paw volumes are measured 5 h after the injection[1].

[1]. Katsumi I, et al. Studies on styrene derivatives. I. Synthesis and antiinflammatory activities of alpha-benzylidene-gamma-butyrolactone derivatives. Chem Pharm Bull (Tokyo). 1986 Jan;34(1):121-9.

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