- 生物活性
PGS-IN-1是有效的前列腺素合成酶 (prostaglandin synthetase) 抑制剂,IC50 值为0.28 μM;也可抑制5-脂肪氧合酶 (5-lipoxygenase) 的活性,IC50 值为 1.05 μM。
- 靶点
5-Lipoxygenase
1.05 μM (IC
50
)
- 体外研究
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 (IC
50
=0.28 μM). PGS-IN-1 also shows potent inhibitory activity against 5-lipoxygenase (IC
50
=1.05 μM).
医药
合成方法:合成的α-苄叉-γ-丁内酯为纯异构体(顺式或反式),PGS-IN-1是反式异构体。