Abstract
One of five compounds, AC-5-1, strongly inhibits 5-lipoxygenase with a half-inhibition dose of 5±0.12×10-8M. However, prostaglandin synthesizing activity is not inhibited until 10-5M. AC-5-1 is a highly selective inhibitor for 5-lipoxygenase. The AC-5-1 at 10-5M inhibits 96% of leukotriene C4 synthesis of mouse peritoneal cells facilitated by calcium-ionophore. Arachidonic acid induced ear edema of mice, an in vivo inflammatory model, involving leukotriene induction, is strongly inhibited by AC-5-1 in a dose-dependent manner. The inhibition is the strongest of any inhibitors of 5-lipoxygenase reported previously. Since the natural compound AC-5-1 can selectively inhibit 5-lipoxygenase and affect in vivo inflammation, it will be interesting to investigate the role of leukotrienes on inflammation and other physiological processes.
