Lipoxygenase inhibitors from the latex of Calotropis Procera

Arch Pharm Res. 2016 Mar 9. doi: 10.1007/s12272-016-0725-9. Online ahead of print.

Abstract

A radical-scavenging, guided phytochemical study of the latex of Calotropis Procera afforded five lignans (1-5), including a new one (4). The structural determination was accomplished using 1D- and 2D-NMR, high-resolution electrospray ionization mass spectrometry (HRESIMS), and correlation with known compounds. Among the isolated compounds, acylated lignans (3-5) showed stronger antioxidant activity than non-acylated derivatives (1,2). Anti-inflammatory activity was evaluated by determining the inhibitory potential against 5- and 15-lipoxygenase enzymes. The highest anti-inflammatory activity was observed in compound 4, with IC50s values of 7.6 µM and 2.7 µM against 5-LOX and 15-LOX, respectively.

Keywords: Anti-inflammatory; Antioxidants; Calotropis procera; Lignans; Lipoxygenase inhibitors.