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Archives of Pharmacal Research 2016-Mar

Lipoxygenase inhibitors from the latex of Calotropis Procera.

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Wael M Abdel-Mageed
Nadia H Mohamed
Miaomiao Liu
Ali A El-Gamal
Omer A Basudan
Mady Ahmed Ismail
Ronald J Quinn
Xueting Liu
Lixin Zhang
Ahmed A M Shoreit

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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.

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