Inhibition of COXs and 5-LOX and activation of PPARs by Australian Clematis species (Ranunculaceae)

Rachel W. Li, Australian Centre for Complementary Medicine Education and Research
G David Lin, Australian Centre for Complementary Medicine Education and Research
David N. Leach, Southern Cross University
Peter G. Waterman, Southern Cross University
Stephen P. Myers, Southern Cross University

Abstract

The species of Clematis (Ranunculaceae) have been traditionally used for inflammatory conditions by indigenous Australians. We have previously reported that the ethanol extract of Clematis pickeringii inhibited COX-1. In this study, we examined the ethanol extracts and fractions of three Clematis species, Clematis pickeringii, Clematis glycinoides and Clematis microphylla, on cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). We further examined the activating effects on the protein expression of peroxisome proliferator-activated receptor alpha (PPARα) and gamma (PPARγ) in HepG2 cells. The ethanol extracts of three Clematis species inhibited the activities of COX-1, COX-2 and 5-LOX in the different extents. The stem extract of Clematis pickeringii showed the highest inhibitory activities among the three species on COX-1, COX-2 and 5-LOX with the IC50 values of 73.5, 101.2 and 29.3 μg/mL. One of its fractions also significantly elevated PPARα expression by 173, 280 and 435% and PPARγ expression by 140, 228 and 296% at 4, 8 and 16 μg/mL, respectively.