No abstract

Interesting antioxidant activities of extracts from different vegetative and reproductive organs of Crataegus monogyna harvested at different stages of growth have been determined by the malondialdehyde-thiobarbituric acid (MDA) test on hepatic microsomal preparations and compared to the contents in total phenolics, proanthocyanidins, catechins, flavonoids, and phenolic acids. The best correlations were established with total phenols while activities in leaves seem to be influenced by flavonoids and in flowers and fruits by proanthocyanidins and catechins.

The arachidonic acid metabolizing enzymes cyclooxygenase-2 (COX-2) and lipoxygenases (LOXs) have been found to be implicated in a variety of cancers, including prostate cancer. To develop new therapeutic treatments, it therefore seemed interesting to design dual COX-2/5-LOX inhibitors. We report here the synthesis and in vitro pharmacological properties of diarylpyrazole derivatives that have in their structure key pharmacophoric elements to obtain optimal interaction with subsites of active pockets in both enzyme systems. Using a molecular modeling approach, a set of SAR data is proposed, highlighting the importance of the sulfonyl group of one of the aryl moieties in terms of proliferation inhibition and/or apoptosis induction.