Anti-inflammatory, cyclooxygenase (COX)-2, COX-1 inhibitory and antioxidant effects of Dysophylla stellata Benth.

Molecular characterization, biological activity, and in silico study of 2-(3,4-dimethoxyphenyl)-3-(4-fluorophenyl)-6-methoxy-4H-chromen-4-one as a novel selective COX-2 inhibitor

“…This method was previously reported by Dyrager et al (2011), in which the introduction of various aryl groups to 3-bromochomones and 3-iodochromones via Suzuki coupling was easily accomplished in the presence of palladium catalyst [31]. In our case, the introduction of the fluorophenyl group to 21 was easily done using the in situ generated palladium nanoparticles in PEG-400 solvent under aerobic condition to give the target product of 2-(3,4-dimethoxyphenyl)-3-(4-fluorophenyl)-6-methoxy-4H-chromen-4-one (22) in good yield (64%). This oxygen-promoted ligand-free Suzuki coupling reaction had been previously reported by Han et al (2007) [33].…”

“…The presence of chromone scaffold in some natural and synthetic compounds without the presence of sulfonyl or sulfonamide moiety had also been reported for possessing good COX inhibition. For example, stellatin (12) and eugenin (13), isolated from Dysophyllastellata were reported to be selective towards COX-2 inhibition [21,22]. On the other hand, a series of chrysin derivatives bearing dichloro group at positions 3' and 4' (e.g compounds 14-16) had been prepared and were found to exhibit good inhibitory activity on prostaglandin production by COX-2 (IC 50 = 0.1-0.5 μM) [23].…”

Plant parts substitution based approach as a viable conservation strategy for medicinal plants: A case study of Premna latifolia Roxb.

“…The experimental animals were divided into groups of control, standard and test of six animals each. The control group animals received only vehicle, the standard group animals received ibuprofen [21] or pentazocine [22] for comparison and the test group animals received the test materials (extracts).…”

Chromones: A Promising Ring System for New Anti‐inflammatory Drugs

“…Several compounds have been isolated from the terpenoid, alkaloid, and flavonoid categories, and their activity as COX inhibitors have been evaluated, amongst which chromone‐based compounds have shown promising inhibitory activities toward both COX‐1 and COX‐2 . In the past few years, several novel compounds containing the chromone core, either isolated from various types of plant or as synthetic derivatives, have demonstrated the capacity to inhibit COX enzymes . For this reason, the chromone scaffold has been used as a basis for the synthesis of new anti‐inflammatory agents…”