首页|Chemical constituents from the flowers of Hypericum monogynum L. with COX-2 inhibitory activity
Chemical constituents from the flowers of Hypericum monogynum L. with COX-2 inhibitory activity
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NSTL
Elsevier
Hypericum monogynum L. (Hypericaceae) has been used as a folk Chinese medicine for the treatment of in-flammatory related diseases. Cyclooxygenase-2 (COX-2) is a crucial target for the development of agents to treat inflammation. To search for anti-inflammatory compounds from traditional Chinese medicines, a chemical constituent study along with COX-2 inhibitory activity analysis was performed for this plant. In this study, sixteen chemical monomers, including three undescribed oxidative degradation polycyclic polyprenylated acylphloroglucinols (PPAPs, hypemoins C-E), two undescribed PPAPs (hypemoins A and B), and 11 known compounds, were identified from the flowers of H. monogynum. Their structures were characterized by HRESIMS, NMR techniques, ECD, and single crystal X-ray diffraction. Four flavonoid derivatives showed remarkable COX-2 inhibitory activities, with IC50 values ranging from 0.220 +/- 0.006 to 1.655 +/- 0.098 mu M. Among these compounds, the possible recognition mechanism between quercetin 3-(6"-O-caffeoyl)-beta-3-D-galactoside and COX-2 was predicted by molecular docking analysis. Moreover, the multidrug resistance reversal activities for the selected compounds were evaluated.
NSTL
Elsevier
