Abstract: The known flavonoids ginkgetin (1), taiwanhomoflavone A (2),taiwanhomoflavone B (3), and taiwanhomoflavone C (4) and eight known lignans:justicidin B (9), justicidin C (10), justicidin D (11), chinensinaphthol methyl ether (12),procumphthalide A (13), procumbenoside A (15), and ciliatosides A (16) and B (17) wereisolated from Cephalotaxus wilsoniana and Justicia species, respectively. The antiplateleteffects of the above constituents on human platelet-rich plasma (PRP) were evaluated. Ofthe compounds tested on human PRP, compounds 1, 4, 9, and 11 showed inhibition ofsecondary aggregation induced by adrenaline. Compound 1 had an inhibitory effect oncyclooxygenase-1 (COX-1). Molecular docking studies revealed that 1 and the related compounds apigenin (5), cycloheterophyllin (6), broussoflavone F (7), and quercetin (8) were docked near the gate of active site of COX-1. It indicated that the antiplatelet effect of 1, 4, 9, and 11 is partially owed to suppression of COX-1 activity and reduced thromboxane formation. Flavonoids, 1, 5, 6, 7, and 8 may block the gate of the active site of COX-1 and interfere the conversion of arachidonic acid to prostaglandin (PG) H2 in the COX-1 active site.
This is an open access article distributed under the
Creative Commons Attribution License which permits unrestricted use, distribution,
and reproduction in any medium, provided the original work is properly cited.
Export to BibTeX
MDPI and ACS Style
Wu, C.-M.; Wu, S.-C.; Chung, W.-J.; Lin, H.-C.; Chen, K.-T.; Chen, Y.-C.; Hsu, M.-F.; Yang, J.-M.; Wang, J.-P.; Lin, C.-N. Antiplatelet Effect and Selective Binding to Cyclooxygenase (COX) by Molecular Docking Analysis of Flavonoids and Lignans. Int. J. Mol. Sci. 2007, 8, 830-841.
Wu C-M, Wu S-C, Chung W-J, Lin H-C, Chen K-T, Chen Y-C, Hsu M-F, Yang J-M, Wang J-P, Lin C-N. Antiplatelet Effect and Selective Binding to Cyclooxygenase (COX) by Molecular Docking Analysis of Flavonoids and Lignans. International Journal of Molecular Sciences. 2007; 8(8):830-841.
Wu, Chien-Ming; Wu, Shu-Chun; Chung, Wan-Jung; Lin, Hsien-Cheng; Chen, Kun-Tze; Chen, Yu-Chian; Hsu, Mei-Feng; Yang, Jwu-Maw; Wang, Jih-Pyang; Lin, Chun-Nan. 2007. "Antiplatelet Effect and Selective Binding to Cyclooxygenase (COX) by Molecular Docking Analysis of Flavonoids and Lignans." Int. J. Mol. Sci. 8, no. 8: 830-841.