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Molecules 2012, 17(5), 4824-4835; doi:10.3390/molecules17054824
Article

Inhibitory Effects of Acetylmelodorinol, Chrysin and Polycarpol from Mitrella kentii on Prostaglandin E2 and Thromboxane B2 Production and Platelet Activating Factor Receptor Binding

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Received: 26 January 2012; in revised form: 9 April 2012 / Accepted: 10 April 2012 / Published: 26 April 2012
(This article belongs to the Section Metabolites)
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Abstract: Acetylmelodorinol, chrysin and polycarpol, together with benzoic acid, benzoquinone and stigmasterol were isolated from the leaves of Mitrella kentii (Bl.) Miq. The compounds were evaluated for their ability to inhibit prostaglandin E2 (PGE2) and thromboxane B2 (TXB2) production in human whole blood using a radioimmunoassay technique. Their inhibitory effect on platelet activating factor (PAF) receptor binding to rabbit platelet was determined using 3H-PAF as a ligand. Among the compounds tested, chrysin showed a strong dose-dependent inhibitory activity on PGE2 production (IC50 value of 25.5 µM), which might be due to direct inhibition of cyclooxygenase-2 (COX-2) enzymatic activity. Polycarpol, acetylmelodorinol and stigmasterol exhibited significant and concentration-dependent inhibitory effects on TXB2 production with IC50 values of 15.6, 19.1 and 19.4 µM, respectively, suggesting that they strongly inhibited COX-1 activity. Polycarpol and acetylmelodorinol showed strong dose-dependent inhibitory effects on PAF receptor binding with IC50 values of 24.3 and 24.5 µM, respectively.
Keywords: Mitrella kentii; chrysin; acetylmelodorinol; polycarpol; prostaglandin E2 (PGE2); thromboxane B2 (TXB2); platelet activating factor (PAF) antagonist Mitrella kentii; chrysin; acetylmelodorinol; polycarpol; prostaglandin E2 (PGE2); thromboxane B2 (TXB2); platelet activating factor (PAF) antagonist
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.

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MDPI and ACS Style

Saadawi, S.; Jalil, J.; Jasamai, M.; Jantan, I. Inhibitory Effects of Acetylmelodorinol, Chrysin and Polycarpol from Mitrella kentii on Prostaglandin E2 and Thromboxane B2 Production and Platelet Activating Factor Receptor Binding. Molecules 2012, 17, 4824-4835.

AMA Style

Saadawi S, Jalil J, Jasamai M, Jantan I. Inhibitory Effects of Acetylmelodorinol, Chrysin and Polycarpol from Mitrella kentii on Prostaglandin E2 and Thromboxane B2 Production and Platelet Activating Factor Receptor Binding. Molecules. 2012; 17(5):4824-4835.

Chicago/Turabian Style

Saadawi, Sakina; Jalil, Juriyati; Jasamai, Malina; Jantan, Ibrahim. 2012. "Inhibitory Effects of Acetylmelodorinol, Chrysin and Polycarpol from Mitrella kentii on Prostaglandin E2 and Thromboxane B2 Production and Platelet Activating Factor Receptor Binding." Molecules 17, no. 5: 4824-4835.


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