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 E 2 (PGE2) and thromboxane B 2 (TXB 2) 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 TXB 2 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.
| Original language | English |
|---|---|
| Pages (from-to) | 4824-4835 |
| Number of pages | 12 |
| Journal | Molecules |
| Volume | 17 |
| Issue number | 5 |
| DOIs | |
| Publication status | Published - May 2012 |
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Keywords
- Acetylmelodorinol
- Chrysin
- Mitrella kentii
- Platelet activating factor (PAF) antagonist
- Polycarpol
- Prostaglandin E (PGE )
- Thromboxane B (TXB )
ASJC Scopus subject areas
- Organic Chemistry
- Medicine(all)
Cite this
Inhibitory effects of acetylmelodorinol, chrysin and polycarpol from mitrella kentii on prostaglandin E2 and thromboxane B2 production and platelet activating factor receptor binding. / Saadawi, Sakina; Jalil, Juriyati; Jasamai, Malina; Jantan, Ibrahim.
In: Molecules, Vol. 17, No. 5, 05.2012, p. 4824-4835.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Inhibitory effects of acetylmelodorinol, chrysin and polycarpol from mitrella kentii on prostaglandin E2 and thromboxane B2 production and platelet activating factor receptor binding
AU - Saadawi, Sakina
AU - Jalil, Juriyati
AU - Jasamai, Malina
AU - Jantan, Ibrahim
PY - 2012/5
Y1 - 2012/5
N2 - 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 E 2 (PGE2) and thromboxane B 2 (TXB 2) 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 TXB 2 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.
AB - 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 E 2 (PGE2) and thromboxane B 2 (TXB 2) 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 TXB 2 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.
KW - Acetylmelodorinol
KW - Chrysin
KW - Mitrella kentii
KW - Platelet activating factor (PAF) antagonist
KW - Polycarpol
KW - Prostaglandin E (PGE )
KW - Thromboxane B (TXB )
UR - http://www.scopus.com/inward/record.url?scp=84861494109&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84861494109&partnerID=8YFLogxK
U2 - 10.3390/molecules17054824
DO - 10.3390/molecules17054824
M3 - Article
VL - 17
SP - 4824
EP - 4835
JO - Molecules
JF - Molecules
SN - 1420-3049
IS - 5
ER -