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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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 languageEnglish
Pages (from-to)4824-4835
Number of pages12
JournalMolecules
Volume17
Issue number5
DOIs
Publication statusPublished - May 2012

Fingerprint

prostaglandins
Thromboxane B2
platelets
Dinoprostone
Stigmasterol
Inhibitory Concentration 50
Thromboxanes
Prostaglandins E
Benzoic Acid
Platelet Activating Factor
radioimmunoassay
Cyclooxygenase 2
Platelets
dosage
Radioimmunoassay
rabbits
benzoic acid
quinones
Blood
Blood Platelets

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

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title = "Inhibitory effects of acetylmelodorinol, chrysin and polycarpol from mitrella kentii on prostaglandin E2 and thromboxane B2 production and platelet activating factor receptor binding",
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.",
keywords = "Acetylmelodorinol, Chrysin, Mitrella kentii, Platelet activating factor (PAF) antagonist, Polycarpol, Prostaglandin E (PGE ), Thromboxane B (TXB )",
author = "Sakina Saadawi and Juriyati Jalil and Malina Jasamai and Ibrahim Jantan",
year = "2012",
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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.

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