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[Inhibitory effect of dauricine on platelet activating factor released from calcimycin-induced mouse peritoneal
1Department of Pharmacology, College of Pharmacy, Second Military Medical University, Shanghai, China.
Abstract:
The effects of dauricine (Dau) on the release of platelet activating factor (PAF) from mouse peritoneal macrophages stimulated by calcimycin (A-23187) was studied. The method of sodium [3H]acetate incorporating into macrophages to synthesize PAF was set up for the first time. Calcimycin (0.2 mumol/L) significantly induced mouse peritoneal macrophages to utilize sodium [3H]acetate to synthesize PAF. PAF released from macrophages medium fluid increased as the concentration of sodium [3H]acetate increased. The maximal amount of PAF released from macrophages was attained by incubating macrophages with sodium [3H]acetate (250 mumol/L) and calcimycin (2 mumol/L) over 30 min. Extracted by CHCl3:CH3OH:H2O (2:2:1.8), separated by thin layer chromatography (TLC) and determined by liquid scintillation counting, PAF released was inhibited significantly by Dau both in time (10-30 min) and dose (1-1000 mumol/L) dependent manners. The IC50 of Dau for the formation of PAF was 2.5 mumol/L. On the same condition PAF release was also significantly inhibited by quinacrine at 500 mumol/L. The results indicate that Dau is a potent inhibitor of PAF synthesis in mouse peritoneal macrophages.
Insights
Dauricine (Dau) effectively inhibits platelet-activating factor (PAF) synthesis in mouse macrophages. This study establishes a novel method for measuring PAF release, crucial for understanding inflammatory responses.
Area of Science:
- Immunology
- Pharmacology
Context:
- Platelet-activating factor (PAF) is a key mediator in inflammatory and allergic reactions.
- Mouse peritoneal macrophages are utilized to study PAF release mechanisms.
Purpose:
- To investigate the inhibitory effects of dauricine (Dau) on PAF release from macrophages.
- To establish and validate a novel method for synthesizing and quantifying PAF using sodium [3H]acetate.
Summary:
- A new method was developed to synthesize platelet-activating factor (PAF) in mouse peritoneal macrophages using sodium [3H]acetate.
- Calcimycin stimulation significantly induced PAF synthesis, with release increasing proportionally to sodium [3H]acetate concentration.
- Dauricine demonstrated potent, dose- and time-dependent inhibition of PAF release, with an IC50 of 2.5 µmol/L. Quinacrine also showed inhibitory effects.
Impact:
- Dauricine emerges as a significant inhibitor of PAF synthesis, offering potential therapeutic applications in inflammatory conditions.
- The established methodology provides a reliable tool for future research on PAF production and its modulation.