Vasoactive intestinal peptide and helodermin inhibit phospholipase A2 activity in vitro
Abstract:
We recently reported that the widely distributed neuropeptide vasoactive intestinal peptide (VIP) reduces inflammatory lung injury due to a variety of agents and inhibits the associated generation of cyclo-oxygenase and lipoxygenase products. We therefore investigated whether VIP may inhibit phospholipase A2 activity, thus reducing the release of arachidonic acid, the common precursor of all eicosanoids. VIP dose-dependently inhibited PLA2 of porcine pancreas and of Naja naja venom, as assessed by the release of free [3H]oleic acid from labeled Escherichia coli phospholipids. The potency of VIP was similar to that of mepacrine, with 50% inhibition at 400-500 microM. The closely related peptide helodermin produced 50% inhibition at 200 microM, but secretin and peptide histidine isoleucineamide produced little or no inhibition. The results suggest that VIP and helodermin selectively inhibit PLA2 in vitro. If this activity is exerted in vivo, it may contribute to the anti-inflammatory activity of these two peptides.
Related Concept Videos
IP3/DAG Signaling Pathway
Acid Suppressive Drugs for Peptic Ulcer Disease: Proton Pump Inhibitors
Gastric acid, a potent cocktail of hydrogen and chloride ions, is produced in specialized parietal cells within the...
Drugs for Peptic Ulcer Disease: Prostaglandin Analogs as Mucosal Protective Agents
Non-steroidal anti-inflammatory drugs (NSAIDs) can induce peptic ulcers by inhibiting cyclooxygenase, decreasing...
Pathophysiology of Peptic Ulcer Disease: Injurious Factors
In the antrum region, G cells secrete the gastrin hormone that binds to gastrin-cholecystokinin-B (CCK2) receptors on parietal and enterochromaffin-like (ECL) cells in the fundic glands. Simultaneously, the vagus nerve releases acetylcholine, which binds to M3...
Intestinal Phase of Digestion
The arrival of the chyme in the small intestine distends the duodenum, which triggers the enterogastric reflex. This distension...
Hormonal Regulation


