Phospholipase inactivation induced by an amino-piperazine derivative: a study at the lipid-water interface.
1-Amino-4-octylpiperazine, AP 22, an antiviral agent causes lipid accumulation in nervous tissue cultures. A physicochemical membrane model was used to demonstrate the formation of a lipid-AP 22 complex hindering phospholipase A2 action. A well defined amphiphilic balance seems essential to explain the mode of action of the drug. The hydrophilic group prevents enzyme-substrate complex formation whereas the hydrophobic group allows the penetration in the lipid layer and determines the stability of the drug-lipid complex. This stability of the drug-lipid association has a direct influence on phospholipase A2 activity but does not affect phospholipase C activity. No inactivation of phospholipase A2 due to a drug-enzyme interaction could be detected.
D006868:Hydrolysis; D008055:Lipids; D008567:Membranes, Artificial; D010740:Phospholipases / Q000037:antagonists & inhibitors*; D010879:Piperazines / Q000494:pharmacology*; D011312:Pressure; D011663:Pulmonary Surfactants; D013499:Surface Properties; D014867:Water
D008055:Lipids; D008567:Membranes, Artificial; D010879:Piperazines; D011663:Pulmonary Surfactants; D014867:Water; D010740:Phospholipases