Effect of a diazafluoranthen derivative on phospholipases A study at the air-water interface |
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Authors: | P Chatelain C Berliner JM Ruysschaert J Jaff |
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Institution: | Laboratoire de Chimie-Physique des Macromolécules aux Interfaces, Université Libre de Bruxelles Belgium |
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Abstract: | AC-3579 (2-N-methylpiperazinomethyl-1,3-diazafluoranthen 1-oxide) produces in rat hepatocytes a hypertrophy of the endoplasmic reticulum.Two possibilities that can explain this phenomenon are (1) that AC-3579 inactivates the phospholipases, and (2) that an AC-3579-lipid interaction hinders the enzymic activity.To demonstrate these hypotheses, a physicochemical model of biological membrane, the lipid-water interface, has been used. Dipalmitoyl dl-α-phosphatidylcholine was spread at the air-water interface, the enzymes (phospholipase A or phospholipase C) dissolved in the aqueous phase.The enzymic reaction was first studied with and without AC-3579 dissolved in the aqueous phase; no enzymic inactivation was observed. However in AC-3579- lipid complex completely inhibited the enzymic reaction in the case of phospholipase A.An explanation is given in terms of steric hindrance to the enzyme-substrate complex formation. |
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