Modification of lipid peroxidation by some known substituted imidazole derivatives. An attempt to correlate their antioxidant activity with lipophilicity.
The antioxidant activity of two antiallergic agents, oxatomide, astemizole and two neuroleptic drugs, penfluridol, pimozide, structurally related, was tested, using heat-inactivated rat hepatic microsomal fraction and linoleic acid. Lipid peroxidation was induced by Fe2+/ascorbic acid and Fe2+, respectively, and evaluated spectrophotometrically as 2-thiobarbituric acid reactive material. It was found that these compounds inhibited significantly the peroxidation of microsomal membranes in a concentration-dependent manner, as well as the peroxidation of linoleic acid. The lipophilicity of the tested compounds, expressed as RM values derived from reversed phase thin layer chromatography (RPTLC), was determined and the relationship between antioxidant activity and lipophilicity was discussed.
Department of Pharmaceutical Chemistry, School of Pharmacy, University of Thessaloniki, Greece.
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Tani
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Rekka
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Kourounakis
D000818:Animals; D000975:Antioxidants; D016589:Astemizole; D001562:Benzimidazoles / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002855:Chromatography, Thin Layer; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology*; D066298:In Vitro Techniques; D015227:Lipid Peroxidation / Q000187:drug effects*; D008055:Lipids / Q000737:chemistry*; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D010395:Penfluridol / Q000494:pharmacology; D010868:Pimozide / Q000494:pharmacology; D010879:Piperazines / Q000494:pharmacology; D051381:Rats
D000975:Antioxidants; D001562:Benzimidazoles; D007093:Imidazoles; D008055:Lipids; D010879:Piperazines; D010868:Pimozide; D010395:Penfluridol; D016589:Astemizole; C015408:oxatomide