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Interaction between phorbol esters and phospholipid in a monolayer model membrane

par Deleers, Michel ;Ruysschaert, Jean Marie ;Malaisse, Willy
Référence Chemico-biological interactions, 42, 3, page (271-278)
Publication Publié, 1982

Article révisé par les pairs

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Résumé :

The possible molecular interaction between phorbol esters and a phospholipid was examined in monolayer films at an air-water interface. The surface pressure isotherms indicated that, at close-to-physiological pressure, there existed a repulsive interaction between the phospholipid and biologically active phorbol esters, such as 12-O-tetradecanoylphorbol-13-acetate (TPA) and phorbol 12,13-didecanoate (PDD). There was a close parallelism between the relative biological potency of different phorbol esters, as tumour promoters, and the magnitude of their repulsive interaction with the phospholipid. These findings raise the possibility that a biophysical interference of phorbol esters with the phospholipid domain of biological membranes may represent an important determinant of their biological actions.