[Anticomplementary activity of a polyanion: pentosan-poly-sulfoester, II.--Mode of action and "in vitro " inhibition of human complement hemolytic activity (author's transl)].
The drug, pentosan-poly-sulfoester (PPS), is a potent in vitro inhibitor of the human complement hemolytic activity. This CH 50 inhibition represents a real anticomplementary activity (ACA), because this drug has no effect on sensitized sheep red blood cells (EA). The inhibition curve of human serum CH 50, by PPS is sigmoidal. The 50% inhibition is obtained for a 1: 650 dilution of PPS, which corresponds to a concentration of 0.08 mg/ml in normal human serum. Hemolytic titrations of C1, C4, C2, C3, and C5 showed a complete inhibition of C4, C2 and C3, and a partial inhibition of C1 (C1q, C1r, C1s, Ca++) and C5, by this drug. The mechanism of such functional inactivation of the different complement components is not yet elucidated.
D003175:Complement C2 / Q000037:antagonists & inhibitors; D003176:Complement C3 / Q000037:antagonists & inhibitors; D003181:Complement C4 / Q000037:antagonists & inhibitors; D003169:Complement Inactivator Proteins; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D010426:Pentosan Sulfuric Polyester / Q000494:pharmacology*; D011134:Polysaccharides / Q000494:pharmacology*
D003175:Complement C2; D003176:Complement C3; D003181:Complement C4; D003169:Complement Inactivator Proteins; D011134:Polysaccharides; D010426:Pentosan Sulfuric Polyester
Activité anticomplémentaire d'un polyanion: le polyester sulfurique de pentosane II.--Mode d'action et inhibition "in vitro" de l'activité hémolytique du complément humain