Inhibition of staphylococcal alpha-toxin. A kinetic evaluation of aromatic polysulphonic acids as inhibitors of haemolysis.
1. The effect of a number of aromatic polysulphonic acids on the kinetics of haemolysis of rabbit erythrocyte suspensions by crude staphylococcal alpha-toxin was studied at pH8.6 and 6.8. 2. All of the inhibitory compounds caused an increase in the prelytic lag time (tau) of the sigmoid haemolysis curves, an increase in the time to reach 50% haemolysis (t((1/2))) and a decrease in the maximum rate of haemolysis (R(max.)). The most inhibitory compounds caused a 50% decrease in R(max.) at concentrations between 0.1 and 0.2mm. 3. The effect of pH varied considerably: compounds (I) and (II) were almost equally inhibitory at both pH values, compounds (IV) and (IX) were more inhibitory at pH6.8 than at pH8.6, and compounds (VII), (VIII), (X), (XI) and (XII) were more inhibitory at pH8.6. 4. Increased time of premixing alpha-toxin with compound (I) caused increased inhibition. 5. An attempt was made, where possible, to relate the inhibitory activity to the structure of the test compound.
D000818:Animals; D000992:Antitoxins; D001555:Benzene Derivatives / Q000494:pharmacology*; D006461:Hemolysis / Q000187:drug effects*; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D009281:Naphthalenes / Q000494:pharmacology*; D011817:Rabbits; D013210:Staphylococcus; D013451:Sulfonic Acids / Q000494:pharmacology*; D014227:Triazines / Q000494:pharmacology*
D000992:Antitoxins; D001555:Benzene Derivatives; D009281:Naphthalenes; D013451:Sulfonic Acids; D014227:Triazines