Inhibitory effect of dioctyl sodium sulfosuccinate on trypsin activity.

The inhibitory effect of dioctyl sodium sulfosuccinate on the proteolytic activity of trypsin was investigate over the pH 6-8 range. The antitryptic activity was determined using two different substrates: casein and N,alpha-benzoyl-DL-arginine-p-nitroanilide hydrochloride. The mechanistic studies revealed the substrate-inhibitor interaction to be the overall major mechanism of inhibition. This interaction was shown to involve substrate depletion, probably involving some primary sites of the natural substrate casein. Some inhibition was also shown to be due to an interaction between the enzyme and the inhibitior molecules. The interactions of the inhibitor with the enzyme and the substrate were irreversible. The possible therapeutic significance of the inhibitory effect of the surfactant is discussed.

[1]  M. Gouda,et al.  Effect of surfactants on absorption through membranes IV: effects of dioctyl sodium sulfosuccinate on absorption of a poorly absorbable drug, phenolsulfonphthalein, in humans. , 1975, Journal of pharmaceutical sciences.

[2]  M. Gouda,et al.  Effect of surfactants on absorption through membranes III: effects of dioctyl sodium sulfosuccinate and poloxalene on absorption of a poorly absorbable drug, phenolsulfonphthalein, in rats. , 1975, Journal of pharmaceutical sciences.

[3]  C. Piantadosi,et al.  Diamidino-.alpha.,.omega.-diphenoxyalkanes. Structure-activity relations for the inhibition of thrombin, pancreatic kallikrein, and trypsin , 1973 .

[4]  C. Dujovne,et al.  Toxicity of a hepatotoxic laxative preparation in tissue culture and excretion in bile in man , 1972, Clinical pharmacology and therapeutics.

[5]  C. Nelson,et al.  The binding of detergents to proteins. I. The maximum amount of dodecyl sulfate bound to proteins and the resistance to binding of several proteins. , 1971, The Journal of biological chemistry.

[6]  A. Baillie,et al.  Carrageenans and the proteolytic activity of human gastric secretion , 1967, The Journal of pharmacy and pharmacology.

[7]  R. Colman Proteolytic enzymes in clinical medicine , 1965, Clinical pharmacology and therapeutics.

[8]  J. Moffat,et al.  Role of Bradykinin in the Development of Acute Pancreatitis , 1964, Nature.

[9]  John Leyden. Webb,et al.  Enzyme and metabolic inhibitors , 1963 .

[10]  William W. Cohen,et al.  The preparation and properties of two new chromogenic substrates of trypsin. , 1961, Archives of biochemistry and biophysics.

[11]  W. Anderson THE ANTIPEPTIC ACTIVITY OF SULPHATED POLYSACCHARIDES , 1961, The Journal of pharmacy and pharmacology.

[12]  J. M. Reiner Behavior of enzyme systems , 1959 .

[13]  M. Dixon The determination of enzyme inhibitor constants. , 1953, The Biochemical journal.

[14]  M. Kunitz,et al.  CRYSTALLINE SOYBEAN TRYPSIN INHIBITOR : II. GENERAL PROPERTIES. , 1947 .

[15]  J. Northrop,et al.  CRYSTALLINE TRYPSIN : II. GENERAL PROPERTIES. , 1932 .