Objective Criteria of Efficacy in Clinical Enzymology

Journal/Book: Exp Med Surg Supplement. 1965; 26-35.

Abstract: Orally administered proteolytic enzymes are absorbed through the human gastrointestinal tract and the absorbed enzymes retain some of their proteolytic activity in spite of any natural inhibitors present in the blood. The following links of evidence support the conclusions.1. When trypsin I131 is given orally to human subjects, measurable radioactivity is found in the protein fraction of the blood serum.2. After bromelain is administered orally to healthy human subjects,, the proteolytic activity of the blood serum as measured by its ability to hydrolyze casein is increased. Similar studies with patients gave equivocal results possibly because the disease process itself stimulates the formation of endogenous proteolytic enzymes or causes the absorption of the enzymes from the blood into the tissues. Another factor may have been the small dosage which was one-half of the recommended therapeutic amount.3. Clinical studies show that the administration of oral proteolytic enzymes hasten the resolution of inflammation, edema, and ecchymoses, and reduce the incidence of postoperative tissue reactions.4. The quantity of dialyzable amino acids and peptides in the blood serum was increased after oral administration of bromelain to hurnan subjects.5. Streptokinase as Varidase administered rectally evoked a positive Ouchterlony gel diffusion response in the blood serum of a majority of the patients treated in such a manner.6. Leucine amino peptidase activity of the urine was considerably increased following streptokinase administered orally. The activity of carboxypeptidase B in the urine was also enhanced by the administration of streptokinase.7. A small oral dose of papain produced an increase of a plasma antithrombin agent. A large dose resulted in a decrease of thrombin clotting time and an acceleration of euglobulin clot Iysis time.8. The esterase activity of the blood serum against N-acetyl-L-tyrosine ethyl ester, a substrate specific for chymotrypsin, was increased after chymotrypsin was given to human subjects orally. 9. Bromelain tagged by conjugation with a fluorescent dyeabsorbed through the gastrointestinal tracts of rabbits as shown by paper electrophoresis in wich the electrophoretic diagrams of material in the blood serum matched diagrams of known samples of bromelain-dye conjugate but did not match those of simple in vitro mixtures of dye with blood serum.

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