PURPOSE: To investigate the binding of @entity2533 ( @entity2533 ) to @entity1 @entity5843 upon oral treatment of @entity1 with proteases. METHODS: Volunteers were given a cocktail of active proteinases (Phlogenzym) composed of trypsin, bromelain and the additive @entity15604 orally over a period of 7 days at low dose followed by a bolus application. Before and after medication plasma was immediately withdrawn and binding of 125I- @entity2533 to the proteinase inhibitor @entity5843 was determined by electrophoresis and gamma-counting. Cell culture experiments were performed to study the effect of transformed @entity5843 on @entity2533 -stimulated proliferation of skin fibroblasts. RESULTS: Ingestion of proteinases was found to trigger the formation of intermediate forms of @entity5843 displaying high affinity to @entity2533 . Maximum binding of @entity2533 was observed 1-2 h after bolus ingestion, and steadily levelled off with time. In vitro experiments demonstrated that complex formation of diverse proteinases (trypsin, alpha-chymotrypsin, bromelain and plasmin) with @entity5843 conferred binding of 125I- @entity2533 , @entity5843 transformed by @entity8776 or proteinases was found to abolish the @entity2533 effect on fibroblasts in cell culture. CONCLUSIONS: Intestinal absorption of proteinases triggers the formation of @entity2533 binding species of @entity5843 in blood. Mediated by this process high concentrations of @entity2533 might be reduced via enhanced clearance of @entity5843 - @entity2533 complexes. Thus, proteinase therapy may have beneficial effects in treatment of @entity82 and certain @entity5 accompanied by excessively high @entity2533 concentrations.

Modulation of growth factor binding properties of XXXX by enzyme therapy.

@entity1 :: ('9606', 'Species') :: ['human', 'patients'] @entity82 :: ('MESH:D005355', 'Disease') :: ['fibrosis'] @entity5843 :: ('2', 'Gene') :: ['alpha2-Macroglobulin', 'alpha2-macroglobulin'] @entity15604 :: ('MESH:D012431', 'Chemical') :: ['rutoside'] @entity5 :: ('MESH:D009369', 'Disease') :: ['cancers'] @entity2533 :: ('7040', 'Gene') :: ['TGF-beta', 'transforming growth factor-beta'] @entity8776 :: ('MESH:C027451', 'Chemical') :: ['methylamine']
@entity5843 :: (2,Gene) :: ['alpha2-macroglobulin']
