Oral heparin results in the appearance of heparin fragments in the plasma of rats

Journal Article · Thu May 01 04:00:00 EDT 1986 · Proc. Natl. Acad. Sci. U.S.A.; (United States)

DOI:https://doi.org/10.1073/pnas.83.9.2964· OSTI ID:5578508

Larsen, A K; Lund, D P; Langer, R; Folkman, J

We have previously shown that angiogenesis inhibition and tumor regression can be accomplished by combinations of heparin or heparin fragments with cortisone. Oral heparin was also effective in combination with cortisone. We now show that a single oral dose of (/sup 35/S)heparin or (/sup 3/H)heparin (15,000 units/kg) results in continuous release of radioactive material into the bloodstream for at least 12 hr. This is associated with the presence of anti-factor Xa activity at a level of approximately equal to 0.1 unit/ml. The radioactive material is identified as oligo-, di-, and monosaccharides by its behavior in chromatographic systems, its possession of anti-factor Xa activity, and the effect of treatment with bacterial heparinase. The heparin fragments are extensively metabolized to fragments without anti-factor Xa activity that are readily subject to urinary excretion.

• Research Organization: Massachusetts Institute of Technology, Cambridge
• OSTI ID: 5578508
• Journal Information: Proc. Natl. Acad. Sci. U.S.A.; (United States), Journal Name: Proc. Natl. Acad. Sci. U.S.A.; (United States) Vol. 9; ISSN PNASA
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
AMINES
ANIMALS
ANTICOAGULANTS
CARBOHYDRATES
CARDIOVASCULAR DISEASES
CHEMOTHERAPY
DISACCHARIDES
DISEASES
DRUGS
HEMATOLOGIC AGENTS
HEPARIN
LABELLED COMPOUNDS
MAMMALS
METABOLISM
MONOSACCHARIDES
MUCOPOLYSACCHARIDES
NEOPLASMS
OLIGOSACCHARIDES
ORAL ADMINISTRATION
ORGANIC COMPOUNDS
ORGANIC SULFUR COMPOUNDS
POLYSACCHARIDES
RATS
RODENTS
SACCHARIDES
THERAPY
THROMBOSIS
TRITIUM COMPOUNDS
VASCULAR DISEASES
VERTEBRATES