The use of protein as a carrier of methotrexate for experimental cancer chemotherapy. III. Human serum albumin-methotrexate derivative, its preparation and basic testing.

The preparation and a more detailed characterization of human serum albumin-methotrexate derivative (HSA-MTX) is described. The synthesis of the derivative was performed by means of 1-ethyl-3-(3'-dimethylaminopropyl)-carbodiimide (in methoiodide form) (WSC). Results of many experiments showed that, on the average, about 26 molecules of methotrexate (MTX) were coupled to one molecule of human serum albumin (HSA).

Organ distribution of fibrinogen-bound methotrexate in mice with Gardner lymphosarcoma.

The distribution of fibrinogen-bound 3H methotrexate was investigated in Gardner lymphosarcoma bearing mice. 3H labeled methotrexate (3H MTX) was covalently bound by means of aminopropyl carbodiimide to bovine and mouse fibrinogen (FBG). The preparations as well as the free 3H MTX were applied i.

The use of protein as a carrier of methotrexate for experimental cancer chemotherapy. II. Chemotherapy of Gardner lymphosarcoma with pea seed lectin-methotrexate derivative.

It was demonstrated that the tumorigenicity of tumor cells preincubated in low concentration of free methotrexate (MTX) has not been changed. On the other hand the preincubation of these cells with pea seed lectin (PL), MTX and PL mixture and especially pea seed lectin-methotrexate derivative (PL-MTX) influenced markedly the tumor cells tumorigenicity. The chemotherapy of Gardner lymphosarcoma (LSG) bearing mice with PL-MTX derivative was performed.