Experiments to increase the selectivity of tumor chemotherapy by means of in vivo activation of transport forms of cancerostatics by exogenous enzymes.
A significant tumor damaging effect (growth inhibition) on transplanted syngeneic sarcoma in mouse was obtained by means of pH-dependent activation of a transport form of a cancerostatic drug by an enzyme foreign to the organism. This effect was achieved by combined administration of 8-0-(alpha-L-arabinofuranosyl)beta-peltatin-A as a transport form of beta-peltatin-A and the exogenous enzyme alpha-L-arabinofuranosidase from Aspergillus niger and additional increase of the acidity of the tumor by injection of glucose. The combined application of the transport form plus enzyme showed a more favorable effect on selectivity than free peltatin when a quantitative comparison was made between the tumor growth inhibition and the damage to the blood picture.
D000818:Animals; D001089:Arabinose / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000378:metabolism; D001711:Biotransformation; D004359:Drug Therapy, Combination; D005947:Glucose / Q000008:administration & dosage; D006026:Glycoside Hydrolases / Q000008:administration & dosage* / Q000378:metabolism; D006863:Hydrogen-Ion Concentration; D007958:Leukocyte Count; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D011034:Podophyllotoxin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism; D012513:Sarcoma, Experimental / Q000097:blood / Q000188:drug therapy* / Q000378:metabolism
D001089:Arabinose; D006026:Glycoside Hydrolases; C019713:alpha-N-arabinofuranosidase; D005947:Glucose; D011034:Podophyllotoxin