[New conjugates of antitumor antibiotic doxorubicin with water-soluble galactomannan: synthesis and biological activity].
New water-soluble conjugates in the form of Schiff bases (DGM-1 and DGM-2) were prepared by the interaction of water-soluble periodate-oxidized galactomannan with doxorubicin or N-(L-lysyl)doxorubicin, respectively. The water-soluble galactomannan (DAVANAT a commercial product of Pro-Pharmaceuticals company) was obtained by partial acidic hydrolysis of high-molecular-mass galactomannan from Cyamopsis tetragonoloba (guar gum) seeds. The conjugate stability was studied in aqueous solutions. The DGM-1 antiproliferative activity was comparable with that of doxorubicin on three models: cell lines of murine melanoma B 16-F1, human breast cancer MCF-7 (HTB-22), and human colon cancer HT-29 (HTB-38). DGM-2 was poorly active in all the three tests. DGM- 1 can thus be regarded as a high-molecular-mass depot form of doxorubicin.
Teviashova
A N
AN
Olsuf'eva
E N
EN
Preobrazhenskaia
M N
MN
Klesov
A A
AA
Zomer
E
E
Platt
D
D
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004317:Doxorubicin / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D005690:Galactose / Q000031:analogs & derivatives; D006801:Humans; D008351:Mannans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051379:Mice; D012995:Solubility; D014867:Water / Q000737:chemistry
D000903:Antibiotics, Antineoplastic; C519224:DGM-1 conjugate; C519226:DGM-2 conjugate; D008351:Mannans; D014867:Water; C012990:galactomannan; D004317:Doxorubicin; D005690:Galactose