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Titolo:
Receptor mediated endocytosis and cytotoxicity of transferrin-mitomycin c conjugate in the HepG2 cell and primary cultured rat hepatocyte
Autore:
Tanaka, T; Fujishima, Y; Kaneo, Y;
Indirizzi:
Fukuyama Univ, Fac Pharm & Pharmaceut Sci, Dept Biopharmaceut, Fukuyama, Hiroshima 7290292, Japan Fukuyama Univ Fukuyama Hiroshima Japan 7290292 , Hiroshima 7290292, Japan
Titolo Testata:
BIOLOGICAL & PHARMACEUTICAL BULLETIN
fascicolo: 3, volume: 24, anno: 2001,
pagine: 268 - 273
SICI:
0918-6158(200103)24:3<268:RMEACO>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
DRUG TARGETING SYSTEM; IN-VIVO DISTRIBUTION; INTERNALIZATION; DISPOSITION; ADRIAMYCIN; PRODRUGS; TISSUES; BINDING; K562;
Keywords:
mitomycin C; transferrin; conjugate; endocytosis; HepG2 cell; antitumor effect;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Tanaka, T Fukuyama Univ, Fac Pharm & Pharmaceut Sci, Dept Biopharmaceut, Fukuyama, Hiroshima 7290292, Japan Fukuyama Univ Fukuyama Hiroshima Japan 7290292 a 7290292, Japan
Citazione:
T. Tanaka et al., "Receptor mediated endocytosis and cytotoxicity of transferrin-mitomycin c conjugate in the HepG2 cell and primary cultured rat hepatocyte", BIOL PHAR B, 24(3), 2001, pp. 268-273

Abstract

Intracellular disposition and cytotoxicity of macromolecular conjugate of mitomycin C (MMC) with transferrin (TF) were examined in the human hepatomacell line HepG2 cell and normal cultured rat hepatocyte. The conjugate (TF-MMC) was specifically bound to the HepG2 cell as well as TF, The number ofthe binding site and the association constant of TF-MMC in the HepG2 cell were 396000 +/- 31000 molecules/cell and 3.24 x 10(7) +/- 0.58 x 10(7) M-1,respectively No difference in the binding parameters of TF-MMC and TF can be detected in the HepG2 tell. The association constant for the TF receptorwas almost identical between HepG2 cell and hepatocyte, however, the numbers of the binding site of TF-MMC and TF in the HepG2 cell were from 40-times to 50-times greater than those in the hepatocyte, Furthermore, TF-MMC wasinternalized into the HepG2 cell and the hepatocyte as well as TF The rates of internalization of TF-MMC and TF into the HepG2 cell were nearly identical to those into the hepatocyte. However, the levels of the internalization into the HepG2 cell were remarkably higher than those into the hepatocyte because the number of receptors in the HepG2 cell was larger than that inthe hepatocyte, and the rate of release from the HepG2 cell was slower than that from the hepatocyte, TF-MMC inhibited the growth of the HepG2 cells. The 50% growth inhibition (GI(50)) of TF-MMC against the HepG2 cell was 0.9 mug MMC/ml, which was a little higher than that of MMC (GI(50) = 0,5 mug/ml). These results indicated that the TF-MMC might be useful for delivery of MMC to the HepG2 cell.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/12/20 alle ore 00:59:01