Document Detail


Bovine serum albumin-doxorubicin conjugate overcomes multidrug resistance in a rat hepatoma.
MedLine Citation:
PMID:  8364920     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A bovine serum albumin-conjugated doxorubicin via the glutaraldehyde bridge (BSA-DXR conjugate) showed potent dose-dependent inhibition of cell growth against daunorubicin-resistant AH66 (AH66DR) cells as well as parental AH66 (AH66P) cells in vitro as compared to treatment with DXR or BSA-glutaraldehyde conjugate without DXR (BSA-GA). In the culture of AH66DR with BSA-DXR conjugate, drug accumulation in the AH66DR cells increased as a function of time up to 24 h reaching approximately the same drug level as AH66P cells treated with DXR. The intracellular accumulation of the BSA-DXR conjugate was inhibited by the addition of ammonium chloride, while that of DXR alone was not inhibited. Intracellular DXR was effluxed rapidly from AH66DR cells, but BSA-DXR conjugate or pharmacologically active DXR adduct remained in the cells at a relatively high concentration over a 36-h time period. The life-prolonging effect of the conjugate was assessed using rats inoculated i.p. with AH66P or AH66DR. The rats were treated with the BSA-DXR conjugate, DXR, a mixture of DXR with BSA, or BSA-GA by either the i.p. or i.v. route. Treatment with DXR had no significant surviving effect as compared to that with saline in AH66P-bearing rats. By contrast, BSA-DXR conjugate showed a significant life-prolonging effect as compared with DXR alone in the same degree both in AH66P- and AH66DR-bearing rats. BSA-GA did not show any toxicity in vivo as well as in vitro. These results indicate that the BSA-DXR conjugate allows DXR to escape from the multidrug resistance mechanism.
Authors:
K Ohkawa; T Hatano; K Yamada; K Joh; K Takada; Y Tsukada; M Matsuda
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Cancer research     Volume:  53     ISSN:  0008-5472     ISO Abbreviation:  Cancer Res.     Publication Date:  1993 Sep 
Date Detail:
Created Date:  1993-10-01     Completed Date:  1993-10-01     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  2984705R     Medline TA:  Cancer Res     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  4238-42     Citation Subset:  IM    
Affiliation:
Department of Biochemistry, Jikei University School of Medicine, Tokyo, Japan.
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MeSH Terms
Descriptor/Qualifier:
Animals
Doxorubicin / metabolism,  pharmacology*
Drug Resistance*
Liver Neoplasms, Experimental / drug therapy*,  metabolism,  pathology
Male
Rats
Serum Albumin, Bovine / metabolism,  pharmacology*
Tumor Cells, Cultured
Chemical
Reg. No./Substance:
0/Serum Albumin, Bovine; 0/doxorubicin-BSA conjugate; 23214-92-8/Doxorubicin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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