Document Detail

Sensitization of multidrug-resistant mouse ascites HD33 and Chinese hamster ovary CHRC5S3 cells by a photoreactive vinblastine derivative, NAPAVIN.
MedLine Citation:
PMID:  2257016     Owner:  NLM     Status:  MEDLINE    
We have synthesized a new photoreactive vinblastine derivative, 3-[[[2-amino(4-azido-2-nitrophenyl)ethyl]amino] carbonyl]-O4-deacetyl-3-de-(methoxycarbonyl)-vincaleukoblastine (NAPAVIN), which absorbs light at around 450 nm. We report here its effects in vitro on multidrug-resistant mouse HD33 Ehrlich-Lettré ascites cells, on Chinese hamster ovary CHRC5S3 cells, on the corresponding drug-sensitive cells, on chemosensitive rat TMA1 mammary carcinoma, and on human SW48 colon carcinoma cells. Cells were incubated with the drug prior to activation by laser light at 457 nm. In Vinca alkaloid-sensitive cells, the short-term effects (30 to 72 h after treatment) of NAPAVIN with and without irradiation on cell proliferation are comparable to those of vinblastine. In drug-resistant cells, NAPAVIN without irradiation reduces the 50% inhibitory concentration 2- to 9-fold, compared with vinblastine. Upon irradiation with an argon laser at 457 nm, the concentration causing 50% inhibition of cell proliferation is further decreased to a total of 9- to 33-fold. Long-term effects (up to 6 wk after treatment) are seen in both sensitive and resistant cells. A single dose of the photoactivated drug causes a 6- to 9-fold larger delay (5 wk) in proliferation, compared with an equal dose of vinblastine.
G Nasioulas; C Granzow; M Stöhr; H Ponstingl
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Cancer research     Volume:  50     ISSN:  0008-5472     ISO Abbreviation:  Cancer Res.     Publication Date:  1990 Jan 
Date Detail:
Created Date:  1990-02-13     Completed Date:  1990-02-13     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  2984705R     Medline TA:  Cancer Res     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  403-8     Citation Subset:  IM    
Project Molecular Biology of Mitosis, German Cancer Research Center, Heidelberg.
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MeSH Terms
Cell Division / drug effects
Cells, Cultured
Drug Resistance
Mitosis / drug effects
Tubulin / metabolism
Vinblastine / analogs & derivatives*,  pharmacology
Reg. No./Substance:
0/Tubulin; 126443-96-7/NAPAVIN; 865-21-4/Vinblastine

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

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