Source:http://linkedlifedata.com/resource/pubmed/id/11741483
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
26
|
pubmed:dateCreated |
2001-12-19
|
pubmed:abstractText |
Mouse sarcoma 180 cell with a 25-fold higher cisplatin (CDDP) resistance, termed S-180cisR, is newly established. S-180cisR cells grow quite slowly in the presence of CDDP with high concentration. This may show that S-180cisR cells modulate the cell cycle to acquire CDDP resistance. P-Glycoprotein is selectively expressed on the surface of S-180cisR, which is not on CDDP-sensitive S-180 parent cells. In an experiment using an inhibitor (verapamil) of P-glycoprotein, cytotoxicity of CDDP against S-180cisR is significantly increased (viz., IC(50) value is decreased) and accumulation of CDDP in S-180cisR cells is also increased. These results indicate that enhanced pumping-out of CDDP by P-glycoprotein should be one of the reasons for the CDDP resistance of S-180cisR. A platinum(II) complex with a cyclometalated 2-phenylpyridine ligand and a nonchelated one (complex 5) is synthesized, and its structure is determined by X-ray structural analysis. Complex 5 has a cyctotoxicity against S-180cisR higher than that of CDDP and its derivatives with 2- or 3-substituted pyridine ligands (complexes 2-4, 6, 7). Complex 5 is incorporated in S-180cisR to an enormously greater extent than CDDP; that is, the ratio of accumulated platinum amount after 3 h is 61.9. In S-180 parent cells, on the other hand, the ratio remains 8.1. This high accumulation of complex 5 into S-180cisR must account for the higher activity of complex 5 against S-180cisR compared to CDDP.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/2-phenylpyridine,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Cisplatin,
http://linkedlifedata.com/resource/pubmed/chemical/Organoplatinum Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/P-Glycoprotein,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Verapamil
|
pubmed:status |
MEDLINE
|
pubmed:month |
Dec
|
pubmed:issn |
0022-2623
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
20
|
pubmed:volume |
44
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
4661-7
|
pubmed:dateRevised |
2003-11-14
|
pubmed:meshHeading |
pubmed-meshheading:11741483-Animals,
pubmed-meshheading:11741483-Antineoplastic Agents,
pubmed-meshheading:11741483-Cell Division,
pubmed-meshheading:11741483-Cisplatin,
pubmed-meshheading:11741483-Crystallography, X-Ray,
pubmed-meshheading:11741483-Drug Resistance, Neoplasm,
pubmed-meshheading:11741483-Drug Screening Assays, Antitumor,
pubmed-meshheading:11741483-Flow Cytometry,
pubmed-meshheading:11741483-Mice,
pubmed-meshheading:11741483-Organoplatinum Compounds,
pubmed-meshheading:11741483-P-Glycoprotein,
pubmed-meshheading:11741483-Pyridines,
pubmed-meshheading:11741483-Sarcoma,
pubmed-meshheading:11741483-Tumor Cells, Cultured,
pubmed-meshheading:11741483-Verapamil
|
pubmed:year |
2001
|
pubmed:articleTitle |
Mononuclear platinum(II) complex with 2-phenylpyridine ligands showing high cytotoxicity against mouse sarcoma 180 cells acquiring high cisplatin resistance.
|
pubmed:affiliation |
Institute of Molecular and Cell Biology, Tsukuba Center, National Institute of Advanced Industrial Science and Technology (AIST), AIST Tsukuba Central 6, 1-1-1 Higashi, Tsukuba, Ibaraki 305-8566, Japan.
|
pubmed:publicationType |
Journal Article
|