Preliminary fluorimetric screening of fourteen palladium complexes as potential antitumor agents.
Making use of the fact that the combination of a drug substance with DNA may inhibit the duplication, synthesis and proliferation of DNA and the consistency of the in vivo and in vitro interactions, the authors worked out a preliminary screening method for testing complex agents as potential antitumor drugs using ethidium bromide as a fluorescence probe. In this report, the method was applied for in vitro testing fourteen synthesized palladium(II)/phenanthroline/amino acid/chloride complexes as potential non-platinum antitumor agents. The fluorimetric screening method was compared with methylene blue tube test and trypan blue dye exclusion assay. All three methods gave agreeable results. Among the complexes tested, [Pd(phen)(lys)]Cl, [Pd(phen)(arg)]Cl and [Pd(phen)(pro)]Cl showed antineoplastic ratios for animal tumor S-180 56%, 50% and 48%, respectively, in accordance with the order of their binding constants with DNA, 7.96 x 10(6), 4.52 x 10(6) and 1.0 x 10(6), respectively. The test results show that fluorimetric method is simple, cheap and rapid, suitable for preliminary screening of antitumor complexes.
Lin
H X
HX
Department of Chemistry and Chemical Engineering, Hunan University, Changsha, PRC.
Li
Z L
ZL
Dai
G L
GL
Bi
Q S
QS
Yu
R Q
RQ
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D004354:Drug Screening Assays, Antitumor; D005260:Female; D008297:Male; D051379:Mice; D009368:Neoplasm Transplantation; D009942:Organometallic Compounds / Q000494:pharmacology* / Q000627:therapeutic use; D010165:Palladium / Q000494:pharmacology* / Q000627:therapeutic use; D012510:Sarcoma 180 / Q000188:drug therapy
D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D010165:Palladium