title: [Cytotoxic effect of palladium (II) inclusion compounds in beta-cyclodextrin].
abstract: BACKGROUND
  Thiosemicarbazones and palladium (II) complexes have antineoplastic activities with mild side effects, for which they are considered new alternative antineoplastic drugs. However, the IC50 ranges of these complexes vary due to differences in their structure and solubility and their sensitivities for various cellular targets. Beta-cyclodextrin is an additive used to improve the solubility and stability of various drugs for therapeutic use, but the combination of beta-cyclodextrin with palladium (II) complexes and thiosemicarbazones has not been tested yet.
  
  
  OBJECTIVE
  To study the cytotoxic effect of palladium (II) inclusion complexes in beta-cyclodextrin.
  
  
  METHODS
  We tested the cytotoxic activity of palladium complexes combined with beta-cyclodextrin in the breast cancer cell line MCF-7 using a sulforhodamine B assay.
  
  
  RESULTS
  We tested the antiproliferative activity of palladium (II) complexes with and without the ligands MePhPzTSC and Ph2PzTSC and with and without beta-cyclodextrin in MCF-7 cells and compared them to that of cisplatin. All combinations showed antiproliferative activity; however, the activity was greater for the combinations that included beta-cyclodextrin: ([Pd (MePhPzTSC) 2] • ß-CD and [Pd (Ph2PzTSC) 2] • ß-CD), at concentrations of 0.14 and 0.49 μM, respectively. The IC50 for this complex was 5-fold lower than that of the ligand-free combinations (1.4 and 2.9 μM, respectively). The IC50 for free palladium (II) complex was 0.571.24 μM and that for cisplatin was 6.87 μM.
  
  
  CONCLUSIONS
  Beta-cyclodextrin significantly enhanced the cytotoxic activities of palladium (II) complexes and thiosemicarbazones probably by improving their solubility and bioavailability. The addition of beta-cyclodextrin is a possible strategy for designing new anticancer drugs.
authors.affiliation: Grupo de Investigación en Biología Molecular y Genética, Universidad de Pamplona, Pamplona, Colombia. najame3@hotmail.com.
authors.forename: Nancy
authors.initials: N
authors.lastname: Jaimes
authors.forename: Siham
authors.initials: S
authors.lastname: Salmen
authors.forename: Melisa Carolina
authors.initials: MC
authors.lastname: Colmenares
authors.forename: Ana Esperanza
authors.initials: AE
authors.lastname: Burgos
authors.forename: Lenka
authors.initials: L
authors.lastname: Tamayo
authors.forename: Rosa Virginia
authors.initials: RV
authors.lastname: Mendoza
authors.forename: Astrid
authors.initials: A
authors.lastname: Cantor
mesh_terms: D000277:Adjuvants, Pharmaceutic / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001682:Biological Availability; D002455:Cell Division / Q000187:drug effects; D002945:Cisplatin / Q000494:pharmacology; D003603:Cytotoxins / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D004357:Drug Synergism; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D007963:Leukocytes, Mononuclear / Q000187:drug effects; D061986:MCF-7 Cells; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000737:chemistry / Q000494:pharmacology*; D010165:Palladium / Q000737:chemistry / Q000494:pharmacology*; D012995:Solubility; D047392:beta-Cyclodextrins / Q000494:pharmacology*
chemical_list: D000277:Adjuvants, Pharmaceutic; D000970:Antineoplastic Agents; D003603:Cytotoxins; D009942:Organometallic Compounds; D047392:beta-Cyclodextrins; D010165:Palladium; C031215:betadex; D002945:Cisplatin
keywords: Palladium; beta-cyclodextrins; breast neoplasm/therapy.; thiosemicarbazone