title: Cytotoxicity of hydrophylic silver carboxylato complexes.
abstract: BACKGROUND
  Gold(I) and platinum(II) d(10) and d(8) electronic complexes such as (Au(PPh(2)CH(2)CH(2)PPh(2))(2))Cl and cisplatin, ((H(3)N)(2)PtCl(2)), possess strong antineoplastic activities. Almost no information is available regarding the anticancer activity of isoelectronic silver(I) d(10) complexes. This study examined the cytotoxicity of stable water-soluble silver(I) carboxylates. The results were related to the cytotoxicity of cisplatin and (Au(PPh(2)CH(2)CH(2)PPh(2))(2))Cl.
  
  
  METHODS
  The silver carboxylates (AgO(2)CCH(2)OCH(3)), 1, (AgO(2)C-CH(2)OCH(2)CH(2)OCH(3)), 2, and (AgO(2)CCH(2)OCH(2)CH(2)OCH(2)CH(2)OCH(3)), 3, were investigated. Cytotoxicity tests were performed on the HeLa (human cervix epitheloid) cancer cell line, resting lymphocytes and PHA (phytohaemagglutinin)-stimulated lymphocyte cultures. Cell survival was measured by means of the colorometric 3-(4,5-dimethylthiazol-2-yl)-diphenyltetrazolium bromide (MTT) assay.
  
  
  RESULTS
  The IC(50) (50% cell growth inhibition) values of 1-3 in the HeLa cells varied between 2.6 and 6.1 μmol dm(-3) with being 1 the most cytotoxic silver complex. Drug activity was inversely proportional to the length of the carboxylato chain length. Complexes 1-3 were 3-5 times more cytotoxic against the HeLa cancer cells than against the PHA stimulated lymphocyte cultures.
  
  
  CONCLUSIONS
  A drug activity-structure relationship exists in that short-chain silver carboxylates are more cytotoxic than long-chain silver carboxylates, but silver d(10) complexes are one order of magnitude less cytotoxic than platinum(II) d(8) or gold(I) d(10) complexes.
authors.affiliation: Department of Chemistry, University of the Free State, Bloemfontein, Republic of South Africa.
authors.forename: Eleanor
authors.initials: E
authors.lastname: Fourie
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Erasmus
authors.forename: Jannie C
authors.initials: JC
authors.lastname: Swarts
authors.forename: André
authors.initials: A
authors.lastname: Tuchscherer
authors.forename: Alexander
authors.initials: A
authors.lastname: Jakob
authors.forename: Heinrich
authors.initials: H
authors.lastname: Lang
authors.forename: Gisela K
authors.initials: GK
authors.lastname: Joone
authors.forename: Constance E J
authors.initials: CE
authors.lastname: Van Rensburg
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D048708:Cell Growth Processes / Q000187:drug effects; D002945:Cisplatin / Q000737:chemistry / Q000494:pharmacology; D056831:Coordination Complexes / Q000737:chemistry* / Q000494:pharmacology*; D005026:Ethylene Glycols / Q000737:chemistry / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D012834:Silver / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D005026:Ethylene Glycols; D012834:Silver; D002945:Cisplatin