PMID- 12109048 OWN - NLM STAT- MEDLINE DCOM- 20020729 LR - 20141120 IS - 0004-4172 (Print) IS - 0004-4172 (Linking) VI - 52 IP - 6 DP - 2002 TI - Effects of gold-chloroquine complexes on respiratory burst of polymorphonuclear leukocytes. PG - 468-74 AB - The effects of gold-chloroquine derivatives with the formula [Au(PR3)(CQ)]PF6 (where R = Ph (1), Et or Me) on the superoxide anion production by human neutrophils (PMNs, polymorphonuclear cells) were investigated. When these complexes (0.1-3 mumol/l) were added to PMNs prior to the activators formyl-methionyl-leucyl-phenylalanine (fMLP) or phorbol myristate acetate (PMA), they inhibited isoluminol-horseradish peroxidase-dependent chemiluminescence (CLisol). The inhibition was a direct result of effects on PMNs since chemiluminescence in the cell-free system (horseradish peroxidase-hydrogen peroxidase-isoluminol) was not affected. The above mentioned concentrations of the complexes did not show in vitro toxicity on the cells. On the other hand, when 1 mumol/l of complex 1 was added to cells after stimulation, the chemiluminescence of PMNs stimulated by PMA was inhibited, but not the chemiluminescence stimulated by fMLP. The gold-chloroquine binding was essential for the referred activity as chemiluminescence was not influenced by the precursors chloroquine (CAS 54-05-7) and AuCl(PPh3). Furthermore, the extent of inhibition of chemiluminescence in PMNs activated by PMA did not increase with the duration of preincubation in presence of 1 mumol/l of 1. Extensive washing of cells after preincubation with 1 mumol/l of 1 reversed the aforementioned inhibition. All these results show that the gold-chloroquine binding can lead to compounds with specific properties that could make them useful in the treatment of some inflammatory diseases. FAU - Navarro, Maribel AU - Navarro M AD - Chemistry Center, Instituto Venezolano de Investigaciones Cientificas (IVIC), Caracas, Venezuela. mnavarro@ivic.ve FAU - Vasquez, Flor AU - Vasquez F FAU - Velasquez, Mait AU - Velasquez M FAU - Medina, Rafael AU - Medina R FAU - Reggio, Ronald AU - Reggio R FAU - Fraile, German AU - Fraile G LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Germany TA - Arzneimittelforschung JT - Arzneimittel-Forschung JID - 0372660 RN - 11062-77-4 (Superoxides) RN - 59880-97-6 (N-Formylmethionine Leucyl-Phenylalanine) RN - 7440-57-5 (Gold) RN - 886U3H6UFF (Chloroquine) RN - 8L70Q75FXE (Adenosine Triphosphate) RN - NI40JAQ945 (Tetradecanoylphorbol Acetate) SB - IM MH - Adenosine Triphosphate/metabolism MH - Cell Survival/drug effects MH - Cell-Free System MH - Chloroquine/*pharmacology MH - Dose-Response Relationship, Drug MH - Gold/*pharmacology MH - Humans MH - In Vitro Techniques MH - Luminescent Measurements MH - N-Formylmethionine Leucyl-Phenylalanine/pharmacology MH - Neutrophils/drug effects/*metabolism MH - Respiratory Burst/*drug effects MH - Superoxides/metabolism MH - Tetradecanoylphorbol Acetate/pharmacology EDAT- 2002/07/12 10:00 MHDA- 2002/07/30 10:01 CRDT- 2002/07/12 10:00 PHST- 2002/07/12 10:00 [pubmed] PHST- 2002/07/30 10:01 [medline] PHST- 2002/07/12 10:00 [entrez] AID - 10.1055/s-0031-1299916 [doi] PST - ppublish SO - Arzneimittelforschung. 2002;52(6):468-74. doi: 10.1055/s-0031-1299916.