Cellular antiproliferative action exerted by auranofin.
Auranofin (AF) is a new orally absorbed coordinated gold compound currently undergoing Phase I studies for its use in the treatment of rheumatoid arthritis. Our investigations with RAJI lymphoma, HeLa carcinoma, and EBV-transformed cells indicate AF exerts an inhibitory effect on DNA, RNA, and protein synthesis as assessed by 3H-thymidine, 3H-uridine, and 3H-leucine uptake, respectively. A rapid and persistent dose dependent inhibition of 3H-thymidine uptake was observed at gold concentrations of 50-100 microgram/dl while all parameters were inhibited after a 24 hr exposure to 100 microgram/dl. Reductions in viability and surface morphological changes were also observed. These results suggest AF exerts a significant inhibitory effect on essential biological processes and functions.
D006051:Aurothioglucose / Q000031:analogs & derivatives* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D002462:Cell Membrane / Q000378:metabolism; D002472:Cell Transformation, Viral / Q000187:drug effects; D004247:DNA / Q000096:biosynthesis; D006046:Gold / Q000031:analogs & derivatives*; D004854:Herpesvirus 4, Human; D006801:Humans; D008214:Lymphocytes / Q000378:metabolism; D010720:Phosphines / Q000494:pharmacology; D014176:Protein Biosynthesis; D012313:RNA / Q000096:biosynthesis; D013936:Thymidine / Q000378:metabolism
D010720:Phosphines; D006051:Aurothioglucose; D012313:RNA; D006046:Gold; D004247:DNA; D013936:Thymidine