Medicinal chemistry of gold. 1993

G G Graham, and J B Ziegler, and G D Champion
School of Physiology and Pharmacology, University of NSW, Kensington, Australia.

In order to determine the mechanism of action of the anti-arthritic gold complexes, it is necessary to understand the physicochemical properties of these complexes and the exchange of ligands which may occur under physiological conditions, since these factors control the cellular uptake and effects of the gold complexes. Present leads to the forms of gold which may be taken up by cells include the metabolism of the injectable complexes to aurocyanide which is quite a potent inhibitor of the oxidative burst of neutrophils and an even more potent inhibitor of the proliferation of lymphocytes. Further metabolism of aurocyanide to Au(III) complexes is also possible. The orally active complex, auranofin, is active in various cellular systems but the relevance of its in vitro actions to its clinical effects is not known, in part, due to its unknown metabolism. A potentially active derivative of auranofin is a presumed metabolite which can be transferred from plasma to red blood cells. If this metabolite is taken up by red blood cells, then it may be taken up by target cells with consequent pharmacological activity.

UI MeSH Term Description Entries
D009000 Monocytes Large, phagocytic mononuclear leukocytes produced in the vertebrate BONE MARROW and released into the BLOOD; contain a large, oval or somewhat indented nucleus surrounded by voluminous cytoplasm and numerous organelles. Monocyte
D009504 Neutrophils Granular leukocytes having a nucleus with three to five lobes connected by slender threads of chromatin, and cytoplasm containing fine inconspicuous granules and stainable by neutral dyes. LE Cells,Leukocytes, Polymorphonuclear,Polymorphonuclear Leukocytes,Polymorphonuclear Neutrophils,Neutrophil Band Cells,Band Cell, Neutrophil,Cell, LE,LE Cell,Leukocyte, Polymorphonuclear,Neutrophil,Neutrophil Band Cell,Neutrophil, Polymorphonuclear,Polymorphonuclear Leukocyte,Polymorphonuclear Neutrophil
D002627 Chemistry, Physical The study of CHEMICAL PHENOMENA and processes in terms of the underlying PHYSICAL PHENOMENA and processes. Physical Chemistry,Chemistries, Physical,Physical Chemistries
D004304 Dosage Forms Completed forms of the pharmaceutical preparation in which prescribed doses of medication are included. They are designed to resist action by gastric fluids, prevent vomiting and nausea, reduce or alleviate the undesirable taste and smells associated with oral administration, achieve a high concentration of drug at target site, or produce a delayed or long-acting drug effect. Dosage Form,Form, Dosage,Forms, Dosage
D004912 Erythrocytes Red blood cells. Mature erythrocytes are non-nucleated, biconcave disks containing HEMOGLOBIN whose function is to transport OXYGEN. Blood Cells, Red,Blood Corpuscles, Red,Red Blood Cells,Red Blood Corpuscles,Blood Cell, Red,Blood Corpuscle, Red,Erythrocyte,Red Blood Cell,Red Blood Corpuscle
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D050607 Organogold Compounds Organic compounds that contain GOLD as an integral part of the molecule. Some are used as ANTIRHEUMATIC AGENTS. The term chrysotherapy derives from an ancient Greek term for gold. Compounds, Organogold
D055598 Chemical Phenomena The composition, structure, conformation, and properties of atoms and molecules, and their reaction and interaction processes. Chemical Concepts,Chemical Processes,Physical Chemistry Concepts,Physical Chemistry Processes,Physicochemical Concepts,Physicochemical Phenomena,Physicochemical Processes,Chemical Phenomenon,Chemical Process,Physical Chemistry Phenomena,Physical Chemistry Process,Physicochemical Phenomenon,Physicochemical Process,Chemical Concept,Chemistry Process, Physical,Chemistry Processes, Physical,Concept, Chemical,Concept, Physical Chemistry,Concept, Physicochemical,Concepts, Chemical,Concepts, Physical Chemistry,Concepts, Physicochemical,Phenomena, Chemical,Phenomena, Physical Chemistry,Phenomena, Physicochemical,Phenomenon, Chemical,Phenomenon, Physicochemical,Physical Chemistry Concept,Physicochemical Concept,Process, Chemical,Process, Physical Chemistry,Process, Physicochemical,Processes, Chemical,Processes, Physical Chemistry,Processes, Physicochemical
D018501 Antirheumatic Agents Drugs that are used to treat RHEUMATOID ARTHRITIS. Anti-Rheumatic Agent,Anti-Rheumatic Drug,Antirheumatic Agent,Antirheumatic Disease-Modifying Second-Line Drug,Antirheumatic Drug,DMARD,Disease-Modifying Antirheumatic Drug,Disease-Modifying Antirheumatic Drugs,Anti-Rheumatic Agents,Anti-Rheumatic Agents, Non-Steroidal,Anti-Rheumatic Drugs,Antirheumatic Disease-Modifying Second-Line Drugs,Antirheumatic Drugs,Antirheumatic Drugs, Disease-Modifying,Disease-Modifying, Antirheumatic Second-Line Drugs,Agent, Anti-Rheumatic,Agent, Antirheumatic,Anti Rheumatic Agent,Anti Rheumatic Agents,Anti Rheumatic Agents, Non Steroidal,Anti Rheumatic Drug,Anti Rheumatic Drugs,Antirheumatic Disease Modifying Second Line Drug,Antirheumatic Disease Modifying Second Line Drugs,Antirheumatic Drug, Disease-Modifying,Antirheumatic Drugs, Disease Modifying,Disease Modifying Antirheumatic Drug,Disease Modifying Antirheumatic Drugs,Disease Modifying, Antirheumatic Second Line Drugs,Drug, Anti-Rheumatic,Drug, Antirheumatic,Drug, Disease-Modifying Antirheumatic,Non-Steroidal Anti-Rheumatic Agents

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