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Please use this identifier to cite or link to this item: http://digitalrepository.fccollege.edu.pk/handle/123456789/2268
Title: In Vitro Distribution of Gold in Serum Proteins after Incubation of Sodium Aurothiomalate and Auranofin with Human Blood and its Pharmacological Significance
Authors: Saeed Iqbal, Mohammad
G. Taqi, Syed
Arif, Muhammad
Wasim, Muhammad
Sher, Muhammad
Keywords: Chrysotherapy . Myocricin® . Auranofin . Electrophoresis . Serum proteins . Neutron activation analysis
Issue Date: 5-Feb-2009
Publisher: researchgate.net
Citation: Iqbal, Mohammad & Kazimi, Syed & Arif, Muhammad & Wasim, Mohammad & Sher, Muhammad. (2009). In Vitro Distribution of Gold in Serum Proteins after Incubation of Sodium Aurothiomalate and Auranofin with Human Blood and its Pharmacological Significance. Biological trace element research. 130. 204-9. 10.1007/s12011-009-8330-0.
Abstract: This study presents a comparative drug–protein, in vitro, binding profile of sodium aurothiomalate and auranofin. It was found that about 40% of total protein-bound gold is attached to albumin after incubation of aurothiomalate with whole blood for 24 h and about 29% of it was with α1-globulin and the least amount was found with γ-globulin (6.1%). On the other hand, approximately 84% of the protein-bound auranofin gold attached to globulins of which 51% was found with β-globulin band. It was almost equally distributed among albumin, α2-globulin and γ-globulin, and showed least affinity for α1-globulin. The gold analyses were performed by standardless instrumental neutron activation method duly validated by use of an established atomic absorption method. The results of this study explain to some extent the difference in, in vivo, pharmacokinetics and pharmacodynamics of the two drugs.
Description: Gold compounds have been in use for treatment of rheumatoid arthritis for about 70 years but several questions relating to efficacy and toxicity still remain unanswered. The two main types of gold compounds available in the market are: (1) injectable preparations and (2) an oral preparation. The injectable preparations include sodium aurothiomalate and the only oral preparation available is 5,(1-thio-ß-D-glucopyranose-2,3,4,6-tetraacetato-S)-(triethylphosphine) gold(I) commonly known as auranofin. These are two different chemical entities shown to have different in vivo chemistry and pharmacokinetics [1]. With a weekly 50-mg injection of sodium aurothiomalate, the peak serum gold concentration goes to approximately 7 μg mL−1 6–8 h after the injection and declines to approximately 3 μg mL−1 within 1 week. The initial serum half life is 5.5 days [2, 3]. Most of the intramuscularly injected gold (>95%) is protein bound, which has been reported to be mainly bound to serum albumin [2, 4]. After oral administration of auranofin the serum gold concentrations reach a peak value between 0.2 and 1 μg mL−1 depending on the dose. The plasma half life has been reported as 16–25 days [2, 5, 6] which is 3–5 times longer than that of sodium aurothiomalate, which is most probably because of drug– protein interactions.
URI: http://202.142.177.21/handle/123456789/2268
Appears in Collections:Chemistry Department

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