METABOLISM AND BIOLOGICAL ACTIVITY OF BENZENESULFONYLTHIAMINE DISULFIDE

概要

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1. Urinary excretion of thiamine in 24 hours after intraperitoneal injection of benzenesulfonylthiamine disulfide (BSTDS), equivalent to 5mg of thiamine-HCl, to rats was about 3 per cent (as thiamine or benzenesulfonyl-thiamine). It is markedly low as compared with thiamine disulfide or thiamine propyl disulfide, suggesting the conversion of BSTDS to thiamine anhydride (TA) in the body. BSTDS was degraded nonenzymatically by rat liver homogenate and it was converted to TA by the reaction with thioglycolate. Its low urinary excretion is possibly due to the conversion of BSTDS to thiamne anhydride. However, thiamine anhydride or its sulfoxide could not be demonstrated as the urinary metabolite.2. The thiamine activity of BSTDS was studied in rats by determining the increase of the body weight. Daily administration of BSTDS equivalent to 100μg of thiamine showed a significant increase but its administration equivalent to 10μg of thiamine was inffective. Oral administration resulted in more rapid rise of body weight than after intraperitoneal injection.
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