The effect of thiamine and oxythiamine preparations on the activities of vitamin B1-dependent enzymes in the body of white mice was studied. It was found that the cellulose oxythiamine derivative was similar to the initial compound in the character and intensity of its antivitamin action. It was also shown that the cellulose thiamine derivative had a prolonged effect in the body, which was manifested in a slower increase in the activities of transketolase, pyruvate dehydrogenase and in the amount of thiamine diphosphate in tissues of vitamin B1-deficient animals, as compared to the effect of thiamine.
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Antimicrob Agents Chemother
December 2024
Research School of Biology, The Australian National University, Canberra, Australia.
Thiamine is metabolized into thiamine pyrophosphate (TPP), an essential enzyme cofactor. Previous work has shown that oxythiamine, a thiamine analog, is metabolized by thiamine pyrophosphokinase (TPK) into oxythiamine pyrophosphate within the malaria parasite and then inhibits TPP-dependent enzymes, killing the parasite and . To identify a more potent antiplasmodial thiamine analog, 11 commercially available compounds were tested against and .
View Article and Find Full Text PDFFront Med (Lausanne)
October 2024
CURANOSTICUM Wiesbaden-Frankfurt, Center for Advanced Radiomolecular Precision Oncology, Wiesbaden, Germany.
Herein we report, for the first time, the therapeutic response of a prostate cancer patient with the thiamine antagonist benfo-oxythiamine (B-OT) added to prostate-specific membrane antigen (PSMA)-targeted radioligand therapy (PRLT). The patient was initially diagnosed as pT3b pN0 (0/7) M0 L0 V0 R0 G3, Gleason score 5 + 5 = 10, with an initial prostate-specific antigen (PSA) level of 4.05 ng/ml.
View Article and Find Full Text PDFACS Omega
October 2024
Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, U.K.
Thiamine (vitamin B1) is essential for energy metabolism, and interruption of its utilization pathways is linked to various disease states. Thiamine pyrophosphate (TPP, the bioactive form of ) functions as a coenzyme of a variety of enzymes. To understand the role of vitamin B1 in these diseases, a chemical approach is to use coenzyme analogues to compete with TPP for the enzyme active site, which abolishes the coenzyme function.
View Article and Find Full Text PDFInt J Mol Sci
April 2024
Department of Clinical Genetics, Medical University of Białystok, Waszyngtona 13, 15-089 Bialystok, Poland.
It is important to search for cytostatic compounds in order to fight cancer. One of them could be 2'-methylthiamine, which is a thiamine antimetabolite with an additional methyl group at the C-2 carbon of thiazole. So far, the cytostatic potential of 2'-methylthiamine has not been studied.
View Article and Find Full Text PDFInt J Mol Sci
January 2024
Belozersky Institute of Physicochemical Biology, Lomonosov Moscow State University, 119234 Moscow, Russia.
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