The responses to antifolates of Toxoplasma gondii were investigated by measuring the dihydrofolate reductase (DHFR) activity, quantity of DHFR mRNA, and single-strand conformational polymorphism (SSCP) pattern. Pyrimethamine (PYM) and methotrexate (MTX) were tested as antifolates. When T. gondii was treated with PYM, the viability was decreased by the increasing concentration of PYM, DHFR activity tended to increase as the passage proceeded, and the quantity of mRNA expressed was also increased according to passages. The viability of T. gondii was decreased by the increasing concentration of MTX, but it was maintained over 40% up to 100 microM MTX. DHFR activity was 77.4% in the 1st passage (1 microM). 82.2% in the 4th passage (10 microM), and 141.3% in the 7th passage (100 microM). But no changes were detected in SSCP pattern of T. gondii exposed to PYM and MTX, both. These results suggested that the response of T. gondii to PYM was regulated by transcriptional level and that, in MTX, the viability of T. gondii was derived from increasing DHFR activity.
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http://dx.doi.org/10.3347/kjp.1998.36.3.191 | DOI Listing |
Eur J Med Chem
February 2025
Natural and Medical Sciences Research Center, University of Nizwa, P.O. Box 33, 616, Nizwa, Oman. Electronic address:
In this present work, we describe the syntheses of a new series of 32 1H-indole-based-meldrum linked 1H-1,2,3-triazole derivatives (2-13, 15a-15f, 16a-16f, 17a-17f and 19a, 19b, 20a), which constitute a new class of 1H-1,2,3-triazoles. Compounds 15a-15f, 16a-16f, 17a-17f have been prepared by employing "click" reactions between substituted 1H-indole-based meldrum alkynes (11, 12 and 13) and substituted aromatic azides (14a-14f) in the presence of copper iodide (CuI) and Hünig's base. Then, the synthesis of compounds 19, 20 through decomposition of meldrum moiety.
View Article and Find Full Text PDFFront Pharmacol
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Dhaka, Dhaka, Bangladesh.
Background: Schott and Hook.f. are two commonly found vegetable species of the genus , found mainly in the Asian region.
View Article and Find Full Text PDFBMC Chem
December 2024
Laboratory of Preservation Technology and Enzyme Inhibition Studies, Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001, India.
Dihydrofolate reductase (DHFR) is an enzyme that plays a crucial role in folate metabolism, which is essential for cell growth and division. DHFR has been identified as a molecular target for numerous diseases due to its significance in various biological processes. DHFR inhibitors can disrupt folate metabolism by inhibiting DHFR, leading to the inhibition of cell growth.
View Article and Find Full Text PDFJ Inflamm Res
December 2024
Central Laboratory of The Lishui Hospital of Wenzhou Medical University, The First Affiliated Hospital of Lishui University, Lishui People's Hospital, Lishui, Zhejiang, 323000, People's Republic of China.
Background: Throughout history, plants have played a crucial role in advancing medicinal treatments by providing a diverse range of compounds for the development of innovative therapies. L. a tropical herb of the Cannaceae family, also known as Indian shot, has a rich history of traditional use in treating ailments like inflammation, malaria, dysentery, fever, dropsy, and diarrhea.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
Department of Physics and Meteorology, School of Sciences, Sao Paulo State University (UNESP), Bauru, Sao Paulo 17033-360, Brazil.
The presence of toxic dyes in industrial waste dramatically diminishes the beneficial effects of remediation efforts. To overcome the hazardous impacts of dyes on biodiversity and environment, we integrated polymers into nanoparticles to substantially enhance their functionality and performance. 2 and 4 wt% of chitosan (CS) and 3 wt% of polyacrylic acid (PAA) doped cadmium selenide (CdSe) nanostructures (NSs) were prepared by co-precipitation approach.
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