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Leishmania donovani: Oral therapy with glycosyl 1,4-dihydropyridine analogue showing apoptosis like phenotypes targeting pteridine reductase 1 in intracellular amastigotes |
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| Authors: | Jaspreet Kaur Biswajit Kumar Singh Rama Pati Tripathi Neeloo Singh |
| Institution: | a Drug Target Discovery and Development Division, Central Drug Research Institute, Chattar Manzil Palace, P.O. Box No. 173, CSIR, Lucknow-226001, India b Division of Parasitology, Central Drug Research Institute, Chattar Manzil Palace, P.O. Box No. 173, CSIR, Lucknow-226001, India c Medicinal and Process Chemistry Division, Central Drug Research Institute, Chattar Manzil Palace, P.O. Box No. 173, CSIR, Lucknow-226001, India d Department of Chemistry, D.A.V. (P.G.) College, Dehradun-248001, India |
| Abstract: | Glycosyl 1,4-dihydropyridine analogue (2,6-dimethyl-4-(3-O-benzyl-1,2-O-isopropylidene-β-l-threo pentofuranos-4-yl)-1-phenyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid diethyl ester) synthesized in our laboratory, inhibited Leishmania donovani infection in vitro and in hamsters (Mesocricetus auratus) when administered orally. This analogue is nontoxic, cell-permeable and orally effective. This glycosyl dihydropyridine analogue functioned through arrest of cells in sub-G0/G1-phase, triggering mitochondrial membrane depolarization-mediated programmed cell death of the intracellular amastigotes. |
| Keywords: | Leishmania donovani Dihydropyridine Antileishmanial activity Flow cytometry Cell cycle arrest |
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