Document Detail

Leishmania donovani: oral therapy with glycosyl 1,4-dihydropyridine analogue showing apoptosis like phenotypes targeting pteridine reductase 1 in intracellular amastigotes.
MedLine Citation:
PMID:  20219462     Owner:  NLM     Status:  MEDLINE    
Glycosyl 1,4-dihydropyridine analogue (2,6-dimethyl-4-(3-O-benzyl-1,2-O-isopropylidene-beta-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.
Jaspreet Kaur; Nasib Singh; Biswajit Kumar Singh; Anuradha Dube; Rama Pati Tripathi; Prashant Singh; Neeloo Singh
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-02-26
Journal Detail:
Title:  Experimental parasitology     Volume:  125     ISSN:  1090-2449     ISO Abbreviation:  Exp. Parasitol.     Publication Date:  2010 Jul 
Date Detail:
Created Date:  2010-05-10     Completed Date:  2010-05-27     Revised Date:  2012-05-23    
Medline Journal Info:
Nlm Unique ID:  0370713     Medline TA:  Exp Parasitol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  310-4     Citation Subset:  IM    
Drug Target Discovery and Development Division, Central Drug Research Institute, Chattar Manzil Palace, CSIR, Lucknow, India.
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MeSH Terms
Administration, Oral
Antiprotozoal Agents / administration & dosage,  chemistry,  pharmacology*
Apoptosis / drug effects
Cell Cycle / drug effects
Cell Line
Dihydropyridines / administration & dosage,  pharmacology*,  therapeutic use
Flow Cytometry
Glycosides / administration & dosage,  pharmacology*,  therapeutic use
Inhibitory Concentration 50
Leishmania donovani / cytology,  drug effects*,  enzymology
Leishmaniasis, Visceral / drug therapy*
Macrophages / parasitology*
Membrane Potential, Mitochondrial / drug effects
Mice, Inbred BALB C
Mitochondrial Membranes / drug effects,  metabolism
Oxidoreductases / drug effects*
Spleen / parasitology
Reg. No./Substance:
0/2,6-dimethyl-4-(3-O-benzyl-1,2-O-isopropylidene-beta-L-threo-pentofuranos-4-y)-1-phenyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid diethyl ester; 0/Antiprotozoal Agents; 0/Dihydropyridines; 0/Glycosides; EC 1.-/Oxidoreductases; EC reductase

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