Leishmania donovani: Oral therapy with glycosyl 1,4-dihydropyridine analogue showing apoptosis like phenotypes targeting pteridine reductase 1 in intracellular amastigotes

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...

Full description

Saved in:
Bibliographic Details
Published in:Experimental parasitology 2010-07, Vol.125 (3), p.310-314
Main Authors: Kaur, Jaspreet, Singh, Nasib, Singh, Biswajit Kumar, Dube, Anuradha, Tripathi, Rama Pati, Singh, Prashant, Singh, Neeloo
Format: Article
Language:English
Subjects:
Administration, Oral
Amastigotes
Animals
Antileishmanial activity
Antiprotozoal Agents - administration & dosage
Antiprotozoal Agents - chemistry
Antiprotozoal Agents - pharmacology
Apoptosis - drug effects
Biological and medical sciences
Cell Cycle - drug effects
Cell cycle arrest
Cell Line
Cricetinae
Dihydropyridine
Dihydropyridines - administration & dosage
Dihydropyridines - pharmacology
Dihydropyridines - therapeutic use
Flow Cytometry
Fundamental and applied biological sciences. Psychology
Glycosides - administration & dosage
Glycosides - pharmacology
Glycosides - therapeutic use
Inhibitory Concentration 50
Leishmania donovani
Leishmania donovani - cytology
Leishmania donovani - drug effects
Leishmania donovani - enzymology
Leishmaniasis, Visceral - drug therapy
Life cycle. Host-agent relationship. Pathogenesis
Macrophages - parasitology
Male
Membrane Potential, Mitochondrial - drug effects
Mesocricetus
Mice
Mice, Inbred BALB C
Mitochondrial Membranes - drug effects
Mitochondrial Membranes - metabolism
Oxidoreductases - drug effects
Phenotype
Protozoa
Spleen - parasitology
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0014-4894
1090-2449
DOI:10.1016/j.exppara.2010.02.011