Effects of 2-deoxy-D-glucose on Acanthocheilonema viteae: rodent filariids as studied by multinuclear NMR spectroscopyt.
A well known glucose antimetabolite, 2-deoxy glucose (2DG) widely used in chemotherapy of cancer along with radiation, was evaluated as an antifilarial agent by nuclear magnetic resonance. The uptake and metabolism of 2DG in the experimental filarial infection Acanthocheilonema viteae was studied by in vivo multinuclear NMR. An unusually long retention time of 2DG6P within these parasites was observed on continuous 31P NMR monitoring, along with a decrease in ATP levels. These results led to therapeutic investigation in A. viteae infected host Mastomys coucha. 2DG showed a remarkable adulticidal activity (73.6%) with 50% sterilization of surviving female worms at a dose of 250 mg/kg x 5, p.o. NMR observations and activity profile substantiate the findings of one another, directed towards the hitting of bioenergetic machinery of A. viteae by macrofilaricidal agent (2DG).
Shukla-Dave
A
A
Division of Parasitology, Central Drug Research Institute, Lucknow 226 001, India.
Roy
R
R
Bhaduri
A P
AP
Chatterjee
R K
RK
D000284:Administration, Oral; D000818:Animals; D000963:Antimetabolites / Q000008:administration & dosage / Q000493:pharmacokinetics; D003847:Deoxyglucose / Q000493:pharmacokinetics / Q000494:pharmacology*; D004153:Dipetalonema / Q000187:drug effects* / Q000378:metabolism*; D004154:Dipetalonema Infections / Q000188:drug therapy / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004734:Energy Metabolism / Q000187:drug effects; D005369:Filaricides / Q000493:pharmacokinetics / Q000494:pharmacology*; D006790:Host-Parasite Interactions; D007773:Lactates / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy / Q000379:methods*; D051379:Mice / Q000469:parasitology*; D016896:Treatment Outcome
D000963:Antimetabolites; D005369:Filaricides; D007773:Lactates; D003847:Deoxyglucose