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A new insulin-mimetic vanadyl complex, (N-pyridylmethylaspartate)oxovanadium(IV) with VO(N2O2) coordination mode, and evaluation of its effect on uptake of D-glucose by Ehrlich ascites tumour cells.

Abstract
Because it has been confirmed that the vanadyl(IV) ion and its complexes act as insulin mimetics, a new organic vanadyl complex, (N-pyridylmethylaspartate)oxovanadium (VOPASP) with VO(N2O2) coordination mode, was prepared. Development of a simple and rapid in-vitro assay is needed for recognition of potent insulin-mimetic complexes. Treatment of Ehrlich ascites tumour cells with 2-deoxyglucose in the presence of vanadyl sulphate, or other vanadyl complexes with the same coordination mode (VOPASP, bis(picolinate)oxovanadium (VOPA) and bis(6-methyl picolinate)oxovanadium (VOMPA)), in the presence of 2-deoxy-D-[1-3H]glucose ([3H]deoxyglucose), resulted in concentration-dependent uptake of 2-deoxyglucose by the cells. The responses of the cells to the vanadyl complexes were reflected, in part, by results obtained from the free fatty acid-releasing assay using rat adipocytes. These results show that the in-vitro assay with Ehrlich ascites tumour cells provides an accurate and rapid assessment of glucose uptake by the cells. The assay is proposed as a means of predicting the insulin-mimetic activity of the vanadyl complexes and for studying the mechanism of action of the complexes.
AuthorsR Tawa, K Uchida, J Taniyama, Y Fujisawa, S Fujimoto, T Nagaoka, K Kanamori, H Sakurai
JournalThe Journal of pharmacy and pharmacology (J Pharm Pharmacol) Vol. 51 Issue 2 Pg. 119-24 (Feb 1999) ISSN: 0022-3573 [Print] England
PMID10217308 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • (N-pyridylmethylaspartate)oxovanadium(IV)
  • Hypoglycemic Agents
  • Insulin
  • Picolinic Acids
  • Vanadium Compounds
  • bis(picolinato)oxovanadium(IV)
  • Tritium
  • Aspartic Acid
  • Vanadates
  • vanadyl sulfate
  • Deoxyglucose
  • Glucose
Topics
  • Animals
  • Aspartic Acid (analogs & derivatives, chemistry, pharmacology)
  • Carcinoma, Ehrlich Tumor (metabolism, pathology)
  • Deoxyglucose (pharmacokinetics)
  • Dose-Response Relationship, Drug
  • Drug Evaluation
  • Glucose (pharmacokinetics)
  • Hypoglycemic Agents (pharmacology)
  • Insulin (pharmacology)
  • Male
  • Mice
  • Picolinic Acids (pharmacology)
  • Rats
  • Rats, Wistar
  • Time Factors
  • Tritium
  • Vanadates (chemistry, pharmacology)
  • Vanadium Compounds (pharmacology)

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