title: 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.
authors.affiliation: Department of Analytical and Bioinorganic Chemistry, Kyoto Pharmaceutical University, Japan.
authors.forename: R
authors.initials: R
authors.lastname: Tawa
authors.forename: K
authors.initials: K
authors.lastname: Uchida
authors.forename: J
authors.initials: J
authors.lastname: Taniyama
authors.forename: Y
authors.initials: Y
authors.lastname: Fujisawa
authors.forename: S
authors.initials: S
authors.lastname: Fujimoto
authors.forename: T
authors.initials: T
authors.lastname: Nagaoka
authors.forename: K
authors.initials: K
authors.lastname: Kanamori
authors.forename: H
authors.initials: H
authors.lastname: Sakurai
mesh_terms: D000818:Animals; D001224:Aspartic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D002286:Carcinoma, Ehrlich Tumor / Q000378:metabolism* / Q000473:pathology; D003847:Deoxyglucose / Q000493:pharmacokinetics; D004305:Dose-Response Relationship, Drug; D004341:Drug Evaluation; D005947:Glucose / Q000493:pharmacokinetics*; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D007328:Insulin / Q000494:pharmacology*; D008297:Male; D051379:Mice; D010848:Picolinic Acids / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013997:Time Factors; D014316:Tritium; D014638:Vanadates / Q000737:chemistry / Q000494:pharmacology*; D017968:Vanadium Compounds / Q000494:pharmacology
chemical_list: C119468:(N-pyridylmethylaspartate)oxovanadium(IV); D007004:Hypoglycemic Agents; D007328:Insulin; D010848:Picolinic Acids; D017968:Vanadium Compounds; C095866:bis(picolinato)oxovanadium(IV); D014316:Tritium; D001224:Aspartic Acid; D014638:Vanadates; C034028:vanadyl sulfate; D003847:Deoxyglucose; D005947:Glucose