Cell-based screening for identification of novel vanadium complexes with multidirectional activity relative to cells associated with metabolic disorders

• Autorzy: Kazek Grzegorz , Głuch-Lutwin Monika , Modryl Barbara , Menaszek Elżbieta , Szklarzewicz Janusz , Gryboś Ryszard , Papież Monika

Identyfikatory

DOI

10.5604/01.3001.0013.1047

• Języki publikacji: EN

Abstrakty

EN

In this study, 110 newly synthesized vanadium complexes from different structural groups were screened in three cell-based models representing the main target tissues for anti-diabetic drugs. In glucose utilization in C2C12 myocyte experiments, 93% of vanadium complexes were shown to have equal or greater activity than bis(maltolato)oxovanadium(IV) (BMOV), the methyl analog of bis(ethylmaltolato)oxovanadium(IV) (BEOV) which has been tested in clinical trials. Moreover, 49% and 50% of these complexes were shown to have equal or greater activity than BMOV in lipid accumulation in 3T3-L1 adipocytes and insulin secretion in RINm5F beta cell experiments, respectively. These results were the basis for the selection of compounds for the subsequent steps in the characterization of anti-diabetic properties. This study provides strong support for the application of screening cell-based assays with a phenotypic approach for the discovery of novel anti-diabetic drugs from the vanadium complex class. This is especially desirable due to the multiple and not fully defined mechanisms of action vanadium compounds.

Słowa kluczowe

EN

vanadium complex; cell-based screening; anti-diabetic activity

PL

kompleks wanadu; badanie przesiewowe oparte na komórkach; aktywność przeciwcukrzycowa

• Wydawca: Państwowa Wyższa Szkoła Zawodowa w Tarnowie
• Czasopismo: Science, Technology and Innovation
• Rocznik: 2019
• Tom: Vol. 4, no. 1
• Strony: 47--54
• Opis fizyczny: Bibliogr. 36 poz., rys. tab.

Twórcy

autor

Kazek Grzegorz

• Department of Pharmacological Screening, Chair of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University Collegium Medicum, Krakow, Poland

autor

Głuch-Lutwin Monika

• Department of Radioligands, Chair of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Collegium Medicum, Medyczna 9, 30-688 Krakow, Poland

autor

Modryl Barbara

• Department of Radioligands, Chair of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Collegium Medicum, Medyczna 9, 30-688 Krakow, Poland

autor

Menaszek Elżbieta

• Department of Cytobiology, Chair of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Collegium Medicum, Medyczna 9, 30-688 Krakow, Poland

autor

Szklarzewicz Janusz

• Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, 30-387, Krakow, Poland

autor

Gryboś Ryszard

• Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, 30-387, Krakow, Poland

autor

Papież Monika

• Department of Cytobiology, Chair of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Collegium Medicum, Medyczna 9, 30-688 Krakow, Poland

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