In vitro study of the insulin-like action of vanadyl-pyrone and -pyridinone complexes with a VO(O4) coordination mode.
The insulin-like action of a novel class of potential insulin-mimetic complexes was investigated in terms of free fatty acid (FFA) release from isolated rat adipocytes. Vanadyl complexes such as VO(ema)2 [(bis(2-ethyl-3-hydroxy-4-pyrone)VO], VO(mpp)2 [bis (3-hydroxy-2-methyl-4(1H)-pyridinone)VO], VO(dmpp)2 [bis(1,2-dimethyl-3-hydroxy-4(1H)-pyridinone)VO] and VO(empp)2 [bis(2-ethyl-3-hydroxy-1-methyl-4(1H)-pyridinone)VO] were tested together with vanadyl sulfate for comparison. The inhibitory effect of the vanadium complexes on FFA release, from rat adipocytes treated with epinephrine, is dependent on concentration and for that reason the results are reported in terms of the IC50 value, the 50% inhibition concentration. The results show that all the complexes have an inhibitory effect on FFA release and that two pyridinone complexes, VO(mpp)2 and VO(empp)2, have a significantly better insulin-mimetic activity than that of vanadyl sulfate.
Rangel
M
M
CEQUP/Instituto de Ciencias Biomedicas de Abel Salazar, Universidade do Porto, Portugal. mcrangel@fc.up.pt
Tamura
A
A
Fukushima
C
C
Sakurai
H
H
D017667:Adipocytes / Q000187:drug effects / Q000378:metabolism; D000818:Animals; D004837:Epinephrine / Q000494:pharmacology; D005230:Fatty Acids, Nonesterified / Q000037:antagonists & inhibitors / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008297:Male; D018716:Molecular Mimicry; D011728:Pyridones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011753:Pyrones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D014638:Vanadates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D005230:Fatty Acids, Nonesterified; D007004:Hypoglycemic Agents; D011728:Pyridones; D011753:Pyrones; C075743:oxovanadium IV; D014638:Vanadates; D004837:Epinephrine