To study insulino-mimetic effects of bis（α-furancarboxylato）oxovanadium（IV）（BFOV）,a orally active antidiabetic vanadyl complex,on glucose uptake and lipogenesis in isolated rat adipocytes were determined by usi...To study insulino-mimetic effects of bis（α-furancarboxylato）oxovanadium（IV）（BFOV）,a orally active antidiabetic vanadyl complex,on glucose uptake and lipogenesis in isolated rat adipocytes were determined by using 2-deoxy-D——glucose and D-glucose,respectively.Lipolysis was assayed by free fatty acids（FFA） released from isolated rat adipocytes treated with epinephrine.The results showed that BFOV,similar to insulin,concentration-dependently significantly enhanced the uptake of 2-deoxy-D——glucose and the transformation from D-glucose to lipid in isolated rat adipocytes,with the EC50 values of（0.31±0.08） mmol·L-1 and（0.49±0.12） mmol·L-1,respectively.Moreover,BFOV markedly inhibited FFA release from isolated rat adipocytes treated with epinephrine,and the IC50 value was（0.30±0.20） mmol·L-1.BFOV had insulino-mimetic effects such as enhancing glucose uptake and lipogenesis,as well as inhibiting lipolysis.展开更多
Vanadium compounds are promising anti-diabetic agents. However, the concern in the toxicity, especially the long-term renal side effect along with diabetic status, is restricting the further development of this metal ...Vanadium compounds are promising anti-diabetic agents. However, the concern in the toxicity, especially the long-term renal side effect along with diabetic status, is restricting the further development of this metal drug. Recently, we have prepared a bis（（5-hydroxy-4-oxo-4H-pyran-2-yl） methyl 2-hydroxy-benzoatato） oxovanadium（BSOV）, which exhibited excellent hypoglycemic effect with low acute toxicity. In order to facilitate the development of anti-diabetic vanadium complexes, especially BSOV, we studied the long-term toxicity and hypoglycemic effect of BSOV in comparison with bis（maltolato） oxovanadium（BMOV） on both non-diabetic and type II diabetic mice. The experiments confirmed a stable hypoglycemic effect for both the vanadium complexes over the testing period（6–7 months）. However, the chronic administration of vanadium compounds slightly increased oxidative stress in ICR mice and the induced renal interstitial edema（RIE） in a part of the diabetic animals associated with low levels of serum albumin. The use of an antioxidant dietary supplement（a combination of vitamin C and Zinc gluconate） could prevent vanadium-induced oxidative stress but have marginal effect on RIE. However, BSOV caused much lower incidence of RIE than BMOV did, suggesting that BSOV is an important step towards the successful development of anti-diabetic vanadium drugs.展开更多
文摘To study insulino-mimetic effects of bis（α-furancarboxylato）oxovanadium（IV）（BFOV）,a orally active antidiabetic vanadyl complex,on glucose uptake and lipogenesis in isolated rat adipocytes were determined by using 2-deoxy-D——glucose and D-glucose,respectively.Lipolysis was assayed by free fatty acids（FFA） released from isolated rat adipocytes treated with epinephrine.The results showed that BFOV,similar to insulin,concentration-dependently significantly enhanced the uptake of 2-deoxy-D——glucose and the transformation from D-glucose to lipid in isolated rat adipocytes,with the EC50 values of（0.31±0.08） mmol·L-1 and（0.49±0.12） mmol·L-1,respectively.Moreover,BFOV markedly inhibited FFA release from isolated rat adipocytes treated with epinephrine,and the IC50 value was（0.30±0.20） mmol·L-1.BFOV had insulino-mimetic effects such as enhancing glucose uptake and lipogenesis,as well as inhibiting lipolysis.
基金National Natural Science Foundation of China(Grant No.21271012)
文摘Vanadium compounds are promising anti-diabetic agents. However, the concern in the toxicity, especially the long-term renal side effect along with diabetic status, is restricting the further development of this metal drug. Recently, we have prepared a bis（（5-hydroxy-4-oxo-4H-pyran-2-yl） methyl 2-hydroxy-benzoatato） oxovanadium（BSOV）, which exhibited excellent hypoglycemic effect with low acute toxicity. In order to facilitate the development of anti-diabetic vanadium complexes, especially BSOV, we studied the long-term toxicity and hypoglycemic effect of BSOV in comparison with bis（maltolato） oxovanadium（BMOV） on both non-diabetic and type II diabetic mice. The experiments confirmed a stable hypoglycemic effect for both the vanadium complexes over the testing period（6–7 months）. However, the chronic administration of vanadium compounds slightly increased oxidative stress in ICR mice and the induced renal interstitial edema（RIE） in a part of the diabetic animals associated with low levels of serum albumin. The use of an antioxidant dietary supplement（a combination of vitamin C and Zinc gluconate） could prevent vanadium-induced oxidative stress but have marginal effect on RIE. However, BSOV caused much lower incidence of RIE than BMOV did, suggesting that BSOV is an important step towards the successful development of anti-diabetic vanadium drugs.
