4.7 Article

Effect of the chloro-substitution on lowering diabetic hyperglycemia of vanadium complexes with their permeability and cytotoxicity

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 12, Pages 6077-6084

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.10.013

Keywords

Salen-type ligands; Substituent effect; Anti-diabetic activity

Funding

  1. National Natural Science Foundation of China [30260118]
  2. Yunnan Natural Science Foundation [2002C0019R]
  3. Yunnan University Science Foundation [2005 Q002A, 2009CD006]

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The effect of the chloro-substitution of dinuclear vanadium (V) complexes on lowering diabetic hyperglycemia was evaluated. The in vivo tests for hypoglycemic activity show that complex 2 at the dose of 10.0 and 20.0 mg V kg(-1), could significantly decrease the blood glucose level. Importantly, our results the chloro substituent increased the insulin-enhancing properties of the complex 2. The two vanadium compounds had permeability above 10(-5) cm/s. It suggested that two complexes permeate via a passive diffusion mechanism. It was also suggested that two complexes has better good lipophilic properties. The cytotoxicity of two complexes on Caco-2 cells suggested the chlorine atom at C4 of complex 2 increased cytotoxicity for vanadium complexes. (C) 2010 Elsevier Masson SAS. All rights reserved.

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