The design, synthesis and in vivo biological evaluations of [V(IV)O(2,6-pyridine diacetatato) (H2O)2] (PDOV): Featuring its prolonged glucose lowering effect and non-toxic nature

A novel vanadyl complex, [V(IV)O(2,6-pyridine diacetatato) (H2O)2] (PDOV) has been synthesized and tested in vivo in a population of STZ-induced diabetic rats. Effective hyperglycemic attenuation was achieved at a relatively low intraperitoneal and oral dosage of the complex and was complemented by...

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Veröffentlicht in:INORGANICA CHIMICA ACTA 2020-05, Vol.504, p.119448, Article 119448
Hauptverfasser: Rambaran, Varma H., Saumya, S.M., Roy, Soumyabrata, Sonu, K.P., Eswaramoorthy, Muthusamy, Peter, Sebastian C.
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Sprache:eng
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Zusammenfassung:A novel vanadyl complex, [V(IV)O(2,6-pyridine diacetatato) (H2O)2] (PDOV) has been synthesized and tested in vivo in a population of STZ-induced diabetic rats. Effective hyperglycemic attenuation was achieved at a relatively low intraperitoneal and oral dosage of the complex and was complemented by a prolonged residual activity over a period of 90 days. [Display omitted] •A novel vanadyl complex, PDOV, has been synthesized and characterized.•pH-controlled release of PDOV from polymer coated mesoporous silica, showed a higher rate of release at pH 7.4 than pH 2.•Intraperitoneal administration of PDOV, at 75 mg/kgbw, decreased blood glucose levels in diabetic rats.•Oral administration of PDOV, at 100 mg/kgbw, decreased blood glucose levels in diabetic rats.•A dosage regime of 1 in every 5 days, was able to maintain lower glucose levels for a period of 90 days. The synthesis and characterization of a novel vanadyl complex, [V(IV)O(2,6-pyridine diacetatato)(H2O)2] (PDOV) is reported. The pH-controlled release of the complex from polymer coated mesoporous silica was demonstrated for possible oral administration; results showed that release at pH 2 was significantly lower than that at pH 7.4. The said complex was subsequently screened for possible anti-diabetic activity, via an in vivo dose-response study (intraperitoneal and oral supplementation of PDOV) for 90 days in streptozotocin (STZ) induced diabetic rats. The results revealed that over a 90 day period, intraperitoneal administration of PDOV (at a dose of 75 mg/kgbw) and oral administration of the PDOV (at a dose of 100 mg/kgbw) were effective in suppressing the hyperglycemic state in the diabetic subjects. Exposure to PDOV was found to have little impact on the insulin levels of diabetics; however improved urea, creatinine, AST and ALT levels were noted.
ISSN:0020-1693
1873-3255
DOI:10.1016/j.ica.2020.119448