Abstract
The effect of compound ZB-16 (a new GPR1 19 receptor agonist) after two-week administration on the endothelial function, glucose and lipid metabolism (total cholesterol, LDL, HDL and triglycerides), lipid peroxidation, and antioxidant system status in rats with experimental type-2 diabetes mellitus (T2DM) has been studied. It was found that the untreated control group of animals exhibited, in addition to sustained hyperglycemia, a decrease in endothelium-dependent vaso- dilation and antioxidant system activity, and increase in the content of LDL and the dyslipidemic index. Administration of ZB-16 (1 mg/kg, p.o.) in rats with T2DM model resulted in reduction of the endothelial dysfunction (improved endothelium-dependent vasodilation by 83% as compared to the control group, p < 0.05). ZB-16 also produced a moderate antioxidant effect of reducing the content of TBA-active products (by 30% as compared to the untreated control, p <0.05) and favored normalization of lipid metabolism indicators.
MeSH terms
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Animals
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Antioxidants / pharmacology*
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Antioxidants / therapeutic use
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Blood Glucose / drug effects
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Blood Glucose / metabolism
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Cell Count
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Cholesterol, HDL / blood
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Cholesterol, LDL / blood
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Diabetes Mellitus, Experimental / blood
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Diabetes Mellitus, Experimental / chemically induced
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Diabetes Mellitus, Experimental / drug therapy*
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Diabetes Mellitus, Experimental / genetics
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Dyslipidemias / blood
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Dyslipidemias / chemically induced
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Dyslipidemias / drug therapy*
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Dyslipidemias / genetics
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Endothelial Cells / drug effects
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Female
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Gene Expression / drug effects
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Hypoglycemic Agents / pharmacology*
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Hypoglycemic Agents / therapeutic use
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Hypolipidemic Agents / pharmacology*
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Hypolipidemic Agents / therapeutic use
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Lipid Metabolism / drug effects
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Lipid Peroxidation / drug effects
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Piperidines / pharmacology*
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Piperidines / therapeutic use
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Pyrimidines / pharmacology*
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Pyrimidines / therapeutic use
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Rats
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Receptors, G-Protein-Coupled / agonists*
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Receptors, G-Protein-Coupled / genetics
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Receptors, G-Protein-Coupled / metabolism
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Streptozocin
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Thiobarbituric Acid Reactive Substances / metabolism
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Triglycerides / blood
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Vasodilation / drug effects
Substances
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Antioxidants
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Blood Glucose
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Cholesterol, HDL
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Cholesterol, LDL
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GPR119 protein, rat
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Hypoglycemic Agents
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Hypolipidemic Agents
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Piperidines
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Pyrimidines
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Receptors, G-Protein-Coupled
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Thiobarbituric Acid Reactive Substances
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Triglycerides
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Streptozocin