| 摘要 |
The invention relates to the field of bioorganic chemistry, pharmaceutical chemistry and technology of drugs and concerns methods for producing preparations of vegetable raw material, which possess hepatoprotective activity. Technical result of the claimed invention is achieved by that the ecologically safe barothermal method is used for producing extract balsam poplar (Populus balsamifera L.) buds with pinostrobin flavonoid content of 0.9% with reference to air-dry raw material by extraction of raw material at a temperature of 150-160°C, pressure of 1.9 atm., for 60 min, separation and purification of thick extract by method of column chromatography with elution with petroleum ether and mixture petroleum ether-ethylacetate 49:1, recrystallisation of isolated technical pinostrobin with further synthesis of pinostrobin oxime (substance for pharmaceutical dosage form). Pinostrobin oxime substance is not toxic, does not cause acute toxic reactions in tests in mice and rats and demonstrates the high hepatoprotective activity in dose of 100 mg/kg of weight, and in the dose of 50 mg/kg eliminates manifestations of cytolysis, cholestasis and mesenchymal inflammation syndromes. Pinostrobin oxime relates to "short-living" products. In rat organism the product is revealed within 2 hours, irrespective of the administered dose and method of administration, penetrates well mainly in vascularised organs (kidneys, liver, lungs), and absolute bioavailability of pinostrobin oxide is 11%. Antioxidant activity of pinostrobin oxime is 20 times as high as that of pinostrobin. Pinostrobin oxime does not produce any toxic effect on the liver, reduces the lipoperoxidation intensity, the triacylglyceride content by 26% in it and increases phospholipid level by 21%, inhibits lipid peroxidation processes in hepatocytes, reducing diene conjugate content by 35%, increasing the activity of antiperoxide protection enzymes - glutathionperoxidase and glutathion reductase up to 54%. |
