Makarenko O. The biochemical mechanisms of osteotropic effect of flavonoids

Dissertation is devoted to investigation of the mechanisms of the regulation of methabolism in osseous tissue with flavonoids, to study of the elastase concept of osteodestructive processes and the substantiation of the elaboration of preparations with flavonoids, providing osteoprotective and anti-inflammatory effect. For the exact identification of flavonoids in vegetable preparations the method of the analysis on the high-performance liquid chromatography in the mode of gradient with mobile phase "methanol - 0,9 % phosphoric acid" was improved. Developed tehnologies and methods of analysis were used to receive preparations from soy beens, wheat germs and citrus peel with controled flavonoid concentration. Using the index IC50 in vitro the ability of flavonoids to impede the formation of active forms of oxygen, inhibit the activity of proteinases, leukocytar elastase and phospholipase А2 was determined. The partially competitive type of inhibiting with flavonoids of the elastase's and trypsin's activities was revealed. Ex vivo the inhibition with flavonoids of osseous elastase and activation of catalase was fixed. In experiments osteoporosis (ovariectomy, prednisolone, alimentary factor) or fluorine intoxication with rats were simulated. The prophylactic introduction of the preparations of flavonoids was shown to prevent the decrease in density of rats femoral bone, the growth in activity of phosphatases, elastase, cathepsin D, the fall of the general proteolytic activity and antioxidant enzymes in osseous tissue, excretion of calcium and reduction of inclusion of calcium into calcified tissues. The destructive role of osseous elastase in resorption of organic matrix of bone was displayed. The group of proteinases, taking part in collagen "maturation" was revealed. The conclusion about the leukocytar origin of osseous elastase was drawn. The preparations with flavonoids for the treatment of osteoporosis "EKSO", "Osteovit", "Biotrit-C" in pills and dental antiinflammatory elixirs "Eksodent", "Biodent", "Apelsinovyj", "Mandarinovyj", "Greipfrutovyj" are grounded.