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Natural products are the inexhaustible source of chemical diversity that can be compared only with the powerful combinatorial chemistry techniques [1]. Plant secondary metabolites (flavonoids, alkaloids, etc) cause active interest in connection with their authentic influence on decrease in risk of occurrence of cardiovascular diseases and with their potential neuroprotective properties. Antioxidant and free radical-scavenging abilities of flavonoids and alkaloids can be a basis of positive effects of many plant extracts (2). In this project the methodology of search of new biologically active compounds from Russian flora as potential neuroprotective drugs on the basis of a combination of methods of semipreparative HPLC, LC-ESI-MS/MS analyses and screening for antioxidant activities and inhibition of mitochondrial permeability transition (MPT) is described.