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Métodos Terapéuticos y Terapias MTCI
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1.
Tsitologiia ; 45(10): 1032-7, 2003.
Artículo en Ruso | MEDLINE | ID: mdl-14989176

RESUMEN

It has been shown that the major alkaloids from plants Chelidonium majus L. and Macleaya (Bocconia) cordata and microcarpa, namely, berberine, sanguinarine, chelidonine, and drugs "Ukrain" (thiophosphoric acid derivative of a sum of the alkaloids isolated from Ch. majus L.) and "Sanguirythrine" (a mixture of the alkaloids sanguinarine and chelerythrine, w/w 3:7, isolated from Macleaya), are irreversible inhibitors of oxidative deamination reaction of serotonin and tyramine as substrates, catalyzed by rat liver mitochondrial monoamine oxidase (MAO). At the same time these substances do not influence the oxidative deamination reaction of benzylamine as substrate (in concentration 1 mM or less). The substrate specificity of this inhibition manifests that mainly the oxidative deamination reactions catalyzed by MAO form A are inhibited by the agents studied. Among the examined agents, alkaloid chelidonine and drug "Ukrain" are the strongest inhibitors of the reaction. Alkaloids berberine and sanguinarine and drug "Sanguirythrine" exhibit a weaker action. Judging from the data obtained, sanguinarine and chelerythrine appear to exert similar inhibitory effects in this reaction, since sanguinarine and "Sanguirythrine" have similar values of bimolecular rate constants of their interaction with mitochondrial MAO. As it is well known, the MAO inhibitors appear to be, as a rule, pronounced antidepressants. The combination of malignotoxicity and antidepressive activity in drug "Ukrain" seems to be favourable for its clinical applications.


Asunto(s)
Alcaloides/farmacología , Mitocondrias Hepáticas/metabolismo , Inhibidores de la Monoaminooxidasa/farmacología , Papaveraceae/química , Plantas Medicinales/química , Alcaloides/química , Alcaloides/aislamiento & purificación , Animales , Masculino , Mitocondrias Hepáticas/efectos de los fármacos , Mitocondrias Hepáticas/enzimología , Estructura Molecular , Inhibidores de la Monoaminooxidasa/química , Inhibidores de la Monoaminooxidasa/metabolismo , Ratas , Ratas Wistar , Serotonina/metabolismo , Especificidad por Sustrato , Tiramina/metabolismo
2.
Bioorg Khim ; 19(11): 1077-80, 1993 Nov.
Artículo en Ruso | MEDLINE | ID: mdl-8285921

RESUMEN

Anticholinesterase activity of carboranyl containing thio- and selenoesters of pentavalent phosphorus acids has been studied. Insertion of the carboranyl substituents in the thioester group of phosphororganic compounds was found to increase the anticholinesterase activity as compared with the thioalkyl analogues. The compounds with B-carboranyl group are less active inhibitors of cholinesterase than their isomers with C-carboranyl group.


Asunto(s)
Inhibidores de la Colinesterasa/farmacología , Ácidos Fosforosos/farmacología , Selenio/química , Compuestos de Sulfhidrilo/química , Acetilcolinesterasa/sangre , Animales , Butirilcolinesterasa/sangre , Inhibidores de la Colinesterasa/química , Ésteres , Caballos , Humanos , Ácidos Fosforosos/química , Relación Estructura-Actividad
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