Effect of GRP119 Receptor Agonist, Compound MBX-2982, on Activity of Human Glucokinase.

Validation of the method for studies of glucokinase activators by the spectrophotometric method in an in vitro test system is carried out. The advantage of NAD coenzyme vs. thio-NAD is proven. Manifest activation of glucokinase by MBX-2982 compound (GPR119 agonist) in a wide range of concentrations is demonstrated experimentally.

Effect of Pyrrolobenzimidazole Derivative RU-792 on Experimental Brain Ischemia.

Compound RU-792 showed pronounced anti-ischemic activity and improved survival of rats with brain ischemia by normalizing parameters of spontaneous motor activity and reducing neurological deficit within 3 post-operative days being superior to the reference drug mexidol by this parameter. RU-792 inhibited the formation of conjugated dienes and malonic dialdehyde and increased activity of the antioxidant enzyme glutathione peroxidase thereby modulating the parameters of free radical oxidation in rats subjected to ischemia more effectively than mexidol.

Experimental study of the effect of a new antioxidant agent on learning and memory.

This work presents the results of studying the effect of a new antioxidant compound enoxyphol on learning and memory in rats.

Antithrombogenic activity of antioxidant compounds.

Antithrombotic activities of enoxifol, a new antioxidant with antiaggregant activity demonstrated in vitro and in vivo, and antioxidant mexidol were compared on the rat model of arterial thrombosis induced by application of 50% ferric chloride. Acetylsalicylic acid (antiaggregant) served as the reference drug. All drugs exhibited dose-dependent antithrombotic activity. Enoxifol was more effective than mexidol, both drugs being more active than the reference drug (acetylsalicylic acid). Taking into account the pathogenesis of the thrombosis in this experimental model, we can hypothesize that the pronounced antithrombotic effect of enoxifol was due to its antiaggregant and antioxidant activities.

Antioxidant properties of pyrrolobenzimidazole derivative RU-792: experimental study.

We studied antioxidant activity of new derivative of pyrrolo[1,2-α]benzimidazole RU-792 and compared its effects on free radical processes with those of the reference antioxidant Trolox in four model free-radical systems. RU-792 had high antioxidant activity determined by its intrinsic antiradical properties. RU-792 was superior to Trolox by antioxidant activity in the models of Fe(2+)-induced chemiluminescence of lipids with 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid), but less effective in the model of luminol-dependent chemiluminescence.

[Antioxidants: current situation and perspectives].

In the overview one can find analysis medico-biological aspects of free radical theory, clinical experience of antioxidants using, perspectives of new active agents and possible directions of theirs practical use.

[Comparative characteristics of antioxidant properties of hypoglycemic agents diabenol and gliclazide].

The antioxidant properties of diabenol and gliclazide with reference to mexidol have been studied in vitro on several model systems, including chemiluminescence (CL) of lipids, CL with generation of reactive oxygen species (ROS), CL dependent on luminol oxidation by peroxy radicals, and the Glavind DPPH free-radical method. Diabenol exhibited the properties of a scavenger of superoxide anions and hydroxy and peroxy radicals in model CL systems with ROS generation. The activity of diabenol in inactivating ROS was about 8 times higher compared to mexidol. However, the antioxidant activity of diabenol in CL with peroxy radical generation was 3 times lower compared to mexidol. Gliclazide demonstrated dose-dependent antioxidant activity only on the model with stable DPPH radicals, where its inhibitory effect was 15 times greater than that of the reference drug.

[Antioxidant and membranoprotective properties of trolox].

The antioxidant and membranoprotective properties of trolox have been studied in vitro. It is established that trolox possesses antioxidant properties, inhibiting ascorbate-dependent lipid peroxidation of liver homogenates and Fe(2+)-induced lipid chemiluminescence of egg-yolk lipids. In addition, trolox exhibits a broad spectrum of antiradical activity and interacts with stable free 2,2-diphenyl-1-picrylhydrazyl radical so as to reduce the generation of luminol radicals and reactive oxygen species and to bind peroxy radicals. Trolox also possessed membranoprotective properties, being capable of reducing the oxidative hemolysis of erythrocytes.

[Study of antiradical activity of new compounds by chemiluminescence].

Antioxidative and antiradical properties of a new antioxidant cerebroprotective drug, enoxifol (benzimidasole derivative), were compared with mexidol by means of three chemiluminescent techniques: luminol autooxidation system, Fe2+-induced lipid chemiluminescence and lucigenin-induced chemiluminescence with superoxide generation by xanthine-xanthine oxidase system. Enoxifol exhibited higher antiradical activity than mexidol. This was shown by suppression of luminol radicals and superoxide anion-radical generation. Antioxidant properties of enoxifol were also demonstrated by decreasing of Fe2+-induced lipid chemiluminescence. The recognized properties of enoxifol influencing chemiluminescent processes confirm the results, obtained earlier by means of indirect methods of free radical processes study in vitro and in vivo (decrease of LPO products, activation of antioxidant enzymes), also can underline its pharmacological effects.

[Modelling of intrauterine hypoxia].

An experimental model of chronic intrauterine hypoxia is proposed. This model reflects the most typical posthypoxic impairments for the above pathology: intrauterine growth retardation, alterations in the placental parameters, posterity death in the neonatal period, physical retardation, postnatal disorders in the CNS functions.

[Anti-ischemic properties of the novel antioxidant enoxifol]. / Protivoishemicheskie svoistva novogo antioksidantnogo sredstva énoksifola.

The antiischemic properties of the new antioxidant drug enoxifol, representing a derivative of N9-imidazo[1,2-a]benzimidazole, was studied in rats on the models of a double-vessel occlusion of common carotid arteries under normal conditions and on the background of irradiation. In addition, we studied the effect of enoxifol on the rehabilitation of experimental animals in the early reperfusion period after total brain ischemia.

Dynamics of the recovery period in rats exposed to global cerebral ischemia.

Global cerebral ischemia-reperfusion was modeled by thermocoagulation of the vertebrobasilar arteries followed by occlusion of both carotid arteries. Behavioral parameters, neurological status, and mnesic functions in rats were studied during the recovery period. It is concluded that this model of ischemia is reproducible and can be used for studying ischemia-reperfusion damages to the brain.

[The effect of compounds with antioxidant properties on thrombocyte functional activity]. / Vliianie soedinenii s antioksidantnymi svoistvami na funktsional'nuiu aktivnost' trombotsitov.

The effect of antioxidant compounds ionol and mexidol and the new phenol derivative N9-imidazo-(1,2 alpha)-benzymidazol (PY-185) on the functional activity of blood platelets was studied. All the compounds under study effectively inhibited blood platelet aggregation both in vitro and in administration into rats, a result of which the blood thrombogenic potential reduced.