摘要 :
The antihypoxic activity of humic acids of Tomsk lowland peat was studied experimentally. It was established that native humic acids of peat (HAP) had pronounced antihypoxic activity after a preventive intragastric administration ...
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The antihypoxic activity of humic acids of Tomsk lowland peat was studied experimentally. It was established that native humic acids of peat (HAP) had pronounced antihypoxic activity after a preventive intragastric administration to mice, increasing the lifespan of animals and decreasing the lethality under hypobaric hypoxic and histotoxic hypoxia conditions. The discovered antihypoxic properties of HAP were probably due to their protective antioxidant properties, which prevent free-radical injury to cells and organelles under hypoxia conditions.
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摘要 :
The antihypoxic activity of humic acids of Tomsk lowland peat was studied experimentally. It was established that native humic acids of peat (HAP) had pronounced antihypoxic activity after a preventive intragastric administration ...
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The antihypoxic activity of humic acids of Tomsk lowland peat was studied experimentally. It was established that native humic acids of peat (HAP) had pronounced antihypoxic activity after a preventive intragastric administration to mice, increasing the lifespan of animals and decreasing the lethality under hypobaric hypoxic and histotoxic hypoxia conditions. The discovered antihypoxic properties of HAP were probably due to their protective antioxidant properties, which prevent free-radical injury to cells and organelles under hypoxia conditions.
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摘要 :
The antihypoxic activity of humic acids of Tomsk lowland peat was studied experimentally. It was established that native humic acids of peat (HAP) had pronounced antihypoxic activity after a preventive intragastric administration ...
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The antihypoxic activity of humic acids of Tomsk lowland peat was studied experimentally. It was established that native humic acids of peat (HAP) had pronounced antihypoxic activity after a preventive intragastric administration to mice, increasing the lifespan of animals and decreasing the lethality under hypobaric hypoxic and histotoxic hypoxia conditions. The discovered antihypoxic properties of HAP were probably due to their protective antioxidant properties, which prevent free-radical injury to cells and organelles under hypoxia conditions.
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Succinic acid bas been found to be able to potentiate the antihypoxic activity of vinpocetin. This property (potentiation) provided grounds for creating a new combined formulation containing vinpocetin and succinic acid, which has...
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Succinic acid bas been found to be able to potentiate the antihypoxic activity of vinpocetin. This property (potentiation) provided grounds for creating a new combined formulation containing vinpocetin and succinic acid, which has more marked antihypoxic activity than the initial single-substance vinpocetin formulation, alone with antiamnestic and anticonvulsive activities.
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The antihypoxic and antioxidant activities of Hibiscus esculentus seeds were investigated employing eight in vitro assay systems. Antihypoxic activity was investigated in two models, haemic and circulatory. The effects were pronou...
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The antihypoxic and antioxidant activities of Hibiscus esculentus seeds were investigated employing eight in vitro assay systems. Antihypoxic activity was investigated in two models, haemic and circulatory. The effects were pronounced in both models of hypoxia. The antihypoxic effects were dose-dependent. The results indicated that the extracts have a protective effect against hypoxia induced lethality in mice. The extracts showed antioxidant activity in some models. IC_(50) for DPPH radical-scavenging activity was 234 ± 8.9 μg ml~(-1) The extracts showed weak nitric oxide-scavenging activity between 0.1 and 1.6 mg ml~(-1). The extracts showed weak Fe~(2+) chelating ability. IC_(50) were 150 ± 13 μg ml~(-1). The extracts also exhibited low antioxidant activity in the linoleic acid model but were capable of scavenging hydrogen peroxide in a concentration dependent manner. The total amount of phenolic compounds in each extract was determined as gallic acid equivalents and total flavonoid contents were calculated as quercetin equivalents from a calibration curve. Pharmacological effects may be attributed, at least in part, to the presence of phenols and flavonoids in the extracts.
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We studied antihypoxic activity of analogs of endogenous cyclic dipeptide cycloprolylglycine in a mouse model of normobaric hypoxia with hypercapnia and found that antixypoxic effect depends on the structure of the substance. It w...
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We studied antihypoxic activity of analogs of endogenous cyclic dipeptide cycloprolylglycine in a mouse model of normobaric hypoxia with hypercapnia and found that antixypoxic effect depends on the structure of the substance. It was shown that different pharmacophores are responsible for the antihypoxic, nootropic, and anxiolytic effects of cycloprolylglycine.
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摘要 :
We studied antihypoxic activity of analogs of endogenous cyclic dipeptide cycloprolylglycine in a mouse model of normobaric hypoxia with hypercapnia and found that antixypoxic effect depends on the structure of the substance. It w...
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We studied antihypoxic activity of analogs of endogenous cyclic dipeptide cycloprolylglycine in a mouse model of normobaric hypoxia with hypercapnia and found that antixypoxic effect depends on the structure of the substance. It was shown that different pharmacophores are responsible for the antihypoxic, nootropic, and anxiolytic effects of cycloprolylglycine.
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N-(2-Dimethylaminoefhyl)carboxamide (1a—d), 2-dimethylaminoethyl alkyl ether (2a,b), and 2-dimethylami-noethyl 2-hydroxy-2-phenethyl ether (3a—c) and its amino and methylene analogues (3d, 4) have been screened for antiamnestic ...
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N-(2-Dimethylaminoefhyl)carboxamide (1a—d), 2-dimethylaminoethyl alkyl ether (2a,b), and 2-dimethylami-noethyl 2-hydroxy-2-phenethyl ether (3a—c) and its amino and methylene analogues (3d, 4) have been screened for antiamnestic and antihypoxic activities in mice. A clear reversing effect on electroconvulsive shock-induced amnesia was found with la—d, 2a,b, and 2-dimethylaminoethyl 2-hydroxy-2-phenylethyI ether (3a). However, a protective effect against hypoxia was only observed with 3a. Compound 3a, which displayed the dual activity, was further investigated for ameliorating effect on CO2-induced memory impairment, and it was found to be more potent than indeloxazine and bifemelane. In addition, the acute toxicity of 3a in mice was significantly lower than that of tacrine, but its serum-to-brain penetration ability in rats was less than that of the reference drugs.
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Peat humic acids (PHAs) were found under experimental normobaric hypoxia with hypercapnia to normalize the activities of succinate- and NAD-dependent energy-production processes and to prevent disconnection of oxidative phosphoryl...
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Peat humic acids (PHAs) were found under experimental normobaric hypoxia with hypercapnia to normalize the activities of succinate- and NAD-dependent energy-production processes and to prevent disconnection of oxidative phosphorylation in mouse cerebral and hepatic mitochondria. The antihypoxic activity of PHAs was comparable with that of the reference antihypoxant dihydroquercetin in mouse brain and exceeded it in liver. The observed normalization by PHAs of oxidative phosphorylation in cerebral and hepatic mitochondria was probably related to their protective properties that prevented free-radical damage of cells and organelles under hypoxic conditions.
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A series of C-substituted N-phenylacetylglycylprolines were synthesized. Their structure-activity (antihypoxic) relationship was studied in normobaric hypoxia tests at i.p. doses of 0.1 - 1 mg/kg as a function of the C-substitutio...
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A series of C-substituted N-phenylacetylglycylprolines were synthesized. Their structure-activity (antihypoxic) relationship was studied in normobaric hypoxia tests at i.p. doses of 0.1 - 1 mg/kg as a function of the C-substitution. The amide and ethyl ester of N-phenylacetylglycyl-L-proline exhibited antihypoxic activity and could cyclize in biological fluids to form cycloprolylglycine that was identical to the endogenous peptide with antihypoxic, neuroprotective, and other types of neuropsychotropic activity. The antihypoxic effect was stereospecific because the D-enantiomers were inactive. These compounds at concentrations of 10(-7) - 10(-5) M also exhibited neuroprotective activity for SH-SY5Y human neuroblastoma cell culture with 6-hydroxydopamine neurotoxicity. The methylamide and analogous free acid of N-phenylacetylglycylproline could not be cyclized into cycloprolylglycine and were inactive. It was concluded that the activity of the substituted glyprolines was associated with their conversion into cycloprolylglycine.
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