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ABSTRACT: Dihydroquercetin effects on the tone of isolated segments of the portal vein of rats were studied. Dihydroquercetin did not modify the basal venous tone, but reduced the amplitude of contractions induced by KCl and norepinephrine hydrotartrate.
Bulletin of Experimental Biology and Medicine 04/2013; 155(1):65-6. · 0.27 Impact Factor
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ABSTRACT: The pharmacokinetics of thiophane have been studied using HPLC. It is demonstrated that the absorption of thiophane upon intragastric
administration at a dose of 100 mg/kg does not exceed 50%. The drug is not excreted with urine but is eliminated in an unchanged
form with bile and is partly metabolized. Thiophane distributes in organs with high perfusion (brain, heart), accumulates
extensively in the liver, and is almost not found in organs with low perfusion
Key wordsthiophane-pharmacokinetics-HPLC
Pharmaceutical Chemistry Journal 04/2012; 44(4):171-174. · 0.37 Impact Factor
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ABSTRACT: Hemorheological and antiaggregant properties of new o-isobornylphenol derivatives were investigated in ex vivo experiments. 4-Methyl-2,6-diisobornylphenol and 2-(dibutylamino)methyl-4-methyl-6-isobornylphenol hydrochloride demonstrated
the maximum hemorheological activity. After intragastric administration, these compounds decreased the blood viscosity at
low shear rates, suppressed the development of blood “hyperviscosity” before incubation (20.0 ± 0.4°C, 1 h), and reduced ADP-induced
(4 × 10–6 M) aggregation of platelets. The hemorheological and antiaggregant effects of the investigated compounds were comparable
to those of pentoxifylline.
Key words
o-isobornylphenol–derivatives–synthesis–hemorheological properties–antiaggregant properties
Pharmaceutical Chemistry Journal 04/2012; 44(10):530-533. · 0.37 Impact Factor
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ABSTRACT: Methods for monitoring the quality of the new pharmaceutical substance 4-methyl-2,6-diisobornylphenol (dibornol) were developed.
Key wordsDibornol substance–analytical methods
Pharmaceutical Chemistry Journal 04/2012; 44(11):639-641. · 0.37 Impact Factor
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M. B. Plotnikov,
A. M. Dygai,
O. I. Aliev,
G. A. Chernyshova,
V. I. Smol’yakova,
A. S. Vasil’ev,
V. A. Markov,
E. V. Vyshlov,
E. I. Vereschagin,
D. N. Kinsht,
P. G. Madonov
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ABSTRACT: We studied the antithrombotic and thrombolytic effects of Trombovazim, a highlypurified proteolytic enzyme preparation obtained
by immobilization of bacterial proteinases (Bacillus) on polyethylene oxide with a molecular weight of 1.5 kDa. Blood absorption of the preparation was evaluated after intragastric
administration. In vitro experiments showed that Trombovazim produces anticoagulant and thrombolytic effects, which manifested in inhibition of fibrin
clot formation and acceleration of its lysis. Drug concentration in the blood was elevated from the 4th to the 7th hour after
intragastric administration of Trombovazim in a dose of 2250 U/kg, being maximum by the 5th hour (0.044±0.011 U/ml). Course treatment with Trombovazim (1000 U intragastrically, twice daily for 3 days) had a thrombolytic
effect on rats with experimental intravascular thrombosis. This effect was manifested in a decrease in thrombus weight and
increase in the percent of rats with recanalization of the occluded carotid artery.
Bulletin of Experimental Biology and Medicine 04/2012; 147(4):438-440. · 0.27 Impact Factor
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ABSTRACT: Venous hypertension and swelling of the hind limbs was demonstrated to develop in rat model of chronic venous insufficiency. It was found that 14-day course of dihydroquercetin (50 mg/kg) and lipoic acid (50 mg/kg) administered intragastrically prevented the increase in hind limb volume and reduced the severity of edema of rat muscle tissue in chronic venous insufficiency.
Bulletin of Experimental Biology and Medicine 11/2011; 152(1):25-7. · 0.27 Impact Factor
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ABSTRACT: Distribution of p-tyrosol in organism was studied in rats after a single intravenous administration in a dose of 200 mg/kg. It was shown that p-tyrosol rapidly penetrates into well perfused organs (brain, heart, kidneys). The maximum concentration ofp-tyrosol in these organs was determined in 1 minute after administration, and the mean distribution constant was within 0.8-1.11. The albumin bound fraction ofp-tyrozol amounted to 0.26-0.30.
Eksperimental'naia i klinicheskaia farmakologiia 01/2011; 74(7):27-9.
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ABSTRACT: Structural changes of eye chorioretinal complex were investigated in 40 adult male outbred albino rats after total transient cerebral ischemia using electron microscopy and morphometric analysis. Furthermore, the influence of a new sterically hindered phenolic antioxidant dibornol on these processes was estimated. Our studies demonstrated that total transient cerebral ischemia in rats resulted in the capillary thrombosis of the choriocapillary lamina of the uvea, structural disturbances of the blood-retinal barrier, degeneration of the retinal neurons and radial glia. Course administration of dibornol was shown to improve the microcirculation and to protect the retinal neuronal structures, pigment epithelium, and radial glia.
Morfologiia (Saint Petersburg, Russia) 01/2011; 140(6):43-7.
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ABSTRACT: Optimum design of preclinical research for pharmacological agents influencing the rheological properties of blood is presented. Models of hyperviscosity syndrome and approaches to studying the hemorheological activity mechanisms are described.
Eksperimental'naia i klinicheskaia farmakologiia 01/2011; 74(12):36-9.
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ABSTRACT: A hepatoprotective effect of thiophan was studied on the model of carbon tetrachloride-induced hepatitis in rats. Therapeutic administration of thiophan repairs the antitoxic function of liver, normalizes cytolysis marker activity, and improves the synthetic function of liver and the carbohydrate and lipid metabolism. The hepatoprotective activity of thiophan is similar to effect of silimarin.
Eksperimental'naia i klinicheskaia farmakologiia 01/2011; 74(8):37-40.
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ABSTRACT: The administration of the extract from Rhaponticum carthamoides (150 mg/kg, p.o., for 10 days) in combination with dosed low-power exercise in rats with experimental myocardial infarction led to an improvement of hemorheological indices, which was manifested by a decrease in the whole blood viscosity, aggregation of erythrocytes, and increase in erythrocyte deformability. In particular, the extract from R. carthamoides contributed to an increase in the hematocrit/blood viscosity, which was indicative of an improvement of the blood overall oxygen transport capacity. In addition, administration of the extract in combination with dosed exercise favored normalization of the lactate and pyruvate concentrations in blood of rats with myocardial infarction.
Eksperimental'naia i klinicheskaia farmakologiia 01/2011; 74(9):7-10.
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ABSTRACT: The pharmacokinetics of 4-methyl-2,6-diisobornylphenol (MDIBP) in rat blood plasma has been studied after intravenous injection. The drug concentration in the plasma was determined using a reverse-phase HPLC procedure. It is shown that MDIBP rapidly penetrates into intensively perfused organs, but is slowly eliminated from the organism (MRT value amounting to 9 h).
Eksperimental'naia i klinicheskaia farmakologiia 01/2011; 74(9):20-2.
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ABSTRACT: Hemorheological activity of 4-methyl-2,6-di-isobornyl phenol, a new o-isobornyl phenol derivative, was studied under conditions of experimental prolonged partial cerebral ischemia. Brain ischemia is associated with hemorheological disorders which can be characterized as blood hyperviscosity syndrome: increased viscosity of the whole blood (within a wide range of shear rates), plasma viscosity, fibrinogen content in blood plasma, and platelet aggregation; deterioration of platelet deformability and reduced availability of oxygen for tissues. A course (5 days) of intragastric 4-methyl-2,6-di-isobornyl phenol (100 mg/kg) prevented the development of blood hyperviscosity syndrome by modulating blood macrorheology (reduction of plasma viscosity and fibrinogen content) and microrheology (reduction of erythrocyte aggregation and improvement of their deformability).
Bulletin of Experimental Biology and Medicine 11/2010; 149(6):721-3. · 0.27 Impact Factor
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ABSTRACT: Along with microangiopathy, one of the main causes of blindness in diabetic retinopathy consists of degeneration of retinal neurons. Electron microscopy and morphometric analysis were used to study structural changes in neurosensory cells, associative, and ganglion neurons in the retina in 30 while mongrel male rats with streptozotocin diabetes for two months and the effects of a new semisynthetic antioxidant 4-methyl-2,6-diisobornylphenol, a screened phenol, were evaluated. Destructive changes were found to affect the outer segments of neurosensory cells and ganglion neurons. The number density of neurosensory and ganglion cells decreased, and the proportion of these cells with pyknotic nuclei increased. 4-Methyl-2,6-diisobornylphenol had neuroprotective actions, preventing destructive changes to neurosensory cells and ganglion neurons.
Neuroscience and Behavioral Physiology 09/2010; 40(7):779-82.
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ABSTRACT: Carbon tetrachloride-induced hepatitis in rats is accompanied by blood hyperviscosity syndrome development. A course intragastric administration of thiophane under these conditions prevents the increase in whole blood viscosity by normalizing the microrheological indices (deformability and aggregation of erythrocytes), which is manifested by increasing oxygen availability for tissues.
Eksperimental'naia i klinicheskaia farmakologiia 08/2010; 73(8):32-4.
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ABSTRACT: The new multifunctional antioxidant 3,5-dimethyl-4-hydroxybenzylthiododecane (DHBD) demonstrated high activity both in vitro and in vivo. Experiments in vitro showed that the antioxidant activity of DHBD significantly exceeded that of the well-known reference drug ionol. A course
of DHBD administration (100 mg/kg, p.o.) significantly decreased the content of lipid peroxidation products in rat brain on
the model of long-term incomplete cerebral ischemia.
Pharmaceutical Chemistry Journal - PHARM CHEM J. 01/2010; 44(4):189-191.
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ABSTRACT: We demonstrated in experiments on rats with left coronary artery occlusion that intravenous administration of 20 mg/kg n-tyrosol during ischemia limited manifestations of oxidative stress in myocardial tissue during early post reperfusion period: content of diene and triene conjugates lowered 16 and 20%, respectively. This was associated with higher preservation of cardiomyocytes and reduction of the infarction zone.
Kardiologiia 01/2010; 50(11):47-9. · 0.20 Impact Factor
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M B Plotnikov,
A M Dygai,
O I Aliev,
G A Chernyshova,
V I Smol'yakova,
A S Vasil'ev,
V A Markov,
E V Vyshlov,
E I Vereschagin,
D N Kinsht,
P G Madonov
[show abstract]
[hide abstract]
ABSTRACT: We studied the antithrombotic and thrombolytic effects of Trombovazim, a highly-purified proteolytic enzyme preparation obtained by immobilization of bacterial proteinases (Bacillus) on polyethylene oxide with a molecular weight of 1.5 kDa. Blood absorption of the preparation was evaluated after intragastric administration. In vitro experiments showed that Trombovazim produces anticoagulant and thrombolytic effects, which manifested in inhibition of fibrin clot formation and acceleration of its lysis. Drug concentration in the blood was elevated from the 4th to the 7th hour after intragastric administration of Trombovazim in a dose of 2250 U/kg, being maximum by the 5th hour (0.044+/-0.011 U/ml). Course treatment with Trombovazim (1000 U intragastrically, twice daily for 3 days) had a thrombolytic effect on rats with experimental intravascular thrombosis. This effect was manifested in a decrease in thrombus weight and increase in the percent of rats with recanalization of the occluded carotid artery.
Bulletin of Experimental Biology and Medicine 05/2009; 147(4):438-40. · 0.27 Impact Factor
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[show abstract]
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ABSTRACT: Cerebral ischemia in rats was accompanied by an increase in erythrocyte degradation, which results from changes in lipid composition of their membranes. The content of lipids and phospholipid fraction (phosphatidylcholine, sphingomyelin, and phosphatidylserine) decreased, while the relative content of lysophospholipids increased in erythrocyte membranes. The course of treatment with Rhaponticum carthamoides extract (150 mg/kg perorally, 5 days) contributed to an increase in the contents of total lipids and phospholipids (primarily of sphingomyelin and phosphatidylserine) and decrease in the ratio of lysophospholipids in the erythrocyte membrane of rats with cerebral ischemia. Morphological characteristics of erythrocytes returned to normal, which manifested in an increase in the number of discocytes and decrease in the count of degenerated cells.
Bulletin of Experimental Biology and Medicine 08/2008; 146(1):45-8. · 0.27 Impact Factor
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ABSTRACT: We studied antithrombogenic and antiplatelet properties of 4-methyl-2,6-diisobornyl phenol, a new promising compound belonging to ortho-isobornyl phenol derivatives, under conditions of intravascular thrombosis and acute cerebral ischemia. It was found that 4-methyl-2,6-diisobornyl phenol prevents intravascular thrombus formation by reducing platelet aggregation and improving antiplatelet activity of the vascular wall.
Bulletin of Experimental Biology and Medicine 04/2008; 145(3):328-30. · 0.27 Impact Factor
