scholarly journals Features of hemostatic activity of 2-[3-methyl-1-h-propyl-7-(1,1-dioxothiethanyl-3) xantinyl-8-thio] acetic acid cyclohexilammonium salt

2013 ◽  
Vol 94 (4) ◽  
pp. 549-552
Author(s):  
F Kh Kamilov ◽  
G A Timirkhanova ◽  
A I Samorodova ◽  
F A Khaliullin ◽  
R A Gubaeva
Keyword(s):  
Acetic Acid ◽  
Male Rats ◽  
Control Group ◽  
Hemostatic Activity ◽  
Platelet Aggregates ◽  
Aggregation Parameters ◽  
Average Size ◽  
Made In

Aim. To study the systemic hemostatic activity of firstly synthesized 2-[3-methyl-1-h-propyl-7-(1,1-dioxotiethanyl-3) xantinyl-8-thio] acetic acid cyclohexilammonium salt in vitro and in vivo. Methods. Experiments in vitro using the blood samples form healthy male donors, and in vivo on male rats by intraperitoneal injection of the equimolar concentrations of researched substances. The effect of the firstly synthesized xantine and etamsylate derivative on the platelet functional activity in vitro and in vivo was studied using a platelet aggregation laser analyzer «Biola 230 LA» (Russia). 20 mkg/ml of adenosinediphosphate and 5 mg/ml of collagen (produced by «Technologia-Standart» company, Russia) were used as an aggregation inducers. Aggregation was analyzed using the AGGR software. General aggregation parameters, maximal aggregation value, maximal aggregation speed, average size of platelet aggregates were analyzed. Experimental assessment of specific systemic hemostatic activity in vivo was made in accordance with the parenchymal hemorrhage model on mature male rats. Coagulation time and blood loss volume were registered. Results. 2-[3-Methyl-1-h-propyl-7-(1,1-dioxotiethanyl-3) xantinyl-8-thio] acetic acid cyclohexilammonium salt showed a pro-aggregative effect both in vitro and in vivo. 2-[3-Methyl-1-h-propyl-7-(1,1-dioxotiethanyl-3) xantinyl-8-thio] acetic acid cyclohexilammonium salt pro-aggregative effect which was observed both in vitro and in vivo increased the systemic hemostatic activity, exceeding the results of the control group and etamsylate group. Conclusion. The findings reveal potentially high systemic hemostatic activity of 2-[3-methyl-1-h-propyl-7-(1,1-dioxotiethanyl-3) xantinyl-8-thio] acetic acid cyclohexilammonium salt and confirm the need for further studies of this compound and its equivalents in order to create highly effective selective hemostasis correctors on their basis.

scholarly journals THE HEMOSTATIC ACTIVITY OF BIS (2-AMINOETHAN-1-SULFONATE) CALCIUM

2018 ◽  
Vol 11 (11) ◽  
pp. 452
Author(s):  
Konstantin G Gurevich ◽  
Aleksandr L Urakov ◽  
Linara I Bashirova ◽  
Aleksandr V Samorodov ◽  
Peter P Purygin ◽  
...  
Keyword(s):  
Male Rats ◽  
Control Group ◽  
Hemorrhagic Diathesis ◽  
Healthy Male ◽  
Systemic Injection ◽  
Hemostatic System ◽  
Stop Time ◽  
Hemostatic Activity

Objective: It is known that local or systemic injection of hemostatic drugs is used to reduce blood loss and number of blood transfusions in patients with hypocoagulation and hemorrhagic diathesis. However, the analysis of literature data shows that the drugs applied for the control of bleeding, traditionally used in medical practice, are not effective enough. This study deals with the systemic hemostatic activity of bis (2-aminoethan-1- sulfonate) calcium in the experiment.Methods: Experimental work in vitro is performed on the blood of healthy male donors, under conditions in vivo it is done on intraperitoneal injection in male rats. Thromboelastography was carried out with apparatus Thromboelastography (TEG) 5000 (Haemoscope Corporation, United States). The influence of first synthesized derivative and ethamsylate on functional activity of platelets was studied using a platelet aggregation analyzer “Biola 230LA” (Russia). Experimental evaluation of the system specific hemostatic activity in vivo was carried out using the model of parenchymatous bleeding in mature male rats. The interference came amid registration of bleeding stop time and extent of blood loss.Results: Bis (2-aminoethan-1-sulfonate) calcium shows procoagulation and proaggregant activity both in vitro and in vivo. Proaggregatory effect of bis (2-aminoethan-1-sulfonate) calcium is successfully implemented in the systemic hemostatic activity in terms of parenchymal bleeding, surpassing the control group and the group of etamsylate.Conclusion: The results of these studies reveal potentially high systemic hemostatic activity of bis (2-aminoethan-1-sulfonate) calcium, urging the need for further study on this compound and its analogs to create on their basis highly efficient, selective correctors of the hemostatic system.

scholarly journals Hepatic one-carbon metabolism in early folate deficiency in rats

1993 ◽  
Vol 291 (1) ◽  
pp. 145-149 ◽  
Author(s):  
M Balaghi ◽  
D W Horne ◽  
C Wagner
Keyword(s):  
Enzyme Activity ◽  
De Novo ◽  
Folate Deficiency ◽  
Male Rats ◽  
Control Group ◽  
Deficient Diet ◽  
Ad Libitum ◽  
Deficient Group

Glycine N-methyltransferase (GNMT) is inhibited by 5-methyltetrahydrofolate polyglutamate in vitro. It is believed to play a regulatory role in the synthesis de novo of methyl groups. We have used the amino-acid-defined diet of Walzem and Clifford [(1988) J. Nutr. 118, 1089-1096] to determine whether folate deficiency in vivo would affect GNMT activity, as predicted by the studies in vitro. Weanling male rats were fed on the folate-deficient diet or a folate-supplemented diet pair-fed to the deficient group. A third group was fed on the folate-supplemented diet ad libitum. Development of folate deficiency rapidly resulted in decreased levels of S-adenosylmethionine (SAM) and elevation of S-adenosylhomocysteine (SAH). The ratios of SAM to SAH were 1.8, 2.7 and 1.5 in the deficient group for weeks 2, 3 and 4 of the experiment, and the values were 9.7, 7.1 and 8.9 for the pair-fed control group and 10.3, 8.8 and 8.0 for the control group ad libitum fed. The activity of GNMT was significantly higher in the deficient group than in either of the two control groups at each time period. This was not due to increased amounts of GNMT protein, but reflected an increase in specific enzyme activity. Levels of folate in both the cytosol and mitochondria were severely lowered after only 2 weeks on the diet. The distribution of folate coenzymes was also affected by the deficiency, which resulted in a marked increase in the percentage of tetrahydrofolate polyglutamates in both cytosol and mitochondria and a very large decrease in cytosolic 5-methyltetrahydrofolate. The increased GNMT activity is therefore consistent with decreased folate levels and decreased inhibition of enzyme activity.

scholarly journals Red kidney bean lectin is a potent cholecystokinin releasing stimulus in the rat inducing pancreatic growth

Gut ◽  
1997 ◽  
Vol 41 (3) ◽  
pp. 333-338 ◽  
Author(s):  
K-H Herzig ◽  
S Bardocz ◽  
G Grant ◽  
R Nustede ◽  
U R Fölsch ◽  
...  
Keyword(s):  
Small Intestine ◽  
Specific Binding ◽  
Male Rats ◽  
Growth Effect ◽  
Control Group ◽  
Maximal Effect ◽  
Pancreatic Growth ◽  
Cck Release

Background—Lectins are proteins capable of specific binding to carbohydrates without altering their covalent structure. As an essential part of plants they are ingested in our daily diet. By binding to glycosyl side chains of receptors lectins can mimic or inhibit the action of the ligand. Oral administration of phytohaemagglutinin (PHA) in rats dose dependently induces growth of the small intestine and the pancreas by an unknown mechanism.Aims—To investigate the mechanism of PHA induced intestinal and pancreatic growth.Methods—Thirty day old male rats were pairfed for 10 days with lactalbumin as a control diet or lactalbumin plus PHA or purified soybean trypsin inhibitor (STI) as a positive control (42 mg/rat/day) with or without 20 μg of the cholecystokinin A (CCK-A) antagonist MK 329. To investigate further the effect of PHA on CCK release intestinal mucosal cells were isolated from rats which were continuously perfused in a perfusion apparatus. CCK release into the medium was assayed.Results—PHA and STI significantly stimulated growth of the pancreas and the small intestine. MK 329 blocked this growth effect in the pancreas but not in the small intestine. In vivo, PHA significantly increased CCK plasma levels from 0.75 to 6.67 (SEM 2.23) compared with 2.3 (0.35) pM in the control group. In addition, in vitro PHA dose dependently stimulated CCK release with a maximal effect at 100 ng/ml.Conclusion—In vivo and in vitro PHA is a potent stimulus for CCK release in the rat, thereby inducing pancreatic growth, whereas intestinal growth is stimulated by a CCK independent mechanism.

scholarly journals Replication of mammalian DNA in vitro. Evidence for initiation from fiber autoradiography.

1979 ◽  
Vol 82 (2) ◽  
pp. 485-493 ◽  
Author(s):  
R Hand ◽  
J R Gautschi
Keyword(s):  
Replication Fork ◽  
Radioactive Tracer ◽  
Cell System ◽  
Unit Size ◽  
Brij 58 ◽  
Thymidine Triphosphate ◽  
Average Size ◽  
Made In

We have used fiber autoradiography to examine the DNA product made in vitro in a lysed cell system. CHO cells were treated with 0.01% Brij-58 and the lysates were incubated at 30 degrees C in a complete reaction mixture for in vitro DNA synthesis with [3H]thymidine triphosphate ([3H]TTP) as the radioactive tracer. Fiber autoradiograms prepared from the DNA showed that it was synthesized on tandemly arranged replication units that were of average size of 20 micrometers, very similar to the size of units found in vivo. The rate of replication fork movement was 25--50% of the in vivo rate. More than 80% of forks stopped functioning by 15 min, and 95% stopped by 60 min. This suggests that synthesis is halted by premature terminations. Evidence for new initiations was provided by replication units with labeled origins in DNA synthesized in an in vitro reaction in which radioactivity was omitted for the first 10 min of incubation. This, plus the observations that the distance between initiation points (replication unit size) is not increased and that premature termination accounts largely for the cessation of synthesis, suggest that significant initiation takes place in this in vitro replication system.

Alcap Delivery Devices and the Sustained Release of Difluoronethylornithine (DFNO) in Vitro and in Vivo Using Male Rats

1987 ◽  
Vol 110 ◽  
Author(s):  
Haned A. Benghuzzi ◽  
Praphulla K. Bajpai
Keyword(s):  
Male Rats ◽  
Control Group ◽  
Sprague Dawley ◽  
Group V ◽  
Group Iii ◽  
Group I ◽  
Body Weights ◽  
Ceramic Implants

AbstractSprague-Dawley albino male rats (25) were divided into five groups consisting of five rats each. Polymer (polylactic acid) impregnated ALCAP capsules filled with 40 mg DFMO were implanted subcutaneously (SC) or intraperitoneally (IP) in Group I and II rats respectively. Rats in Group III were implanted with empty polymer impregnated ALCAP capsules (ALCAP control). Group IV rats were administered orally 3% DFMO in drinking water. Rats in Group V served as controls. Blood samples were collected every week for nine weeks via the tail artery. The concentration of DFNO in the plasma was determined. Data obtained showed that the levels of DFMO in the serum of rats in groups I, I, and IV were 64.71 ±4.08. 219.18 ± 14.48, 16.71 ± 5.21 ug ml−1, respectively at the end of nine weeks. Body weights of the controls and DFMO treated rats were not significantly different (p<0.05). The diarrhea often noted in rats treated orally with DFHO was not observed in rats implanted with ALCAP or ALCAP capsules filled with DFMO. The results of this study suggest that: (1) polymer impregnated ALCAP ceramic implants can be used to deliver DFMO in vivo in a sustained manner for long durations of time, and (2) a ceramic system can be designed to deliver DFNO and drugs such as DFMO in a sustained manner over long durations of time in humans.

Glucocorticoid–dependent maintenance of CYP2C11–dependent oxidation in male rat liver in vivo

2000 ◽  
Vol 19 (2) ◽  
pp. 126-131 ◽  
Author(s):  
M Murray
Keyword(s):  
Rat Liver ◽  
Male Rats ◽  
Male Rat ◽  
Hormonal Factors ◽  
Adrenal Hormones ◽  
Male Specific ◽  
Physiological Correlate ◽  
Made In

1 Hormonal factors participate in the regulation of xenobiotic metabolising enzymes in liver. Hepatic xenobiotic oxidation capacity is decreased in adrena-lectomised rats, which directly implicates adrenal hormones in the control of cytochrome P450 (CYP) expression. In addition, recent studies in cultured hepatocytes have demonstrated that low concentra-tions of glucocorticoid upregulate the male-specific CYP2C11, which is a major enzyme that catalyses xenobiotic and steroid hydroxylations in rat liver. The present study evaluated whether glucocorticoid or mineralocorticoid may be the adrenal factor that contributes to the in vivo expression of CYP2C11 in liver. 2 Adrenalectomy of male rats selectively decreased CYP2C11-dependent 2a-/16a-hydroxylation of testos-terone and other steroid substrates to 60-70% of control, whereas activities mediated by other constitu-tive CYPs were unaffected. The decrease in CYP2C11 activity was due to impaired protein expression in liver after adrenalectomy. Administration of dexametha-sone (DEX; 0.2 mg/kg i.p. daily for 6 days) restored CYP2C11 activity and protein, whereas the mineralo-corticoid deoxycorticosterone (DOC) and adrenocorti-cotropic hormone (ACTH) were ineffective. 3 These findings establish that glucocorticoids have a partial role in the maintenance of CYP2C11 expression and associated microsomal oxidation in liver and provide a physiological correlate for similar observa-tions made in vitro in hepatocyte culture.

In-vitro- und In-vivo-Wirkung von Schilddrüsenhormon auf das Wachstum von Neuroblastomzellen

1990 ◽  
Vol 29 (03) ◽  
pp. 120-124
Author(s):  
R. P. Baum ◽  
E. Rohrbach ◽  
G. Hör ◽  
B. Kornhuber ◽  
E. Busse
Keyword(s):  
Cell Differentiation ◽  
Neuroblastoma Cells ◽  
Control Group ◽  
Initial Value ◽  
Initial Rise ◽  
Biphasic Effect ◽  
Contrast Microscopy ◽  
Morphological Sign

The effect of triiodothyronine (T3) on the differentiation of cultured neuroblastoma (NB) cells was studied after 9 days of treatment with a dose of 10-4 M/106 cells per day. Using phase contrast microscopy, 30-50% of NB cells showed formation of neurites as a morphological sign of cellular differentiation. The initial rise of the mitosis rate was followed by a plateau. Changes in cyclic nucleotide content, in the triphosphates and in the activity of the enzyme ornithine decarboxylase (ODC) were assessed in 2 human and 2 murine cell lines to serve as biochemical parameters of the cell differentiation induced by T3. Whereas the cAMP level increased significantly (3 to 7 fold compared with its initial value), the cGMP value dropped to 30 to 50% of that of the control group. ATP and GTP increased about 200%, the ODC showed a decrease of about 50%. The present studies show a biphasic effect of T3 on neuroblastoma cells: the initial rise of mitotic activity is followed by increased cell differentiation starting from day 4 of the treatment.

In Vivo Effect of Suloctidil as an Antiplatelet Agent

1979 ◽  
Vol 41 (03) ◽  
pp. 465-474 ◽  
Author(s):  
Marcia R Stelzer ◽  
Thomas S Burns ◽  
Robert N Saunders
Keyword(s):  
Ex Vivo ◽  
Antiplatelet Agent ◽  
Ratio Method ◽  
Platelet Aggregate ◽  
Permanent Effect ◽  
Platelet Aggregates ◽  
5 Ht Uptake ◽  
High Doses

SummaryThe relationship between the effects of suloctidil in vivo as an antiplatelet agent and in vitro as a modifier of platelet serotonin (5-HT) parameters was investigated. Suloctidil was found to be effective in reducing platelet aggregates formation in the retired breeder rat as determined using the platelet aggregate ratio method (PAR) with an ED50 of 16.1 mg/kg 24 hours post administration. In contrast to the hypothesis that 5-HT depletion is involved in the anti-aggregatory mechanism of suloctidil, no correlation was found between platelet 5- HT content and this antiplatelet activity. Reduction of platelet 5-HT content required multiple injections of high doses (100 mg/kg/day) of suloctidil. Suloctidil administration for 8 days at 100 mg/kg/day, which lowered platelet 5-HT content by 50%, resulted in no permanent effect on ex vivo platelet 5-HT uptake or thrombin-induced release, nor alteration in the plasma 5-HT level. However, these platelets exhibited a short-lived, significant increase in percent leakage of 5-HT after 30 minutes of incubation. Therefore, suloctidil treatment at high doses may with time result in platelet 5-HT depletion, however this effect is probably not related to the primary anti-aggregatory activity of the drug.

Accumulation of Macromolecular Particles in the Reticuloendothelial System (RES) Mediated by Platelet Aggregation and Disaggregation

1969 ◽  
Vol 22 (03) ◽  
pp. 496-507 ◽  
Author(s):  
W.G van Aken ◽  
J Vreeken
Keyword(s):  
Platelet Aggregation ◽  
Degradation Products ◽  
Reticuloendothelial System ◽  
Caproic Acid ◽  
Carbon Particles ◽  
Carbon Clearance ◽  
Aggregation And Disaggregation ◽  
Platelet Aggregates

SummaryCarbon particles cause platelet aggregation in vitro and in vivo. Prior studies established that substances which modify thrombocyte aggregation also influence the rate at which carbon is cleared from the blood.This study was performed in order to elucidate the mechanism by which the carbon-platelet aggregates specifically accumulate in the RES.Activation of fibrinolysis by urokinase or streptokinase reduced the carbon clearance rate, probably due to generated fibrinogen degradation products (FDP). Isolated FDP decreased the carbon clearance and caused disaggregation of platelets and particles in vitro. Inhibition of fibrinolysis by epsilon-amino-caproic acid (EACA), initially accelerated the disappearance of carbon and caused particle accumulation outside the RES, predominantly in the lungs. It is supposed that platelet aggregation and locally activated fibrinolysis act together in the clearance of particles. In the normal situation the RES with its well known low fibrinolytic activity, becomes the receptor of the particles.

Protective Effect of Boswellic Resin Against Memory Loss and Alzheimer’s Induced by Aluminum Tetrachloride and D-Galactose (Experimental study in Mice)

2020 ◽  
Author(s):  
K. Zerrouki ◽  
N. Djebli ◽  
L. Gadouche ◽  
I. Erdogan Orhan ◽  
F. SezerSenol Deniz ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Protective Effect ◽  
Cell Damage ◽  
Memory Loss ◽  
Control Group ◽  
Total Extract ◽  
Swiss Mice ◽  
Octyl Acetate

Nowadays, because of the industrialization, a lot of contaminant were available ; the consequences of this availability are apparition of diseases including neurodegeneration. Neurodegenerative diseases of the human brain comprise a variety of disorders that affect an increasing percentage of the population. This study is based on the effect of the Boswellic resin, which is from a medicinal plant and known for its antioxidant effects on nerve cell damage. The objective of this work was to evaluate the in vitro and in vivo effects of the Boswellic resin on anticholinesterase activity and Alzheimer’s disease (AD) induced by D-galactose and aluminum tetrachloride in Swiss mice. Chemical composition of the resin essential oil was identified by the CG-MS analysis. The antioxidant activity was also assessed by the DMPD and metal chelation methods. In order to understand the mechanism of memory improvement, the acetylcholinesterase, AChE, and butyrylcholinesterase, BChE, inhibitory assays were performed. In vivo part of the study was achieved on Swiss mice divided into four groups: control, AD model, treated AD, and treated control group. The identification of chemical composition by CG-MS reach the 89.67% of the total extract compounds presented some very important molecules (p-Cymene, n-Octyl acetate, α-Pinene…). The present study proves that Boswellic resin improves memory and learning in treated Alzheimer’s group, modulates the oxidative stress and be involved in the protective effect against amyloid deposition and neurodegeneration, and stimulates the immune system in mice’s brain.

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