scholarly journals Investigation of Aronia Melanocarpa Fruit Juice for Sedative-Hypnotic Effects in Rats

2018 ◽  
Vol 11 (1) ◽  
pp. 77-82
Author(s):  
Miroslav Ts. Eftimov ◽  
StefkaV. Valcheva-Kuzmanova

Summary Aronia melanocarpa fruit juice (AMFJ) has been intensively studied for effects on the central nervous system. The study aimed to investigate AMFJ for possible sedative-hypnotic effects in rats after acute and subchronic administration. Male Wistar rats were treated orally with three doses of AMFJ (2.5, 5.0 and 10.0 ml/kg) either once (acute treatment) or in 30 days (subchronic treatment). Control rats were similarly treated with distilled water. The tests were performed 1 hour after the last AMFJ administration. The possible sedative-hypnotic effects of the juice were investigated in the open field test (OFT) and thiopental-induced sleeping time test. Substances with sedative-hypnotic effects decrease locomotor activity in the OFT and prolong the time of thiopental-induced sleep. The results from the OFT showed that neither the acute, nor the subchronic treatment of rats with all AMFJ doses affected the horizontal and vertical locomotor activity significantly. The two patterns of administration of AMFJ (acute and subchronic) had no significant effect on the duration of thiopental-induced sleep. The lack of effect of AMFJ on locomotor activity and the lack of prolongation of thiopental-induced sleep showed that AMFJ did not display sedative-hypnotic effects in rats.

2016 ◽  
Vol 35 (9) ◽  
pp. 958-965 ◽  
Author(s):  
VR Coelho ◽  
K Sousa ◽  
TR Pires ◽  
DKM Papke ◽  
CG Vieira ◽  
...  

Vigabatrin (VGB) is an antiepileptic drug thatincreases brain γ-aminobutyric acid (GABA) levels through irreversible inhibition of GABA transaminase. The aim of this study was to evaluate neurotoxicological effects of VGB measuring motor activity and genotoxic and mutagenic effects after a single and repeated administration. Male Wistar rats received saline, VGB 50, 100, or 250 mg/kg by gavage for acute and subchronic (14 days) treatments and evaluated in the rotarod task. Genotoxicity was evaluated using the alkaline version of the comet assay in samples of blood, liver, hippocampus, and brain cortex after both treatments. Mutagenicity was evaluated using the micronucleus test in bone marrow of the same animals that received subchronic treatment. The groups treated with VGB showed similar performance in rotarod compared with the saline group. Regarding the acute treatment, it was observed that only higher VGB doses induced DNA damage in blood and hippocampus. After the subchronic treatment, VGB did not show genotoxic or mutagenic effects. In brief, VGB did not impair motor activities in rats after acute and subchronic treatments. It showed a repairable genotoxic potential in the central nervous system since genotoxicity was observed in the acute treatment group.


2018 ◽  
Vol 13 (8) ◽  
pp. 1934578X1801300
Author(s):  
Gislei F. Aragão ◽  
Manoel O. de Moraes Filho ◽  
Paulo N. Bandeira ◽  
Antônio P. Frota Junior ◽  
Yasmin Ingrid S. Oliveira de ◽  
...  

A triterpenic mixture of α and β-amyrin (AMY) extracted from Protium heptaphyllum has demonstrated several pharmacological effects, including activity in the central nervous system. The aim of this study was to evaluate the effect of AMY administration on locomotor activity of mice by the open field test using some monoaminergic agonists and antagonists and the cerebral cortex levels of monoamines and their major metabolites by high-performance liquid chromatography. Mice were treated acutely with AMY at doses of 1, 2.5 and 5 mg/kg given intraperitoneally and with the pharmacological agents and placed in open field test, then the animals were sacrificed and the cerebral cortex extracted, and monoamines were assayed in tissue homogenates. AMY at 1, 2.5 and 5 mg/kg decreased locomotor activity of animals by 25, 31 and 39%, respectively in the open field test. Ondasentron, doxazosin, oxymetazoline and clonidine did not reverse the inhibitory effect of 5 mg/kg AMY. Venlafaxine and yohimbine reversed the inhibitory effect of 5 mg AMY. In the cortex, the 5-HT and 5-HIAA were significantly reduced by the administration of AMY. NE and HVA were also reduced with 2.5 and 5 mg/kg AMY, while Dopamine and DOPAC were not increased with AMY. In conclusion, AMY decreased locomotor activity of animals accompanied by a decrease in 5-HT and NE levels in the cerebral cortex, this locomotor effect is reversed by drug that blocker the α-2-adrenoreceptor.


2016 ◽  
Vol 33 (S1) ◽  
pp. s289-s289
Author(s):  
Y. Zhang ◽  
F. Liu ◽  
Z. Dai ◽  
B. Wu ◽  
Q. Wu

ObjectiveTo observe the effect of Qing Huan Ling and (or) risperidone on locomotor activity and explorative behavior of schizophrenia mice model by open field test.MethodsSeventy kunming mice were randomly divided into 5 groups, one group as blank group. The rest groups ip MK-801 continuously 14 day, then randomly numbered: model group, risperidone group, Qing Huan Ling group and risperidone combined Qing Huan Ling group. Ig give corresponding drugs for each group 4 weeks, observe the change of locomotor activity and explorative behavior by open field test.ResultsAfter Ig 4 weeks, compared with the blank group, there were no obvious difference in locomotor activity and explorative behavior between risperidone group, Qing Huan Ling group and the combined group. Compared with the model group, risperidone had statistics meaning in the repression of explorative behavior (P < 0.05),the combined group has statistics meaning in the repression of locomotor activity and explorative behavior (78.92 ± 36.18 m vs. 186.92 ± 41.08 m, P < 0.01).ConclusionQing Huan Ling regulate the central nervous system of schizophrenia mice model; when combined with risperidone, it restrain the central nervous system of schizophrenia mice model and the effect is stronger than risperidone alone.Disclosure of interestThe authors have not supplied their declaration of competing interest.


Folia Medica ◽  
2019 ◽  
Vol 61 (4) ◽  
pp. 579-583 ◽  
Author(s):  
Vesela A. Borisova ◽  
Miroslav Tz. Eftimov ◽  
Stefka V. Valcheva-Kuzmanova

Background: The fruit juice from Chaenomeles japonica var. maulei (Mast.) Lavall,e is very rich in polyphenolic compounds. Aim: The aim of the current study was to investigate the effects of Chaenomeles maulei fruit juice (CMFJ) on reserpine-induced beha-vioral changes in rats. Materials and methods: The experimental design included a total of 50 animals, divided in the following groups: control, R, R+CMFJ2.5, R+CMFJ5, and R+CMFJ10. All groups except the control received a single intraperitoneal injection of reserpine while the Control group was injected with the vehicle. CMFJ was applied through an orogastric cannula at 0, 19, and 23 hours after reserpine injection at doses of 2.5 ml/kg, 5 ml/kg, and 10 ml/kg to groups R+CMFJ2.5, R+CMFJ5, and R+CMFJ10, respectively. The groups control and R received distilled water (10 ml/kg) at the same time points. The open field test (OFT) and the forced swim test (FST) were carried out. In the OFT, crossings and rearings were recorded as a measure of locomotor activity. In the FST, the immobility time served as a measure of depressive-like behavior. Results: In the OFT, the number of crossings of rats were significantly reduced (p<0.05) by reserpine. CMFJ antagonized the effects of reserpine on rat locomotor activity. In the FST, reserpine caused an insignificant reduction of the immobility time while CMFJ reversed this effect probably by increasing the locomotor activity. Conclusion: CMFJ reversed reserpine-induced hypokinesia in rats. This effect of CMFJ might be attributed to the polyphenols found in very high concentrations in the juice.


2020 ◽  
Vol 19 (5) ◽  
pp. 336
Author(s):  
Luiza Minato Sagrillo ◽  
Viviane Nogueira De Zorzi ◽  
Luiz Fernando Freire Royes ◽  
Michele Rechia Fighera ◽  
Beatriz Da Silva Rosa Bonadiman ◽  
...  

Physical exercise has been shown to be an important modulator of the antioxidant system and neuroprotective in several diseases and treatments that affect the central nervous system. In this sense, the present study aimed to evaluate the effect of physical exercise in dynamic balance, motor coordination, exploratory locomotor activity and in the oxidative and immunological balance of rats treated with vincristine (VCR). For that, 40 adult rats were divided into two groups: exercise group (6 weeks of swimming, 1h/day, 5 days/week, with overload of 5% of body weight) and sedentary group. After training, rats were treated with 0.5 mg/kg of vincristine sulfate for two weeks or with the same dose of 0.9% NaCl. The behavioral tests were conducted 1 and 7 days after each dose of VCR. On day 15 we carried out the biochemical analyzes of the cerebellum. The physical exercise was able to protect against the loss of dynamic balance and motor coordination and, had effect per se in the exploratory locomotor activity, and neutralize oxidative stress, damage DNA and immune damage caused by VCR up to 15 days after the end of the training protocol. In conclusion, we observed that previous physical training protects of the damage motor induced by vincristine.Key-words: exercise, oxidative stress, neuroprotection, cerebellum.


2019 ◽  
Vol 15 (1) ◽  
pp. 102-118 ◽  
Author(s):  
Carolina Campos-Rodríguez ◽  
José G. Trujillo-Ferrara ◽  
Ameyali Alvarez-Guerra ◽  
Irán M. Cumbres Vargas ◽  
Roberto I. Cuevas-Hernández ◽  
...  

Background: Thalidomide, the first synthesized phthalimide, has demonstrated sedative- hypnotic and antiepileptic effects on the central nervous system. N-substituted phthalimides have an interesting chemical structure that confers important biological properties. Objective: Non-chiral (ortho and para bis-isoindoline-1,3-dione, phthaloylglycine) and chiral phthalimides (N-substituted with aspartate or glutamate) were synthesized and the sedative, anxiolytic and anticonvulsant effects were tested. Method: Homology modeling and molecular docking were employed to predict recognition of the analogues by hNMDA and mGlu receptors. The neuropharmacological activity was tested with the open field test and elevated plus maze (EPM). The compounds were tested in mouse models of acute convulsions induced either by pentylenetetrazol (PTZ; 90 mg/kg) or 4-aminopyridine (4-AP; 10 mg/kg). Results: The ortho and para non-chiral compounds at 562.3 and 316 mg/kg, respectively, decreased locomotor activity. Contrarily, the chiral compounds produced excitatory effects. Increased locomotor activity was found with S-TGLU and R-TGLU at 100, 316 and 562.3 mg/kg, and S-TASP at 316 and 562.3 mg/kg. These molecules showed no activity in the EPM test or PTZ model. In the 4-AP model, however, S-TGLU (237.1, 316 and 421.7 mg/kg) as well as S-TASP and R-TASP (316 mg/kg) lowered the convulsive and death rate. Conclusion: The chiral compounds exhibited a non-competitive NMDAR antagonist profile and the non-chiral molecules possessed selective sedative properties. The NMDAR exhibited stereoselectivity for S-TGLU while it is not a preference for the aspartic derivatives. The results appear to be supported by the in silico studies, which evidenced a high affinity of phthalimides for the hNMDAR and mGluR type 1.


2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Jimena Soutelo ◽  
Yanina Alejandra Samaniego ◽  
Elsa Zotta ◽  
María Cecilia Fornari ◽  
Carlos Reyes Toso ◽  
...  

Background. There is a gender disparity in the incidence, prevalence, and progression of renal disease. The object of this paper is to evaluate the presence and type of renal lesion in normogonadic and hypogonadic male rats in a mild hyperuricemia induced condition and exposed to a high-fructose diet. Methods. 56 adult male Wistar rats were used. Animals were divided into two groups, one normogonadic (NGN) and one hypogonadic (HGN), and each group was divided into four subgroups in accordance with the treatment: control with only water (C), fructose (F), oxonic acid (OA), and fructose + oxonic acid (FOA). Renal changes were evaluated by measuring glomerulosclerosis, fibrosis, and arteriolar media/lumen (M/L) ratio.Results. The OA and FOA groups presented significantly hypertension (p<0.001). The OA group significantly increased (p<0.05) the percentage of glomerulosclerosis as well as the FOA group (p<0.001). When comparing NGN versus HGN, we observed a trend to a lower glomerulosclerosis in the latter. A higher arteriolar M/L ratio was observed in the OA (p<0.05) and FOA (p<0.001). Conclusion. Hyperuricemia conditions and a high-fructose diet favor blood pressure increase together with changes in the arteriolar media/lumen ratio and renal glomerular damage. These changes were more apparent in normogonadic animals.


2020 ◽  
Author(s):  
William N. Sanchez ◽  
Jose A. Pochapski ◽  
Leticia F. Jessen ◽  
Marek Ellenberger ◽  
Rainer K. Schwarting ◽  
...  

AbstractBackground and PurposeCurrently, no effective drug exists to treat cocaine use disorders, which affect millions of people worldwide. Benzodiazepines are potential therapeutic candidates, as microdialysis and voltammetry studies have shown that they can decrease dopamine release in the nucleus accumbens of rodents. In addition, we have recently shown that diazepam blocks the increase in dopamine release and the affective marker 50-kHz ultrasonic vocalizations (USV) induced by DL-amphetamine in rats.Experimental ApproachHere we tested whether administration of 2.5 mg·kg−1 diazepam (i.p.) in adult male Wistar rats could block the effects of 20 mg·kg−1 cocaine (i.p.) on electrically evoked phasic dopamine release in the nucleus accumbens measured by fast-scan cyclic voltammetry, as well as 50-kHz USV and locomotor activity.Key ResultsCocaine injection increased evoked dopamine release up to 3-fold within 5 min and the increase was significantly higher than baseline for at least 90 min. The injection of diazepam 15 min later attenuated the cocaine effect by nearly 50% and this attenuation was maintained for at least 30 min. Stimulant drugs, natural rewards and reward predictive cues are known to evoke 50-kHz USV in adult rats. In the present study, cocaine increased the number of 50-kHz USV of the flat, step, trill, and mixed kinds by 12-fold. This effect was at maximum 5 min after cocaine injection, decreased with time and lasted at least 40 min. Diazepam significantly blocked this effect for the entire duration of the session. The distance travelled by control rats during a 40-min session of exploration in an open field was at maximum in the first 5 min and decayed progressively until the end of the session. Cocaine-treated rats travelled significantly longer distances when compared to the control group, while diazepam significantly attenuated cocaine-induced locomotion by up to 50%.Conclusions and implicationThese results suggest that the neurochemical, affective, and stimulant effects of cocaine can be mitigated by diazepam.What is already knownDiazepam decreases dopamine release in the rodent nucleus accumbens (NAc) and reduces some effects produced by DL-amphetamine.What this study addsDiazepam attenuated the increase in phasic dopamine release caused by cocaine.Diazepam blocked the effect of cocaine on 50-kHz USV and locomotor activity.Clinical significanceThis study demonstrates that diazepam can block specific effects of cocaine that likely contribute to addiction.


2020 ◽  
Vol 6 (4) ◽  
pp. 51-57
Author(s):  
Ekaterina E. Yakovleva ◽  
Eugeny R. Bychkov ◽  
Maria M. Brusina ◽  
Levon B. Piotrovsky ◽  
Petr D. Shabanov

Objective: To study the antiparkinsonian activity of new 1,2-substituted imidazole-4,5-dicarboxylic acids in dopaminergic transmission suppression tests in mice and rats. Materials and methods: On a model of reserpine extrapyramidal disorders, the derivatives of imidazole-dicarboxylic acids (IEM2258, IEM2248, IEM2247) were injected into the lateral brain ventricles of the mice 30 minutes after injecting reserpine at the doses of 0.1–0.5 mmol. Locomotor activity was analyzed in the Open-field test 2 hours later. In the catalepsy model, the studied agents were injected, using a pre-implanted cannula, with a simultaneous intraperitoneal injection of haloperidol. The severity of catalepsy was assessed with the Morpurgo method. Amantadine was used as a comparator drug in all the tests. Results: It was shown that IEM2258 significantly increased the main indicators of locomotor activity in the Open-field test at all the studied doses. The value of the antiparkinsonian effect of IEM2258 at doses of 0.4–0.5 mmol significantly exceeded that of amantadine. The antiparkinsonian effect of IEM2247 was maximally expressed and was significantly different from those in the control and comparator group at doses of 0.2 and 0.3 mmol. For all the experimental groups, a significant decrease in the manifestations of catalepsy in comparison with control indexes was determined. Discussion: The results made it possible to suggest the involvement of imidazole-4,5-dicarboxylic acids derivatives in the process of experimental improvement of dopaminergic neuromodulation and efficiency in animals. Conclusion: The data showed a significant dose-dependent antiparkinsonian activity of new imidazole-4,5-dicarboxylic acid derivatives, which makes it promising to develop these agents and to further search for effective and safe antiparkinsonian drugs in this pharmacological class. Graphical abstract


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