Anticompulsive effects of novel derivatives of coumarin in rats

2021 ◽  
Vol 19 (3) ◽  
pp. 339-344
Author(s):  
Bakhodir B. Daliev ◽  
Eugenii R. Bychkov ◽  
Leonid V. Myznikov ◽  
Andrei A. Lebedev ◽  
Petr D. Shabanov

BACKGROUND: Until now, the neurotropic effect, in particular the effect on the emotional behavior of oxy-coumarins, has not been adequately studied. There are only few data on their central action. Currently, research is underway on the synthesis of new compounds based on natural oxy-coumarins, which will potentially have a higher biological activity. AIM: Was to study the central action of new oxycoumarin-based compounds IEM-2886, LVM-99, LVM-S144, in particular, on compulsive behavior in rats. MATERIALS AND METHODS: To assess the behavior of Wistar rats, the Marble-test and Elevated plus maze methods were used. Oxycoumarin derivatives (IEM-2886, LVM-99, LVM-S144) were injected intraperitoneally at doses of 1, 10 and 25 mg/kg. The effectiveness of the drugs was judged by the number of balls buried in the Marble test and by the duration of staying in the open and closed sleeves of the Elevated plus maze. Results. It was shown that in the Marble test, oxycoumarin-based compounds (IEM-2886, LVM-99, LVM-S144) caused a decrease in the number of buried balls, which shows their anti-compulsive effect. After administration of IEM-2886, LVM-99, LVM-S144 (125 mg / kg) compounds, dose-dependent effects were observed (p 0.05). The elevated plus maze test did not show the anxiolytic effect typical for tranquilizers. Moreover, after the administration of IEM-2886 and LVM-S144 at a dose of 25 mg / kg, an increase in the time spent in the closed sleeve of the maze (p 0.05) was observed, i.e. an anxiogenic effect. CONCLUSION: Thus, oxy-coumarin-based compounds are selective for the assessment of anticompulsive effects.

2021 ◽  
Author(s):  
Siamak Shahidi ◽  
Asghar Dindar ◽  
Alireza Komaki ◽  
Reihaneh Sadeghian

Abstract ObjectiveAnxiety behavior is regulated by different neurotransmitter systems. There has been no direct relationship between endocannabinoid and cholinergic systems on anxiety in previous studies. This study investigated the effects of each of these systems separately and simultaneously using Donepezil (Cholinesterase inhibitor) and URB-597 (endocannabinoid degrading enzyme inhibitor) on anxiety-like behavior. MethodEighty-eight male mice were divided into eleven groups (n=8) including control (saline), diazepam (0.3 mg /kg), URB-597 (0.1, 0.3, or 1 mg /kg), donepezil (0.5, 1 or 2 mg/kg) and the combination of the two drugs at low, medium and high doses. All treatments were injected intraperitoneally 30 minutes before the elevated plus maze test. ResultsSeparate administration of URB597, donepezil or diazepam increased the number and time spent of open arms compared to the control group. Concurrent administration of URB and donepezil at low, medium and high doses did not change the number of open arms entries compared to the control group, but they reduced the number of entries to the closed arms. ConclusionsThese results suggest that strengthening any cholinergic or endocannabinoid system has anxiolytic effect similar to diazepam. However, the interaction of these two systems has fewer anxiolytic effects compared to the effects of each alone. It seems that these drugs alone may represent a strategy for the treatment of anxiety disorders.


Dose-Response ◽  
2019 ◽  
Vol 17 (4) ◽  
pp. 155932581989126 ◽  
Author(s):  
Hafiz Muhammad Asif ◽  
Abdul Hayee ◽  
Muhammad Rahil Aslam ◽  
Khalil Ahmad ◽  
Abdul Sattar Hashmi

The present work was carried out to assess the Onosma bracteatum anxiolytic and antidepressant properties. Swiss albino mice (male) were fed orally with hydroalcoholic extract at different doses 50, 100, and 200 mg 1 hour prior to test with the standard diazepam and fluoxetine. Anxiolytic and antidepressant activities were evaluated by using open field, elevated plus maze, force swimming, and tail suspension test. Results of open field test showed an increase in number of line crossing as well as number of rearing in dosage-dependent design. Although results of elevated plus maze test evidently showed antianxiety effect of O bracteatum by increasing the time spent in open arms along with decreasing the time spent in closed arms in dosage-dependent way. For the evaluation of antidepressant effect, O bracteatum diminished the immobility time and expanded mobility time in forced swim model in dosage-dependent way. Likewise, O bracteatum expanded time span of mobility along with diminished immobility time in tail suspension method in dosage-dependent way. Outcome demonstrated that plant at the dose of 200 mg/kg body weight showed significant potential which was similar to that standard diazepam and fluoxetine. Hence, O bracteatum may be used as potent natural psychotherapeutic agent against the mental disorders.


1992 ◽  
Vol 43 (2) ◽  
pp. 529-535 ◽  
Author(s):  
Ümit Sayin ◽  
Nuhan Purali ◽  
Tuncer Özkan ◽  
Tuncay Altug ◽  
Sevim Büyükdevrim

Biomolecules ◽  
2019 ◽  
Vol 9 (12) ◽  
pp. 892 ◽  
Author(s):  
Rade Vukovic ◽  
Igor Kumburovic ◽  
Jovana Joksimovic Jovic ◽  
Nemanja Jovicic ◽  
Jelena S. Katanic Stankovic ◽  
...  

Since cisplatin therapy is usually accompanied with numerous toxicities, including neurotoxicity, that involve tissue oxidative damage, the aim of this study was to evaluate the possible protective effect of N-acetylcysteine (NAC) on the anxiogenic response to cisplatin (CIS). Thirty-two male Wistar albino rats divided into four groups (control, cisplatin, NAC, and CIS + NAC). All treatments were delivered intraperitoneally. On day one, the control and cisplatin groups received saline while the NAC and CIS + NAC groups were administered with NAC (500 mg/kg). On the fifth day, the control group received saline while the CIS group was treated with cisplatin (7.5 mg/kg), the NAC group again received NAC (500 mg/kg), and the CIS + NAC group was simultaneously treated with cisplatin and NAC (7.5 and 500 mg/kg, respectively). Behavioral testing, performed on the tenth day in the open field (OF) and elevated plus maze (EPM) tests, revealed the anxiogenic effect of cisplatin that was significantly attenuated by NAC. The hippocampal sections evaluation showed increased oxidative stress (increased lipid peroxidation and decline in antioxidant enzymes activity) and proapoptotic action (predominantly by diminished antiapoptotic gene expression) following a single dose of cisplatin. NAC supplementation along with cisplatin administration reversed the prooxidative and proapoptotic effects of cisplatin. In conclusion, the results obtained in this study confirmed that antioxidant supplementation with NAC may attenuate the cisplatin-induced anxiety. The mechanism of anxiolytic effect achieved by NAC may include the decline in oxidative damage that down regulates increased apoptosis and reverses the anxiogenic action of cisplatin.


Pharmacology ◽  
2009 ◽  
Vol 84 (6) ◽  
pp. 356-366 ◽  
Author(s):  
Mehrnaz Rezvanfard ◽  
Mohammad-Reza Zarrindast ◽  
Payvand Bina

2004 ◽  
Vol 176 (2) ◽  
pp. 115-122 ◽  
Author(s):  
Regina H. Silva ◽  
Sonia R. Kameda ◽  
Rita C. Carvalho ◽  
Andr� L. Takatsu-Coleman ◽  
Suzy T. Niigaki ◽  
...  

2001 ◽  
Vol 15 (2) ◽  
pp. 142-147 ◽  
Author(s):  
Hisashi Kuribara ◽  
Hisato Iwata ◽  
Hideo Tomioka ◽  
Reiko Takahashi ◽  
Kazumi Goto ◽  
...  

2020 ◽  
Vol 9 (5) ◽  
pp. 329-332
Author(s):  
Kwasi Adomako Ohemeng ◽  
◽  
Peace Doe ◽  
Mariam Adoley Pappoe ◽  
Dzifa Thywill Gordor ◽  
...  

Introduction: Natural products since time immemorial have been the source of traditional medicine. A number of well-known anxiolytic agents currently used have several side effects that limit their use. Among medicinal plants, leaves of Annona muricata (AM) are being recommended by traditional healers for the management of anxiety. This study is performed to evaluate the anxiolytic activity of the aqueous and ethanolic extracts of the leaves and bark of Annona muricata. Methodology: Aqueous and ethanolic extracts of the leaves and bark of Annona muricata were prepared and assessed for anxiolytic effect using the elevated plus maze (EPM) model. The antianxiety activity of the extracts were compared to the control (distilled water 10ml/kg) and standard drug Diazepam (5mg/kg). Results and discussion: All doses of the aqueous leaf extract of Annona muricata exhibited significant increase in mean entries into open arms (P<0.01) and mean time spent in open arms (P<0.05) compared to the control. 100mg/kg and 400mg/kg of the ethanolic bark extract of Annona muricata showed significant increase in open arm entries (P<0.01) with 100mg/kg also showing an increase in time spent in open arms which was significant. Conclusion: This study demonstrated that both the aqueous and ethanolic extracts of the leaves and bark of Annona muricata exert an anxiolytic effect on rats which substantiates its traditional use in the management of anxiety.


2021 ◽  
Vol 71 (2) ◽  
pp. 279-291
Author(s):  
Federico Argüelles-Tello ◽  
José Eduardo Roa-Coria ◽  
Ángel Zúñiga-Romero ◽  
Juan Carlos Huerta-Cruz ◽  
Geovanna Nalley Quiñonez-Bastidas ◽  
...  

AbstractThe current study investigates the anorectic interaction and safety of the mazindol-metformin combination in rats. Isobologram and interaction index were used to determine anorectic interaction between mazindol and metformin in the sweetened milk model. The safety profile of the mazindol-metformin combination was determined by measuring anxiety, blood pressure, hematic biometry and blood chemistry. An acute dose of mazindol and metformin administered per os, individually or as a mixture, has reduced the milk consumption in rats in a dose-dependent manner. Theoretical effective dose 40 (ED40t) did not differ from the experimental effective dose 40 (ED40e) obtained with the mazindol-metformin mixture in the anorexia experiments, by Student′s t-test. In addition, the interaction index confirmed the additive anorectic effect between both drugs. A single oral dose of ED40e mazindol-metformin mixture induced anxiolysis in the elevated plus-maze test. Moreover, oral administration of mazindol-metformin combination for 3 months significantly decreased glycemia, but not blood pressure nor other parameters of hematic biometry and blood chemistry. Results suggest that mazindol-metformin combination exerts an additive anorectic effect, as well as anxiolytic and hypoglycemic properties. Mazindol-metformin combination might be useful in obese patients with anxiety disorders or diabetes risk factors.


2009 ◽  
Vol 4 (4) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Francesco Maione ◽  
Maria Camela Bonito ◽  
Mariantonella Colucci ◽  
Virginia Cozzolino ◽  
Angela Bisio ◽  
...  

The potential anxiolytic and anti-depressive activity of CMP1 was studied in the elevated plus-maze test and in the forced swimming test. Furthermore, CMP1 sedative activity was evaluated in pentobarbital treated animals; the effect of CMP1 on spontaneous motor activity (total locomotion) was also evaluated. Our data show that CMP1, at doses that did not affect locomotion, was able to induce anxiolytic and sedative, but not anti-depressive effects. In conclusion, our results represent first evidence for an anxiolytic activity of this diterpenoid from Salvia cinnabarina.


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