scholarly journals Fast-acting effects of l-tetrahydropalmatine on depression and anxiety in mice

2019 ◽  
pp. 01-12
Author(s):  
Rui Li ◽  
Wai-Kin Mat ◽  
Wing-Man Chan ◽  
T Yiu-Cheong Ho ◽  
Rigil K Yeung ◽  
...  

The racemate dl-tetrahydropalmatine (dl-THP) is known for its analgesic and sedative effects, and has been shown by us to be a potential agent for the treatment of anxiety.Herein, to delineate the therapeutic potentials of its different isomeric forms, the behavioral effects of l-THP, dl-THP and d-THP were compared regarding their anxiolytic and antidepressant properties in mouse behavioral models using the elevated plus-maze test and tail suspension test respectively. The anxiolytic and antidepressant effects of both l-THP and dl-THP were evident in forty-five minutes following oral administration. Moreover, l-THP exhibited much greater anxiolytic potency in the elevated plus-maze (0.1-2.5 mg/kg) and antidepressant potency in the tail suspension test (0.5-5.0 mg/kg) than dl-THP, whereas d-THP was inactive in either of these tests. As well, l-THP enhanced sociability and preference for social novelty at 0.1-0.5 mg/kg in Crawley’s three-chamber behavioral tests, and inhibited the amphetamine-induced manic-like hyperactivity of amphetamine-sensitized mice at 0.05-0.2 mg/kg. These pharmacological actions of l-THP were unaccompanied by any significant locomotor or myorelaxant side-effects. Co-administration of flumazenil, a GABAA receptor antagonist, inhibited the anxiolytic and antidepressant effects of l-THP, even though the binding affinity of l-THP was higher for dopamine D2-like receptors than for GABAA receptors. On this basis, l-THP displayed potential as a fast-acting drug for the treatment of anxiety, depression and bipolar disorder. Keywords: l-THP; dl-THP; Anxiolysis; Antidepressant; GABAA receptor; Fast-acting

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.


2016 ◽  
Vol 3 (1) ◽  
pp. 1 ◽  
Author(s):  
Vishnu Nayak Badavath ◽  
Alok Kumar ◽  
Surender Singh Jadav ◽  
Ashok Kumar Pattnaik ◽  
Venkatesan Jayaprakash ◽  
...  

A series of nine 3-(2-hydroxyphenyl)-5-aryl-N-phenyl-4,5-dihydropyrazole-1-carbothioamide derivative s (3a-3i) that were earlier reported as potent rMAO-A inhibitors were evaluated for their antidepressant activity in Porsolt's behavioral despair test (forced swim test) and Tail Suspension test activity, among them, compounds (3e and 3h) were found to have potent antidepressant activity. Reduction in duration of immobility was significant for all the compounds in Porsolts swim test compared with tail suspension test. 3h was further evaluated for anxiolytic activity in Elevated plus maze and was found to be devoid of it.


2018 ◽  
Vol 7 (2) ◽  
pp. 207-211
Author(s):  
Shravan Kumar Nanumala ◽  
◽  
B Varsha Priyanka ◽  
N Divya ◽  
S Shalini ◽  
...  

Objective: The present study was designed to investigate the anti-stress activity of Cassia auriculata ethanolic seed extract in mice. Methodology: The anti-stress effect was evaluated by using Elevated plus maze (EPM), Force swimming test (FST) and Tail suspension test (TST). The ECS at a doses (250,500 and 1000 mg/kg p.o.) and standard (diazepam 2 mg/kg i.p and fluoxetine 20 mg/kg i.p) was administered. Results: The extract showed the increased in the number of entries and time spent in open arm in Elevated plus maze and decreased in the immobility time in both Force swimming test and Tail suspension test. Conclusion: The effect of ESC on animal behavior was concordant with a significant regulation of GABA and stress hormones. Therefore, this study was attempted to demonstrate the preventive potential of ECS against stress disorders at in vivo levels


Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3536 ◽  
Author(s):  
Israt Jahan ◽  
Marzia Rahman Tona ◽  
Sanjida Sharmin ◽  
Mohammed Aktar Sayeed ◽  
Fatamatuz Zuhura Tania ◽  
...  

Chukrasia velutina is a local medicinal plant commonly known as chikrassy in Bangladesh, India, China, and other South Asian countries. The leaves, bark, and seeds are vastly used as herbal medicine for fever and diarrhea, and its leaves essential oils are used for antimicrobial purposes. In this study, we discuss the neuropsychiatric properties of C. velutina leaves through several animal models, quantitative and qualitative phytochemical analysis, and computational approaches. Neuropsychiatric effects were performed in rodents on the methanolic extract of C. velutina leaves (MECVL). Antidepressant, anxiolytic, and sedative effects experimented through these rodent models were used such as the force swimming test (FST), tail suspension test (TST), hole board test (HBT), elevated plus maze test (EPMT), light/dark box test (LDBT), open field test (OFT), and hole cross test (HCT). In these rodent models, 200 and 400 mg/kg doses were used which exhibited a significant result in the force swimming and tail suspension test (p < 0.001) for the antidepressant effect. In the anxiolytic study, the results were significant in the hole board, elevated plus maze, and light/dark box test (p < 0.001) for doses of 200 and 400 mg/kg. The result was also significant in the open field and hole cross test (p < 0.001) for sedative action in the sake of similar doses. Moreover, qualitative and quantitative studies were also performed through phytochemical screening and GC-MS analysis, and fifty-seven phytochemical compounds were found. These compounds were analyzed for pharmacokinetics properties using the SwissADME tool and from them, thirty-five compounds were considered for the molecular docking analysis. These phytoconstituents were docking against the human serotonin receptor, potassium channel receptor, and crystal structure of human beta-receptor, where eight of the compounds showed a good binding affinity towards the respective receptors considered to the reference standard drugs. After all of these analyses, it can be said that the secondary metabolite of C. velutina leaves (MECVL) could be a good source for inhibiting the neuropsychiatric disorders which were found on animal models as well as in computational studies.


Author(s):  
Ismail O. Ishola ◽  
Olufunsho Awodele ◽  
Chinedum O. Eluogu

Abstract:: HeMI (12.5–100 mg/kg, p.o.) was administered 1 h before subjecting the animal to the forced swim test (FST), tail suspension test (TST) and elevated plus maze tests (EPM).: HeMI (12.5–100 mg/kg, p.o.) treatment produced significant reduction in immobility time [F(6.56)=8.35, p<0.001], [F(6,56)=7.55, p<0.001] in the FST and TST, respectively. Moreover, co-administration of sub-therapeutic doses of imipramine or fluoxetine with HeMI (3.125 mg/kg) elicited significant reduction in time spent immobile in the FST. However, pretreatment of mice with parachlorophenylalanine, metergoline, yohimbine or sulpiride abolished the antidepressant-like effect elicited by HeMI. In the EPM, HeMI produced significant [F(5,42)=8.91, p<0.001] increase in open arms exploration by 75.55 % and this effect was blocked by pretreatment of mice with flumazenil or metergoline.: Findings from this study showed antidepressant-like effect of


Author(s):  
SWATI SINGH ◽  
ASHUTOSH UPADHYAY ◽  
ANUP KUMAR SIRBAIYA

Objective: Celastrus paniculatus Willd, family Celastraceae is an important medicinal plant distributed all over India. Due to the presence of antioxidative polyphenols in C. paniculatus Willd have received much attention for health-promoting properties by scavenging the free radicals, the purpose of this study is to understand neuropharmacological, anti-stress activity, and toxicity studies of standardized seeds extract of “C. paniculatus Willd. Methods: The sun dried C. paniculatus Willd seeds were collected and extracted with ethanol by maceration. Then, the ethanolic extract was subjected to phytochemical screening. The acute toxicity of the ethanolic extract of C. paniculatus was observed as per the Organization for Economic Co-operation and Development guideline no. 423. Neuropharmacological and anti-stress effects were analyzed and evaluated by using physical stress models such as Swimming endurance test, Anoxic tolerance test, Tail suspension test (TST), and Elevated plus maze test. For this study, Swiss albino mice (20–30 g) were divided into five groups of six animals each. Distilled water administered as vehicle in control group and standard group received Withania somnifera (100 mg/kg) while C. paniculatus Willd ethanolic extract (100, 200, and 400 mg/kg) was given orally for 7 days. Results and Discussion: Change in immobility time in swim endurance, first clonic convulsion produced in anoxic tolerance test, immobility time in TST and open arms entry in elevated plus maze test was recorded as parameters. The ethanolic extracts of C. paniculatus Willd significantly reduces the immobility timing along with increases the swimming endurance time, and clonic convulsion timing in anoxic tolerance test in comparison of control group. In tail suspension significant decrease in immobility time and increased open arm entry in elevated plus maze were observed as compare to control group. Conclusion: C. paniculatus Willd has potential as a medicinal plant and it showed protective effect for the stress prevention as the alkaloids are present as main constituents.


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