Abstract
Background Calotropis procera has been widely used traditionally for its analgesic and anti-inflammatory effects. It is also reportedly used in ethnomedicine for mental health disorders including epilepsy even in the absence of supporting scientific data. Thus, the potential of the plant to affect neurological functions was evaluated. Methods Irwin's test was performed to determine the effect of the oral administration of the extract (30–3000 mg kg−1) on gross behaviour and physiological function. The activity meter, rotarod, pentylenetetrazol- (PTZ-) induced convulsion, pentobarbitone-induced sleep test, and the tail immersion tests were used to evaluate the spontaneous activity, neuromuscular function, convulsive threshold, sedation, and analgesic effects of the Calotropis procera extract (30–1000 mg/kg), respectively, in mice. Results Calotropis procera extract (CPE) exhibited significant (p < 0.0001) anticonvulsant and analgesic effects. There was a significant increase in withdrawal latency of the CPE-treated animals in the tail immersion test for analgesia (p < 0.0001), while latency and duration of PTZ-induced convulsions were positively modulated. Calotropis procera extract showed significant (p < 0.0001) central nervous system depressant effects in pentobarbitone-induced hypnosis at 100–1000 mg/kg and spontaneous activity test (30–1000 mg/kg). The extract also depicted impaired motor coordination at 100–1000 mg/kg dose levels. LD50 was estimated to be above 1000 mg kg−1. Conclusions Calotropis procera extract has significant central nervous system depressant and analgesic effects in mice.
Highlights
Calotropis procera has been widely used traditionally for its analgesic and anti-inflammatory effects
The brain has been regarded as an immune-privileged organ, which was not susceptible to inflammation or immune activation and was thought to be largely unaffected by systemic inflammatory and immune responses. is view has been revised significantly with the realization that proinflammatory cytokines and other mediators play an essential role in CNS inflammation through microglia activation and its downstream mechanisms that lead to neurodegenerative effects. is mechanism is recognized in several CNS disorders such as depression, Parkinson’s disease, Alzheimer’s disease, and epilepsy [10]
Fresh leaves of Calotropis procera were collected from Iture (5°05′54.6′′N, 1°18′48.7′′W), a town near the University of Cape Coast (UCC), from August to December 2015. e leaves were identified by a botanist at the School of Biological Sciences Herbarium, the University of Cape Coast, and the voucher specimen (UCC/SBSH/15/M044) was deposited at the Herbarium
Summary
Cognitive and neurological disorders are a major challenge for public health globally, in developing countries where cultural factors and inadequate access to modern healthcare have led to dependence on conventional medicines [1]. ese neurological disorders tend to be the leading cause of impairment worldwide, and their proportion among all health problems to the overall burden is growing. e brunt of the burden from neurological conditions lies in low- and middle-income countries [2]. Is view has been revised significantly with the realization that proinflammatory cytokines and other mediators play an essential role in CNS inflammation through microglia activation and its downstream mechanisms that lead to neurodegenerative effects. Latex proteins of C. procera have been shown to have CNS activity as reflected in their potentiation of pentobarbital-induced sleeping time and their anticonvulsant action in a PTZ-induced seizure model. E methods employed in this study were adapted from the core battery of assessment of the central nervous system as proposed by the International Conference on Harmonization (ICH) S7A Guideline for Safety Pharmacology [12]. Ese are generally simple tests employed in safety assessment and are frequently applied at the very beginning of the discovery process to screen substances with a potential for CNS benefit or risk and measure gross behavioural signs, locomotor activity, seizure, and pain thresholds. An activity meter cage was used to determine the effect of C. procera on locomotor activity, while the effects of the plant extract on neuromuscular coordination were assessed using the rotarod test. e analgesic activity of the plant was evaluated in a tail immersion assay. e sleepenhancing effects and potential anticonvulsant actions were determined using a pentobarbitone-induced sleeping time and pentylenetetrazol-induced seizure models, respectively
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