Evaluation of the anticonvulsant and muscle relaxant effects of the methanol root bark extracts of Annona senegalensis

AbstractObjectiveTo investigate the potentials of the root bark of Annona (A.) senegalensis in the control of seizure and related hypnotic and motor incoordination effects in mice using experimental models.MethodsThe methanol extract (ME) of the root bark of A. senegalensis was studied in mice using pentylenetetrazole (PTZ) induced convulsions, phenobarbitone induced sleeping time and motor coordination test on rota-rod performance. Acute toxicity and lethality (LD50) test as well as phytochemical analysis were also carried out.ResultsThe extract (200, 400, 800 mg/kg) exhibited a non-dose dependent significant (P <0.05) delay in the onset of both tonic and clonic phases of seizure induced by PTZ (60 mg/kg, s.c.) as well as offered a 100% protection (200 mg/kg) in mice from PTZ induced seizures. The extract significantly (P <0.05) decreased the latency and increased the duration of phenobarbitone induced sleeping time. At 200 mg/kg, the extract exhibited a significant (P <0.05) motor incoordination. The acute toxicity test revealed an oral LD50 of 1 296 mg/kg, while the phytochemical studies showed the presence of alkaloids, resins, glycosides, carbohydrate, reducing sugar, flavonoids, terpenoids, saponins and tannins.ConclusionThe extract of A. senegalensis possessed anticonvulsant activity with pronounced hypnotic and muscle relaxant effects

Evaluation of antidiabetic potentials of Phyllanthus niruri in alloxan diabetic rats

The antidiabetic potentials of methanol extract (ME) of aerial parts of Phyllanthus niruri L (Euphorbiaceae) was evaluated in normal and alloxan diabetic rats. The results showed that ME significantly (P&lt;0.05) reduced fasting blood sugar in a dose-related manner and suppressed thepostprandial rise in blood glucose after a heavy glucose meal in normoglycaemic rats. Chronic oral administration of ME caused a significant (P&lt;0.05) dose-related reduction in blood glucose levels as well as total cholesterol and triglycerides levels in diabetic and normoglycaemic rats. Sub-chronic toxicity study showed that ME-treated rats had significant (P&lt;0.05) reductions in haemoglobin (Hb) levels, red blood cell (RBC) and white blood cell (WBC) counts followed by a gradual rise which did not,however, attain basal levels; however, there was a progressive rise in the WBC of ME-treated diabetic rats. Also ME-treated and control rats had increases in weight throughout the study. Histological studies showed that ME-treated diabetic rats had the tissue architecture of their pancreas restored as against the control groups where there was evidence of necrosis. The acute toxicity and lethality test of ME in mice gave an oral LD50 of 471.2 mg/kg. Results suggest that extract of aerial parts of P. niruri has great potentials as anti-diabetic remedy

Anti-inflammatory activity of fatty extract of Vitalleria paradoxa Kernel (Shea butter) and pattern of its clinical use in arthritis in Enugu, South East Nigeria

Background: The fatty seed extract of Vitellaria paradoxa Kernel (Sapotaceae) commonly called “Shea butter”, is a popular remedy for arthritis in west Africa. This study investigated the knowledge, prevalence and pattern of use of Shea butter in clinically diagnosed arthritic patients as well as its effects on acute (topical and systemic) and chronic inflammation in rodents.Methods: Knowledge, prevalence and pattern of use were determined using pre-tested questionnaire in clinically diagnosed patients whereas the anti-inflammatory activity was studied using xylene-induced mouse ear edema, carrageenan-induced rat paw edema, formaldehyde-induced arthritis in rats and cotton pellet granuloma test in rats.Results: The results showed that of the 164 respondents, 94.1% know about Shea butter and 59.6% have used it mainly as a massage ointment once or twice daily. However, 73.7% of the users combine this remedy with analgesics to achieve relief. The pharmacological tests showed that topical application of Shea butter inhibited acute edema of the mouse ear. Systemic oral administration caused significant (p<0.05) suppression of the development of systemic acute edema of the rat paw in a non-dose related manner. Twice daily topical application of Shea butter significantly (p<0.05) inhibited the edematous response to formaldehyde arthritis whereas once daily administration was not effective. Shea butter also caused a significant (p<0.05) non-dose related inhibition of granuloma tissue formation on implanted cotton pellets.Conclusions: These findings provide a scientific rationale for the use of Shea butter in treatment of disorders of inflammation in traditional medicine

ANTI-DIARRHOEAL AND ANTISPASMODIC EFFECTS OF LEAF EXTRACT OF PTEROCARPUS SANTALINOIDES

Diarrhoea is one of the popular gastrointestinal disorders with high mortality especially in children. Certain medicinal plants are being used in traditional medicine practice to treat and control diarrhoea. One of such plants is the leaves of Pterocarpus santalinoides. The need to scientifically ascertain this folkloric claim and the possible identification of the active constituents therein motivated this study. The methanol leaf extract of P. santalinoides was prepared and screened for activity using castor-oil induced diarrhoea, gastrointestinal motility tests (charcoal transit test) and inhibition of contraction induced by histamine (H) and acetylcholine (Ach) on isolated rabbit jejunum. The results indicated that the extract at 200 mg/kg dose exhibited a significant inhibition (P &lt; 0.05) of castor-oil induced diarrhoea when compared with a standard antidiarrhoeal agent, diphenoxylate hydrochloride (5 mg/kg). The extract also at 200 mg/kg dose level showed a significant inhibition (P&lt;0.05) on gastrointestinal motility when compared with the vehicle (3 % Tween 80). The extract also exhibited a dose dependent inhibition on the contraction induced by acetylcholine and histamine on rabbit jejunum as well as the abolition of spontaneous pendular movements of the smooth muscles of the rabbit jejunum. The acute toxicity study exhibited an LD50 greater than 5000 mg/kg. The phytochemical screening revealed the presence of carbohydrates, resins, terpenoids, steroids, saponins. The extract exhibited both antidiarrhoeal and antispasmodic effects which could be through inhibition of histaminergic and cholinergic mechanisms via their respective receptors abundant in the GIT. The antidiarrhoeal effect of this plant can be explored for therapeutic advantages as an alternative for treatment of diarrhoea and further research is expected to confirm the active phytochemical constituent(s) responsible for the activity. Keywords: P. santalinoides, antidiarrhoeal, antispasmodic and rabbit jejunumNigerian Journal of Pharmaceutical Research, Vol. 8 No 1 pp. 138 - 144 (September 2010

Anti-inflammatory activity of fatty extract of Vitalleria paradoxa Kernel (Shea butter) and pattern of its clinical use in arthritis in Enugu, South East Nigeria

Background: The fatty seed extract of Vitellaria paradoxa Kernel (Sapotaceae) commonly called “Shea butter”, is a popular remedy for arthritis in west Africa. This study investigated the knowledge, prevalence and pattern of use of Shea butter in clinically diagnosed arthritic patients as well as its effects on acute (topical and systemic) and chronic inflammation in rodents.Methods: Knowledge, prevalence and pattern of use were determined using pre-tested questionnaire in clinically diagnosed patients whereas the anti-inflammatory activity was studied using xylene-induced mouse ear edema, carrageenan-induced rat paw edema, formaldehyde-induced arthritis in rats and cotton pellet granuloma test in rats.Results: The results showed that of the 164 respondents, 94.1% know about Shea butter and 59.6% have used it mainly as a massage ointment once or twice daily. However, 73.7% of the users combine this remedy with analgesics to achieve relief. The pharmacological tests showed that topical application of Shea butter inhibited acute edema of the mouse ear. Systemic oral administration caused significant (p&lt;0.05) suppression of the development of systemic acute edema of the rat paw in a non-dose related manner. Twice daily topical application of Shea butter significantly (p&lt;0.05) inhibited the edematous response to formaldehyde arthritis whereas once daily administration was not effective. Shea butter also caused a significant (p&lt;0.05) non-dose related inhibition of granuloma tissue formation on implanted cotton pellets.Conclusions: These findings provide a scientific rationale for the use of Shea butter in treatment of disorders of inflammation in traditional medicine

Wound healing properties of stem bark extract of Tabebuia rosea

The wound healing properties of the methanol stem bark extract of Tabebuia rosea (Bignoniaceae) were evaluated in rats using the excision wound model. Extraction of the powdered plant material by continuous extraction in a soxhlet afforded 5.73% w/w of the Tabebuia methanol extract (TME). Phytochemical analysis and acute toxicity LD50  tests were also performed. The results showed that TME and formulation of the extract in petroleum jelly (PE) significantly (P < 0.05) reduced the wound diameter as well as epithelialisation time of the excised wound. The extract (TME) and the formulations (PE) produced 100% healing on the 14th day post excision which is comparable to the healing exhibited by a standard agent, Cicatrin powder. Phytochemical analysis of the extract indicated the presence of alkaloids, carbohydrates, flavonoids, glycosides, proteins, steroids, tannins and terpenoids. The  acute toxicity test indicated an LD50 of 2154 mg/kg.Keywords: Tabebuia rosea, wound healing, excision, ratsJournal of Pharmaceutical and Allied Sciences, Vol. 7 No.4 (2010

Protein interactions in the murine cytomegalovirus capsid revealed by cryoEM

Cytomegalovirus (CMV) is distinct among members of the Herpesviridae family for having the largest dsDNA genome (230 kb). Packaging of large dsDNA genome is known to give rise to a highly pressurized viral capsid, but molecular interactions conducive to the formation of CMV capsid resistant to pressurization have not been described. Here, we report a cryo electron microscopy (cryoEM) structure of the murine cytomegalovirus (MCMV) capsid at a 9.1 Å resolution and describe the molecular interactions among the ∼3000 protein molecules in the MCMV capsid at the secondary structure level. Secondary structural elements are resolved to provide landmarks for correlating with results from sequence-based prediction and for structure-based homology modeling. The major capsid protein (MCP) upper domain (MCPud) contains α-helices and β-sheets conserved with those in MCPud of herpes simplex virus type 1 (HSV-1), with the largest differences identified as a “saddle loop” region, located at the tip of MCPud and involved in interaction with the smallest capsid protein (SCP). Interactions among the bacteriophage HK97-like floor domain of MCP, the middle domain of MCP, the hook and clamp domains of the triplex proteins (hoop and clamp domains of TRI-1 and clamp domain of TRI-2) contribute to the formation of a mature capsid. These results offer a framework for understanding how cytomegalovirus uses various secondary structural elements of its capsid proteins to build a robust capsid for packaging its large dsDNA genome inside and for attaching unique functional tegument proteins outside. ELECTRONIC SUPPLEMENTARY MATERIAL: Supplementary material is available for this article at 10.1007/s13238-013-3060-7 and is accessible for authorized users