Adewale Fadaka

Curcumin administration suppress acetylcholinesterase gene expression in cadmium treated rats

HIGHLIGHTSCurcumin prevents Cd neurotoxicity.Curcumin exhibited inhibitory effect on acetycholinesterase activity.Curcumin suppress acetylcholinesterase gene expression in cadmium treated rats. ABSTRACT Curcumin, the main polyphenolic component of turmeric (Curcuma longa) rhizomes have been reported to exert anticholinesterase potential with limited information on how they regulate acetylcholinesterase (AChE) gene expression. Hence, this study sought to evaluate the effect of curcumin on cerebral cortex acetylcholinesterase (AChE) activity and their mRNA gene expression level in cadmium (Cd)‐treated rats. Furthermore, in vitro effect of different concentrations of curcumin (1–5 &mgr;g/mL) on rat cerebral cortex AChE activity was assessed. Animals were divided into six groups (n = 6): group 1 serve as control (without Cd) and receive saline/vehicle, group 2 receive saline plus curcumin at 25 mg/kg, group 3 receive saline plus curcumin 50 mg/kg, group 4 receive Cd plus vehicle, group 5 receive Cd plus curcumin at 25 mg/kg and group 6 receive Cd plus curcumin at 50 mg/kg. Rats received Cd (2.5 mg/kg) and curcumin (25 and 50 mg/kg, respectively) by oral gavage for 7 days. Acetylcholinesterase activity was measured by Ellmans method and AChE expression was carried out by a quantitative reverse transcriptase polymerase chain reaction (RT‐qPCR) assay. We observed that acute administration of Cd increased acetylcholinesterase activity and in addition caused a significant (P < 0.05) increase in AChE mRNA levels in whole cerebral cortex when compared to control group. However, co‐treatment with curcumin inhibited AChE activity and alters AChE mRNA levels when compared to Cd‐treated group. In addition, curcumin inhibits rat cerebral cortex AChE activity in vitro. In conclusion, curcumin exhibit anti‐acetylcholinesterase activity and suppressed AChE mRNA gene expression level in Cd exposed rats, thus providing some biochemical and molecular evidence on the therapeutic effect of this turmeric‐derived compound in treating neurological disorders including Alzheimers disease.

Evaluation of acute and subacute toxicity of aqueous extract of Crassocephalum rubens leaves in rats

ETHNOPHARMACOLOGICAL RELEVANCE Crassocephalum rubens is found throughout tropical Africa including the Indian Ocean islands. The leaves are commonly eaten in form of soups and sauces in South-Western Nigeria, also in other humid zones of Africa. Traditionally, it is used as an antidote against any form of poisoning; used to treat stomach and liver complaints; and externally to treat burns, sore eyes, earache, leprosy and breast cancer. In this study, acute and subacute toxicity of aqueous extract of C. rubens leaves was evaluated in rats in order to assess its safety profile. MATERIALS AND METHODS In acute toxicity study, rats were given a single oral administration of aqueous extract of C. rubens leaves at graded doses (250-5000mg/kg). The animals were monitored for behavioural changes and possible mortality over a period of 24h and thereafter, for 14 days. In the subacute toxicity study, rats of both sexes were administered C. rubens orally at doses of 250mg/kg, 500mg/kg, 750mg/kg and 1000mg/kg body weight daily, for 28 days. Rats were observed weekly for any changes in general behaviour and body weights. In addition, other relevant parameters were assayed at the end of the main and reversibility study periods. RESULTS There was no observed adverse effect; including mortality in the animals. The extract caused no significant difference in the body weights as well as organs weights of treated groups when compared with the control groups. Haematological and biochemical parameters also revealed no toxic effects of the extract on rats. Histological assessments were normal in liver and kidney. CONCLUSIONS It can therefore be suggested based on the results from this study that aqueous extract of C. rubens leaves, at dosage levels up to 1000mg/kg, is non-toxic and could also offer protection on some body tissues. Aqueous extract of C. rubens could therefore, be considered safe. This study supports the application of Crassocephalum rubens in traditional medicine.

Ameliorative Activity of Ethanol Extract of Artocarpus heterophyllus Stem Bark on Pancreatic β-Cell Dysfunction in Alloxan-Induced Diabetic Rats

This study sought to investigate the ameliorative effects of ethanol extract Artocarpus heterophyllus (EAH) in alloxan-induced diabetic rats. The rats were divided into 6 groups, with groups 1 and 2 serving as nondiabetic and diabetic control, respectively; group 3 serving as diabetic rats treated with 5 mg/kg glibenclamide; and groups 4 to 6 were diabetic rats treated with 50, 100, and 150 mg/kg of EAH, respectively. Assays determined were serum insulin, lipid peroxidation, and antioxidant enzyme activities. EAH stem bark reduced fasting blood glucose and lipid peroxidation levels and increased serum insulin levels and activities of antioxidant enzymes. Data obtained demonstrated the ability of EAH stem bark to ameliorate pancreatic β-cell dysfunction in alloxan-induced diabetic rats.

Protective Influence of Ficus asperifolia Miq Leaf Extract on Carbon tetrachloride (CCL4)-Induced Testicular Toxicity in rat’s Testes.

The aim of this study was to investigate the ability of the polyphenolic rich Ficus asperifolia (Miq.) leaf extract in protecting rat testes against carbon tetrachloride-induced testicular damage in male Wistar rats. Thirty rats (weighing 140 - 180 g) were divided into five groups. In each treatment groups, aqueous extract of F. asperifolia (100, 200 and 400 mg/kg bw) administered by oral gavage for 21 days before exposure to carbon tetrachloride (CCl4) 3 mL kg 1i.p. were used to test protective influence of the plant extract. Protective influence were observed on antioxidant marker enzymes such as reduced glutathione (GSH) levels, catalase (CAT), glutathione peroxidase (GPx), superoxide dismutase (SOD), and malonaldehyde (MDA) and histological examination.. Animal exposure to the CCl4 resulted in significant elevation in the MDA with concomitant depletion (p < 0.05) in the level of GPx, CAT and SOD activities compared with control. Daily oral administration of F. asperifolia showed beneficial and ameliorative effects in all biochemical parameter evaluated. Histopathological alteration in testes was observed in CCl4 untreated rats and was ameliorated inCCl4 rats treated with F. asperifolia. Result shows that the aqueous leaf extract of F. asperifolia has ameliorative effect against carbon tetrachloride-induced testicular toxicity.

In vitro antioxidant activities and inhibitory effects of phenolic extract of Senecio biafrae (Oliv and Hiern) against key enzymes linked with type II diabetes mellitus and Alzheimer's disease

Abstract The phenolic extract of Senecio biafrae leaves was investigated to determine the in vitro antioxidant, phenolic profiles, and inhibition of key enzymes relevant to type II diabetes mellitus (α‐amylase and α‐glucosidase) and Alzheimers disease (acetylcholinesterase and butrylcholinesterase). The phenolic extract demonstrated significant scavenging abilities against all in vitro antioxidant parameters assessed. Reversed‐phase HPLC of the extract revealed the presence of gallic acid, chlorogenic, caffeic acid, rutin, quercetin, and kaempferol. The extract also inhibited activities of α‐amylase (IC 50 = 126.90 μg/ml), α‐glucosidase (IC 50 = 139.66 μg/ml), acetylcholinesterase (IC 50 = 347.22 μg/ml), and butrylcholinesterase (IC 50 = 378.79 μg/ml), which may be attributed to the antioxidant potential of the extract and its phenolic composition. Therefore, this study suggests that the leaves of S. biafrae may be useful in the management of diabetes mellitus and Alzheimers disease.