Chromolaena odorata (L.) R. M. King and H. Robinson Leaves Aqueous Extract Improves the Femoral Head in Ethanol-Induced Osteonecrosis in Rats.

Chronic alcohol consumption damages bone formation and causes bone pathology, including osteonecrosis of the femoral head. The aim of this work was to evaluate the effects of the leaf aqueous extract of Chromolaena odorata (C. odorata) on the femoral head in ethanol-induced osteonecrosis in rats. Animals received alcohol (40°) at 3 g/kg for 12 weeks. A group of animals were sacrificed to attest to the instalment of osteonecrosis by using histopathological analysis. The remaining animals received alcohol concomitantly with the plant extract (150, 300, or 600 mg/kg) or diclofenac (1 mg/kg) for 28 additional days. At the end of the experimental period, biochemical parameters including total cholesterol, triglycerides, calcium, alkaline phosphatase (ALP), reduced glutathione (GSH), malondialdehyde (MDA), nitrite, superoxide dismutase (SOD), and catalase activities were measured. Histopathological and histomorphometry analyses of femurs were also assessed. The administration of alcohol, irrespective of the experimental period, induced a significant increase in total cholesterol (p < 0.05) and triglyceride (p < 0.01) and a decrease in ALP (p < 0.05) and calcium (p < 0.05-p < 0.001) levels. Intoxicated animals showed an alteration in oxidative stress parameters accompanied by a significant drop in bone cortical thickness and density with necrosis and marked bone resorption. The concomitant administration of the plant with ethanol reversed the alcohol-induced bone defect, characterized by the improvement of the lipid profile (p < 0.001), bone calcium concentration (p < 0.05), bone ALP activity (p < 0.001), oxidative stress parameters, improved cortical bone thickness (p < 0.01), and bone density (p < 0.05). These results are supported by the absence of bone resorption with an obvious effect at a dose of 300 mg/kg. The pharmacological effect of the extract on ethanol-induced osteonecrosis of the femoral head is probably due to its osteogenic, hypolipidemic, and antioxidant properties, justifying its use in Cameroonian folk medicine for articulation and bone pain management.

Acute and Subchronic Toxicity Studies on the Aqueous Extract of the Plant Mixture (Bidens pilosa and Cymbopogon citratus Aerial Parts) in Rat Model.

Bidens pilosa (B. pilosa) and Cymbopogon citratus (C. citratus) are plants used individually or in combination in the traditional treatment of several ailments such as cardiovascular disorders. In order to valorise their traditional use, a toxicological study was conducted on the aqueous extract of the mixture of aerial parts of B. pilosa and C. citratus. The acute and subchronic toxicity studies were conducted according to the OECD 425 and 407 guidelines. Regarding the acute study, the aqueous extract of the mixture of B. pilosa and C. citratus 50 : 50 (2000 and 5000 mg/kg) was administered once to rats of both sexes. In the subchronic study, the aqueous extract of the mixture of B. pilosa and C. citratus (200, 400 and 800 mg/kg) was administered once daily to rats for 28 days. The aqueous extract of the mixture of B. pilosa and C. citratus (2000 and 5000 mg/kg) did not cause death and did not induce any apparent sign of toxicity during the 14 days of observation. The DL50 of the extract is therefore greater than 5000 mg/kg. Taken daily for 28 days, the extract had no significant effect on selected parameters (creatinine, AST, ALT, urea, and uric acid) of renal and hepatic function, as well as on the number of some blood cells. However, the aqueous extract of the mixture of B. pilosa and C. citratus (200 and 400 mg/kg) caused a significant (p < 0.05; p < 0.001, respectively) decrease in creatinine levels in male rats as compared to normal control animals. In females, the aqueous extract of the mixture of B. pilosa and C. citratus (200 and 400 mg/kg) resulted in a significant (p < 0.05) increase in total cholesterol levels as compared to normal control animals. The study showed that the aqueous extract of the mixture of B. pilosa and C. citratus has a low toxicity and does not cause any injury to the liver, kidney, lungs, or spleen.

Protective Effects of Anthocleista djalonensis Extracts against Pentylenetetrazole-Induced Epileptic Seizures and Neuronal Cell Loss: Role of Antioxidant Defense System.

Oxidative stress and neurodegeneration are involved in the initiation of epileptogenesis and progression of epileptic seizures. This study was aimed at investigating the anticonvulsant, antioxidant, and neuroprotective properties of active fractions isolated from Anthocleista djalonensis root barks in pentylenetetrazole mouse models of epileptic seizures. Bioactive-guided fractionation of Anthocleista djalonensis (AFAD) extracts using acute pentylenetetrazole (90 mg/kg) induced generalised tonic-clonic seizures, which afforded a potent anticonvulsant fraction (FPool 5). Further fractionation of AFAD was performed by high-performance liquid chromatography, which yielded fifteen subfractions, which were chemically characterised. In addition, AFAD was tested against convulsions or spontaneous kindled seizures induced, respectively, by acute (50 mg/kg) or subchronic (30 mg/kg) injection of pentylenetetrazole. Finally, oxidative stress markers, brain GABA content, and neuronal cell loss were evaluated in AFAD-treated pentylenetetrazole-kindled mice. Administration of AFAD significantly protected mice against acute pentylenetetrazole (90 mg/kg)-induced convulsions. In acute pentylenetetrazole (50 mg/kg)-induced hippocampal and cortical paroxysmal discharges, AFAD significantly decreased the number of crisis, the cumulative duration of crisis, and the mean duration of crisis. Additionally, AFAD significantly decreased the number of myoclonic jerks and improved the seizure score in subchronic pentylenetetrazole-induced kindled seizures. The pentylenetetrazole-induced alteration of oxidant-antioxidant balance, GABA concentration, and neuronal cells in the brain were attenuated by AFAD treatment. This study showed that AFAD protected mice against pentylenetetrazole-induced epileptic seizures possibly through the enhancement of antioxidant defence and GABAergic signalling. These events might be correlated with the amelioration of neuronal cell loss; hence, AFAD could be a potential candidate for the treatment of epilepsy.

Antihypertensive and antidiabetic activities of Erythrina senegalensis DC (Fabaceae) stem bark aqueous extract on diabetic hypertensive rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Erythrina senegalensis is traditionally used in Cameroon for its relaxing and hypoglycemic properties in the treatment of cardiovascular diseases and diabetes. AIM OF THE STUDY: High blood pressure and diabetes mellitus are frequently linked. These pathologies represent major risk factors for cardiovascular and renal diseases. The present study was designed to evaluate the antidiabetic and antihypertensive activity of the stem bark of Erythrina senegalensis aqueous extract in male hypertensive diabetic rats (HDR). MATERIALS AND METHODS: Hypertension and diabetes were induced by oral administration of sucrose (15%) and ethanol (40°) at doses of 1.5 g/kg and 5 g/kg respectively for 30 days, followed by an intravenous injection of streptozotocin (STZ; 40 mg/kg). A control group of 5 rats received distilled water (10 mL/kg) followed by intravenous injection of 0.9% NaCl (1 mL/100 g). HDR were divided into 4 groups of 5 rats each according to their blood glucose level and continued to receive ethanol in association with: distilled water (10 mL/kg); group I, metformin (200 mg/kg)+nifedipine (10 mg/kg); group II, plant extract (100 and 200 mg/kg) group IV and V, respectively for 28 days. At the end of the treatment, hemodynamic parameters were recorded by the direct method. Animals were sacrificed; blood and organs (aorta, heart, liver, and kidneys) were collected for biochemical and histological analysis. Phytochemistry and HPLC-DAD-HRESI-MS were used to determine the major compounds of the extract. RESULTS: The administration of sucrose, alcohol, and STZ resulted in a significant increase in blood glucose, hemodynamic parameters, and body weight loss. A significant decrease in pancreatic islets size, nitrite, GSH, SOD and catalase activity was observed in HDR. There was also a significant increase in serum triglycerides, total cholesterol, creatinine, bilirubin, and transaminases activity in HDR. The aqueous extract of E. senegalensis, as well as the metformin + nifedipine combination, significantly improved all these parameters. HPLC coupled to both diode array and mass spectrometry detectors revealed the presence of 15 compounds and 11 of them were identified. CONCLUSION: These results suggest that the aqueous extract of E. senegalensis possess antihypertensive, hypoglycemic, hypolipidemic, cardiomodulator and antioxidant properties involved in the improvement of the metabolic disorders found in HDR. This may be due at least in part to the presence of Erysenegalensein (D, O, N, E), Warangalone, senegalensin and 6,8-diprenylgenistein identified in the extract.

Antihypertensive Activity of Leersia hexandra Sw. (Poaceae) Aqueous Extract on Ethanol-Induced Hypertension in Wistar Rat.

Leersia hexandra (L. hexandra) is used in traditional medicine to treat many diseases including hypertension. This study aimed to evaluate the curative effects of the aqueous extract of L. hexandra on hypertension. Hypertension was induced in rats by oral administration of ethanol (5 g/kg/day) for five weeks. The animals were divided into 2 groups: one group of 5 rats receiving distilled water (10 mL/kg) and another group of 20 rats receiving ethanol. At the end of the 5 weeks of administration of ethanol, the animals were divided into 4 groups of 5 rats each: one group of hypertensive rats receiving distilled water (10 mL/kg), another one receiving nifedipine (10 mg/kg), and two groups of hypertensive rats receiving L. hexandra at doses of 100 and 200 mg/kg, respectively. The results showed that ethanol induced a significant increase in the mean arterial pressure (MAP) and heart rate of normotensive rats. The administration of the extract (100 and 200 mg/kg) or nifedipine caused a significant decrease of MAP compared to hypertensive rats. Ethanol induced a significant increase of lipid profile, the atherogenic index, creatinine, and transaminase activities. Ethanol also induced a significant decrease in serum HDL-cholesterol and antioxidant markers evaluated. Treatment of hypertensive rats with L. hexandra or nifedipine significantly improved lipid profile, hepatic and renal functions, and antioxidant status. The curative effect of L. hexandra extract on hypertension is probably related to its antihypertensive, hypolipidemic, and antioxidant activities, which justifies its empirical use in the treatment of hypertension.

Antipsychotic and sedative effects of the leaf extract of Crassocephalum bauchiense (Hutch.) Milne-Redh (Asteraceae) in rodents.

ETHNOPHARMACOLOGICAL RELEVANCE: Crassocephalum bauchiense (Hutch.) Milne-Redh (Asteraceae) has been used as a medicine for the treatment of epilepsy, insomnia, dementia and psychotic disorders in Cameroonian traditional medicine. AIM OF THE STUDY: This study was designed to examine whether the aqueous extract and the alkaloid fraction prepared from the leaves of Crassocephalum bauchiense possess antipsychotic and sedative properties in rodents. MATERIALS AND METHODS: The rectal temperature of mice was recorded with a probe thermometer at a constant depth. Novelty-induced rearing behavior is used to evaluate a central excitatory locomotor behavior in mice. The antipsychotic effects of the extracts were assessed using the apomorphine animal model of psychosis. The catalepsy test was tested based on the ability of the leaves extracts of Crassocephalum bauchiense to alter the duration of akinesia by placing the naive mice with both forelegs over a horizontal bar. The extracts of Crassocephalum bauchiense effects were evaluated on sodium pentobarbital-induced sleeping time. In addition, gamma-aminobutyric acid concentrations in the brain treated mice were also estimated. RESULTS: The aqueous extract and the alkaloid fraction from Crassocephalum bauchiense caused dose-dependent inhibition of novelty-induced rearing behavior, decreased the apomorphine-induced stereotypy and fighting, and had significant fall of the body temperature. The aqueous extract prolonged the sodium pentobarbital sleeping time. This prolongation was not reversed by bicuculline, a light-sensitive competitive antagonist of GABA(A) receptors complex. However, the effect of the aqueous extract on sodium pentobarbital-induced sleeping time was blocked by N-methyl-ß-carboline-3-carboxamide, a partial inverse agonist of the benzodiazepine site in the GABA(A) receptor complex and flumazenil, a specific antagonist of the benzodiazepine site in the GABAA receptor complex. In biochemical experiments, the concentration of the inhibitory amino acid, gamma-aminobutyric acid, was significantly increased in the brain of animals treated with the aqueous extract of Crassocephalum bauchiense and sodium valproate. CONCLUSIONS: The results show that the antipsychotic and sedative properties of Crassocephalum bauchiense are possibly mediated via the blockade of dopamine D-2 receptors and GABAergic activation, respectively. However, pharmacological and chemical studies are continuing in order to characterize the mechanism(s) responsible for these neuropharmacological actions and also to identify the active substances present in the extracts of Crassocephalum bauchiense.