In Vitro Antimalarial Susceptibility of Plasmodium falciparum and Plasmodium berghei Isolates to Selected Antimalarial Agents, Column Chromatographic Subfractions of Glyphaea brevis Leaves Extract and FTIR and GCMS of SF8.

Malaria still remains a life-threatening parasitic disease with universal targets set for control and elimination. This study aimed to evaluate the in vitro antimalarial susceptibility of Plasmodium falciparum isolates and Plasmodium berghei to selected antimalarial agents and column chromatographic subfractions of Glyphaea brevis leaves extract and FTIR and GCMS of SF8. Trager and Jensen as well as World Health Organisation (WHO) standardised in vitro micro-test system methods were used to determine susceptibility on the patients' blood samples; Column chromatographic procedure was carried out to obtain 11 pooled fractions; FTIR and GCMS were used to determine functional groups and phytochemicals respectively. In vitro anti-plasmodial activity against P. falciparum clinical isolates had IC50 range of 1.03 µg/mL-7.63 µg/mL while their IC50 against P. berghei ranges from 4.32 µg/mL-7.89 µg/mL. Subfraction 8 (SF8) had the least IC50 of 4.32 µg/mL. The FTIR spectrum showed the presence of isoprenoid, alcohol, phenol, alkane, alkenes, ester, carboxylic acids, aromatics and nitro compounds while GCMS identified dodecanoic acid, methyl ester; carotol; hexadecanoic acid, methyl ester; 9-octadecenoic acid (Z)-, methyl ester (oleic acid); methyl stearate; heptadecanoic acid, 16-methyl-, methyl ester; all with their antimalarial reported activities. In conclusion, G. brevis has a great potential for drug development against malaria parasite since it inhibited schizont growth and possesses phytocompounds with antimalarial report.

Antidiabetic, Antioxidant and Anti-Inflammatory Activities of Residual Aqueous Fraction of Ethulia conyzoides in Induced Type 2 Diabetic Rats.

Oxidative stress and inflammation have been proven to be implicated in the pathogenesis of type 2 diabetes. Recent studies showed that Ethulia conyzoides had in-vitro antioxidant activity. This study investigated the in-vivo antidiabetic, antioxidant, and anti-inflammatory potential of the residual aqueous fraction of Ethulia conyzoides in type 2 diabetic-induced male Wistar rats. Sub-acute antidiabetic studies were done with varying doses (100, 200, and 400 mg/kg body weight) of residual aqueous fraction for 21 days. Blood glucose levels, serum insulin, and in vivo antioxidant and pro-inflammatory cytokines-tumour necrosis factor-α (TNF-α) and interleukin-1ß (IL-1ß) -were measured at the end of the treatment. When rats were given different concentrations of residual aqueous fraction, there was a significant (p < 0.05) reduction in blood glucose, malondialdehyde (MDA), IL-1ß, and TNF-α levels, as well as a significant (p < 0.05) increase in SOD (superoxide dismutase), catalase and insulin levels when compared to the diabetic control group. Furthermore, the 400 mg/kg body weight dosage concentration was found to be the most effective. This result suggests that the residual aqueous fraction of Ethulia conyzoides possesses significant antidiabetic, antioxidant and anti-inflammatory activities.

Vitex doniana Leaves Extract Ameliorates Alterations Associated with 7, 12-Dimethyl Benz[a]Anthracene-Induced Mammary Damage in Female Wistar Rats.

Vitex doniana leaves are used traditionally in West Africa for the treatment of swellings and cancer. We investigated if Vitex doniana leaves extract could ameliorate 7, 12-dimethylbenz[a]anthracene (DMBA)-induced mammary damage. Female Wistar rats aged 52 ± 2 day were administered 80 mg/kg DMBA. After monitoring for 150 day, rats were administered 0, 50, 100, 200 mg/kg Vitex doniana and 20 mg/kg Tamoxifen for 14 day. Serum estrogen receptor-α, IL-1ß and TNF -α levels were determined using ELISA kits. Oxidative stress markers in mammary tissue homogenates were determined using standard spectrophotometric methods. Histopathological examination was done using hematoxylin and eosin staining and cyclooxygenase-2 (COX-2) expression using immunohistochemistry. Liquid chromatography-mass spectrometry was used to determine components present in the extract. Although tumors were not observed, significantly (p < 0.05) lower estrogen receptor-α, malondialdehyde, IL-1ß and TNF -α levels, significantly (p < 0.05) higher glutathione and catalase activity, attenuation of malignant epithelial hyperplasia and mild COX-2 expression were observed in rats administered Vitex doniana when compared to DMBA-induced untreated control. Liquid chromatography-mass spectrometry analysis of the V. doniana extract revealed the presence of 4,5-dihydroxy-7-methoxy-6-methylflavone and vanillylamine, which are compounds with reported antioxidant and anti-inflammatory effects. Collectively, treatment with Vitex doniana ameliorated some derangement observed in DMBA-induced rats.

Phytochemical analysis, antioxidant and anti-inflammatory potential of FERETIA APODANTHERA root bark extracts.

BACKGROUND: Inflammation has been implicated in many disorders, including cancer and available therapies elicit adverse effects. Plants of the family Rubiaceae have shown potency against inflammation. The anti-inflammatory and anti-oxidant potential of Feretia apodanthera was investigated in this study to evaluate its effectiveness. METHODS: The phytochemical, antioxidant and anti-inflammatory potential of root bark (n-Hexane, diethyl ether, ethanol and aqueous) extracts of Feretia apodanthera was investigated in this study. The extracts were subjected to various chemical tests for phytochemical constituents; their antioxidant activity was determined using in-vitro DPPH radical scavenging activity assay and their anti-inflammatory activity was determined using carrageenan induced paw oedema model. FTIR and GCMS analysis was done to determine the compounds present. RESULTS: Phytochemical screening of extracts revealed the presence of unsaturated steroids, triterpenes, cardiac glycosides, tannins, saponin and alkaloids. Vitamin C had a median inhibitory concentration (IC50) of 0.038 mg/ml which was lower than IC50 of all the extracts. Of all the extracts, ethanol extract had the lowest IC50 (0.044 mg/ml) which is comparable to vitamin C. Anti-inflammatory studies showed that the inflammation inhibition potential of 400 mg/kg body weight of all the extracts was significantly lower (p < 0.05) than the standard ketoprofen (50 mg/kg) at the first three hours but significantly higher (p < 0.05) at the fourth hour. At the fifth hour, the inflammation inhibition potential of diethyl ether, ethanol and aqueous extracts were significantly higher (p < 0.05) than that of the standard. FTIR analysis showed the presence of ketones, amines, alkenes and carboxylic groups. GCMS analysis revealed compounds that are potential anti-inflammatory agents. CONCLUSION: This study revealed that extracts of Feretia apodanthera possess anti-inflammatory effects against right hind paw oedema of albino rats and can act as an effective antioxidant.

Oxidative Stress and Carcinogenesis: Potential of Phytochemicals in Breast Cancer Therapy.

Breast cancer remains a burden in both developed and developing countries, with higher mortality in developing countries. Attempts to eradicate cancer have not been successful despite the progress made in the development of more novel chemotherapeutic drugs. Reactive-oxygen-species-mediated oxidative stress is known to play a role in breast cancer pathogenesis via genetic and epigenetic modifications, resulting in uncontrolled cell proliferation. Phytochemicals could provide leads for the development of alternative therapeutic agents due to their antioxidant activity, as well as their ability to induce apoptosis in cancer cells. However, most of the studies carried out using in vitro models do not continue with further studies in estrogen-receptor-positive in vivo breast cancer models, or fail to examine the possible biochemical mechanisms of phytochemical-based amelioration. This review examines oxidative-stress-mediated carcinogenesis and the potential of phytochemicals as anticancer agents.

Sickled Erythrocytes Reversal and Membrane Stabilizing Compounds in Telfairia occidentalis.

Background and Purpose. Traditional management of sickle cell disease (SCD) is ubiquitous in Africa. In south-eastern Nigeria, Telfairia occidentalis (T. occidentalis) is strongly recommended for consumption by SCD patients, owing to its presumed therapeutic effect. This study investigates the antisickling and membrane regenerative potentials of T. occidentalis in sickled erythrocytes. Experimental Approach. Sickled erythrocytes obtained from SCD patients were treated with sodium metabisulphite (2%) to induce further sickling. Heat and hypotonic-induced lyses of red blood cells' membranes were also carried out. The RBCs were treated with varying concentration (10.0, 1.0, and 0.1 mg mL(-1) and 0.5, 1.0, 1.5, 2.0, and 2.5 mg mL(-1), resp.) of T. occidentalis extracts as treatment regimen for in vitro antisickling and membrane stabilizing assays. Extract with peak activity was purified and reused in antisickling assay. Key Results. The antisickling activity of aqueous and methanolic extracts of leaves, seeds, and stem of Telfairia occidentalis at 10.0, 1.0, and 0.1 mg mL(-1) revealed that the aqueous leaves extract (10 mg mL(-1)) exhibited the highest antisickling activity (64.03%) which was significantly (p < 0.05) higher than that of the stem (47.30%) and seeds (37.50%). Partially purified fractions recorded improved antisickling effect (peak activity of 70%). Characterization (using GC-MS) of the most active fraction revealed some bioactive compounds. In the membrane stabilizing assay, methanolic and aqueous stem extracts of T. occidentalis showed the highest effect of 71.85% and 61.29%, respectively. Conclusions and Implications. The results provide scientific evidence for ethnopharmacological use of T. occidentalis in the management of SCD.

Hepatocurative potential of Vitex doniana root bark, stem bark and leaves extracts against CCl4-induced liver damage in rats

<p><b>OBJECTIVE</b>To evaluate the hepatocurative effects of aqueous root bark, stem bark and leaves of Vitex doniana in carbon tetrachloride (CCl4) induced liver damage and non induced liver damage albino rats.</p><p><b>METHODS</b>A total of 60 albino rats (36 induced liver damage and 24 non induced liver damage) were assigned into liver damage and non liver damage groups of 6 rats in a group. The animals in the CCl4 induced liver damage groups, were induced by intraperitoneal injection with a single dose of CCl4 (1 mL/kg body weight) as a 1:1(v/v) solution in olive oil and were fasted for 36 h before the subsequent treatment with aqueous root bark, stem bark and leaves extracts of Vitex doniana and vitamin E as standard drug (100 mg/kg body weight per day) for 21 d, while the animals in the non induced groups were only treated with the daily oral administration of these extracts at the same dose. The administration of CCl4 was done once a week for a period of 3 weeks.</p><p><b>RESULTS</b>There was significant (P<0.05) increase in concentration of all liver marker enzymes, alanine aminotransferase, aspartate aminotransferase and alkaline aminotransferase (ALT, AST and ALP) and significant (P<0.05) decrease in albumin in the CCl4 induced liver damage control when compared to the normal control. The extracts caused a significant (P<0.05) reduction in the serum activities of liver marker enzymes (ALT, AST and ALP) and a significant (P<0.05) increase in albumin of all the induced treated groups. Only stem bark extract and vitamin E significantly (P<0.05) increased total protein. All the extracts significantly (P<0.05) lowered serum creatinine whereas only root bark extract significantly (P<0.05) lowered serum level of urea in the rats with CCl4 induced liver damage.</p><p><b>CONCLUSION</b>Hepatocurative study shows that all the plant parts (root bark, stem bark and leaves) possess significant hepatocurative properties among other therapeutic values justifying their use in folklore medicine.</p>

Hepatocurative potential of Vitex doniana root bark, stem bark and leaves extracts against CCl

Objective: To evaluate the hepatocurative effects of aqueous root bark, stem bark and leaves of Vitex doniana in carbon tetrachloride (CCl

Bio-content of Telferia occidentalis and their effect on methemoglobin formation in sickled erythrocytes

Objective: To perform phytochemical and mineral analyses on leaves, stem and seeds of Telferia occidentalis (T. occidentalis), and examine the inhibition of methemoglobin build-up in sickled erythrocytes. Methods: The phytochemical evaluation was carried out by qualitative and quantitative analyses, whereas mineral elements were quantitatively analyzed. The effect of T. occidentalis on methemoglobin formation in sickled erythrocytes was examined using the ratio of ferric ion (Fe

Bio-content of Telferia occidentalis and their effect on methemoglobin formation in sickled erythrocytes

OBJECTIVE@#To perform phytochemical and mineral analyses on leaves, stem and seeds of Telferia occidentalis (T. occidentalis), and examine the inhibition of methemoglobin build-up in sickled erythrocytes.@*METHODS@#The phytochemical evaluation was carried out by qualitative and quantitative analyses, whereas mineral elements were quantitatively analyzed. The effect of T. occidentalis on methemoglobin formation in sickled erythrocytes was examined using the ratio of ferric ion (Fe(2+)) to ferrous ion (Fe(3+)) concentration, as index.@*RESULTS@#The phytochemical evaluation showed the presence of total phenolics, cyanogenic glycosides, flavonoids and alkaloids. Mineral analysis revealed potassium, magnesium, sodium, iron and zinc. Extract concentrations (0.2%-0.8% w/v) of leaves, seeds and stem of T. occidentalis have shown the ability to inhibit the formation of methemoglobin in sickled erythrocytes. The methanolic leaves extract showed the highest effect at 0.8% w/v.@*CONCLUSIONS@#These results suggest that T. occidentalis has the capacity to mop-up methemoglobin in sickled erythrocytes, and may therefore enhance oxygen-hemoglobin binding and transport in sickle cell disease patients.

In vivo antioxidant effect of aqueous root bark, stem bark and leaves extracts of Vitex doniana in CCl4 induced liver damage rats

<p><b>OBJECTIVE</b>The antioxidant effects of aqueous root bark, stem bark and leaves of Vitex doniana (V. doniana) were evaluated in carbon tetrachloride (CCl4) induced liver damage and non induced liver damage albino rats.</p><p><b>METHODS</b>A total of 60 albino rats (36 induced liver damage and 24 non induced liver damage) were assigned into liver damage and non liver damage groups of 6 rats in a group. The animals in the CCl4 induced liver damage groups, were induced by intraperitoneal injection with a single dose of CCl4 (148 mg·ml(-1)·kg(-1) body weight) as a 1:1 (v/v) solution in olive oil and were fasted for 36 h before the subsequent treatment with aqueous root bark, stem bark and leaves extracts of V. doniana and vitamin E as standard drug (100 mg/kg body weighy per day) for 21 d, while the animals in the non induced groups were only treated with the daily oral administration of these extracts at the same dose. The administration of CCl4 was done once a week for a period of three weeks.</p><p><b>RESULTS</b>The liver of CCl4 induced not treated group showed that the induction with CCl4, significantly (P<0.05) increased thiobarbituric acid reactive substance (TBARS) and significantly (P<0.05) decreased superoxide dismutase (SOD) and catalase (CAT). However there was no significant (P>0.05) difference between TBARS, SOD and CAT in the liver of the induced treated groups and normal control group. In the kidney, TBARS showed no significant (P>0.05) difference between the normal and the induced groups, SOD was significantly (P<0.05) reduced in the CCl4 group compared to standard drug and normal control groups, CAT was significantly (P<0.05) increased in root and vitamin E groups when compared to induced not treated group. The studies also showed that when the extracts were administered to normal animals, there was no significant (P>0.05) change in the liver and kidney level of TBARS, SOD and CAT compared with the normal control except in the kidney of animals treated with stem extract where TBARS was significantly (P<0.05) lowered compared to control group.</p><p><b>CONCLUSION</b>The result of the present study suggests that application of V. doniana plant would play an important role in increasing the antioxidant effect and reducing the oxidative damage that formed both in liver and in kidney tissues. However stem bark has potential to improve renal function in normal rats.</p>