In vitro anti-cholinesterase and anti-oxidant activity of three standardised polyherbal products used for memory enhancing in ethnomedicine of South-East Nigeria

Background: Polyherbal standardised extracts used in ethnomedicine of Eastern Nigeria for memory improvements were evaluated for anti-cholinesterases and anti-oxidant properties. Methods: Anti-cholinesterase, anti-oxidant, and total phenolic and flavonoid contents were established using standard procedures. Results: The three polyherbal extracts exhibited significant concentration dependent acetylcholinesterase (AChE) inhibitory activity (P = 0.001). The highest AChE inhibition was observed with the Neocare Herbal Tea (NHT) with 99.7% (IC50 = 324 μg/mL); whereas the Herbalin Complex Tea (HCT) and Phytoblis Herbal Tea (PHT) exhibited 73.8% (IC50 = 0.2 μg/mL) and 60.6% (IC50 = 0.7 μg/mL) inhibition, respectively, relative to eserine at 100% inhibition (IC50 = 0.9 μg/mL) at 200 μg/mL. The order of percentage increase in inhibition of AChE was NHT > HCT > PHT; while the order of decrease in potency was HCT > PHT > NHT. Radical scavenging activities of HCT, NHT and PHT were 82.13% (IC50 = 0.08 μg/mL), 77.43% (IC50 = 0.01 μg/mL) and 76.28% (IC50 = 0.3 μg/mL), respectively, at 1 mg/mL concentrations. The reducing power revealed a dose-dependent effect, with NHT > PHT > HCT. The order of total phenolics content in the extracts were PHT > HCT > NHT, and for total flavonoids content: PHT > NHT > HCT. Conclusion: The three polyherbal standardised products possess significant acetylcholinesterase inhibitory activity and secondary metabolites that could collectively contribute to their memory-enhancing effects

Hepatoprotective and antioxidant activities of Spondias mombin leaf and stem extracts against carbon tetrachloride-induced hepatotoxicity

Objective Spondias mombin L. is a tree used in folk medicine in Nigeria for the treatment of hepatitis. This study was carried out to comparatively evaluate the hepatoprotective and antioxidant effects of S. mombin leaf and stem (SML and SMS) methanolic extracts in a rat model of carbon tetrachloride (CCl4)-induced hepatotoxicity. Methods Forty-two rats were distributed into seven groups. Groups A and B received water; groups C and D received 500 and 1000 mg/kg SML extract, respectively; groups E and F received 500 and 1000 mg/kg SMS extract, respectively; and group G received 100 mg/kg silymarin. Water, the two extracts, and silymarin were administered daily by oral gavage for 7 days. Hepatotoxicity was induced in groups B to G by the administration of CCl4 once on the seventh day. After 48 h, rats were sacrificed, and tissues and serum samples were examined for histological and biochemical indices of hepatotoxicity. Results Administration of CCl4 resulted in liver injury with significant elevation in the hepatocellular injury markers alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), total bilirubin (TBIL), and conjugated bilirubin (CBIL), associated with a significant reduction in total circulatory protein. Pretreatment with SML and SMS extracts at both doses significantly ameliorated liver injury; lowered ALT, AST, ALP, TBIL, and CBIL levels; elevated cellular glutathione levels as well as catalase and superoxide dismutase activities; and decreased the levels of thiobarbituric acid reactive substances. Conclusion This study provides preliminary evidence supporting the potential therapeutic benefit of S. mombin in xenobiotic-induced hepatotoxicity

Role of oxidative stress in antituberculous drugs (individuals and combined) cytotoxicity in HepG2 cells

Hepatotoxicity is a common side and toxic effect of Antituberculous (Anti-TB) drugs with reported higher incidence with anti-TB combinations. Oxidative stress was shown to have a role. This study examined oxidative stress effects of the first line Anti-TB drugs; Rifampicin (RIF), isoniazid (INH) and pyrazinamide PZA (individually and combined) on HepG2 cells. MTT assay (3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) was used to study the cytotoxic effect of the tested Anti-TB drugs. The effect of anti-TB drugs on total glutathione HepG2 cells and the production of reactive oxygen species (ROSs) were studied (individually and in combinations). Furthermore, the protective effect of the antioxidant reduced glutathione was assayed. The data revealed that the tested anti-TB were cytotoxic to HepG2 cells. RIF was the most potent. The tested drugs in their estimated IC50s, to different extents, enhanced significantly (P<0.0001) ROSs production and decreased total glutathione (P <0.0001). Furthermore, 48 hours pre-treatment with INH (3mM) significantly increased ROS production and decreased glutathione with RIF (0.1mM) (P <0.01 and P <0.05 respectively) and PZA (10 mM) (P <0.01 and P <0.05 respectively). Combined RIF (0.1mM) and INH (3mM) significantly decreased total glutathione (P<0.05 for each) and increased ROSs production (P<0.05) in HepG2 cells (P<0.05 for each). Interestingly, reduced glutathione (GSH) significantly decreased the cytotoxicity of RIF and INH (P=0.005 and 0.015, respectively). These data showed that oxidative stress play a crucial role in anti-TB induced hepatotoxicity, which can be alleviated by inclusion of antioxidant in therapy, though there is need of clinical trials. Moreover, combined anti-TB therapy should be considered as a risk factor with any other oxidative liver injuries

ANTIDIARRHEAL MECHANISM AND IONIC PROFILE OF CARPOLOBIA LUTEA ETHANOLIC STEM-BARK EXTRACT IN RATS.

Background: The stem-bark extract of Carpolobia lutea (Polygalaceae), used in ethno-medicine as anti-diarrhea was pharmacologically evaluated. This was the first report of assessment of the ethanolic stem extract (ESE), of C. lutea as anti-diarrhoeal agent in rats. The anti-diarrhoeal effects, acute toxicity and ionic profile are investigated and reported. Materials and Methods: The acute toxicity was established using Lock’s method. The anti-diarrhoeal effects were demonstrated using castor oil-induced diarrheal and fluid accumulation and its effect on normal intestinal transit. The mechanism elucidated using yohimbine, isosorbide dinitrate, and diphenoxylate. The elemental and ionic profile of ESE was established using inductively coupled argon-plasma emission spectrometer and potentiometric titration respectively. The finger print of ESE was revealed by Jasco (Tokyo, Japan), HPLC and active compounds by phytochemical screening using standard procedure. Results: The LD50 obtained is 866.025 mg/kg (i.p). The doses of 43.3, 86.6, and 173.2 mg/kg of ESE showed inhibition of castor oil–induced diarrheal (

Anti-acetylcholinesterase activity and antioxidant properties of extracts and fractions of Carpolobia lutea

Context: There is an unmet need to discover new treatments for Alzheimer’s disease. This study determined the anti-acetylcholinesterase (AChE) activity, DPPH free radical scavenging and antioxidant properties of Carpolobia lutea G. Don (Polygalaceae).Objective: To quantify C. lutea anti-AChE, DPPH free radical scavenging, and antioxidant activities, and cell cytotoxicity.Materials and methods: Plant stem, leaves, and roots were subjected to sequential solvent extractions, and screened for anti-AChE activity across a concentration range of 0.02-200 μg//mL. Plant DPPH radical scavenging activity, reducing power, and total phenolic and flavonoid content were determined, and cytotoxicity evaluated using human hepatocytes.Results: C. lutea exhibited concentration dependent anti-AChE activity. The most potent inhibitory activity for the stem was the crude ethanol extract and hexane stem fraction oil (IC₅₀ = 140 μg/mL); for the leaves the chloroform leaf fraction (IC₅₀ = 60 μg/mL/mL); and for roots, the methanol, ethyl acetate, and aqueous root fractions (IC₅₀ = 0.3-3 μg/mL). Dose-dependent free radical scavenging activity and reducing power were observed with increasing stem, leaf, or root concentration. Total phenolics were highest in the stem: ~632 mg gallic acid equivalents/g for a hexane stem fraction oil. Total flavonoid content was highest in the leaves: ~297 mg quercetin equivalents/g for a chloroform leaf fraction. At 1 μg/mL, only the crude ethanol extract oil was significantly cytotoxic to hepatocytes.Discussion and conclusion: C. lutea possesses anti-AChE activity and beneficial antioxidant capacity indicative of its potential development as a treatment of Alzheimer’s and other diseases characterized by a cholinergic deficit

Anti-inflammatory and antinociceptive activities of Solenostemon monostachyus aerial part extract in mice

Objective: Solenostemon monostachyus is used in traditional medicine for the treatment of various ailments such as ulcer, hypertension, pains and inflammatory diseases. Evaluation of anti-inflammatory and analgesic activities of S. monostachyus aerial parts was carried out to ascertain its uses in traditional medicine. Materials and Methods: The aerial parts of S. monostachyus was cold extracted by soaking the dried powdered material in ethanol. The aerial parts crude extract (75 –225 mg/kg) of  S. monostachyus was investigated for analgesic and anti-inflammatory activities using various experimental models; acetic acid, formalin and thermal- induced pains models for analgesic study and carrageenin, egg albumin and xylene – induced edema models for anti-inflammatory investigation. Results: The extract caused a significant (pConclusion: The anti-inflammatory and analgesic effects of this plant may in part be mediated through the chemical constituents of the plant and the results of the analgesic action suggest central and peripheral mechanisms. The findings of this work confirm the ethno medical use of this plant to treat inflammatory conditions

Amino acid, Antioxidant and Ion Profiles of Carpolobia lutea (Polygalaceae)

Purpose: To evaluate the amino acid, antioxidant and ionic profiles of Carpolobia lutea leaf (Polygalaceae) extract (CLL). Methods: The powdered leaf was macerated and subjected to gradient solvent extraction with nhexane, chloroform, ethyl acetate and ethanol for 72 h to obtain their respective fractions. Amino acid analysis was by cation-exchange chromatography using automated amino acid analyser. Antioxidant potential was obtained by spectrophotometric assay using 2, 2-Diphenyl-1-picrylhydrazyl DPPH while elemental and ionic analyses were carried out by atomic absorption spectrophotometry and potentiometric titration, respectively. Results: MProline, alanine, serine, valine, glycine, glutamate and lysine were found in the ethanol fraction while lysine, phenyl alanine, glycine and serine were present in the ethyl acetate fraction but not in the non-polar fractions, n-hexane and chloroform. The ethyl acetate fraction contained more lysine, phenyl alanine, glycine and serine the other leaf fractions. Minimal radical scavenging activity of all the fractions was recorded. The most abundant cations in the extract were potassium and phosphorus (2.16 ± 0.05 and 1.90 ± 0.06 mg/g, respectively) while the most abundant anion was phosphate with a concentration of 23.23 ± 4.61 mg/g for the aqueous leaf fraction. Conclusion: The study shows that CLL fractions contain variety of amino acids which could promote wound healing, as well as major and minor elemental ions which, as essential body electrolytes, are required for various metabolic processes in the body

Amino acid, Antioxidant and Ion Profiles of Carpolobia lutea Leaf (Polygalaceae)

Purpose: To evaluate the amino acid, antioxidant and ionic profiles of Carpolobia lutea leaf (Polygalaceae) extract (CLL).Methods: The powdered leaf was macerated and subjected to gradient solvent extraction with n-hexane, chloroform, ethyl acetate and ethanol for 72 h to obtain their respective fractions. Amino acid analysis was by cation-exchange chromatography using automated amino acid analyser. Antioxidant potential was obtained by spectrophotometric assay using 2, 2-Diphenyl-1-picrylhydrazyl DPPH while elemental and ionic analyses were carried out by atomic absorption spectrophotometry and potentiometric titration, respectively.Results: Proline, alanine, serine, valine, glycine, glutamate and lysine were found in the ethanol fraction while lysine, phenyl alanine, glycine and serine were present in the ethyl acetate fraction but not in the non-polar fractions, n-hexane and chloroform. The ethyl acetate fraction contained more lysine, phenyl alanine, glycine and serine the other leaf fractions. Minimal radical scavenging activity of all the fractions was recorded. The most abundant cations in the extract were potassium and phosphorus (2.16 +/- 0.05 and 1.90 +/- 0.06 mg/g, respectively) while the most abundant anion was phosphate with a concentration of 23.23 +/- 4.61 mg/g for the aqueous leaf fractionConclusion: The study shows that CLL fractions contain variety of amino acids which could promote wound healing, as well as major and minor elemental ions which, as essential body electrolytes, are required for various metabolic processes in the body.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP