Isolation of novel para-pentyl phenyl benzoate from Mondia whitei.(Hook.F.) skeels (periplocaceae), its structure, synthesis and neuropharmacological evaluation

Background: Mondia whitei L. (Hook. F.) Skeels (Periplocaceae) is a medicinal plant used locally in managing pain, fever, loss of appetite and as aphrodiasc in the South-Western states of Nigeria. However, the fruit is consumed habitually in the South-Eastern states of Nigeria, leading to speculation that it may possess some central nervous system effect but which has not been scientifically investigated, hence this study.Methodology: Fresh fruits of Mondia whitei were collected and identified by a taxonomist. They were chopped into small pieces and extracted with absolute ethanol. The crude extract was subjected to various chromatographic techniques to isolate a novel compound whose structure was elucidated from the analysis of the crystal data and by extensive use of spectroscopy. The structure was confirmed by synthesis. The compound was subjected to anxiolytic and sedative activity assay. Computational analysis of the receptor binding event of isolated compound at the gamma amino butyric acid A receptor was also evaluated.Results: The structure of the compound was elucidated as para pentyl phenyl benzoate. The neuropharmacological evaluation of the compound indicated significant (p<0.05) depression of the central nervous system. The binding characteristics of the compound to gamma amino butyric acid A receptors appears to be more favorable than those obtained for gamma amino butyric acid, chlorpromazine, benzamidine, and is comparable with the affinity obtained for pentobarbitone and diazepam.Conclusion: These present data provide evidence for the role of para pentyl phenyl benzoate in the habitual consumption of the fruit as well as its central nervous system activities.Keywords: Mondia whitei, Periplocaceae, isolation and synthesis, sedative and anxiolytic effect and Para pentylphenyl benzoat

Chemical and biological studies of Lobelia flaccida (C. Presl) A.DC leaf: a medicinal plant used by traditional healers in Eastern Cape, South Africa

Purpose: To investigate the phytochemical constituents, acute toxicity and biological activities of Lobelia herb (dried leaf of Lobelia flaccida; family: Campanulaceae), a popular medicinal agent used to manage pain and epilepsy among other indications in Eastern Cape Region of South Africa.Methods: Essential oil (EO) obtained from the dried leaf was analysed with gas chromatography-mas spectroscopy GC/MS while an infusion extract of the herb was obtained by soaking in hot boiled water (100 oC) for 24 h, filtered and the filtrate dried in vacuo. Phytochemical screening of the infusion extract was performed to detect the presence of secondary plant metabolites and relative abundance of some of the metabolites. The aqueous extract was evaluated for oral (p.o.) acute toxicity (LD50) using the Lorke’s method [30];, thereafter the extract was tested for anti-inflammatory activity on carrageenaninduced rat paw oedema at 250 and 500 mg/kg, p.o., normal saline and aspirin (100 mg/kg, p.o.) used as negative and positive controls respectively. Finally, the extract at 500 and 1000 mg/kg, p.o. was tested for anticonvulsant activity on pentylene tetrazol (85 mg/kg, intraperitoneally)-induced convulsion model in mice, normal saline and diazepam (1 mg/kg, i.p.) served as negative and positive control groups respectively.Results: EO yield was 0.022 % w/w and the two major compounds identified were acetophenone (26.37 %) and caryophyllene (17.35 %). Phytochemical screening showed high concentration of alkaloids, saponins and flavonoids among other constituents. LD50 of the aqueous extract was ≥ 5000 mg/kg per oral while the aqueous extract exhibited significant (p < 0.01) anti-inflammatory activity on carrageenan-induced rat paw oedema comparable to aspirin but insignificant anticonvulsant activity on pentylene tetrazol-induced convulsion when compared with diazepam.Conclusion: Lobelia herb is non-toxic, and possesses significant anti-inflammatory and mild anticonvulsant activities. It is suggested that the essential oil of this herb should be screened for pharmacological activities.Keywords: Lobelia flaccida, Essential oil, Gas chromatography/mass spectroscopy analysis , Infusion extract, Acute toxicity, Anti-inflammatory, Anti-convulsan

Isolation of novel para-pentyl phenyl benzoate from Mondia whitei. (Hook.F) Skeels (Periplocaceae), its structure, synthesis, and neuropharamacological evaluation

Background: Mondia whitei L. (Hook. F.) Skeels (Periplocaceae) is a medicinal plant used locally in managing pain, fever, loss of appetite and as aphrodiasc in the South-Western states of Nigeria. However, the fruit is consumed habitually in the South-Eastern states of Nigeria, leading to speculation that it may possess some central nervous system effect but which has not been scientifically investigated, hence this study. Methodology: Fresh fruits of Mondia whitei were collected and identified by a taxonomist. They were chopped into small pieces and extracted with absolute ethanol. The crude extract was subjected to various chromatographic techniques to isolate a novel compound whose structure was elucidated from the analysis of the crystal data and by extensive use of spectroscopy. The structure was confirmed by synthesis. The compound was subjected to anxiolytic and sedative activity assay. Computational analysis of the receptor binding event of isolated compound at the gamma amino butyric acid A receptor was also evaluated. Results: The structure of the compound was elucidated as para pentyl phenyl benzoate. The neuropharmacological evaluation of the compound indicated significant (p<0.05) depression of the central nervous system. The binding characteristics of the compound to gamma amino butyric acid A receptors appears to be more favorable than those obtained for gamma amino butyric acid, chlorpromazine, benzamidine, and is comparable with the affinity obtained for pentobarbitone and diazepam. Conclusion These present data provide evidence for the role of para pentyl phenyl benzoate in the habitual consumption of the fruit as well as its central nervous system activities

CHEMICAL ANALYSIS AND BIOLOGICAL POTENTIAL OF VALERIAN ROOT AS USED BY HERBAL PRACTITIONERS IN THE EASTERN CAPE PROVINCE,

Background: Herbal practitioners in the Eastern Cape of South Africa use valerian root (Valeriana capensis, Valerianaceae) to manage pains, arthritis and inflammation. The herb prepared from this plant was studied to determine the chemical composition of it’s essential oil, carried out phytochemical screening and biological activities on its infusion extract as used by the herbal practitioner. Materials and Methods: Essential oil of Valerian root was obtained by hydrodistillation and subjected to chemical analyses. Infusion extract of the Valerian root was screened to determine its secondary metabolites and the relative abundance of some major metabolites. The infusion extract was further evaluated for acute toxicity (LD50), anti-inflammatory and analgesic activities in rodents. Results: The yield of the essential oil was 0.18% w/w. The GC/MS analysis indicated the presence of 42 compounds with major ones being caryophyllene oxide (18.11%), viridiflorol (9.37%) and bornyl acetate (8.84%). Phytochemicals found in the infusion extract were alkaloids, saponins, tannins and flavonoids while quantitative screenings showed saponins and flavonoids accounted for 6.39% and 7.40% respectively. The LD50 of the extract was found to be 3808 mg/kg per oral. The infusion extract of the root (250-500 mg/kg, p.o.) caused significant (

Behavioural activities and chemical composition of fresh leaf essential oil of Plectranthus aegyptiacus from Southwest Nigeria in mice

Objectives: This study determined the chemical composition of essential oil obtained from fresh leaf of Plectranthus aegyptiacus, and evaluated it for novelty-induced behavioural (NIB) and determine its mechanism(s) of action in mice. Methods: The oil was hydro-distillated, and analyzed using gas chromatography-mass spectrometry. The effects of the oil (50, 100 and 150 mg/kg; i.p., n=6) on novelty-induced behavioural was assessed using open field test and head dipping on hole board. Probable mechanism(s) were evaluated using antagonists: flumazenil, naloxone and cyproheptadine at 2 mg/kg each, atropine and yohimbine at 5 mg/kg and 1 mg/kg respectively. Key Findings: The LD50 values obtained were 2154 and 490 mg/kg for oral and intraperitoneal routes respectively. The oil (50, 100 and150 mg/kg) significantly (p less 0.05, 0.01 and 0.01) inhibited all NIB and head dips. Flumazenil significantly (p less than 0.05) reversed the effect of the oil on NIB; atropine, naloxone and cyproheptadine significantly (p less than 0.01, 0.01 and 0.001) potentiated inhibitory effect on NIB respectively, while yohimbine showed no significantly effect. The analyzed oil showed 61 compounds, and the major compounds were carvacrol, germacrene-D, p-cymene and [1,1'-Bicyclopentyl]-2,2'-diol. Conclusions: The study concluded that the oil possessed central nervous system depressant activity, which could be mediated mainly through augmentation of GABAergic neurotransmission, while cholinergic-(muscarinic), adrenergic and serotonergic pathways may be involved

ISOLATION OF NOVEL PARA-PENTYL PHENYL BENZOATE FROM MONDIA WHITEI.(HOOK.F.) SKEELS (PERIPLOCACEAE), ITS STRUCTURE, SYNTHESIS AND NEUROPHARMACOLOGICAL EVALUATION.

Background: Mondia whitei L. (Hook. F.) Skeels (Periplocaceae) is a medicinal plant used locally in managing pain, fever, loss of appetite and as aphrodiasc in the South-Western states of Nigeria. However, the fruit is consumed habitually in the South-Eastern states of Nigeria, leading to speculation that it may possess some central nervous system effect but which has not been scientifically investigated, hence this study. Methodology: Fresh fruits of Mondia whitei were collected and identified by a taxonomist. They were chopped into small pieces and extracted with absolute ethanol. The crude extract was subjected to various chromatographic techniques to isolate a novel compound whose structure was elucidated from the analysis of the crystal data and by extensive use of spectroscopy. The structure was confirmed by synthesis. The compound was subjected to anxiolytic and sedative activity assay. Computational analysis of the receptor binding event of isolated compound at the gamma amino butyric acid A receptor was also evaluated. Results: The structure of the compound was elucidated as para pentyl phenyl benzoate. The neuropharmacological evaluation of the compound indicated significant (

Antinociceptive and Anti-Inflammatory Activities of the Ethanol Extract of Annona muricata L. Leaves in Animal Models

Antinociceptive and anti-inflammatory activities of the ethanol extract from Annona muricata L. leaves were investigated in animal models. The extract delivered per oral route (p.o.) reduced the number of abdominal contortions by 14.42% (at a dose of 200 mg/kg) and 41.41% (400 mg/kg). Doses of 200 and 400 mg/kg (p.o) inhibited both phases of the time paw licking: first phase (23.67% and 45.02%) and the second phase (30.09% and 50.02%), respectively. The extract (p.o.) increased the reaction time on a hot plate at doses of 200 (30.77% and 37.04%) and 400 mg/kg (82.61% and 96.30%) after 60 and 90 minutes of treatment, respectively. The paw edema was reduced by the ethanol extract (p.o.) at doses of 200 (23.16% and 29.33%) and 400 mg/kg (29.50% and 37.33%) after 3 to 4 h of application of carrageenan, respectively. Doses of 200 and 400 mg/kg (p.o.), administered 4 h before the carrageenan injection, reduced the exudate volume (29.25 and 45.74%) and leukocyte migration (18.19 and 27.95%) significantly. These results suggest that A. muricata can be an active source of substances with antinociceptive and anti-inflammatory activities