Phytochemical investigation and anti-inflammatory property of ethanol-water extract of the roots of Anthocleista djalonensis A. Chev. (Gentianiaceae)

Anthocleista djalonensis A.Chev. (Gentianiaceae) a plant of West African origin is used for the treatment of inflammatory disorders traditionally. Phytochemical screening of the plant root material gave positive result for tannins, saponins and carbohydrate; but negative for alkaloids and flavonoids. The ethanol-water (1:1) extract of the root material was subjected to anti-inflammatory activity using experimental animal model. From the results obtained, the crude extract showed significant activity (p < 0.05) comparable to the reference drug used. Chromatographic separation of the crude extract furnished a yellow viscous liquid, identified spectroscopically as sweroside. The pure compound was also subjected to anti-inflammatory activity, this showed significant activity (p < 0.05) at 100 mg/kg. The results of the study showed the justification of the use of the plant in the treatment of inflammatory disorders in ethnomedicine.Key words: Anti-inflammatory activity, Anthocleista djalonensis, ethanol-water extract, swerosid

Synthesis, Anti-inflammatory and Anti-nociceptive Evaluation of Palmitoyl Benzamides

Purpose: To synthesize and characterize palmitoyl amino benzamides, and to evaluate them for possible anti-inflammatory and anti-nociceptive activities.Methods: Palmitoyl amino benzamides were synthesized by the opening of isatoic anhydride ring with respective amino acids (glycine, β-alanine and γ-aminobutyric acid) and the condensation of the product with palmitoyl chloride. The final products were purified on column chromatography, eluting with dichloromethane/ethyl acetate. All the compounds were unequivocally characterized using the combination of infra red (IR), 1H and 13C (nuclear magnetic resonance (NMR), mass spectrometry (MS) and elemental analysis. In vivo anti-inflammatory and anti-nociceptive activities of the synthesized compounds at 20, 50 and 100mg/kg doses were carried out using carrageenan-induced paw oedema in rat and acetic acid-induced writhing in mice, respectively. Aspirin was used at a dose of 100mg/kg as the reference drug.Results: The compounds were obtained in high yield (70 – 90 %) and purity. The anti-inflammatory results showed a poor activity for the compounds except o-palmitoylamino N-carboxyethyl benzamide which produced significant inhibition (p < 0.05) at a dose of 50 mg/kg (43.8 % oedema inhibition) while the reference drug, aspirin, showed 51.3 % inhibition. The anti-nociceptive study, however, showed good inhibition (p < 0.05) of acetic acid-induced writhing, with o-palmitoylamino Ncarboxymethylbenzamide producing 86.2 % inhibition at 100 mg/kg dose compared with the reference drug (aspirin) which gave 74.3 % inhibition at 100 mg/kg.Conclusion: The findings of this study indicate that the synthesized compounds, though displaying poor anti-inflammatory activity, do possess promising anti-nociceptive activity.Keywords: Anti-inflammatory, Analgesic, Benzamide, Palmitoyl, Glycine, β-Alanine, γ-Aminobutyric acid, Aspiri

Smooth muscle relaxant activity of 3- carbomethoxylpyridine from Pyrenacantha staudtii leaf on isolated rat uterus

Pyrenacantha staudtii leaf (Icacinaceae) is a medicinal herb used in ethnomedicine for the treatment of threatened abortion and gastrointestinal disorders. Previous chemical work in our laboratory reported the isolation and characterization of 3- carbomethoxylpyridine from the methanolic extract of this plant. The inhibitory effect of the crude extract on isolated rat uterus was also established. The objective of this study was to investigate the inhibitory activity of the isolated compound, 3- carbomethoxylpyridine,on rat isolated uterine preparation. This was achieved by subjecting the compound to uterine preparation in an organ bath containing a physiological salt solution of De Jalon. The contractions were recorded with an FT03 transducer attached to an Ugo Basil recorder. The study has shown for the first time that 3-carbomethoxylpyridine has a relaxant effect on the smooth muscle of the uterus promotingrelaxation of the spontaneous and oxytocin-induced contractions

Reactions of O-Amino-N-(1,1-Dimethylprop-2-Ynyl)-Benzamide

Carbonylation of o-amino-N-(1,1-dimethylprop-2-ynyl)-benzamide 3 with ethyl chloroformate gave 2-carbethoxyamino-N-(1,1-dimethylprop- 2-ynyl)-benzamide 6. Attempted cyclization of 6 under basic conditions did not give the quinazoline 8 but an oxazole 7. When 3 was also refluxed in triethylorthoformate-acetic anhydride mixture, 2-acetylamino-N-(1,1-dimethylprop- 2-ynyl)-benza-mide 4 was formed as the major compound with negligible amount of 3-(1,1- dimethylprop-2-ynyl)-quinazolin-4-(3H)-one 5

Biochemical and histopathological studies on the methanolic extract of Jatropha tanjorensis (J.L. Ellis and Soroja) leaves

This study seeks to evaluate the biochemical and the histopathological characteristics of rats administered with various doses of methanolic extract of Jatropha tanjorensis leaf. Wistar albino rats fed with 500 mg/kg and 2 g/kg of methanolic extract of Jatropha tanjorensis leaf for 28 days were dissected and vital organs collected for histopathological examination after blood had been taken for biochemical evaluation The biochemical parameters assessed were Na+, Ca2+, Cl-, HCO3-, K+, albumin, creatinine, total protein, urea, alkaline phosphatase, alanine transaminase and aspartate transaminase. The plant extract did not affect the levels of serum electrolytes, proteins and liver enzymes significantly. There was a mild hypertrophy of the vascular vessels of the liver, heart, spleen and the kidney at a dose of 500 mg/kg and 2000 mg/kg of the plant extract. The results suggest that the methanolic extract may be safe to the animals at the stated doses.Keywords: Biochemical, histopathology, enzymes, Jatropha tanjorensi