Extracts of Leptadenia hastata Leaf, a Famine Food and Traditional Remedy for Furuncles, Suppress Inflammation in Murine Models.

The effects of the methanol extract (LHE), hexane (LHHF), ethylacetate (LHEF) and methanol (LHMF) fractions of leaf of Leptadenia hastata on acute and chronic inflammation were studied. Furthermore, the effects of LHE on acetic acid induced increase in vascular permeability, carrageenan induced leucocyte migration and membrane stability were evaluated. The LHE and fractions were also subjected to phytochemical analysis. The LHE, LHEF and LHMF significantly (p < 0.05) suppressed topical ear edema, systemic paw edema, global edematous response to formaldehyde arthritis and granuloma tissue growth. The LHE suppressed acetic acid induced vascular permeability and carrageenan-induced leucocyte migration, and also stabilized the erythrocyte membrane. An acute toxicity test in mice established an oral LD50 > 5 g/kg for LHE. The LHEF elicited the greatest inhibition, suggesting that the observed anti-inflammatory effects may be attributable to the flavonoids abundant in the fraction. These findings demonstrate that the effectiveness of L. hastata leaf in the treatment of furuncles may largely derive from anti-inflammatory activities mediated through inhibition of both increase in vascular permeability and leucocyte migration, and stabilization of cell membranes.

Antimicrobial Effects of a Lipophilic Fraction and Kaurenoic Acid Isolated from the Root Bark Extracts of Annona senegalensis.

Root bark preparation of Annona senegalensis Pers. (Annonaceae) is used in Nigerian ethnomedicine for treatment of infectious diseases. Extraction of the A. senegalensis powdered root bark with methanol-methylene chloride (1 : 1) mixture yielded the methanol-methylene extract (MME) which was fractionated to obtain the ethyl acetate fraction (EF). The EF on further fractionation gave two active subfractions, F1 and F2. The F1 yielded a lipophilic oily liquid while F2 on purification, precipitated white crystalline compound, AS2. F1 was analyzed using GC-MS, while AS2 was characterized by proton NMR and X-ray crystallography. Antibacterial and antifungal studies were performed using agar-well-diffusion method with 0.5 McFarland standard and MICs calculated. GC-MS gave 6 major constituents: kaur-16-en-19-oic acid; 1-dodecanol; 1-naphthalenemethanol; 6,6-dimethyl-bicyclo[3.1.1]hept-2-ene-2-ethanol; 3,3-dimethyl-2-(3-methylbuta-1,3-dienyl)cyclohexane-1-methanol; 3-hydroxyandrostan-17-carboxylic acid. AS2 was found to be kaur-16-en-19-oic acid. The MICs of EF, F1, and AS2 against B. subtilis were 180, 60, and 30 µg/mL, respectively. AS2 exhibited activity against S. aureus with an MIC of 150 µg/mL, while F1 was active against P. aeruginosa with an MIC of 40 µg/mL. However, the extracts and AS2 exhibited no effects against Candida albicans and Aspergillus niger. Therefore, kaurenoic acid and the lipophilic fraction from A. senegalensis root bark exhibited potent antibacterial activity.

Studies on the antiulcer and gastrointestinal effects of stem bark extract of Bridelia ferruginea.

The antiulcer and gastrointestinal effects of methanol stem bark extract (BFME) of Bridelia ferruginea Benth. (Euphorbiaceae) and its solvent fractions-dichloromethane (DCMF) and methanol (MF)-were studied using indomethacin- and ethanol-induced ulcers in rats, small intestinal transit of charcoal meal in mice, and the effects on acetylcholine-induced contractions of the isolated guinea pig ileum. The extract and fractions significantly (P<0.05) protected the rats against ethanol and indomethacin-induced ulcers and inhibited small intestinal propulsion in the order of magnitude: DCMF>MF>BFME. On the guinea pig ileum, MF (0.05 - 6.40 mg/ml) elicited no inhibition, DCMF (5 - 40 µg/ml) antagonized acetylcholine-induced contractions of the guinea pig ileum with IC50 of 10.47µg/ml, while BFME (0.05 - 12.80 mg/ml) contracted the guinea pig ileum with EC50 of 1 mg/ml. Oral LD50 of BFME in mice was estimated to be 2,154 mg/kg. Phytochemistry tests revealed the presence of tannins, saponins, steroids, terpenoids, flavonoids and resins in BFME, MF tested positive for tannins, saponins, steroids, terpenoids, and flavonoids, while DCMF gave positive reactions for flavonoids, steroids, terpenoids and resins. These findings suggest that constituents of the stem bark of B. ferruginea possess antiulcer properties. In addition, some non-polar constituents possess spasmolytic activity while spasmogenic activity is likely associated with some polar constituents.

The anti-inflammatory and antinociceptive properties of the chloroform fraction from Phyllanthus niruri plant is mediated via the peripheral nervous system.

Phyllanthus niruri (Euphorbiaceae) is used folklorically for the treatment of diabetes, malaria, fever, diarrhea, liver disease, and urolithiasis. As an initial step toward isolating compounds effective against inflammation and pain, this study is aimed at providing scientific evidence for the anti-inflammatory, antinociceptive, and antipyretic properties of the chloroform soluble fraction (PNF1) of Phyllanthus niruri methanol extract in rats and mice. Three doses of PNF1 [25, 50, 100 mg/kg body weight (bw)] were used. Screening was done using acetic-acid-induced writhing, egg-albumin-induced pedal inflammation, Randall-Selitto test, hot-plate test, and yeast-induced pyresis as experimental models. Results show that PNF1 significantly (p < .01) inhibited writhing response induced by acetic acid at all doses used by 56.2%-66.7% and caused significant (p < .05, p < .01) reduction of yeast-induced pyrexia (21.6%-40.9%). Significant (p < .01) reduction of egg albumin-induced inflammation was observed only at a dose of 100 mg PNF1/kg bw, which was comparable with the effect produced by aspirin (100 mg/kg bw). At 50 and 100 mg/kg bw, PNF1 significantly (p < .05, p < .01) increased pain threshold of inflamed tissue in the Randall-Selitto test but did not increase response to thermally induced pain in the hot-plate test. It is concluded that PNF1 possesses antipyretic, anti-inflammatory, and antinociceptive effects that are peripherally mediated. This justifies its use in traditional medicine and its potential as a candidate for further development.