Ursane-Type Triterpenes, Phenolics and Phenolic Derivatives from Globimetula braunii Leaf.

Globimetula braunii is a hemi-parasitic plant used in African ethnomedicine for the management of microbial infections, rheumatic pain and tumors amongst others. We report the isolation and characterization of eight compounds with their antioxidant and antimicrobial activities. The air-dried powdered leaf was macerated in EtOH/H20 (4:1). The extract was solvent-partitioned into n-hexane, EtOAc, n-BuOH and aqueous fractions. The fractions were screened for their antioxidant properties, using DPPH, FRAP, TAC and FIC assays. Antimicrobial analysis was performed using the micro-broth dilution method. The active EtOAc fraction was purified for its putative compounds on a repeated silica gel column chromatography monitored with TLC-bioautography. The isolated compounds were characterized using spectroscopic methods of UV, FT-IR, NMR and MS. Eight compounds (1-8) were isolated and characterized as 13,27-cycloursane (1), phyllanthone (2), globraunone (3), three phenolics: methyl 3,5-dihydroxy-4-methoxybenzoate (4), methyl 3-methyl-4-hydroxybenzoate (5) and guaiacol (6), as well as two phenol derivatives: 4-formaldehyde phenone (7) and 6-methoxy-2H-inden-5-ol (8). The study identified 4 and 6 as natural antioxidant compounds with potential as antimicrobial agents.

Evaluation of ethnomedical claim III: anti-hyperglycemic activities of Gongronema latifolium root and stem.

BACKGROUND: The insulinotropic activity of the combined root and stem of Gongronema latifolium (Asclepiadaceae) was evaluated to justify its African ethnomedicinal use in the management of diabetes. METHODS: A methanolic extract and its chromatographic fractions (A1 -A6 ) were tested for glucose-reducing and in vitro insulin-stimulating abilities using glucose-loaded rats and INS-1 cells, respectively. In vivo insulin-releasing activities for the significantly (P<0.05) active antihyperglycemic A5 and A6 and in vitro insulinotropic activity of the C1 fraction and its isolated constituents were also similarly determined. RESULTS: The extract (100 mg/kg) had higher in vivo antihyperglycemic activity than the individual A1 -A6 , indicating a synergistic effect of the plant constituents. Higher in vivo insulin release in response to A5 (100 mg/kg) than A6 , agreed with their in vivo antihyperglycemic activities and confirmed insulin release as a mechanism of action of the plant. Compared with 5.6 mmol/L glucose (negative control), the extract and the A3 , A6 , and C1 (all at 100.0 µg/mL) elicited significantly higher in vitro insulin release that was similar to that of glibenclamide (1.0 µg/mL; P>0.05). Fraction C1 yielded a 1:1 mixture of α-amyrin and ß-amyrin cinnamates (1a:1b), lupenyl cinnamate (2), lupenyl acetate (3), and two unidentified triterpenoids, Y and Z. The 1a:1b mixture (100.0 µg/mL) demonstrated the highest insulinotropic activity that was comparable (P>0.05) to that of glibenclamide (1.0 µg/mL). CONCLUSIONS: The results confirm pancreatic activity as a mechanism underlying the antidiabetic action of G. latifolium and justify its ethnomedical use.

In-vitro evaluation of anti-trichomonal activities of Eugenia uniflora leaf.

Eugenia uniflora, used ethnomedically in some tropical countries as an anti-infective, has shown anti-malarial and anti-trypanocidal activities. Therefore using bioactivity guided fractionation, anti-trichomonal activity of E. uniflora leaf was investigated. Anti-trichomonal activities of leaf methanol extract and its fractions against Trichomonas gallinae as well as their cytotoxicities using an in vitro haemaglutination assay were determined. Anti-trichomonacidal activities of the extract improved on purification up to a stage. Subfractions E(2-5) had LC(50) and LC(90) values of 4.77 - 5.28, 18.49 - 25.00 and 4.53 - 5.18, 18.32 - 19.07 µg/ml at 24 and 48 hrs, respectively that were better than those of metronidazole. Further purification of E(2-5) led to loss of activity suggesting that the active components were probably working synergistically and additively. Demonstration of low haemaglutination titre values of 0.00 - 5.33 by methanolic extract and its partition fractions suggested their low toxicity profile. The established safety of the leaf indicated that its anti-trichomonal activity was not due to non-specific cytotoxicity, hence could be used in ethnomedicine as an anti-trichomonal agent.