No abstract

We describe here three urea-based soluble epoxide hydrolase (sEH) inhibitors from the root of the plant Pentadiplandra brazzeana. The concentration of these ureas in the root was quantified by LC-MS/MS, showing that 1, 3-bis (4-methoxybenzyl) urea (MMU) is the most abundant (42.3 μg/g dry root weight). All of the ureas were chemically synthesized, and their inhibitory activity toward recombinant human and recombinant rat sEH was measured. The most potent compound, MMU, showed an IC50 of 92 nM via fluorescent assay and a Ki of 54 nM via radioactivity-based assay on human sEH. MMU effectively reduced inflammatory pain in a rat nociceptive pain assay. These compounds are among the most potent sEH inhibitors derived from natural sources. Moreover, inhibition of sEH by these compounds may mechanistically explain some of the therapeutic effects of P. brazzeana.

This study aims to evaluate the anti-inflammatory, cytotoxicity, and genotoxicity activities of Dissotis multiflora (Sm) Triana and Paullinia pinnata Linn used traditionally in Cameroon to treat infectious diseases. Phytochemical screening was carried out using the LC-MS procedure. The ferrous oxidation-xylenol orange (FOX) assay was used to determine the 15-lipoxygenase (15-LOX) inhibitory activity of the plant samples. The tetrazolium-based colorimetric (MTT) assay was performed using Vero cells. The Ames test was carried out using Salmonella typhimurium TA98 and TA100 tester strains. LC-MS chromatogram of D. multiflora led to the identification of four known compounds, namely, 5-(3,5-dinitrophenyl)-2H-tetrazol (2), 2,2'-{[2-(6-amino-9H-purine-9-yl)ethyl]imino}diethanol (14), 1,2,5-oxadiazolo [3,4-b]pyrazine, 5,6-di (3,5-dimethyl-1-piperidyl) (19), and nimbolinin D (20) while four compounds were also identified in P. pinnata known as 2-hydroxycarbamoyl-4-methyl-pentanoic acid (2), pheophorbide A (16), 1-[4-({2-[(1-methyl-1H-indol-5-yl)amino]-4-pyrimidinyl}oxy)-1-naphthyl]-3-[1-(4 methylphenyl)-3-(2-methyl-2-propanyl)-1H-pyrazol-5-yl]urea (17), and nimbolinin D (18). D. multiflora and P. pinnata inhibited 15-LOX activity in concentration-dependent manner. The LC50 (concentration that kills 50% of cells) values of the extracts ranged from 0.13 ± 00 to 1 ± 00 mg/mL for P. pinnata and D. multiflora, respectively. P. pinnata was cytotoxic at concentrations tested while D. multiflora was not. The selectivity index (SI) values ranged from 0.16 to 10.30 on Vero cell lines. No genotoxic effect was observed against both strains tested. These extracts are sources of compounds which can be used to control infectious diseases and associated inflammation. However, caution should be taken while using P. pinnata for medicinal purposes.

The chemical composition of the essential oils obtained by hydrodistillation of fresh leaves from Hyptis lanceolata, H. pectinata, H. spicigera and H. suaveolens growing in Cameroon were analysed by GC and GC–MS. The oil of H. suaveolens was rich in sabinene (20.6%), β‐caryophyllene (17.5%) and bergamotol (10.9%), while the oil of H. pectinata contained germacrene D (28.0%) and β‐caryophyllene (22.1%) as the major constituents. H. spicigera oil contained α‐pinene (28.3%), β‐caryophyllene (19.1%), limonene (13.4%) and ß‐pinene (10.3%) as the main components. The most abundant constituents identified in the oil of H. lanceolata were β‐pinene (40.7%) and germacrene D (19.9%). These chemical profiles were compared with literature results; relative similarities were found in chemical compositions of each species, but some quantitative and qualitative variations were noted. Copyright © 2005 John Wiley & Sons, Ltd.

The aim of this work was to characterize the essential oil (EO) of Eryngium foetidum (EfEO) and assess its activity toward Listeria monocytogenes in broth and during thermal inactivation of the pathogen in pineapple juice. In this respect, EfEO was chemically characterized, and its antilisteria potential in broth as a function of pH, cell load, and EfEO concentration was assessed through a central composite design. Furthermore, the inactivation kinetics of L. monocytogenes in the juice were assessed by combining EfEO and low pasteurization temperatures. A total of 81 compounds were identified from EfEO. The reduction of pH and cell load increased EO activity. The use of only 15 ppm of EfEO during pasteurization of pineapple juice at 60°C reduced the time required for a 4-log reduction in L. monocytogenes CFU/ml by 74.9% (i.e., from 8.5 to 2.1 min) compared with treatment without EfEO. It could be concluded that EfEO activity toward L. monocytogenes increases with the reduction of pH and that it can be used at sublethal concentrations in combination with low temperatures in pineapple juice pasteurization. This study demonstrates that EO-assisted pasteurization is a promising strategy for the reduction of thermal impact during juice production. EfEO is easily available and compatible with many juices and is thus promising for industrial application.