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Main Compounds (main + compound)
Selected AbstractsPharmacokinetics of E-6087, a new anti-inflammatory agent, in rats and dogsBIOPHARMACEUTICS AND DRUG DISPOSITION, Issue 6 2001Raquel F. Reinoso Abstract The pharmacokinetics of E-6087, a newly developed cyclooxygenase-2 inhibitor, was studied in rats and dogs after single oral and intravenous doses. In both animal species, E-6087 was characterized by a long elimination half-life (20,35 h), a low plasma clearance (0.10,0.22 l h,1 kg,1) and a relatively large volume of distribution (2,6 l kg,1). Oral bioavailability was lower in dogs than in rats whereas a faster elimination was found in rats. Multiple peaks were present regardless of administration route and animal species, suggesting the existence of enterohepatic circulation. Gender effect on the pharmacokinetics of E-6087 was only found in rats, with greater exposure and longer elimination in females than in males. Food intake reduced the bioavailability (,22%) with no apparent changes in the absorption rate. After oral dosing of 1, 5 and 25 mg kg,1 to rats, linearity was lost at the highest dose due to the low aqueous solubility of E-6087. Drug absorption was improved by micronization. E-6087 and E-6132, (a pharmacologically active metabolite), showed different pharmacokinetics. The higher percentage of E-6087 at early times suggests that E-6087 is the main compound responsible for in vivo activity, although E-6132 would contribute to the activity at later times. Copyright © 2001 John Wiley & Sons, Ltd. [source] Fumigant toxicity of Korean medicinal plant essential oils and components from Asiasarum sieboldi root against Sitophilus oryzae L.FLAVOUR AND FRAGRANCE JOURNAL, Issue 2 2008Junheon Kim Abstract Medicinal plant essential oils and components from Asiasarum sieboldi were tested for their insecticidal activities against the rice weevil Sitophilus oryzae, using a fumigation bioassay. Responses varied with plant material and concentration. The LC50 value of A. sieboldi essential oil against rice weevil was 2.37 µg/ml air. Analysis by gas chromatography,mass spectrometry led to the identification of 20 compounds from A. sieboldi essential oil. Among identified compounds, five main compounds were tested for their insecticidal activity against rice weevil and compared to the toxicity of dichlorvos. Responses varied with compound and dose. Eucarvone was the most toxic, followed by safrole, with LC50 values of 3.32 and 11.27 µg/ml, respectively. LC50 values of other compounds were >25 µg/ml. The LC50 value of dichlorvos was 0.0081 µg/ml. Copyright © 2008 John Wiley & Sons, Ltd. [source] Chemical composition of the essential oils from Eriocephalus africanus L. var. africanus populations growing in SpainFLAVOUR AND FRAGRANCE JOURNAL, Issue 6 2007Hugo Merle Abstract Essential oils from the aerial parts of three Eriocephalus africanus L. var. africanus populations were analysed by means of GC,FID and GC,MS. Sixty-one constituents were identified, representing more than 96% of the total oil composition. Artemisia ketone (56.46,56.58%), intermedeol (9.19,11.63%) and , -eudesmol (4.26,5.64%) were the main compounds. Application of the Pearson correlation coefficient showed high similarity between the nine samples analysed. Copyright © 2007 John Wiley & Sons, Ltd. [source] Chemical composition and olfactory characterization of essential oils of fruits and seeds of African pear (Dacryodes edulis (G. Don) H. J. Lam) from CameroonFLAVOUR AND FRAGRANCE JOURNAL, Issue 2 2005Leopold Jirovetz Abstract The composition of the essential oil of Dacryodes edulis (G. Don) H. J. Lam (Burseraceae) fruits and seeds from Cameroon were investigated by gas chromatographic,spectroscopic (GC,FID and GC,MS) and olfactory methods to identify those volatiles responsible for the characteristic aroma of this commonly known African pear. Monoterpenes, such as , -pinene (fruits/seeds: 22.3/21.5%), , -pinene (13.7/19.7%), limonene (7.2/27.5%) and , -phellandrene (10.8/12.1%) were found to be main compounds of these essential oils. A correlation of the identi,ed constituents of the two essential oils of African pear from Cameroon with their single odour impressions is also given. Copyright © 2004 John Wiley & Sons, Ltd. [source] Chemical variability of Artemisia vulgaris L. essential oils originated from the Mediterranean area of France and CroatiaFLAVOUR AND FRAGRANCE JOURNAL, Issue 5 2003I. Jerkovic Abstract The essential oils of Artemisia vulgaris L. originating from France and Croatia were subjected to detailed GC,MS analysis in order to determine possible similarities and differences between them and their chemical compositions, depending on the stage of development. Plant materials were collected in Provence (France) and Dalmatia (Croatia) at four different stages of development: vegetative (June), buds (July), ,owering (August) and seeding (September). Comparison of the chemical composition and content, depending on phenological stages in both localities, shows qualitative similarity, but also the noticeable difference in the amounts of most components. First, the chemical composition of main compounds is very different; Croatian oils are rich in hydrocarbons, which are absent or present in low amounts in French oils. Also, with regard to the yield of essential oils, the yields from Croatian oils were higher (0.09,0.61%) than these from French oil (0.04,0.15%) at each development stage, respectively. Copyright © 2003 John Wiley & Sons, Ltd. [source] Trypanocidal and antifungal activities of p -hydroxyacetophenone derivatives from Calea uniflora (Heliantheae, Asteraceae)JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 5 2004Andréa Mendes do Nascimento The dichloromethane extract of underground parts of Calea uniflora (Heliantheae, Asteraceae) exhibited trypanocidal and antifungal activities. Four p -hydroxyacetophenone derivatives were isolated as the main compounds: 2-senecioyl-4-(hydroxyethyl)-phenol (1), 2-senecioyl-4-(angeloyloxy-ethyl)-phenol (2), and two new derivatives, 2-senecioyl-4-(methoxyethyl)-phenol (3) and 2-senecioyl-4-(pentadecanoyloxyethyl)-phenol (4). 1 and 4 were active towards Trypanosoma cruzi trypomastigotes, reducing their number by 70 and 71% at 500 ,g mL,1, whereas 2 and 3 were inactive. All the compounds tested showed antifungal activity with minimal inhibitory concentration values between 500 and 1000 ,g mL,1 against pathogenic Candida spp. and dermatophytes. The isolation, structure elucidation, NMR spectral assignments and bioactivity results of these compounds are reported. [source] Allyl-thiosulfinates, the Bacteriostatic Compounds of Garlic against Helicobacter pyloriBIOTECHNOLOGY PROGRESS, Issue 1 2004Pablo Cañizares Allicin and allyl-methyl plus methyl-allyl thiosulfinate from acetonic garlic extracts (AGE) have been isolated by high-performance liquid chromatography. These compounds have shown inhibition of the in vitro growth of Helicobacter pylori(Hp), the bacterium responsible for serious gastric diseases such as ulcers and even gastric cancer. A chromatographic method was optimized and used to isolate these thiosulfinates. The method developed has allowed the isolation of natural thiosulfinates extracted from garlic by organic solvents and is an easy and cheap methodology that avoids complex synthesis and purification procedures. The capacity and effectiveness of isolated natural thiosulfinates have been tested, and this has enabled the identification of the main compounds responsible for the bacteriostatic activity shown by AGE origin of these kinds of organosulfur compounds along with ethanolic garlic extracts (EGE). Additionally, microbiological analyses have suggested that these compounds show a synergic effect on the inhibition of the in vitro growth of Hp. The results described here facilitate the process of obtaining garlic extracts with optimal bacteriostatic properties. The product is obtained in a way that avoids expensive purification methods and will allow the design of live tests with the aim of investigating the potential for the use of these garlic derivatives in the treatment of patients with Hp infections. [source] | ||||||||||