1,721,018 research outputs found
Thiazolyl and isothiazolyl azomethine derivatives with antiinflammatory and antioxidant activities. Synthesis, biological evaluation and structure activity relationships study
No full textThiazolyl and isothiazolyl azomethine derivatives with anti-inflammatory and antioxidant activities
No full textSeveral thiazolyl/benzothiazolyl/benzo[d] isothiazolyl Schiff bases and hydrazones have been tested as anti-inflammatory agents and five new compounds have been synthesized. The anti-inflammatory activity was examined in vivo using the carrageenin induced mice paw edema test (inhibition 16.3-64 %). The compounds were tested for antioxidant activity as hydroxyl scavengers and for their ability to interact with the stable free radical 1,1-diphenyl-2-picryl- hydrazyl (DPPH). Both anti-inflammatory and antioxidant activities depended on some structural characteristics of the synthesized compounds
Design, synthesis and biological evaluation of new coumarin mannich bases as mono-aminoxidase B (MAO-B) inhibitors and anti-inflammatory agents
No full textLC-MS- A nd NMR-Guided Isolation of Monoterpene Dimers from Cultivated Thymus vulgaris Varico 3 Hybrid and Their Antityrosinase Activity
No full textTargeted isolation based on a combination of NMR and HPLC-PDA-MS of a dichloromethane extract of Thymus vulgaris Varico 3 aerial parts afforded one new p-cymene dimer, 6,3′,4′-trihydroxy-5,5′-diisopropyl-2,2′-dimethylbiphenyl (1), together with two known p-cymene derivatives (2 and 3), as well as five known compounds, namely, thymol (4), oleanolic acid (5), ursolic acid (6), cirsimaritin (7), and xanthomicrol (8). The structural elucidation of all compounds was performed by spectroscopic analyses, including 1D and 2D NMR, and HRESIMS experiments. The biphenyls were assayed for their inhibitory activity on tyrosinase. Compounds 2 and 3 showed negligible activity on tyrosinase, while compound 1 effectively inhibited the enzyme with 35% (± 0.3) inhibitory activity, higher than the inhibition of the reference compound kojic acid (18.6 ± 0.02)
Antioxidant and antiinflammatory activities of Sideritis perfoliata subsp. perfoliata (Lamiaceae)
No full textSideritis perfoliata L. subsp. perfoliata is a plant widely used in folk medicine in Greece since antiquity because of its antiinflammatory, antirheumatic, antiulcer, digestive and vasoprotective properties. Phytochemical investigations of the polar extracts afforded four flavonoid glycosides, four phenylpropanoic glycosides, caffeic acid and one iridoid, ajugoside. Reactive oxygen species (ROS) are implicated in the aetiology of several inflammatory processes. In the present study polar fractions and isolated compounds from S. perfoliata subsp. perfoliata were evaluated for their antioxidant activity using DPPH spectrophotometric and TBA lipid peroxidation assays, as well as for their antiinflammatory activity using the soybean lipoxygenase bioassay. All extracts and isolated compounds showed significant antioxidant and inhibitory activity against soybean lipoxygenase. These findings give support to the ethnopharmacological use of the plant in the treatment of several inflammatory ailments. Copyright © 2008 John Wiley & Sons, Ltd
Phenolic compounds with antioxidant activity from Anthemis tinctoria L. (Asteraceae)
No full textFrom the aerial parts of Anthemis tinctoria L. subsp. tinctoria var. pallida DC. (Asteraceae), one new cyclitol glucoside, conduritol F-1-O-(6′-O-E-p-caffeoyl)-β-D-glucopyranoside (1), has been isolated together with four flavonoids, nicotiflorin (2), isoquercitrin (3), rutin (4) and patulitrin (5). The structures of the isolated compounds were established by means of NMR, MS, and UV spectral analyses. Methanolic extract and pure isolated compounds were examined for their free radical, scavenging activity, using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free stable radical, and for their inhibitory activity toward soybean lipoxygenase, using linoleic acid as substrate. Compounds 1 and 5 showed a strong scavenging effect in the DPPH radical assay. In addition 5 also exhibited high inhibitory activity on soybean lipoxygenase. © 2007 Verlag der Zeitschrift für Naturforschung
Analysis of the essential oil of Origanum dubium growing wild in Cyprus. Investigation of its antioxidant capacity and antimicrobial activity
No full textThe volatile composition of Origanum dubium in two different maturation stages has been studied. The essential oils were obtained by hydrodistillation in a modified Clevenger-type apparatus, and their analyses were performed by GC and GC-MS. Identification of the components was made by comparison of mass spectra and retention indices with literature records and by cochromatography with authentic compounds. Carvacrol was shown to be the main constituent. The essential oils were evaluated for antimicrobial activity and proved to be active against all tested microorganisms. Furthermore, their potential antioxidant activity was investigated and found to be significant in scavenging O 2-. The samples were further evaluated for inhibition of soybean lipoxygenase LOX and showed high inhibitory activity. © Georg Thieme Verlag KG Stuttgart
Composition and antioxidant activity of the essential oils of Xylopia aethiopica (Dun) A. Rich. (Annonaceae) leaves, stem bark, root bark, and fresh and dried fruits, growing in Ghana
No full textThe chemical composition of the essential oils obtained from the leaves, the barks of the stem and the root, as well as from the fresh and dried fruits of Xylopia aethiopica, growing in Ghana, was investigated by gas chromatography/mass spectrometry analyses. Kováts indices, mass spectra, and standard compounds were used to identify a total of 93 individual compounds. The monoterpene hydrocarbons formed the main portion in all studied samples. β-Pinene was predominant in all cases, while trans-m-mentha-1(7),8-diene was the main compound in the essential oils of the leaves and the barks of roots and stems. Their potential antioxidant activity was also investigated and found to be significant in scavenging superoxide anion radical
Antioxidant, anti-inflammatory potential and chemical constituents of Origanum dubium Boiss., growing wild in Cyprus
No full textOriganum dubium Boiss. is a flavouring herb widely used in Cyprus. In this study, both lipophilic and polar extracts of the aerial parts of O. dubium were investigated for their chemical contents and their antioxidant potential. Overall, 20 constituents were isolated and identified, belonging mainly to three significant classes of compounds: terpenes, phenolic derivatives, such as hydroquinone glycosides and flavonoids and alicyclic derivatives. None of them was previously reported as constituent of O. dubium The inhibitory potencies of all total extracts and the isolated compounds on lipid peroxidation and their interaction with 1,1-diphenyl-picrylhydrazyl (DPPH) activity is discussed. The polar extract showed strong interaction with DPPH stable radical and significant inhibition of lipoxygenase and lipid peroxidation
Anthranilic Acid Based CCK1 Receptor Antagonists: Preliminary Investigation On Their Second “Touch point”
No full textIn this phase of structure–affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude greater than the lead and, as a general rule, it points out how the hypothesized receptorial pocket which accommodates the Phe residue allows much more structural modification than that interacting with the N-terminal group
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