Search results for "C50"
showing 10 items of 182 documents
The Inclusion of a Supercritical Fluid Extract, Obtained From Honey Bee Pollen, in the Diet of Gilthead Sea Bream (Sparus aurata), Improves Fish Immu…
2020
In the present study, the immune-stimulatory effect of two levels of honey bee pollen (5 and 10%, P5 and P10 treatment, respectively) and its supercritical fluid extract (0. 5 and 1%, E0.5 and E1, respectively) included in the diet, was tested in gilthead seabream (Sparus aurata). The in vivo trial was preceded by the evaluation of antioxidant properties of three different bee pollen extracts obtained by water, ethanol 80%, and Supercritic Fluids Extraction (SFE). The preliminary evaluation attested that the SFE showed the lowest extraction yield (10.47%) compared to ethanol 80% (48.61%) and water (45.99%). SFE extract showed good antioxidant properties with high polyphenol content (13.06 m…
Constituents of Peperomia vulcanica Baker & C. H. Wright (Piperaceae) with antiparasitic activity
2021
Abstract The investigation of the CH2Cl2-MeOH (1:1) extract of Peperomia vulcanica which showed antileishmanial activity during preliminary screening led to the isolation of two previously unknown compounds named peperolignan (1) and peperotannin (2) along with 13 known compounds. Their structures were determined on the basis of their spectroscopic data. The isolated compounds were assessed in vitro for their antileishmanial and antiplasmodial activities against Leishmania donovani 1S (MHOM/SD/62/1S) promastigotes and the Plasmodium falciparum chloroquine-sensitive 3D7 strain (Pf3D7), respectively. They were also assessed for their cytotoxicity on Raw 264.7 macrophage cells. The mixture of …
Flavonoids from Erythrina schliebenii
2017
Prenylated and O-methylflavonoids including one new pterocarpan (1), three new isoflavones (2–4), and nineteen known natural products (5–23) were isolated and identified from the root, stem bark, and leaf extracts of Erythrina schliebenii. The crude extracts and their constituents were evaluated for antitubercular activity against Mycobacterium tuberculosis (H37Rv strain), showing MICs of 32–64 μg mL–1 and 36.9–101.8 μM, respectively. Evaluation of their toxicity against the aggressive human breast cancer cell line MDA-MB-231 indicated EC50 values of 13.0–290.6 μM (pure compounds) and 38.3 to >100 μg mL–1 (crude extracts).
Oxygenated Cembrene Diterpenes from Sarcophyton convolutum: Cytotoxic Sarcoconvolutum A–E
2021
The soft coral genus Sarcophyton contains the enzymatic machinery to synthesize a multitude of cembrene-type diterpenes. Herein, highly oxygenated cembrenoids, sarcoconvolutum A–E (1–5) were purified and characterized from an ethyl acetate extract of the red sea soft coral, Sarcophyton convolutum. Compounds were assemblies according to spectroscopic methods including FTIR, 1D- and 2D-NMR as well as HRMS. Metabolite cytotoxicity was tested against lung adenocarcinoma, cervical cancer, and oral-cavity carcinoma (A549, HeLa and HSC-2, respectively). The most cytotoxic compound, (4) was observed to be active against cell lines A549 and HSC-2 with IC50 values of 49.70 and 53.17 μM, respectively.
Discovery of 5-benzyl-3-phenyl-4,5-dihydroisoxazoles and 5-benzyl-3-phenyl-1,4,2-dioxazoles as potent firefly luciferase inhibitors.
2013
Luciferase reporter assays are commonly used in high-throughput screening methods. Here, we report new firefly luciferase (FLuc) inhibitors based on 5-benzyl-3-phenyl-4,5-dihydroisoxazoles and 5-benzyl-3-phenyl-1,4,2-dioxazoles, which showed up as "false positives" in a luciferase reporter gene-based assay for nuclear receptor antagonists. The inhibition was shown to be noncompetitive for both natural enzyme substrates (d-luciferin and ATP) and selective to FLuc and proven to arise from a direct interaction between the enzyme and the inhibitor. Of the 63 evaluated compounds, 28 showed significantly better inhibition potency than the well-known inhibitor resveratrol (IC(50) = 59 nM), with fi…
The Belle II Physics Book
2019
cd. autorów: L. Cao48,‡, G. Caria145,‡, G. Casarosa57,‡, C. Cecchi56,‡,D. Cˇ ervenkov10,‡,M.-C. Chang22,‡, P. Chang92,‡, R. Cheaib146,‡, V. Chekelian83,‡, Y. Chen154,‡, B. G. Cheon28,‡, K. Chilikin77,‡, K. Cho70,‡, J. Choi14,‡, S.-K. Choi27,‡, S. Choudhury35,‡, D. Cinabro170,‡, L. M. Cremaldi146,‡, D. Cuesta47,‡, S. Cunliffe16,‡, N. Dash33,‡, E. de la Cruz Burelo9,‡, E. de Lucia52,‡, G. De Nardo54,‡, †Editor. ‡Belle II Collaborator. §Theory or external contributing author. M. De Nuccio16,‡, G. De Pietro59,‡, A. De Yta Hernandez9,‡, B. Deschamps129,‡, M. Destefanis60,‡, S. Dey116,‡, F.Di Capua54,‡, S.Di Carlo75,‡, J. Dingfelder129,‡, Z. Doležal10,‡, I. Domínguez Jiménez125,‡, T.V. Dong30,26,…
Combined heterologies for monoclonal antibody-based immunoanalysis of fluxapyroxad
2018
Nowadays, instrumental methodologies and rapid bioanalytical techniques complement each other for the analysis of toxic chemical compounds. Fluxapyroxad was commercialized a few years ago as a fungicide and today it is being used worldwide to control a variety of pests. In the present study, the development of monoclonal antibody-based immunochemical methods for the analysis of this chemical in food samples was evaluated for the first time. Novel haptens were synthesized and protein bioconjugates were prepared. High-affinity and specific monoclonal antibodies to fluxapyroxad were generated from two haptens with alternative linker tethering sites. Haptens with linker site heterology and a st…
The role of size and protein shells in the toxicity to algal photosynthesis induced by ionic silver delivered from silver nanoparticles
2019
Abstract Because of their biocide properties, silver nanoparticles (AgNPs) are present in numerous consumer products. The biocidal properties of AgNPs are due to both the interactions between AgNP and cell membranes and the release of dissolved silver (Ag+). Recent studies emphasized the role of different nanoparticle coatings in complexing and storing Ag+. In this study, the availability of dissolved silver in the presence of algae was assessed for three AgNPs with different silver contents (59%, 34% and 7% of total Ag), silver core sizes and casein shell thicknesses. The impact of ionic silver on the photosynthetic yield of Chlamydomonas reinhardtii was used as a proxy to estimate the amo…
In-vitro test system for the evaluation of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) inhibitors based on a single HPLC run with UV detect…
2001
Objective and Design: The aim of this study was to develop a new, whole-cell test system which is easy to handle and requires a standard equipment for the parallel screening of COX-1 and COX-2 inhibitors.¶Materials: Bovine aortic endothelial cells (BAECs).¶Treatment and methods: Unstimulated bovine aortic coronary endothelial cells (BAECs) were used as a source of COX-1 and BAECs pretreated with ASA (100 μM) and activated with phorbol myristate acetate (PMA) were used as a source of COX-2. The time- and concentration-dependent induction of COX-2 expression in the BAECs was evaluated by a kinetic profile (HPLC analysis) and detected by Western-Blot analysis using polyclonal antibodies agains…
Erysacleuxins C and D, new isoflavones from the twigs of Erythrina sacleuxii Hua and their cytotoxic activity
2020
Two previously undescribed isoflavones, erysacleuxin C (1) and erysacleuxin D (2), together with seven known compounds (3–9), were isolated and identified from the EtOAc extract of the twigs of Erythrina sacleuxii Hua (Leguminosae). The structures of the isolated compounds were determined on the basis of their spectroscopic and spectrometric data. Evaluation of their cytotoxicity against the human cancer HeLa-S3 cell lines indicated IC50 values of 130.4, 54.9 and 73.9 µM for erysacleuxin C (1), erysacleuxin D (2) and butin (9), respectively. Keywords: Erythrina sacleuxii, Leguminosae, Isoflavone, Erysacleuxin C, Erysacleuxin D, Cytotoxicity