Search results for "I.5"

showing 10 items of 399 documents

Metabolite profile and in vitro activities of Phagnalon saxatile (L.) Cass. relevant to treatment of Alzheimer’s disease

2009

The present study describes for the first time the in vitro properties (inhibition of NO production and anticholinesterase) of Phagnalon saxatile (L.) Cass. (Asteraceae). The methanolic extract showed antioxidant activity that was measured by DPPH assay and beta-carotene bleaching test. The same extract inhibited NO production in the murine monocytic macrophage cell line RAW 264.7. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition was assessed by modifications of Ellman's method. Purification of the MeOH extract of P. saxatile allowed the isolation of phenolic compounds. Among them, the compounds that most effectively inhibited lipopolysaccharide-induced NO production …

AntioxidantDPPHmedicine.medical_treatmentMetaboliteAsteraceaePharmacologyNitric OxideInhibition of NO productionCell LineMicechemistry.chemical_compoundPhagnalon saxatileAlzheimer DiseaseDrug DiscoverymedicineCaffeic acidAnimalsHumansSettore BIO/15 - Biologia FarmaceuticaIC50ButyrylcholinesterasePharmacologyPlant Extractsinhibition of NO production Alzheimer's diseaseSettore CHIM/06 - Chimica OrganicaGeneral MedicineAcetylcholinesterasePhenolic compoundsAlzheimers diseasechemistryBiochemistryPhagnalon saxatile asteraceae phenolic compoundButyrylcholinesteraseAcetylcholinesteraseCholinesterase InhibitorsLuteolinJournal of Enzyme Inhibition and Medicinal Chemistry
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Polyphenol Characterization, Antioxidant and Skin Whitening Properties of Alnus cordata Stem Bark

2019

In this study, we investigated the phenolic composition of the crude extract (MeOH 80 %) of Alnus cordata (Loisel.) Duby stem bark (ACE) and its antioxidant and skin whitening properties. RP-LC-DAD analysis showed a high content of hydroxycinnamic acids (47.64 %), flavanones (26.74 %) and diarylheptanoids (17.69 %). Furthermore, ACE exhibited a dose-dependent antioxidant and free-radical scavenging activity, expressed as half-maximal inhibitory concentration (IC50 ): Oxygen radical absorbance capacity (ORAC, IC50 1.78 μg mL-1 )>Trolox equivalent antioxidant capacity (TEAC, IC50 3.47 μg mL-1 )>2,2-Diphenyl-1-picrylhydrazyl (DPPH, IC50 5.83 μg mL-1 )>β-carotene bleaching (IC50 11.58 μg mL-1 )…

AntioxidantOxygen radical absorbance capacityDPPHmedicine.medical_treatmentTrolox equivalent antioxidant capacityBioengineeringAlnus cordata; antimelanogenic activity; Betulaceae; mushroom tyrosinase; polyphenols; RP-LC-DAD analysis; zebrafish; Alnus; Animals; Antioxidants; Biphenyl Compounds; Enzyme Inhibitors; Monophenol Monooxygenase; Picrates; Plant Bark; Plant Extracts; Polyphenols; Skin; ZebrafishAlnus01 natural sciencesBiochemistryAntioxidantschemistry.chemical_compoundPicratesmedicineAnimalsFood scienceEnzyme InhibitorsMolecular BiologyIC50ZebrafishSkinbiologyMonophenol MonooxygenasePlant Extracts010405 organic chemistryBiphenyl CompoundsPolyphenolsSkin whiteningGeneral ChemistryGeneral Medicinebiology.organism_classificationAlnus cordata0104 chemical sciences010404 medicinal & biomolecular chemistrychemistryPolyphenolPlant BarkMolecular Medicine
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Xenopus Oocyte’s Conductance for Bioactive Compounds Screening and Characterization

2019

Background: Astaxanthin (ATX) is a lipophilic compound found in many marine organisms. Studies have shown that ATX has many strong biological properties, including antioxidant, antiviral, anticancer, cardiovascular, anti-inflammatory, neuro-protective and anti-diabetic activities. However, no research has elucidated the effect of ATX on ionic channels. ATX can be extracted from shrimp by-products. Our work aims to characterize ATX cell targets to lend value to marine by-products. Methods: We used the Xenopus oocytes cell model to characterize the pharmacological target of ATX among endogenous Xenopus oocytes&rsquo

AntioxidantSodiummedicine.medical_treatmentXenopuschemistry.chemical_elementEndogeny+Sodium ChannelsCatalysisArticleAmilorideInorganic Chemistrylcsh:ChemistryXenopus laevischemistry.chemical_compoundXenopus oocyte INaAstaxanthinDrug DiscoverymedicineAnimalsPhysical and Theoretical ChemistryMolecular BiologyIC50lcsh:QH301-705.5SpectroscopyXenopus oocyte INa+Biological Productsbioactive compoundsbiologySodium channelOrganic Chemistry<i>Xenopus</i> oocyte INa<sup>+</sup>marine natural productsGeneral Medicinebiology.organism_classificationElectrophysiological PhenomenaComputer Science ApplicationsShrimpastaxanthinchemistryBiochemistrylcsh:Biology (General)lcsh:QD1-999OocytesInternational Journal of Molecular Sciences
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A tetraazahydroxypyridinone derivative as inhibitor of apple juice enzymatic browning and oxidation

2022

Abstract Enzymatic browning in fruits and vegetables can produce undesirable colour changes and adversely affect the taste, flavour, and nutritional value. This fact poses a challenge to the food industry to apply appropriate inhibitors to control enzymatic browning to maintain food quality. Accordingly, this study aims to evaluate the effect of small mazamacrocyclic compounds modified with a hydroxypyridinone similar to kojic acid on enzymatic browning, total polyphenols and antioxidant activity in apple juice. The results showed how these compounds interact with the tyrosinase enzyme in a complex interaction inhibiting its activity. The hydroxypyridinone attached to the macrocycle (I1) wa…

AntioxidantTyrosinasemedicine.medical_treatmentFlavourchemistry.chemical_compoundchemistryPolyphenolBrowningmedicineFood scienceFood qualityKojic acidIC50Food ScienceLWT
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Constituents of Peperomia vulcanica Baker &amp; 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 …

Antiparasiticmedicine.drug_classLeishmania donovaniPeperomia vulcaniaPlant Science01 natural sciencesBiochemistryAntiplasmodialmedicineAntileishmanialCytotoxicityIC50biologyTraditional medicine010405 organic chemistryChemistryPeperomia vulcanicaPlasmodium falciparumPeperotanninPiperaceaePiperaceaebiology.organism_classificationPeperolignanIn vitro0104 chemical sciences010404 medicinal & biomolecular chemistryAgronomy and Crop ScienceBiotechnologyPhytochemistry Letters
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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.

Aquatic Organismssarcoconvolutum A–EMagnetic Resonance Spectroscopy<i>Sarcophyton convolutum</i>StereochemistryQH301-705.5MetaboliteEthyl acetatePharmaceutical ScienceAntineoplastic AgentsArticleHeLaInhibitory Concentration 50Structure-Activity Relationshipchemistry.chemical_compoundCell Line TumorDrug DiscoveryIc50 valuesAnimalsCytotoxic T cellBiology (General)CytotoxicityIndian OceanPharmacology Toxicology and Pharmaceutics (miscellaneous)cembrenoidschemistry.chemical_classificationbiologyChemistrySarcophyton<i>Sarcophyton convolutum</i>; sarcoconvolutum A–E; cembrenoids; cytotoxicitySarcophyton convolutumAnthozoabiology.organism_classificationEnzymecytotoxicityDiterpenesDrug Screening Assays AntitumorMarine Drugs
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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…

AzolesModels MolecularMagnetic Resonance SpectroscopyStereochemistryDrug Evaluation PreclinicalResveratrolCell Linechemistry.chemical_compoundInhibitory Concentration 50Drug DiscoveryScreening methodIc50 valuesPotencyAnimalsLuciferaseEnzyme InhibitorsLuciferasesIC50ta116chemistry.chemical_classificationFirefliesEnzymechemistryNuclear receptorBiochemistryMolecular MedicineJournal of medicinal chemistry
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Feeding Ecology of Harbour Seals (Phoca vitulina) in Southern Norway

2017

Master's thesis Aquatic Ecology BIO500 - University of Agder 2017 In order to understand ecosystem dynamics and functions it is vital to have knowledge about relationships between predator and prey. Harbour seals (Phoca vitulina) are piscivorous marine mammals found at or near the top of marine food webs. Being mainly piscivores, harbour seals have the potential to come into conflict with fishermen and fisheries. Recently, as the Skagerrak and Kattegat population of harbour seals has increased, claims that seals are depleting the cod population have surfaced. Using scat sampling and otolith identification, harbour seal diet was estimated in four separate locations along the coast of souther…

BIO500VDP::Matematikk og Naturvitenskap: 400::Zoologiske og botaniske fag: 480::Marinbiologi: 497
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Natural selection against offshore Atlantic cod (Gadus morhua) in Skagerrak fjords?

2016

Master's thesis Aquatic Ecology BIO500 - University of Agder 2016 The marine environment was previously presumed to be demographically “open”, and marineorganisms were thought to have pronounced gene flow over vast areas due to their potentialof dispersal during early life stages. However, recent studies have suggested a degree of selfrecruitmentwithin segments of coastal and offshore areas for several marine species. Two ofthe forces acting on this structuring are retention of early life stages and homing of adultindividuals. This study looks at the distribution of early life stages of the Atlantic cod (Gadusmorhua) in two Norwegian fjords divided into inshore-offshore transects, and study…

BIO500VDP::Mathematics and natural science: 400::Zoology and botany: 480::Marine biology: 497
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Analysering av miljø-DNA for kartlegging av marin fiskefauna

2016

Masteroppgave akvatisk økologi BIO500 - Universitetet i Agder 2016 Marine ecosystems worldwide are currently threatened due to overfishing and other humanimpacts. To monitor marine fish, which represents a main component in present monitoring ofmarine ecosystem health, one is mainly depending on invasive and selective methods. Thesemethods are also dependent on physical identification of species, which in many cases can bedifficult, or in some cases, impossible. Such limitations of traditional surveillance methodshave created a demand for alternative methods. One such alternative is the environment-DNAmethod, i.e. analysis of genetic material from a sample collected in the environment.In th…

BIO500VDP::Mathematics and natural science: 400::Zoology and botany: 480::Marine biology: 497
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