Search results for "Mace"

showing 10 items of 4713 documents

Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents

2004

Several 2,3-diaryl-1,3-thiazolidin-4-ones were synthesized and evaluated as anti-HIV agents. The results of the in vitro tests showed that some of them were highly effective inhibitors of HIV-1 replication at 30-50 nM concentrations with minimal cytotoxicity, thereby acting as non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs).

Anti-HIV activity23-diaryl-13-thiazolidin-4-oneAnti-HIV AgentsCell SurvivalT-LymphocytesDrug Evaluation PreclinicalPharmaceutical SciencePharmacologyVirus ReplicationStructure-Activity RelationshipDrug DiscoveryStructure–activity relationshipHumansCytotoxicityCell survivalAnti hiv activityMolecular StructureAnti hivChemistryvirus diseasesSettore CHIM/08 - Chimica FarmaceuticaReverse transcriptaseIn vitroThiazolesViral replicationHIV-2HIV-1NNRTIsReverse Transcriptase Inhibitors
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Eight-Membered Rings With Two Heteroatoms 1,3

2022

Eight-membered rings with two heteroatoms in a 1,3-relationship, namely 1,3-diazocine, 2H-1,3-oxazocine, 2H-1,3-thiazocine, 4H-1,3-dioxocin, 4H-1,3-oxathiocin, and 4H-1,3-dithiocin, are discussed in this chapter, that covers the literature from 2007 to October 2020 (SciFindern search) and reports the chemistry of uncondensed derivatives, heterocines fused to carbocycles and heterocycles, as well as bridged heterocines. Among eight-membered 1,3-diheterocines, 1,3-diazocines and 1,3-oxazocines are the two largest classes, based on the number of publications, mostly due to the studies of the synthesis of these cyclic systems, their pharmacological properties and/or their important industrial a…

Anti-HIV agentsCold-menthol receptor TRPM8 modulators13-DiazocineCholesterylester transfer protein (CETP) inhibitors4H-13-DithiocinSettore CHIM/08 - Chimica FarmaceuticaHistone deacetylase 6 inhibitorsEquilibrative nucleoside transporter 1 (ENT1) inhibitors4H-13-OxathiocinAnticancer agents4H-13-Dioxocin2H-13-OxazocineBiosynthetic pathways of 1 3-heterocines2H-13-Thiazocine
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Chemical composition of the essential oil from Thapsia garganica L. (Apiaceae) grown wild in Sicily and its antimicrobial activity.

2015

In this study, the chemical composition of the essential oil from flowers and leaves of Thapsia garganica L. collected in Sicily was evaluated by GC and GC-MS. The main components of T. garganica flower oil (T.f.) were chamazulene (58.3%), humulene oxide II (9.0%), tricosane (8.2%) and pentacosane (8.2%). Also the oil from leaves (T.l.) was characterised by high content of chamazulene (49.2%). Other abundant metabolites were 1,4-dimethylazulene (18.5%), (E)-phytol (6.3%) and neophytadiene (5.1%). The comparison with other studied oils of genus Thapsia is discussed. Antimicrobial activity against several micro-organisms, including some ones infesting historical art craft, was also determined.

Anti-Infective AgentAntifungal Agentshumulene oxide IIPlant Science01 natural sciencesThapsia garganicaBiochemistrylaw.inventionAnalytical Chemistrychemistry.chemical_compoundAnti-Infective AgentslawAntifungal AgentSettore BIO/15 - Biologia FarmaceuticaChemical compositionSicilyThapsia1-dimethylazulenebiologyHumuleneChemistryMicrobial Sensitivity TestchamazuleneAntimicrobialThapsia (plant)Anti-Bacterial Agentsvolatile componentFlowerPlant LeaveThapsia garganicaFlowersMicrobial Sensitivity TestsGas Chromatography-Mass SpectrometryBotanyAnti-Bacterial AgentOils VolatileEssential oilApiaceaeantimicrobial activityBacteria010405 organic chemistryChamazuleneOrganic ChemistryFungiSettore CHIM/06 - Chimica Organicabiology.organism_classification0104 chemical sciencesPlant Leaves010404 medicinal & biomolecular chemistryApiaceaeNatural product research
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Biomedical Applications of Polylactide (PLA) and Its Copolymers.

2018

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Anti-Infective AgentPolyestersMicrofluidicsPolyesterPharmaceutical ScienceBiocompatible Materials02 engineering and technology01 natural sciencesAnalytical ChemistryPolymerizationlcsh:QD241-441Nanoparticlelcsh:Organic chemistryAnti-Infective AgentsDrug DiscoveryCopolymerHumansPhysical and Theoretical ChemistryDrug CarrierBiocompatible MaterialDrug CarriersPolymer scienceTissue Scaffolds010405 organic chemistryChemistryOrganic Chemistry021001 nanoscience & nanotechnologyBone Diseases Infectious0104 chemical sciencesBone Diseases Infectioun/aEditorialMicrofluidicChemistry (miscellaneous)PeptideMolecular MedicineNanoparticles0210 nano-technologyPeptidesHumanMolecules (Basel, Switzerland)
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The Nonvolatile and Volatile Metabolites of Prangos ferulacea and Their Biological Properties

2019

Abstract Prangos ferulacea (L.) Lindl. (Fam. Apiaceae), an orophilous species of eastern Mediterranean and western Asia, possesses a number of biological properties that are worthy of exploitation in different fields. Phytochemical investigations revealed the presence of coumarins, prenyl-coumarins, and furano-coumarins as the main constituents of this species, as well as several flavonoids. Among prenyl-coumarins, osthol is a promising apoptotic agent quite selective toward cancer cells. In addition, the essential oils have been extensively investigated, and several chemotypes have been identified. This work reviews the literature on this species published between 1965 and 2018, describes …

Anti-Infective AgentPrangos ferulaceaPharmaceutical Science01 natural sciencesAntioxidantsAnalytical Chemistrylaw.inventionchemistry.chemical_compoundAnti-Infective AgentslawDrug Discoveryheterocyclic compoundsAnalgesicsbiologyTraditional medicinePhytochemicalprenyl-coumarinsMolecular MedicineAntioxidantfurano-coumarinOstholHumanCoumarinessential oilBiological propertyAnimalsHumansHypoglycemic AgentsVolatile metabolitesEssential oilPharmacologyPrangos ferulaceacoumarinsApiaceaeHypoglycemic AgentChemotypeAnimalPlant Extracts010405 organic chemistryOrganic ChemistryPrangos ferulacea; Apiaceae; coumarins; prenyl-coumarins; furano-coumarinsSettore CHIM/06 - Chimica Organicabiology.organism_classification0104 chemical sciencesprenyl-coumarin010404 medicinal & biomolecular chemistryComplementary and alternative medicinechemistrySettore BIO/03 - Botanica Ambientale E ApplicataAnalgesicApiaceaefurano-coumarinsPlanta Medica
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Anti-arthritic activity of a lipophilic woad (Isatis tinctoria) extract

2006

A dichloromethane extract of Isatis tinctoria was tested in the adjuvant-induced arthritis model in rats. The extract (150 mg/kg p. o.) leads to a significant reduction of paw oedema. Radiographic, histological and clinical assessment confirmed reduced damage of cartilage and signs of inflammatory response in comparison to untreated control. No significant differences were observed in the tissular levels of cyclooxygenases 1 and -2, and of inducible nitric oxide synthase in Isatis treated and untreated animals. High dose treatment with Isatis extract for two weeks did not result in macroscopic lesions of the gastric mucosa.

Anti-Inflammatory AgentsAdministration OralPharmaceutical ScienceArthritisPharmacognosyAnalytical Chemistrylaw.inventionArthritis RheumatoidMicelawDrug DiscoveryGastric mucosamedicineAnimalsEdemaIsatisPharmacologyDose-Response Relationship DrugbiologyTraditional medicinePlant Extractsbusiness.industryMacrophagesOrganic ChemistryIsatisbiology.organism_classificationmedicine.diseaseRatsIsatis tinctoriaRadiographyNitric oxide synthaseDose–response relationshipmedicine.anatomical_structureComplementary and alternative medicineRats Inbred Lewbiology.proteinMolecular MedicineFemalePhytotherapybusinessPhytotherapyPlanta Medica
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Chemical Constituents and Pharmacological Properties ofPoria cocos

2011

Poria cocos (Polyporaceae) is a saprophytic fungus that grows in diverse species of Pinus. Its sclerotium, called fu-ling or hoelen, is used in traditional Chinese and Japanese medicine for its diuretic, sedative, and tonic effects. Various studies of this fungus have demonstrated its marked anti-inflammatory activity in different experimental models of acute and chronic inflammation. It is widely used as a constituent of many preparations in Asian medicine, but the number of research papers on its clinical properties is insufficient for establishing its efficacy and safety from a scientific point of view. In this review, we have compiled all the published data concerning the chemistry, pha…

Anti-Inflammatory AgentsPharmaceutical ScienceAntineoplastic AgentsInflammationBiologyPharmacognosyAnalytical ChemistryImmune systemJapanPolysaccharidesPsoriasisDrug DiscoverymedicineHumansImmunologic FactorsSecretionMedicine Chinese TraditionalPolyporaceaePharmacologyBiological ProductsTraditional medicineOrganic ChemistryPoriamedicine.diseasebiology.organism_classificationTriterpenesPolyporusComplementary and alternative medicinePhytochemicalMolecular Medicinemedicine.symptomPlanta Medica
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Anti-inflammatory and tight junction protective activity of the herbal preparation STW 5-II on mouse intestinal organoids

2021

Abstract Background Irritable bowel syndrome (IBS) is a functional bowel disorder, in which recurrent abdominal pain is associated with defecation or a change in bowel habits. STW 5-II is a combination of six medicinal herbs with a clinically proven efficacy in managing IBS. Aim This study aims to establish an in vitro IBS model using mouse intestinal organoids and to explore the anti-inflammatory and tight junction protective activities of the multi-herbal preparation STW 5-II. Methods Intestinal organoids were cultured in 1:1 Matrigel™ and medium domes. Inflammation and tight junction disruption were induced by a cocktail of cytokines (TNFα, IFNγ, IL-1β, IL-6) and bacterial proteins (LPS,…

Anti-Inflammatory AgentsPharmaceutical ScienceInflammationPharmacologyTight JunctionsProinflammatory cytokineIrritable Bowel SyndromeMice03 medical and health sciencesOrgan Culture Techniques0302 clinical medicineWestern blotDownregulation and upregulationDrug DiscoverymedicineOrganoidAnimalsComputer SimulationIntestinal MucosaIrritable bowel syndrome030304 developmental biologyPharmacology0303 health sciencesTight junctionmedicine.diagnostic_testPlant Extractsbusiness.industryNF-kappa Bmedicine.diseaseIntestinesOrganoidsDisease Models AnimalSTAT1 Transcription FactorGene Expression RegulationComplementary and alternative medicine030220 oncology & carcinogenesisZonula Occludens-1 ProteinMolecular MedicineTumor necrosis factor alphaInflammation Mediatorsmedicine.symptombusinessPhytomedicine
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Pharmacological Properties of Shikonin – A Review of Literature since 2002

2013

The naphthoquinone shikonin is the main active principle of Zicao, a traditional Chinese herbal medicine made from the dried root of Lithospermum erythrorhizon. Studies carried out over the past 30 years have provided a scientific basis for the use of Zicao which has been long employed in folk medicine to treat a variety of inflammatory and infectious diseases. In particular, shikonin has been shown to possess many diverse properties, including antioxidant, anti-inflammatory, antithrombotic, antimicrobial, and wound healing effects. The fact that shikonin shows so many beneficial properties has increased the interest in this molecule dramatically, especially in the past few years. The aim o…

Anti-Inflammatory AgentsPharmaceutical SciencePlant RootsAntioxidantsAnalytical ChemistryAnti-Infective AgentsFibrinolytic AgentsChinese traditionalDrug DiscoveryBotanyHumansMedicineMedicine Chinese TraditionalPharmacologyFolk medicineWound HealingPlants MedicinalbiologyTraditional medicinebusiness.industryLithospermumActive principleOrganic ChemistryLithospermum erythrorhizonbiology.organism_classificationComplementary and alternative medicineMolecular MedicinebusinessNaphthoquinonesPlanta Medica
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Polycerasoidol, a Natural Prenylated Benzopyran with a Dual PPARα/PPARγ Agonist Activity and Anti-inflammatory Effect

2019

Dual peroxisome proliferator-activated receptor-α/γ (PPARα/γ) agonists regulate both lipid and glucose homeostasis under different metabolic conditions and can exert anti-inflammatory activity. We investigated the potential dual PPARα/γ agonism of prenylated benzopyrans polycerasoidol (1) and polycerasoidin (2) and their derivatives for novel drug development. Nine semisynthetic derivatives were prepared from the natural polycerasoidol (1) and polycerasoidin (2), which were evaluated for PPARα, -γ, -δ and retinoid X receptor-α activity in transactivation assays. Polycerasoidol (1) exhibited potent dual PPARα/γ agonism and low cytotoxicity. Structure–activity relationship studies revealed th…

Anti-Inflammatory AgentsRXRα/PPARγPharmaceutical ScienceRetinoid X receptorPharmacology01 natural sciencesAnalytical ChemistryStructure-Activity Relationshipchemistry.chemical_compoundTransactivationPrenylationPOLYCERASOIDOLDrug DiscoveryHumansStructure–activity relationshipGlucose homeostasisBenzopyransPPAR alphaMOLECULAR MODELINGCytotoxicityPrenylationPharmacologyMolecular Structure010405 organic chemistryChemistry[CHIM.ORGA]Chemical Sciences/Organic chemistryOrganic ChemistryCiencias QuímicasNATARUL PRODUCTSPeroxisome0104 chemical sciencesBenzopyranPPAR gamma010404 medicinal & biomolecular chemistryQuímica OrgánicaComplementary and alternative medicineMolecular MedicineCIENCIAS NATURALES Y EXACTAS
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