0000000000519330

AUTHOR

Nunzio Cardullo

0000-0003-1480-0861

showing 3 related works from this author

Spaghetti Enriched with Inulin: Effect of Polymerization Degree on Quality Traits and α-Amylase Inhibition.

2022

Inulin is considered a dietary fiber and represents a noteworthy ingredient for food biofortification due to its health effects and its neutral taste. The aim of the work was the evaluation of the quality of pasta produced using whole-meal flours of two ancient Sicilian landraces (Senatore Cappelli-CAP and Timilia—TIM) fortified with two types of inulin (long-chain topinambur inulin IT and low-chain chicory inulin IC), at two different levels of substitution (2 and 4%) to evaluate its possible effect on α-amylase inhibition. The color indices L* and a* were mainly influenced by cultivars, while IT improved the sensory attributes, mainly the elasticity sensation, and influenced l…

inulin; durum wheat; Sicilian landraces; spaghetti; quality; aminoacids; glycemic index; α amylase? amylaseSettore CHIM/10 - Chimica Degli AlimentiSicilian landracesOrganic ChemistryFlourInulinPharmaceutical Sciencedurum wheataminoacidsAnalytical ChemistryPolymerizationα amylaseChemistry (miscellaneous)qualityDrug DiscoveryMolecular Medicineglycemic indexCookingPhysical and Theoretical ChemistrySicilian landracealpha-AmylasesaminoacidspaghettiTriticumMolecules (Basel, Switzerland)
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2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors

2016

International audience; 2,3-Dihydrobenzofurans are proposed as privileged structures and used as chemical platform to design small compound libraries. By combining molecular docking calculations and experimental verification of biochemical interference, we selected some potential inhibitors of microsomal prostaglandin E2 synthase (mPGES)-1. Starting from low affinity natural product 1, by our combined approach we identified the compounds 19 and 20 with biological activity in the low micromolar range. Our data suggest that the 2,3-dihydrobenzofuran derivatives might be suitable bioinspired lead compounds for development of new generation mPGES-1 inhibitors with increased affinity.

0301 basic medicine300323-Dihydrobenzofuran privileged structure; Cancer; Inflammation; Molecular docking; mPGES-1 inhibitors; Biochemistry; Clinical Biochemistry; Molecular Biology; Molecular Medicine; Organic Chemistry; Drug Discovery3003 Pharmaceutical Science; 3003Amino Acid MotifsClinical BiochemistryGene ExpressionPharmaceutical Science01 natural sciencesClinical biochemistryBiochemistry[ CHIM ] Chemical SciencesProtein Structure Secondary[ SDV.CAN ] Life Sciences [q-bio]/Cancerchemistry.chemical_compoundLow affinityDrug DiscoveryEnzyme Inhibitors23-Dihydrobenzofuran privileged structure; Molecular docking; mPGES-1 inhibitors; Cancer; InflammationProstaglandin-E SynthasesCancerAnti-Inflammatory Agents Non-SteroidalBiological activityProto-Oncogene Proteins c-metIntramolecular OxidoreductasesMolecular Docking SimulationMolecular dockingMolecular Medicinelipids (amino acids peptides and proteins)Cell SurvivalStereochemistryMolecular Sequence Data2Antineoplastic Agents[SDV.CAN]Life Sciences [q-bio]/Cancer3-Dihydrobenzofuran privileged structureInhibitory Concentration 50Structure-Activity Relationship03 medical and health sciencesCell Line TumorMicrosomesHumans[CHIM]Chemical SciencesMolecular BiologyBenzofuransInflammationNatural product010405 organic chemistryDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryEpithelial CellsmPGES-1 inhibitorsCombinatorial chemistryCombined approach0104 chemical sciences030104 developmental biologychemistryDrug DesignDrug Screening Assays Antitumor
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Synthesis of Rosmarinic Acid Amides as Antioxidative and Hypoglycemic Agents

2019

Type 2 diabetes mellitus (T2DM) is an important metabolic disorder for which there is an urgent need for new antidiabetic drugs. α-Glucosidase inhibition is an established protocol for T2DM therapy. Because hyperglycemia causes oxidative tissue damage, the development of agents with both α-glucosidase inhibition and antioxidant activity from natural or natural-derived polyphenols such derivatives of rosmarinic acid (RA) represents an attractive therapeutic option. We report a study on amides 1-10 derived from RA and their evaluation for yeast α-glucosidase inhibition and antioxidant activity (DPPH and ORAC tests). All amides showed higher inhibitory activity than that of RA, were by far mor…

3003DrugAntioxidantDPPHProton Magnetic Resonance Spectroscopymedia_common.quotation_subjectmedicine.medical_treatmentPharmaceutical ScienceOxidative phosphorylationPharmacologyDepsides01 natural sciencesAntioxidantsAnalytical Chemistrychemistry.chemical_compoundDrug DiscoverymedicineHypoglycemic AgentsSettore BIO/15 - Biologia FarmaceuticaCarbon-13 Magnetic Resonance SpectroscopyIC50media_commonAcarbosePharmacology010405 organic chemistrydiabetes mellituDrug Discovery3003 Pharmaceutical ScienceRosmarinic acidOrganic ChemistrySettore CHIM/06 - Chimica OrganicaComplementary and Alternative Medicine2708 DermatologyAmidesamide0104 chemical sciences010404 medicinal & biomolecular chemistryRosmarinic acidComplementary and alternative medicinechemistryCinnamatesPolyphenolAnalytical Chemistry; Molecular Medicine; Pharmacology; 3003; Drug Discovery3003 Pharmaceutical Science; Complementary and Alternative Medicine2708 Dermatology; Organic ChemistryMolecular Medicineα-glucosidasemedicine.drug
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