0000000000288914

AUTHOR

Paolo Coghi

showing 10 related works from this author

Crystal Structures and Cytotoxicity of ent-Kaurane-Type Diterpenoids from Two Aspilia Species

2018

A phytochemical investigation of the roots of Aspilia pluriseta led to the isolation of ent-kaurane-type diterpenoids and additional phytochemicals (1⁻23). The structures of the isolated compounds were elucidated based on Nuclear Magnetic Resonance (NMR) spectroscopic and mass spectrometric analyses. The absolute configurations of seven of the ent-kaurane-type diterpenoids (3⁻6, 6b, 7 and 8) were determined by single crystal X-ray diffraction studies. Eleven of the compounds were also isolated from the roots and the aerial parts of Aspilia mossambicensis. The literature NMR assignments for compounds 1 and 5 were revised. In a cytotoxicity assay, 12α-methoxy-ent-kaur-9(11),1…

Lung Neoplasms<i>Aspilia mossambicensis</i>Pharmaceutical ScienceCrystal structureAspilia plurisetaAsteraceaePlant Roots01 natural sciencesAnalytical Chemistryent-kaurane diterpenoid.Drug DiscoveryAspilia mossambicensisCytotoxicityEnt kauraneta116Organisk kemiMolecular StructurebiologyChemistryLiver NeoplasmsHep G2 CellsMass spectrometricterpeenitPhytochemicalChemistry (miscellaneous)solunsalpaajatMolecular MedicinecytotoxicityasterikasvitDiterpenes KauraneAspilia<i>ent</i>-kaurane diterpenoidCarcinoma HepatocellularCell SurvivalStereochemistry010402 general chemistryta3111Articlelcsh:QD241-441lcsh:Organic chemistryHumans<i>Aspilia pluriseta</i>Physical and Theoretical ChemistryIC50x-ray crystallography010405 organic chemistrycytostatic drugsOrganic Chemistryta1182Adenocarcinoma Bronchiolo-AlveolarPlant Components AerialAsteraceaebiology.organism_classificationluonnonaineetX-ray crystal structurenaturally occurring substances0104 chemical sciencesA549 Cellsent-kaurane diterpenoidröntgenkristallografiaterpenesMolecules
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N-Desmethyldauricine Induces Autophagic Cell Death in Apoptosis-Defective Cells via Ca2+ Mobilization

2017

Resistance of cancer cells to chemotherapy remains a significant problem in oncology. Mechanisms regulating programmed cell death, including apoptosis, autophagy or necrosis, in the treatment of cancers have been extensively investigated over the last few decades. Autophagy is now emerging as an important pathway in regulating cell death or survival in cancer therapy. Recent studies demonstrated variety of natural small-molecules could induce autophagic cell death in apoptosis-resistant cancer cells, therefore, discovery of novel autophagic enhancers from natural products could be a promising strategy for treatment of chemotherapy-resistant cancer. By computational virtual docking analysis,…

0301 basic medicinePharmacologyProgrammed cell deathautophagyKinaseDrug discoveryAutophagylcsh:RM1-950BiologyCell biology03 medical and health sciences030104 developmental biologylcsh:Therapeutics. PharmacologyApoptosisautophagic cell deathN-desmethyldauricineSERCACancer cellCytotoxic T cellPharmacology (medical)apoptosis-resistantProtein kinase AOriginal ResearchFrontiers in Pharmacology
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Synthesis, computational docking and biological evaluation of celastrol derivatives as dual inhibitors of SERCA and P-glycoprotein in cancer therapy.

2021

Abstract A series of eleven celastrol derivatives was designed, synthesized, and evaluated for their in vitro cytotoxic activities against six human cancer cell lines (A549, HepG2, HepAD38, PC3, DLD-1 Bax-Bak WT and DKO) and three human normal cells (LO2, BEAS-2B, CCD19Lu). To our knowledge, six derivatives were the first example of dipeptide celastrol derivatives. Among them, compound 3 was the most promising derivative, as it exhibited a remarkable anti-proliferative activity and improved selectivity in liver cancer HepAD38 versus human normal hepatocytes, LO2. Compound 6 showed higher selectivity in liver cancer cells against human normal lung fibroblasts, CCD19Lu cell line. The Ca2+ mob…

SERCAAntineoplastic AgentsApoptosisPharmacologySarcoplasmic Reticulum Calcium-Transporting ATPaseschemistry.chemical_compoundStructure-Activity RelationshipCell Line TumorDrug DiscoverymedicineCytotoxic T cellHumansATP Binding Cassette Transporter Subfamily B Member 1P-glycoproteinCell ProliferationPharmacologyBinding SitesbiologyOrganic ChemistryCancerGeneral Medicinemedicine.diseaseMolecular Docking SimulationchemistryApoptosisDocking (molecular)CelastrolCell cultureDrug Resistance NeoplasmDrug Designbiology.proteinDrug Screening Assays AntitumorPentacyclic TriterpenesEuropean journal of medicinal chemistry
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CCDC 1868319: Experimental Crystal Structure Determination

2020

Related Article: Souaibou Yaouba, Arto Valkonen, Paolo Coghi, Jiaying Gao, Eric M. Guantai, Solomon Derese, Vincent K. W. Wong, Máté Erdélyi, Abiy Yenesew|2018|Molecules|23|3199|doi:10.3390/molecules23123199

Space GroupCrystallographymethyl 9-hydroxy-15-[(2-methylbut-2-enoyl)oxy]kaur-16-en-18-oateCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1868324: Experimental Crystal Structure Determination

2020

Related Article: Souaibou Yaouba, Arto Valkonen, Paolo Coghi, Jiaying Gao, Eric M. Guantai, Solomon Derese, Vincent K. W. Wong, Máté Erdélyi, Abiy Yenesew|2018|Molecules|23|3199|doi:10.3390/molecules23123199

Space GroupCrystallographyCrystal SystemCrystal StructureCell Parameterskaur-9(11)-en-18-oic acidExperimental 3D Coordinates
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CCDC 1868322: Experimental Crystal Structure Determination

2020

Related Article: Souaibou Yaouba, Arto Valkonen, Paolo Coghi, Jiaying Gao, Eric M. Guantai, Solomon Derese, Vincent K. W. Wong, Máté Erdélyi, Abiy Yenesew|2018|Molecules|23|3199|doi:10.3390/molecules23123199

Space GroupCrystallographyCrystal Systemkauran-18-oic acidCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1868321: Experimental Crystal Structure Determination

2020

Related Article: Souaibou Yaouba, Arto Valkonen, Paolo Coghi, Jiaying Gao, Eric M. Guantai, Solomon Derese, Vincent K. W. Wong, Máté Erdélyi, Abiy Yenesew|2018|Molecules|23|3199|doi:10.3390/molecules23123199

Space GroupCrystallographyCrystal SystemCrystal StructureCell Parameters15-[(2-methylbut-2-enoyl)oxy]-1617-epoxykauran-18-oic acidExperimental 3D Coordinates
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CCDC 1868320: Experimental Crystal Structure Determination

2020

Related Article: Souaibou Yaouba, Arto Valkonen, Paolo Coghi, Jiaying Gao, Eric M. Guantai, Solomon Derese, Vincent K. W. Wong, Máté Erdélyi, Abiy Yenesew|2018|Molecules|23|3199|doi:10.3390/molecules23123199

Space GroupCrystallographyCrystal SystemCrystal StructureCell Parameters411b-dimethyl-8-methylene-12344a567891011b-dodecahydro-6a9-methanocyclohepta[a]naphthalene-4-carboxylic acidExperimental 3D Coordinates
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CCDC 1868318: Experimental Crystal Structure Determination

2020

Related Article: Souaibou Yaouba, Arto Valkonen, Paolo Coghi, Jiaying Gao, Eric M. Guantai, Solomon Derese, Vincent K. W. Wong, Máté Erdélyi, Abiy Yenesew|2018|Molecules|23|3199|doi:10.3390/molecules23123199

Space GroupCrystallographyCrystal SystemCrystal Structure9-hydroxy-15-[(2-methylbut-2-enoyl)oxy]kaur-16-en-18-oic acidCell ParametersExperimental 3D Coordinates
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CCDC 1868323: Experimental Crystal Structure Determination

2020

Related Article: Souaibou Yaouba, Arto Valkonen, Paolo Coghi, Jiaying Gao, Eric M. Guantai, Solomon Derese, Vincent K. W. Wong, Máté Erdélyi, Abiy Yenesew|2018|Molecules|23|3199|doi:10.3390/molecules23123199

Space GroupCrystallographyCrystal SystemCrystal StructureCell Parameters15-[(2-methylbut-2-enoyl)oxy]kaur-16-en-18-oic acidExperimental 3D Coordinates
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