0000000001216865

AUTHOR

Cindy Horwedel

showing 2 related works from this author

Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties

2010

Abstract Artemisinins are plant products with a wide range of medicinal applications. Most prominently, artesunate is a well tolerated and effective drug for treating malaria, but is also active against several protozoal and schistosomal infections, and additionally exhibits anti-angiogenic, anti-tumorigenic and anti-viral properties. The array of activities of the artemisinins, and the recent emergence of malaria resistance to artesunate, prompted us to synthesize and evaluate several novel artemisinin-like derivatives. Sixteen distinct derivatives were therefore synthesized and the in vitro cytotoxic effects of each were tested with different cell lines. The in vivo anti-angiogenic proper…

DrugArtemisininsSwinemedia_common.quotation_subjectmalariaArtemisia annuaAngiogenesis InhibitorsDrug resistanceArtemisia annuaP-glycoproteinPharmacologychemotherapyStructure-Activity Relationshipchemistry.chemical_compoundIn vivoparasitic diseasesmedicineAnimalscancerArtemisininCells CulturedZebrafishCell Proliferationmedia_commondrug resistancebiologyPlant ExtractsArticlesCell BiologyFlow Cytometrybiology.organism_classificationArtemisininsIn vitrochemistryArtesunateMolecular Medicinemedicine.drugJournal of Cellular and Molecular Medicine
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Cytotoxicity of Artesunic Acid Homo- and Heterodimer Molecules toward Sensitive and Multidrug-Resistant CCRF-CEM Leukemia Cells

2010

A novel approach to circumvent multidrug resistance is hybridization of natural products in dimers. We analyzed homodimers of two artesunic acid molecules and heterohybrids of artesunic acid and betulin in human CCRF-CEM and multidrug-resistant P-glycoprotein-overexpressing CEM/ADR5000 leukemia cells. Multidrug-resistant cells were not cross-resistant to the novel compounds. Collateral sensitivity was observed for artesunic acid homodimer. Artesunic acid and artesunic acid homodimer induced G0/G1 cell cycle arrest, apoptosis, and formation of reactive oxygen species.

Spectrometry Mass Electrospray IonizationMagnetic Resonance SpectroscopyCell SurvivalApoptosischemistry.chemical_compoundCell Line TumorDrug DiscoverymedicineHumansCytotoxicitychemistry.chemical_classificationReactive oxygen speciesFormazansLeukemiaBetulinCell CycleSuccinatesCell cycleFlow Cytometrymedicine.diseaseArtemisininsTriterpenesMultiple drug resistanceLeukemiachemistryBiochemistryDrug Resistance NeoplasmCell cultureApoptosisMolecular MedicineReactive Oxygen SpeciesJournal of Medicinal Chemistry
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