0000000000447627

AUTHOR

Gert Fricker

showing 4 related works from this author

Cytotoxicity and inhibition of P-glycoprotein by selected medicinal plants from Thailand.

2014

Abstract Ethnopharmacological relevance Thai medicine has a long tradition of tonifying medicinal plants. In the present investigation, we studied the flower extracts of Jasminum sambac, Mammea siamensis, Mesua ferrea, Michelia alba, Mimusops elengi, and Nelumbo nucifera and speculated that these plants might influence metabolism and substance flow in the body. Materials and methods Isolation of porcine brain capillary endothelial cells (PBCECs) as well as multidrug-resistance CEM/ADR5000 leukemia cells, MDA-M;B-231 breast cancer, U-251 brain tumor, and HCT-116 colon cancer cells were used. The calcein-acetoxymethylester (AM) assay was used to measure inhibition of P-glycoprotein transport.…

SwineMesua ferreaMimusops elengiFlowersPharmacologyBlood–brain barrierchemistry.chemical_compoundCell Line TumorNeoplasmsDrug DiscoverymedicineAnimalsHumansATP Binding Cassette Transporter Subfamily B Member 1CytotoxicityP-glycoproteinPharmacologyMedicine East Asian TraditionalPlants MedicinalbiologyTraditional medicinePlant ExtractsMammeaBrainEndothelial Cellsmedicine.diseasebiology.organism_classificationThailandAntineoplastic Agents PhytogenicDrug Resistance MultipleLeukemiamedicine.anatomical_structurechemistryBlood-Brain BarrierDrug Resistance Neoplasmbiology.proteinEndothelium VascularGrowth inhibitionJournal of ethnopharmacology
researchProduct

Alkamides from Echinacea angustifolia Interact with P-Glycoprotein of Primary Brain Capillary Endothelial Cells Isolated from Porcine Brain Blood Ves…

2013

The blood-brain barrier prevents the passage of toxic compounds from blood circulation into brain tissue. Unfortunately, drugs for the treatment of neurodegenerative diseases, brain tumors, and other diseases also do not cross the blood-brain barrier. In the present investigation, we used isolated porcine brain capillary endothelial cells and a flow cytometric calcein-AM assay to analyze inhibition of P-glycoprotein, a major constituent of the blood-brain barrier. We tested 8 alkamides isolated from Echinacea angustifolia and found that four of them inhibited P-glycoprotein-mediated calcein transport in porcine brain capillary endothelial cells.

ATP Binding Cassette Transporter Subfamily BPolyunsaturated AlkamidesSwinePharmaceutical ScienceATP-binding cassette transporterCapillary endothelial cellsPharmacologyBlood–brain barrierEchinaceaAnalytical Chemistrychemistry.chemical_compoundDrug DiscoverymedicineAnimalsCells CulturedP-glycoproteinPharmacologyDose-Response Relationship DrugMolecular StructurebiologyEchinacea angustifoliaOrganic ChemistryBrainEndothelial CellsBiological TransportFlow CytometryFluoresceinsbiology.organism_classificationCalceinmedicine.anatomical_structureComplementary and alternative medicinechemistryBlood-Brain BarrierBlood circulationbiology.proteinMolecular MedicinePorcine brainPlanta Medica
researchProduct

Nitensidine A, a guanidine alkaloid from Pterogyne nitens, is a novel substrate for human ABC transporter ABCB1.

2014

The Pterogyne nitens (Fabaceae) tree, native to South America, has been found to produce guanidine alkaloids as well as bioactive flavonols such as kaempferol, quercetin, and rutin. In the present study, we examined the possibility of interaction between human ATP-binding cassette (ABC) transporter ABCB1 and four guanidine alkaloids isolated from P. nitens (i.e., galegine, nitensidine A, pterogynidine, and pterogynine) using human T cell lymphoblast-like leukemia cell line CCRF-CEM and its multi-drug resistant (MDR) counterpart CEM/ADR5000. In XTT assays, CEM/ADR5000 cells were resistant to the four guanidine alkaloids compared to CCRF-CEM cells, although the four guanidine alkaloids exhibi…

ATP Binding Cassette Transporter Subfamily BLeukemia T-CellStereochemistryATPasePharmaceutical ScienceATP-binding cassette transporterGuanidineschemistry.chemical_compoundStructure-Activity RelationshipCell Line TumorDrug DiscoveryHumansheterocyclic compoundsBinding siteGuanidineCytotoxicityP-glycoproteinPharmacologyAdenosine TriphosphatasesbiologyPlant ExtractsAlkaloidFabaceaeFluoresceinsAntineoplastic Agents PhytogenicDrug Resistance MultipleMolecular Docking SimulationComplementary and alternative medicinechemistryBiochemistryVerapamilDrug Resistance Neoplasmbiology.proteinMonoterpenesMolecular MedicineATP-Binding Cassette TransportersKaempferolPhytotherapyPhytomedicine : international journal of phytotherapy and phytopharmacology
researchProduct

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
researchProduct