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  • The aim of the present study was to determine the structural requirements for dibenzocyclooctadiene lignans essential for P-glycoprotein inhibition. Altogether 15 structurally related lignans isolated from Schisandra chinensis or prepared by modification of their backbone were investigated, including three pairs of enantiomers. P-Glycoprotein inhibition was quantified using a doxorubicin accumulation assay in human promyelotic leukemia HL60/MDR cells overexpressing P-glycoprotein. A preliminary quantitative structure-activity relationship analysis revealed three main structural features involved in P-glycoprotein inhibition: a 1,2,3-trimethoxy moiety, a 6-acyloxy group, and the absence of a 7-hydroxy group. The most effective inhibitors, (-)-gomisin N (1) and (+)-deoxyschizandrin [(+)-2], were selected for further evaluation of their effects.
  • The aim of the present study was to determine the structural requirements for dibenzocyclooctadiene lignans essential for P-glycoprotein inhibition. Altogether 15 structurally related lignans isolated from Schisandra chinensis or prepared by modification of their backbone were investigated, including three pairs of enantiomers. P-Glycoprotein inhibition was quantified using a doxorubicin accumulation assay in human promyelotic leukemia HL60/MDR cells overexpressing P-glycoprotein. A preliminary quantitative structure-activity relationship analysis revealed three main structural features involved in P-glycoprotein inhibition: a 1,2,3-trimethoxy moiety, a 6-acyloxy group, and the absence of a 7-hydroxy group. The most effective inhibitors, (-)-gomisin N (1) and (+)-deoxyschizandrin [(+)-2], were selected for further evaluation of their effects. (en)
Title
  • Identification of Key Structural Characteristics of Schisandra chinensis Lignans Involved in P-Glycoprotein Inhibition
  • Identification of Key Structural Characteristics of Schisandra chinensis Lignans Involved in P-Glycoprotein Inhibition (en)
skos:prefLabel
  • Identification of Key Structural Characteristics of Schisandra chinensis Lignans Involved in P-Glycoprotein Inhibition
  • Identification of Key Structural Characteristics of Schisandra chinensis Lignans Involved in P-Glycoprotein Inhibition (en)
skos:notation
  • RIV/00216224:14110/14:00077244!RIV15-MSM-14110___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • S, V
http://linked.open...iv/cisloPeriodika
  • 10
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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  • 20292
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  • RIV/00216224:14110/14:00077244
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • RESISTANCE-ASSOCIATED PROTEIN-1; MEDIATED MULTIDRUG-RESISTANCE; CANCER-CELLS; DIBENZOCYCLOOCTADIENE LIGNANS; ABSOLUTE STRUCTURE; DRUG-RESISTANCE; GOMISIN-N; CONSTITUENTS; BAILL; SCHIZANDRIN (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [BB8541612882]
http://linked.open...i/riv/nazevZdroje
  • Journal of Natural Products
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 77
http://linked.open...iv/tvurceVysledku
  • Slaninová, Iva
  • Šmejkal, Karel
  • Adámková, Lenka
  • Koubíková, Ludmila
  • Páchniková, Gabriela
  • Slanina, Jiří
  • Čarnecká, Martina
  • Humpa, Otakar
http://linked.open...ain/vavai/riv/wos
  • 000343786100013
issn
  • 0163-3864
number of pages
http://bibframe.org/vocab/doi
  • 10.1021/np500521v
http://localhost/t...ganizacniJednotka
  • 14110
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