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@proceedings{1404290,
author = {Drabinová, Martina and Čarnecká, Martina and Páchniková, Gabriela and Humpa, Otakar and Slaninová, Iva and Slanina, Jiří},
booktitle = {XVIII. Setkání biochemiků a molekulárních biologů},
keywords = {lignans; P-glycoprotein},
language = {eng},
isbn = {978-80-210-8765-1},
title = {P-glycoprotein inhibition by dibenzocyclooctadiene lignans from Schisandra chinensis},
url = {http://orion.chemi.muni.cz/setkani/Setkani18/index.htm},
year = {2017}
}
TY - CONF
ID - 1404290
AU - Drabinová, Martina - Čarnecká, Martina - Páchniková, Gabriela - Humpa, Otakar - Slaninová, Iva - Slanina, Jiří
PY - 2017
TI - P-glycoprotein inhibition by dibenzocyclooctadiene lignans from Schisandra chinensis
SN - 9788021087651
KW - lignans
KW - P-glycoprotein
UR - http://orion.chemi.muni.cz/setkani/Setkani18/index.htm
N2 - The structural requirements for P-glycoprotein inhibition by dibenzocyclooctadiene lignans were studied. Altogether 15 structurally related lignans isolated from Schisandra chinensis or prepared by their modification were investigated, including three pairs of enantiomers. P-Glycoprotein inhibition was quantified using a doxorubicin accumulation assay in human promyelocytic 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 lignans restored the cytotoxic effect of doxorubicin in HL60/MDR cells and when combined with a subtoxic concentration of this compound increased the proportion of G2/M cells significantly, which is a usual response to treatment with this anticancer drug. The five most effective dibenzocyclooctadiene lignans found so far have met two of the three conditions; however, none of the lignans tested met all three structural prerequisites. The final structure-to-MDR reversing activity relationship has not been established due to a limited number of lignans.
ER -
DRABINOVÁ, Martina, Martina ČARNECKÁ, Gabriela PÁCHNIKOVÁ, Otakar HUMPA, Iva SLANINOVÁ and Jiří SLANINA. P-glycoprotein inhibition by dibenzocyclooctadiene lignans from Schisandra chinensis. In \textit{XVIII. Setkání biochemiků a molekulárních biologů}. 2017. ISBN~978-80-210-8765-1.
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