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@article{1205567,
author = {Slanina, Jiří and Páchniková, Gabriela and Čarnecká, Martina and Koubíková, Ludmila and Adámková, Lenka and Humpa, Otakar and Šmejkal, Karel and Slaninová, Iva},
article_location = {Washington},
article_number = {10},
doi = {http://dx.doi.org/10.1021/np500521v},
keywords = {RESISTANCE-ASSOCIATED PROTEIN-1; MEDIATED MULTIDRUG-RESISTANCE; CANCER-CELLS; DIBENZOCYCLOOCTADIENE LIGNANS; ABSOLUTE STRUCTURE; DRUG-RESISTANCE; GOMISIN-N; CONSTITUENTS; BAILL; SCHIZANDRIN},
language = {eng},
issn = {0163-3864},
journal = {Journal of Natural Products},
title = {Identification of Key Structural Characteristics of Schisandra chinensis Lignans Involved in P-Glycoprotein Inhibition},
volume = {77},
year = {2014}
}
TY - JOUR
ID - 1205567
AU - Slanina, Jiří - Páchniková, Gabriela - Čarnecká, Martina - Koubíková, Ludmila - Adámková, Lenka - Humpa, Otakar - Šmejkal, Karel - Slaninová, Iva
PY - 2014
TI - Identification of Key Structural Characteristics of Schisandra chinensis Lignans Involved in P-Glycoprotein Inhibition
JF - Journal of Natural Products
VL - 77
IS - 10
SP - 2255-2263
EP - 2255-2263
PB - American Chemical Society
SN - 01633864
KW - RESISTANCE-ASSOCIATED PROTEIN-1
KW - MEDIATED MULTIDRUG-RESISTANCE
KW - CANCER-CELLS
KW - DIBENZOCYCLOOCTADIENE LIGNANS
KW - ABSOLUTE STRUCTURE
KW - DRUG-RESISTANCE
KW - GOMISIN-N
KW - CONSTITUENTS
KW - BAILL
KW - SCHIZANDRIN
N2 - 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. Both these 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.
ER -
SLANINA, Jiří, Gabriela PÁCHNIKOVÁ, Martina ČARNECKÁ, Ludmila KOUBÍKOVÁ, Lenka ADÁMKOVÁ, Otakar HUMPA, Karel ŠMEJKAL and Iva SLANINOVÁ. Identification of Key Structural Characteristics of Schisandra chinensis Lignans Involved in P-Glycoprotein Inhibition. \textit{Journal of Natural Products}. Washington: American Chemical Society, 2014, vol.~77, No~10, p.~2255-2263. ISSN~0163-3864. Available from: https://dx.doi.org/10.1021/np500521v.
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