Other formats:
BibTeX
LaTeX
RIS
@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.
|