64121-95-5Relevant articles and documents
Identification of key structural characteristics of schisandra chinensis lignans involved in P-glycoprotein inhibition
Slanina, Jii,Pachnikova, Gabriela,arnecka, Martina,Porubova Koubikova, Ludmila,Adamkova, Lenka,Humpa, Otakar,mejkal, Karel,Slaninova, Iva
, p. 2255 - 2263 (2014)
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.
Structure-activity relationships of lignans from Schisandra chinensis as platelet activating factor antagonists
Lee, Im Seon,Jung, Keun Young,Oh, Sei Ryang,Park, Si Hyung,Ahn, Kyung Seop,Lee, Hyeong-Kyu
, p. 265 - 267 (2007/10/03)
We studied the structure-activity relationships of lignans from Schisandra chinensis and their derivatives as platelet activating factor (PAF) antagonists. Strong activity was shown in lignans without an ester group at C-6, a hydroxyl group at C-7 or a methylene dioxy moiety and with an R-biphenyl configuration. 6(7)-Dehydroschisandrol A, a derivative of schisandrol A, showed the highest activity (IC50, 2.1 x 10-6 M) in this study.
Kadsulignans L-N, three dibenzocyclooctadiene lignans from Kadsura coccinea
Liu Jia-Sen,Li Liang
, p. 241 - 245 (2007/10/02)
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