Phenylethanoid Glycosides from Digitalis purpurea and Penstemon linarioides with PKCα-Inhibitory Activity

作者：Bing‐Nan Zhou, Brian D. Bahler, Glenn A. Hofmann, Michael R. Mattern, Randall K. Johnson, David G. I. Kingston · 发表于：Journal of Natural Products · 年份：1998 · DOI：10.1021/np980147s · 被引用次数：65 · 研究领域：Phytochemistry and Biological Activities、Phytochemical Studies and Bioactivities、Natural product bioactivities and synthesis

In a continuation of our search for potential tumor inhibitors from plants, it was found that the CH2Cl2-MeOH (1:1) extracts from Digitalis purpurea and Penstemon linarioides both showed PKCalpha-inhibitory bioactivity. Bioassay-directed fractionation of the extract from D. purpurea yielded the new, weakly active phenylethanoid glycoside 2-(3-hydroxy-4-methoxy-phenyl)-ethyl-O-(alpha-L-rhamnosyl)-(1-->3) -O- (alpha-L-rhamnosyl)-(1-->6)-4-O-E-feruloyl-beta-D-glucopy ran oside (1) together with the four known compounds calceolarioside A (2), calceolarioside B (3), forsythiaside (4), and plantainoside D (5). The extract from P. linarioides yielded the three known glycosides leucosceptoside A (6), acteoside (7), and poliumoside (8), together with the iridoid plantarenaloside (9). All of the isolated compounds, except compound 9, showed inhibitory activity against PKCalpha with IC50 values (in microM) of 125 (1), 0.6 (2), 4.6 (3), 1.9 (4), 14.8 (5), 19.0 (6), 9.3 (7), and 24.4 (8).