Corradi Elisabetta, Schmidt Nadine, Räber Nathalie, De Mieri Maria, Hamburger Matthias, Butterweck Veronika, Potterat Olivier
Division of Pharmaceutical Biology, University of Basel, Switzerland.
Institute for Pharma Technology, School of Life Sciences, University of Applied Sciences Northwestern Switzerland, Muttenz, Switzerland.
Planta Med. 2017 Oct;83(14-15):1149-1158. doi: 10.1055/s-0043-109098. Epub 2017 Apr 27.
Phenolic constituents of (Salicaceae) and antiproliferative activity of an extract and individual compounds were investigated in immortalized human non-tumorigenic keratinocytes (HaCaT). A MeOH extract from aerial parts afforded several flavonoids, including luteolin and apigenin glycosides (- and ) and catechin (), two procyanidin fractions, and the phenolic glucosides picein (), triandrin (), and salicortin (). In an adenosine triphosphate assay, the MeOH extract reduced cell viability by approximately 60 % at a concentration of 100 µg/mL. Cell proliferation was assessed with a BrdU incorporation ELISA assay. The extract inhibited proliferation of HaCaT cells in a concentration-dependent manner, with approximately 50 % inhibition at 100 µg/mL. In time-lapse assays, the extract showed distinct inhibitory effects on cell migration at concentrations of 12.5, 25, and 50 µg/mL. The activity of selected constituents was also determined. Luteolin-7-O--glucuronide () significantly inhibited cell proliferation at concentrations of 10 and 50 µM. In contrast, luteolin-7-O--glucopyranoside () and a procyanidin fraction (P1) had only weak effects, while picein () and salicortin () did not affect cell proliferation. Luteolin-7-O--glucuronide (10 µM) and, to a lesser extent, the procyanidin fraction (10 µg/mL) also inhibited cell migration.
研究了杨柳科植物的酚类成分以及一种提取物和单个化合物在永生化人非致瘤角质形成细胞(HaCaT)中的抗增殖活性。地上部分的甲醇提取物得到了几种黄酮类化合物,包括木犀草素和芹菜素糖苷( - 和 )以及儿茶素( )、两个原花青素组分,还有酚类糖苷云杉新苷( )、三齿素( )和水杨苷( )。在三磷酸腺苷测定中,甲醇提取物在浓度为100 μg/mL时使细胞活力降低了约60%。用BrdU掺入ELISA测定法评估细胞增殖。该提取物以浓度依赖性方式抑制HaCaT细胞的增殖,在100 μg/mL时抑制率约为50%。在延时测定中,该提取物在浓度为12.5、25和50 μg/mL时对细胞迁移显示出明显的抑制作用。还测定了所选成分的活性。木犀草素 - 7 - O - - 葡萄糖醛酸苷( )在浓度为10和50 μM时显著抑制细胞增殖。相比之下,木犀草素 - 7 - O - - 吡喃葡萄糖苷( )和一个原花青素组分(P1)只有微弱作用,而云杉新苷( )和水杨苷( )不影响细胞增殖。木犀草素 - 7 - O - - 葡萄糖醛酸苷(10 μM)以及程度较轻的原花青素组分(10 μg/mL)也抑制细胞迁移。