Graduate School of Pharmaceutical Sciences, Chiba University, 1-33 Yayoi-cho, Inage-ku, Chiba 263-8522, Japan.
J Nat Med. 2011 Jan;65(1):234-6. doi: 10.1007/s11418-010-0471-0. Epub 2010 Oct 1.
A screening study using a luciferase assay to identify natural products which inhibit Wnt signaling was carried out. The bioassay-guided fractionation of aerial parts of a plant, Impatiens balsamina, led to the isolation of 2-methoxy-1,4-naphthoquinone (1) as an active compound. Compound 1 inhibited the TCF/β-catenin (TOP) transcriptional activity (IC(50) 2.9 µM), while it decreased the transcriptional activity of FOP (mutated TCF-binding site)-transfected cells at >5 µM.
采用萤光素酶 assay 进行了一项筛选研究,以鉴定抑制 Wnt 信号的天然产物。生物活性导向分离,从凤仙花属植物(Impatiens balsamina)的地上部分中分离得到 2-甲氧基-1,4-萘醌(1)作为活性化合物。化合物 1 抑制 TCF/β-catenin (TOP) 转录活性(IC(50) 2.9 μM),而在 >5 μM 时则降低了突变 TCF 结合位点(FOP)转染细胞的转录活性。