Department of Materials Science and Technology, Faculty of Engineering, Gifu University, 1-1 Yanagido, Gifu, 501-1193, Japan.
J Nat Med. 2013 Jul;67(3):460-7. doi: 10.1007/s11418-012-0697-0. Epub 2012 Aug 2.
Flavonoids are widely occurring polyphenols that are found in plants. The aim of this study was to investigate the structure-activity relationships of 5,7-dihydroxyflavones, with a focus on the effect of B ring structure substitution on the antiproliferative effects of the compounds in human leukemia HL-60 cells. We prepared a series of 5,7-dihydroxyflavones and evaluated their ability to inhibit the proliferation of HL-60 cells by using the MTT assay. The apoptosis- and cell differentiation-inducing ability of the most potent flavones were investigated using staining and morphological analyses. This study explored the antileukemic and chemopreventive potency of 5,7-dihydroxyflavones, particularly diosmetin and chrysoeriol, which have both hydroxy and methoxy groups on the B ring.
类黄酮是广泛存在于植物中的多酚类化合物。本研究旨在探讨 5,7-二羟基黄酮的构效关系，重点研究 B 环结构取代对化合物在人白血病 HL-60 细胞中抗增殖作用的影响。我们制备了一系列 5,7-二羟基黄酮，并通过 MTT assay 评估它们抑制 HL-60 细胞增殖的能力。通过染色和形态分析研究了最有效的黄酮类化合物诱导细胞凋亡和分化的能力。本研究探讨了 5,7-二羟基黄酮，特别是 B 环上既有羟基又有甲氧基的芫花素和芹菜素的抗白血病和化学预防潜力。
