Division of Bioscience and Biotechnology, BMIC, Konkuk University, MoleNBio, Seoul 143-701, Republic of Korea.
Int J Mol Med. 2012 Mar;29(3):403-8. doi: 10.3892/ijmm.2011.857. Epub 2011 Dec 12.
Naringenin has been shown to display various biological effects such as antioxidant, anticancer, anti-inflammatory, and antiviral activities. Taxifolin inhibits the production of lipopolysaccharide-induced prostaglandin E, and fustin suppresses the activity of acetylcholinesterase. They all belong to flavanone which is a class of flavonoids with a C6-C3-C6 skeleton. Since the anticancer activities of flavanone derivatives have rarely been reported, we examined the effects of 26 flavanone derivatives on HCT116 colorectal cancer cells. Our results suggest that flavanone derivatives control the expression of cell cycle regulatory proteins, which blocks G1 cell cycle progression and inhibits the clonogenicity of HCT116 cells. In addition, in order to design flavanone derivatives that show better anticancer activity, structure-activity relationships were examined.
柚皮素具有抗氧化、抗癌、抗炎和抗病毒等多种生物学作用。杨梅素抑制脂多糖诱导的前列腺素 E 的产生，而莰非醇抑制乙酰胆碱酯酶的活性。它们都属于黄烷酮类，是具有 C6-C3-C6 骨架的黄酮类化合物之一。由于黄烷酮衍生物的抗癌活性很少被报道，我们研究了 26 种黄烷酮衍生物对结肠直肠癌细胞 HCT116 的影响。我们的结果表明，黄烷酮衍生物控制细胞周期调节蛋白的表达，从而阻止 G1 细胞周期进程并抑制 HCT116 细胞的集落形成能力。此外，为了设计显示更好抗癌活性的黄烷酮衍生物，我们研究了构效关系。
