Abe Shogo, Hirose Saki, Nishitani Mami, Yoshida Ichiro, Tsukayama Masao, Tsuji Akihiko, Yuasa Keizo
a Department of Biological Science and Technology , Tokushima University Graduate School , Tokushima , Japan.
b Laboratory of Nutritional Science, Department of Food Science and Nutrition , Shikoku Junior College , Tokushima , Japan.
Biosci Biotechnol Biochem. 2018 Dec;82(12):2064-2071. doi: 10.1080/09168451.2018.1514246. Epub 2018 Sep 5.
A variety of polyphenols have been isolated from plants, and their biological activities have been examined. Sudachitin (5,7,4'-trihydroxy-6,8,3'-trimethoxyflavone) is a polymethoxyflavone that is isolated from the peel of Citrus sudachi. Although we previously reported that sudachitin possesses an anti-inflammatory activity, its other biological activities are not yet understood. In this study, we report a novel biological activity of sudachitin, which selectively induced apoptosis in human keratinocyte HaCaT cells. Another polymethoxyflavone, nobiletin (5,6,7,8,3',4'-hexamethoxyflavone), promoted autophagy but not apoptosis in HaCaT cells. On the other hand, 3'-demethoxysudachitin (5,7,4'-trihydroxy-6,8-dimethoxyflavone) failed to induce apoptosis and autophagy. These results show that three polymethoxyflavones have different effects on apoptosis and autophagy in HaCaT cells. Understanding the structure and biological activity of polymethoxyflavones may lead to the discovery of potential candidates for cancer drug development without significant toxic side effects. Abbreviations: ROS: reactive oxygen species; DMSO: dimethyl sulfoxide; MTT: 3-(4, 5-dimethylthiazol-2yl)-2, 5-diphenyltetrazolium bromide; GAPDH: glyceraldehyde-3-phosphate dehydrogenase; PARP: poly(ADP-ribose) polymerase; PI: propidium iodide; MAPK: mitogen-activated protein kinase.
多种多酚已从植物中分离出来，并且对其生物活性进行了研究。酸橘苷（5,7,4'-三羟基-6,8,3'-三甲氧基黄酮）是一种从酸橘果皮中分离出来的多甲氧基黄酮。尽管我们之前报道过酸橘苷具有抗炎活性，但其其他生物活性尚不清楚。在本研究中，我们报道了酸橘苷的一种新的生物活性，它能选择性地诱导人角质形成细胞HaCaT细胞凋亡。另一种多甲氧基黄酮，川陈皮素（5,6,7,8,3',4'-六甲氧基黄酮），在HaCaT细胞中促进自噬但不诱导凋亡。另一方面，3'-去甲氧基酸橘苷（5,7,4'-三羟基-6,8-二甲氧基黄酮）未能诱导凋亡和自噬。这些结果表明，三种多甲氧基黄酮对HaCaT细胞的凋亡和自噬有不同的影响。了解多甲氧基黄酮的结构和生物活性可能会发现潜在的癌症药物开发候选物，且无明显的毒副作用。缩写：ROS：活性氧；DMSO：二甲基亚砜；MTT：3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐；GAPDH：甘油醛-3-磷酸脱氢酶；PARP：聚（ADP-核糖）聚合酶；PI：碘化丙啶；MAPK：丝裂原活化蛋白激酶。
