Tao Yexing, Yu Qian, Huang Yuting, Liu Ruiting, Zhang Xiwen, Wu Ting, Pan Siyi, Xu Xiaoyun
College of Food Science and Technology, Huazhong Agricultural University, Wuhan 430070, China.
Key Laboratory of Environment Correlative Dietology (Ministry of Education), Huazhong Agricultural University, Wuhan 430070, China.
Antioxidants (Basel). 2022 Sep 28;11(10):1922. doi: 10.3390/antiox11101922.
(PCR-C), rich in polymethoxyflavones (PMFs), has potential anticancer bioactivity and its quality will be improved during storage. However, the main factors influencing the PCR-C quality during its storage remain unclear. In this study, multivariate analysis was performed to investigate free and bound PMFs of PCR-C during storage. The anticancer effects of purified PCR-C flavonoid extracts (PCR-CF) and the important PMFs were evaluated using A549 cells. The results showed that PCR-C samples exhibited remarkable differences in free PMFs during storage, which fell into three clusters: Cluster 1 included fresh (fresh peel) and PCR-C01 (year 1); Cluster 2 consisted of PCR-C03 (year 3) and PCR-C05 (year 5); and PCR-C10 (year 10) was Cluster 3. 3,5,6,7,8,3',4'-heptamethoxyflavone, tangeretin, and isosinensetin were identified as the most important PMFs distinguishing the various types of PCR-C according to its storage periods. Moreover, PCR-CF inhibited A549 cell proliferation and induced cell cycle arrest at G2/M phase, cell apoptosis, and ROS accumulation, and all anticancer indices had an upward tendency during storage. Additionally, tangeretin and 3,5,6,7,8,3',4'-heptamethoxyflavone exhibited anticancer effects on A549 cells, whereas isosinensetin displayed no anticancer effect, indicating that tangeretin and 3,5,6,7,8,3',4'-heptamethoxyflavone jointly contributed to anticancer activity of PCR-C during storage. PCR-CF and the most important PMFs killed cancer cells (A549 cells) but had no cytotoxicity to normal lung fibroblast cells (MRC-5 cells). Overall, the high quality of long-term stored PCR-C might be due to the anticancer effects of tangeretin and 3,5,6,7,8,3',4'-heptamethoxyflavone.
富含多甲氧基黄酮（PMFs）的陈皮（PCR-C）具有潜在的抗癌生物活性，其品质在储存过程中会得到改善。然而，储存期间影响PCR-C品质的主要因素仍不清楚。在本研究中，进行了多变量分析以研究储存期间PCR-C的游离和结合PMFs。使用A549细胞评估纯化的PCR-C类黄酮提取物（PCR-CF）和重要PMFs的抗癌作用。结果表明，PCR-C样品在储存期间的游离PMFs存在显著差异，分为三个簇：簇1包括新鲜（新鲜果皮）和PCR-C01（第1年）；簇2由PCR-C03（第3年）和PCR-C05（第5年）组成；PCR-C10（第10年）为簇3。根据其储存期，3,5,6,7,8,3',4'-七甲氧基黄酮、橘红素和异川陈皮素被确定为区分不同类型PCR-C的最重要PMFs。此外，PCR-CF抑制A549细胞增殖，诱导细胞周期停滞在G2/M期、细胞凋亡和ROS积累，并且所有抗癌指标在储存期间都有上升趋势。此外，橘红素和3,5,6,7,8,3',4'-七甲氧基黄酮对A549细胞具有抗癌作用，而异川陈皮素没有抗癌作用，表明橘红素和3,5,6,7,8,3',4'-七甲氧基黄酮共同促成了储存期间PCR-C的抗癌活性。PCR-CF和最重要的PMFs杀死癌细胞（A549细胞），但对正常肺成纤维细胞（MRC-5细胞）没有细胞毒性。总体而言，长期储存的PCR-C的高品质可能归因于橘红素和3,5,6,7,8,3',4'-七甲氧基黄酮的抗癌作用。
