Department of Biomedical-Chemical Engineering, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon-si, Gyeonggi-do 14662, Republic of Korea.
College of Pharmacy and Integrated Research Institute of Pharmaceutical Sciences, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon-si, Gyeonggi-do 14662, Republic of Korea.
Int J Pharm. 2020 Aug 30;586:119597. doi: 10.1016/j.ijpharm.2020.119597. Epub 2020 Jul 3.
Anthocyanins, commonly extracted from aronia, exhibit excellent in antioxidant activity and anti-cancer activity. However, anthocyanins are not only easily oxidized in water but also rapidly disappear from the body, thus requiring a large amount of administration. To solve these limitations, we selected fucoidan, an anionic polymer, to produce an anthocyanin-fucoidan nanocomplex (AFNC) with enhanced absorption and chemical stability by ionic bonding and π-π stacking between anthocyanins. In vitro, AFNC showed increased cell permeability absorption and plasma chemical stability than free anthocyanins. AFNC suppressed the epithelial mesenchymal transition (EMT) signal including IκBα/NF-κB signaling pathway and the release of pro-inflammatory cytokines. In vivo, AFNC exhibited 3.24-fold higher bioavailability than free anthocyanin in rats. AFNC effectively suppressed the generation of carcinogenesis in the 7,12-Dimethylbenz(a)anthracene (DMBA)/12-O-tetradecanoylphorbol-13-acetate (TPA) well-known tumorigenesis model. These results could be used to extend the applications of anthocyanins in anti-cancer treatment and in health care foods, and various pharmaceutical industries.
花色苷通常从黑果腺肋花楸中提取，具有出色的抗氧化活性和抗癌活性。然而，花色苷不仅在水中容易氧化，而且在体内迅速消失，因此需要大量的给药。为了解决这些限制，我们选择了阴离子聚合物褐藻糖胶，通过花色苷之间的离子键和π-π堆积，产生了具有增强吸收和化学稳定性的花色苷-褐藻糖胶纳米复合物（AFNC）。在体外，AFNC 表现出比游离花色苷更高的细胞通透性吸收和血浆化学稳定性。AFNC 抑制上皮间质转化（EMT）信号，包括 IκBα/NF-κB 信号通路和促炎细胞因子的释放。在体内，AFNC 在大鼠中的生物利用度比游离花色苷高 3.24 倍。AFNC 有效抑制了 7,12-二甲基苯并（a）蒽（DMBA）/12-O-十四烷酰佛波醇-13-乙酸酯（TPA）这一著名的肿瘤发生模型中的致癌生成。这些结果可用于扩展花色苷在抗癌治疗和保健品以及各种制药行业中的应用。
