Chen Yen Chu, Chen Bing Huei
Department of Food Science, Fu Jen Catholic University New Taipei City 242 Taiwan
RSC Adv. 2018 Jan 9;8(5):2323-2337. doi: 10.1039/c7ra12297g.
The objectives of this study were to extract curcuminoid from L. (), a vital medicinal plant demonstrated to possess many biological activities, and prepare the curcuminoid extract and microemulsion for studying the inhibition mechanism of HT-29 colon cancer cells. Results showed that a total of 3 curcuminoids including curcumin, demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC), were separated within 10 min by using an Eclipse XDB-18 column and a gradient mobile phase of 0.1% formic acid solution (A) and acetonitrile (B). The curcuminoid microemulsion composed of soybean oil, Tween 80, ethanol and water was prepared with a high stability and mean particle size of 10.9 nm, zeta-potential of -65.2 mV and encapsulation efficiency of 85.7%. Both curcuminoid extract and microemulsion were effective in inhibiting HT-29 cell growth with the IC being 3.83 and 2.51 μg mL after 24 h incubation, respectively, but further reduced to 2.23 and 1.94 μg mL, after 48 h incubation. Both treatments could decrease the proportion of both viable and necrosis cells and increase the proportion of both early and late apoptosis cells in a dose-dependent manner, with the cell cycle arrested at the S phase. Also, both treatments could up-regulate p53 expression and down-regulate cyclin A and CDK2 expressions through a p21-independent pathway. In addition, the expressions of Bax and cytochrome C as well as the activities of caspase-8, caspase-9 and caspase-3 increased for the curcuminoid extract, while the curcuminoid microemulsion showed the same trend with the exception that an insignificant change ( > 0.05) in Bax expression was observed. Collectively, this study demonstrated that the curcuminoid microemulsion prepared from may possess great potential for the treatment of colon cancer in the future.
本研究的目的是从一种已证明具有多种生物活性的重要药用植物姜黄中提取姜黄素类化合物,并制备姜黄素类提取物和微乳剂,以研究其对HT-29结肠癌细胞的抑制机制。结果表明,使用Eclipse XDB-18柱和由0.1%甲酸溶液(A)和乙腈(B)组成的梯度流动相,在10分钟内分离出了包括姜黄素、去甲氧基姜黄素(DMC)和双去甲氧基姜黄素(BDMC)在内的总共3种姜黄素类化合物。由大豆油、吐温80、乙醇和水组成的姜黄素类微乳剂制备成功,具有高稳定性,平均粒径为10.9 nm,ζ电位为-65.2 mV,包封率为85.7%。姜黄素类提取物和微乳剂均能有效抑制HT-29细胞生长,孵育24小时后IC50分别为3.83和2.51 μg/mL,但孵育48小时后分别降至2.23和1.94 μg/mL。两种处理均能以剂量依赖的方式降低活细胞和坏死细胞的比例,增加早期和晚期凋亡细胞的比例,使细胞周期停滞在S期。此外,两种处理均能通过不依赖p21的途径上调p53表达,下调细胞周期蛋白A和CDK2表达。此外,姜黄素类提取物使Bax和细胞色素C的表达以及caspase-8、caspase-9和caspase-3的活性增加,而姜黄素类微乳剂呈现相同趋势,只是观察到Bax表达变化不显著(P>0.05)。总体而言,本研究表明,从姜黄制备的姜黄素类微乳剂未来可能具有治疗结肠癌的巨大潜力。