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Preparation of curcuminoid microemulsions from Curcuma longa L. to enhance inhibition effects on growth of colon cancer cells HT-29

机译:姜黄中姜黄素微乳的制备以增强对结肠癌细胞HT-29生长的抑制作用

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The objectives of this study were to extract curcuminoid from Curcuma longa L. (C. longa), 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 IC50 being 3.83 and 2.51 μg mL?1 after 24 h incubation, respectively, but further reduced to 2.23 and 1.94 μg mL?1, 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 (p > 0.05) in Bax expression was observed. Collectively, this study demonstrated that the curcuminoid microemulsion prepared from C. longa may possess great potential for the treatment of colon cancer in the future.
机译:这项研究的目的是从被证明具有许多生物学活性的重要药用植物 Curcuma longa L.( C。longa )中提取姜黄素,并制备姜黄素提取物和微乳液用于研究HT-29结肠癌细胞的抑制机制。结果显示,使用Eclipse XDB-18色谱柱和0.1%甲酸溶液(A)和乙腈的梯度流动相,在10分钟内分离出了3种姜黄素,包括姜黄素,去甲氧基姜黄素(DMC)和双去甲氧基姜黄素(BDMC)。 (B)。制备了由大豆油,吐温80,乙醇和水组成的类姜黄素微乳,具有高稳定性,平均粒径为10.9 nm,ζ电位为〜65.2 mV,包封效率为85.7%。姜黄素提取物和微乳剂均能有效抑制HT-29细胞生长,IC 50 为3.83和2.51μgmL ?1 孵育24小时后,但孵育48小时后进一步降低至2.23和1.94μgmL ?1 。两种处理均可以剂量依赖的方式降低存活细胞和坏死细胞的比例,并增加早期和晚期凋亡细胞的比例,并且细胞周期停滞在S期。而且,两种治疗都可以通过非p21依赖性途径上调p53表达,并下调cyclin A和CDK2表达。此外,姜黄素提取物的Bax和细胞色素C的表达以及caspase-8,caspase-9和caspase-3的活性增加,而姜黄素微乳液显示出相同的趋势,只是变化不明显(< em> p C制备的。 longa 在将来可能具有治疗结肠癌的巨大潜力。

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