Department of Biological Sciences, School of Natural Sciences, University of Tabriz, 51555 Tabriz, Iran.
Department of Biosciences, University of Salzburg, Hellbrunnerstrasse 34, 5020 Salzburg, Austria.
Phytomedicine. 2019 Apr;57:183-190. doi: 10.1016/j.phymed.2018.11.017. Epub 2018 Nov 15.
Curcumin, the polyphenolic constituent of turmeric, has been recognized as an effective anticancer agent in the treatment of breast cancer. However, the poor bioavailability of curcumin triggers finding of new approaches for elevating its therapeutic efficiency.
We aimed to use gemini surfactant nanocarriers for curcumin in order to overcome its limitations.
We investigated the in vitro characterization of gemini surfactant-curcumin (Gemini-Cur) and examined its antiproliferative & apoptotic activities on breast cancer cell lines.
Gemini-Cur polymersomes were synthesized through nanoprecipitation method and characterized by dynamic light scattering (DLS), transmission and scanning electron microscopies, HPLC and X-ray diffraction (XRD). The anticancer effect of Gemini-Cur nanoparticles was studied on three different breast cancer cell lines including MCF-7, SkBr-3 and MDA-MB-231 through uptake kinetics, viability & cytotoxicity recordings and apoptotic assays. Furthermore, qRT-PCR was performed to evaluate the expression of apoptotic genes including p16INK4a, p14ARF, Bax and Bcl-2.
According to physicochemical analysis, the average particle size, zeta potential value and drug entrapment efficiency for Gemini-Cur compound were recorded as 161 ± 6.2 nm, +5.32 mV and 89.13% ± 0.93, respectively. XRD analysis also confirmed the incorporation of curcumin in gemini surfactant micelles. Regarding the enhanced cellular uptake of sphere shaped Gemini-Cur, our data showed that this nano compound suppresses cancer cell proliferation via induction of apoptosis. Moreover, qRT-PCR analysis revealed that Gemini-Cur could effectively upregulate the expression of p16INK4a, p14ARF and Bax, while significantly decreasing the Bcl-2 expression in these breast cancer cells.
Our data demonstrates the great potential of gemini surfactants for efficient delivery of curcumin and subsequently, the improvement of its anticancer effect. Therefore, it is sagacious to support the idea that Gemini-Cur nano compound might have the potential to be considered as an anticancer agent.
姜黄素是姜黄中的多酚成分，已被公认为治疗乳腺癌的有效抗癌药物。然而，姜黄素的生物利用度差促使人们寻找新的方法来提高其治疗效果。
我们旨在使用双子表面活性剂纳米载体来递送姜黄素，以克服其局限性。
我们研究了双子表面活性剂-姜黄素（Gemini-Cur）的体外特性，并研究了其对乳腺癌细胞系的增殖抑制和凋亡活性。
通过纳米沉淀法合成 Gemini-Cur 聚合物囊泡，并通过动态光散射（DLS）、透射和扫描电子显微镜、高效液相色谱（HPLC）和 X 射线衍射（XRD）进行表征。通过摄取动力学、活力和细胞毒性测定以及凋亡测定研究 Gemini-Cur 纳米颗粒对三种不同乳腺癌细胞系 MCF-7、SkBr-3 和 MDA-MB-231 的抗癌作用。此外，通过 qRT-PCR 评估凋亡基因 p16INK4a、p14ARF、Bax 和 Bcl-2 的表达。
根据理化分析，Gemini-Cur 化合物的平均粒径、Zeta 电位值和药物包封效率分别为 161±6.2nm、+5.32mV 和 89.13%±0.93。XRD 分析也证实了姜黄素掺入双子表面活性剂胶束中。由于球形 Gemini-Cur 的细胞摄取增强，我们的数据表明，这种纳米复合物通过诱导细胞凋亡抑制癌细胞增殖。此外，qRT-PCR 分析显示，Gemini-Cur 能够有效上调 p16INK4a、p14ARF 和 Bax 的表达，同时显著降低这些乳腺癌细胞中 Bcl-2 的表达。
我们的数据表明，双子表面活性剂在有效递送姜黄素方面具有巨大潜力，从而提高其抗癌效果。因此，支持 Gemini-Cur 纳米复合物有可能被认为是一种抗癌药物的观点是明智的。
