UNESP - São Paulo State University - IBILCE - Institute of Biosciences, Humanities and Exact Sciences - Department of Biology - Rua Cristóvão Colombo, 2265 - Bairro Jardim Nazareth, CEP 15054-010 São José do Rio Preto, São Paulo, Brazil.
UNESP - São Paulo State University- Faculty of Pharmaceutical Sciences of Araraquara - Department of Bioprocess and Biotechnology, Rodovia Araraquara/Jaú, Km 01, s/n, Campos Ville, CEP 14800-903 Araraquara, São Paulo, Brazil.
Bioorg Med Chem. 2019 May 1;27(9):1882-1890. doi: 10.1016/j.bmc.2019.03.044. Epub 2019 Mar 22.
Curcumin, a natural compound has several antineoplastic activities and is a promising natural photosensitizer used in photodynamic therapy. However, its low solubility in physiological medium limit the clinical use of curcumin. This study aimed to analyze the action of curcumin-nanoemulsion, a new and well-designed Drug Delivery System (DDS+) molecule, used as a photosensitizing agent in photodynamic therapy in an in vitro breast cancer model, MCF-7 cells. The empty nanoemulsion fulfils all necessary requirements to be an excellent DDS. Furthermore, the use of curcumin-nanoemulsion in photodynamic therapy resulted in a high phototoxic effect after activation at 440 nm, decreasing to <10% viable tumor cells after two irradiations and increasing the reactive oxygen species (ROS) production. The use of curcumin-nanoemulsion associated with photodynamic therapy resulted in an increase in the levels of caspase 3/7 activity for the studied MCF-7 cell model, indicating that this therapy triggers a cascade of events that lead to cell death, such as cellular apoptosis. In conclusion, curcumin-nanoemulsion proved to be efficient as a photosensitizing agent, had phototoxic effects, significantly decreased the proliferation of MCF-7 cells and stimulating the ROS production in combination with photodynamic therapy, so, this formulation has a great potential for use in treatment of breast cancer.
姜黄素是一种天然化合物,具有多种抗肿瘤活性,是一种很有前途的天然光敏剂,用于光动力疗法。然而,其在生理介质中的低溶解度限制了其在临床上的应用。本研究旨在分析姜黄素纳米乳(一种新的、设计良好的药物输送系统(DDS+)分子)在体外乳腺癌模型 MCF-7 细胞中的光动力治疗中的作用。空纳米乳乳液符合成为优秀 DDS 的所有必要要求。此外,在 440nm 下激活后,姜黄素纳米乳乳液在光动力治疗中产生了很高的光毒性效应,两次照射后使肿瘤细胞的存活率降至<10%,并增加了活性氧(ROS)的产生。姜黄素纳米乳乳液与光动力疗法的联合应用导致所研究的 MCF-7 细胞模型中 caspase 3/7 活性增加,表明这种治疗引发了一系列导致细胞死亡的事件,如细胞凋亡。总之,姜黄素纳米乳乳液作为光敏剂的效果良好,具有光毒性作用,显著降低了 MCF-7 细胞的增殖,并刺激了 ROS 的产生,与光动力疗法相结合,因此,这种制剂在乳腺癌的治疗中有很大的应用潜力。