Nanoscopy, Istituto Italiano di Tecnologia, via Morego 30, Genoa 16163, Italy; Nikon Imaging Center, Istituto Italiano di Tecnologia, via Morego 30, Genoa 16163, Italy; Department of Physics, University of Genoa, via Dodecaneso 33, Genoa 16146, Italy.
Institute for Bioengineering of Catalonia (IBEC), the Barcelona Institute of Science and Technology (BIST), Barcelona, Spain.
Life Sci. 2019 Sep 15;233:116710. doi: 10.1016/j.lfs.2019.116710. Epub 2019 Jul 29.
The naturally occurring compound curcumin has been proposed for a number of pharmacological applications. In spite of the promising chemotherapeutic properties of the molecule, the use of curcumin has been largely limited by its chemical instability in water. In this work, we propose the use of water soluble proteins to overcome this issue in perspective applications to photodynamic therapy of tumors.
Curcumin was bound to bovine serum albumin and its photophysical properties was studied as well as its effect on cell viability after light exposure through MTT assay and confocal imaging.
Bovine serum albumin binds curcumin with moderate affinity and solubilizes the hydrophobic compound preserving its photophysical properties for several hours. Cell viability assays demonstrate that when bound to serum albumin, curcumin is an effective photosensitizer for HeLa cells, with better performance than curcumin alone. Confocal fluorescence imaging reveals that when curcumin is delivered alone, it preferentially associates with mitochondria, whereas curcumin bound to bovine serum albumin is found in additional locations within the cell, a fact that may be related to the higher phototoxicity observed in this case.
The higher bioavailability of the photosensitizing compound curcumin when bound to serum albumin may be exploited to increase the efficiency of the drug in photodynamic therapy of tumors.
天然存在的化合物姜黄素已经被提出用于许多药理学应用。尽管该分子具有有前途的化疗特性，但由于其在水中的化学不稳定性，姜黄素的使用在很大程度上受到限制。在这项工作中，我们提出使用水溶性蛋白质来克服这一问题，以期应用于肿瘤的光动力疗法。
将姜黄素与牛血清白蛋白结合，并研究其光物理性质以及在光暴露后通过 MTT 测定和共聚焦成像对细胞活力的影响。
牛血清白蛋白与姜黄素具有中等亲和力结合，并溶解疏水性化合物，使其光物理性质保持数小时。细胞活力测定表明，当与血清白蛋白结合时，姜黄素是 HeLa 细胞的有效光敏剂，其性能优于单独的姜黄素。共聚焦荧光成像显示，当单独递送姜黄素时，它优先与线粒体结合，而与牛血清白蛋白结合的姜黄素则存在于细胞内的其他位置，这一事实可能与在这种情况下观察到的更高光毒性有关。
当与血清白蛋白结合时，光敏化合物姜黄素的更高生物利用度可用于提高药物在肿瘤光动力疗法中的效率。
