Department of Chemistry, Ben-Gurion University of the Negev, Beer Sheva84105, Israel.
Department of Chemistry, School of Advanced Sciences, Vellore Institute of Technology, Vellore632014, India.
Bioconjug Chem. 2022 Sep 21;33(9):1663-1671. doi: 10.1021/acs.bioconjchem.2c00282. Epub 2022 Sep 6.
Resveratrol, a natural polyphenol, exhibits beneficial health properties and has been touted as a potential anti-tumor agent. Here, we demonstrate potent anti-cancer effects of carbon dots (C-dots) synthesized from resveratrol. The mild synthesis conditions retained resveratrol functional moieties upon the carbon dots' (C-dots) surface, an important requisite for achieving specificity toward cancer cells and biological activities. Indeed, the disruptive effects of the resveratrol-C-dot were more pronounced in several cancer cell types compared to normal cells, underscoring targeting capabilities of the C-dots, a pertinent issue for the development of cancer therapeutics. In particular, we observed impairment of mitochondrial functionalities, including intracellular calcium release, inhibition of cytochrome-C oxidase enzyme activity, and mitochondrial membrane perturbation. Furthermore, the resveratrol C-dots were more potent than either resveratrol molecules alone, known anti-cancer polyphenolic agents such as curcumin and triphenylphosphonium, or C-dots prepared from different carbonaceous precursors. This study suggests that resveratrol-synthesized C-dots may have promising therapeutic potential as anti-cancer agents.
白藜芦醇是一种天然多酚，具有有益的健康特性，被誉为潜在的抗肿瘤药物。在这里，我们证明了由白藜芦醇合成的碳点（C-dots）具有强大的抗癌作用。温和的合成条件保留了碳点（C-dots）表面的白藜芦醇功能部分，这是实现对癌细胞特异性和生物活性的重要要求。事实上，与正常细胞相比，白藜芦醇-C-dot 的破坏作用在几种癌细胞类型中更为明显，这突出了 C-dots 的靶向能力，这是癌症治疗发展的一个重要问题。特别是，我们观察到线粒体功能的损伤，包括细胞内钙释放、细胞色素-C 氧化酶活性的抑制和线粒体膜扰动。此外，与单独的白藜芦醇分子、已知的抗癌多酚类药物如姜黄素和三苯基膦，或由不同碳质前体制备的 C-dots 相比，白藜芦醇合成的 C-dots 更有效。这项研究表明，白藜芦醇合成的 C-dots 可能具有作为抗癌药物的潜在治疗潜力。
