双子型大黄素纳米粒对人结直肠癌细胞 HCT-116 的细胞毒性和凋亡作用。
Cytotoxic and apoptotic potential of gemini-chrysophanol nanoparticles against human colorectal cancer HCT-116 cell lines.
机构信息
Department of Pharmacognosy, College of Pharmacy, Hawler Medical University, Erbil, Kurdistan Region, Iraq.
出版信息
BMC Pharmacol Toxicol. 2022 Jul 23;23(1):56. doi: 10.1186/s40360-022-00597-z.
BACKGROUND
Colorectal cancer is among the most common cancers and accounts for nearly 9% of all cancers in the world. Chrysophanol is a naturally occurring anthraquinone exerts a number of pharmacological activities such as anti-inflammation, anti-cancer, anti-bacterial, anti-viral, and anti-oxidant effects. This study aims to produce a novel gemini chrysophanol nanoparticles (Gemini-Chr NPs), and to evaluate its anti-cancer effect on the human colorectal cancer cell lines.
METHODS
Gemini-Chr NPs were synthesized through nanoprecipitation method and characterized by dynamic light scattering and scanning electron microscopy, Anti-cancer activities were examined through MTT assay on HCT-116 cancer cells, apoptosis was investigated via Annexin V-FITC/PI dual stain assay. Furthermore, the expression of Bax, Bcl-2 and P53 genes were evaluated using real-time PCR and western blotting assay. RESULTS: The average particle diameter of the synthesized Gemini-Chr NPs and zeta potential were recorded as 120 nm and 14.4 mV, respectively. In comparison to the normal cells, the cytotoxicity assay confirmed that Gemini-Chr NPs preferentially killed colorectal cancer cells via induction of apoptosis. Moreover, Gemini-Chr NPs could upregulate the expression of Bax in both cancerous and normal cells (p ≤ 0.05) and decreasing the Bcl-2 expression in only tumor cells (p ≤ 0.01), while the expression of P53 is modulated in tumor cells (p ≤ 0.05).
CONCLUSIONS
Gemini surfactants could be considered for efficient delivery and improvement of anti-cancer effect of chrysophanol. Gemini-Chr NPs might have the potential for developing novel therapeutic agent against colorectal cancer.
背景
结直肠癌是最常见的癌症之一，约占全球癌症的 9%。大黄酸是一种天然存在的蒽醌，具有多种药理活性，如抗炎、抗癌、抗菌、抗病毒和抗氧化作用。本研究旨在制备新型双子大黄酸纳米粒（Gemini-Chr NPs），并评价其对人结直肠癌细胞系的抗癌作用。
方法
通过纳米沉淀法合成 Gemini-Chr NPs，并通过动态光散射和扫描电子显微镜进行表征，通过 MTT 法在 HCT-116 癌细胞上检测抗癌活性，通过 Annexin V-FITC/PI 双重染色法检测细胞凋亡。此外，采用实时 PCR 和 Western blot 法检测 Bax、Bcl-2 和 P53 基因的表达。
结果
合成的 Gemini-Chr NPs 的平均粒径和 zeta 电位分别为 120nm 和 14.4mV。与正常细胞相比，细胞毒性试验证实 Gemini-Chr NPs 通过诱导细胞凋亡优先杀死结直肠癌细胞。此外，Gemini-Chr NPs 可上调两种癌细胞和正常细胞中 Bax 的表达（p≤0.05），并降低仅在肿瘤细胞中 Bcl-2 的表达（p≤0.01），而 P53 的表达在肿瘤细胞中受到调节（p≤0.05）。
结论
双子表面活性剂可用于有效传递和提高大黄酸的抗癌作用。Gemini-Chr NPs 可能有潜力成为治疗结直肠癌的新型治疗剂。
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