Background: Linalool is a monoterpene compound with various potential therapeutic applications in several medical fields. Previous studies have indicated the activity of linalool against cell lines; however, its high level of toxicity restricts its use. The aim of this study was to design and manufacture compounds with a novel structure that can be used for loading linalool, to reduce its toxicity and improve its reachable ability.
Methods: We synthesized and characterized a new molecule for loading linalool onto gold nanoparticles (GNPs) capped with glutathione and conjugated with a CALNN peptide. Linalool was loaded onto the GNPs via the reaction of the surface groups of both linalool and the GNPs. Moreover, the target peptide could be loaded onto the surface of the GNPs via a chemical reaction. The cytotoxic effects of linalool–GNP (LG) and linalool–GNP–CALNN peptide (LGC) conjugates against ovarian cancer cells were investigated, as were the possible mechanisms underlying the induction of apoptosis.
Results: Our findings illustrated the significant antiproliferative effect of LG and LGC on SKOV-3 cells. The cytotoxicity assay demonstrated that LG and LGC were selectively toxic in cancer cells and induced apoptosis by activating caspase-8, the p53 protein, and various proteins involved in apoptosis. The present data demonstrated that LG and LGC have a high therapeutic potential and should be given particular consideration as anticancer drug-delivery systems, as LG and LGC were remarkably more cytotoxic against a cancer cell line than were linalool and GNPs alone.
Conclusion: We concluded that LG and LGC are promising compounds that can be used for treating ovarian cancer (SKOV-3) cells via the induction of apoptosis through extrinsic and intrinsic pathways.



中文翻译：

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负载芳樟醇的谷胱甘肽修饰的金纳米粒子与 CALNN 肽偶联作为 SKOV-3 细胞系中的凋亡诱导剂和 NF-κB 易位抑制剂

背景：芳樟醇是一种单萜化合物，在多个医学领域具有多种潜在的治疗应用。以前的研究表明芳樟醇对细胞系的活性；然而，它的高毒性限制了它的使用。本研究的目的是设计和制造具有新型结构的化合物，可用于负载芳樟醇，以降低其毒性并提高其可达性。
方法：我们合成并表征了一种用于将芳樟醇加载到金纳米粒子 (GNP) 上的新分子，该金纳米粒子 (GNP) 用谷胱甘肽封端并与 CALNN 肽缀合。通过芳樟醇和 GNP 的表面基团的反应将芳樟醇加载到 GNP 上。此外，目标肽可以通过化学反应加载到 GNP 表面。研究了芳樟醇-GNP (LG) 和芳樟醇-GNP-CALNN 肽 (LGC) 缀合物对卵巢癌细胞的细胞毒性作用，以及诱导细胞凋亡的可能机制。
结果：我们的研究结果说明了 LG 和 LGC 对 SKOV-3 细胞的显着抗增殖作用。细胞毒性试验表明，LG 和 LGC 在癌细胞中具有选择性毒性，并通过激活 caspase-8、p53 蛋白和各种参与细胞凋亡的蛋白质来诱导细胞凋亡。目前的数据表明，LG 和 LGC 具有很高的治疗潜力，应特别考虑作为抗癌药物递送系统，因为 LG 和 LGC 对癌细胞系的细胞毒性明显高于单独的芳樟醇和 GNP。
结论：我们得出结论，LG 和 LGC 是有前景的化合物，可通过外在和内在途径诱导细胞凋亡来治疗卵巢癌 (SKOV-3) 细胞。