Trifolirhizin 以 PTK6 为靶点诱导自噬,对鼻咽癌有抗肿瘤作用。

IF 3.5 4区 医学 Q2 CHEMISTRY, MEDICINAL Drug Development Research Pub Date : 2024-10-11 DOI:10.1002/ddr.70000
Yong Wang, Yang Fang
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引用次数: 0

摘要

三叶一枝花苷是一种天然黄酮苷,已被证实对多种人类恶性肿瘤具有抗肿瘤活性。根据公共数据库 SuperPred (https://prediction.charite.de/),PTK6 被确定为 trifolirhizin 的直接靶点。PTK6在多种肿瘤中的过表达与肿瘤的恶性发展密切相关。因此,本研究旨在阐述三唑醇对鼻咽癌细胞生物学行为的影响,并探究其内在机制。本研究首先从靶向抑制PTK6的角度阐明了三唑醇在鼻咽癌恶性进展中的抑瘤功能。本研究采用CCK-8检测细胞活力、EdU染色检测细胞增殖、末端脱氧核苷酸转移酶DUTP缺口标记(TUNEL)染色检测细胞凋亡以及免疫荧光染色检测LC3表达。此外,还通过 Western 印迹分析检测了增殖相关蛋白、凋亡相关蛋白和自噬相关蛋白的水平。此外,研究人员还对三叶蓟素与 PTK6 进行了分子对接,以寻找化合物与蛋白质的结合潜力。结果表明,三叶蓟素能抑制鼻咽癌细胞的增殖,促进其凋亡,并能增强鼻咽癌细胞的自噬作用。此外,研究还验证了三叶桐素以PTK6为靶点,负调控PTK6的表达。PTK6 上调后,三唑醇对鼻咽癌细胞恶性行为的抑制作用以及三唑醇对鼻咽癌细胞自噬的增强作用部分消失。总之,研究结果表明,三唑醇可下调PTK6的表达,从而诱导自噬,发挥其在鼻咽癌中的抗肿瘤活性。
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Trifolirhizin targets PTK6 to induce autophagy and exerts antitumor effects in nasopharyngeal carcinoma

Trifolirhizin, a natural flavonoid glycoside, has been proved to exert antitumor activities in various human malignant tumors. PTK6 was identified as a direct target of trifolirhizin based on public database SuperPred (https://prediction.charite.de/). Overexpressed PTK6 in a variety of tumors is closely associated with the malignant development of tumors. Herein, this present research was formulated to elaborate the effects of trifolirhizin on the biological behaviors of nasopharyngeal carcinoma (NPC) cells and to probe into the intrinsic mechanisms. The current study firstly elucidated the tumor-inhibiting functions of trifolirhizin in NPC malignant progression from the perspective of targeting inhibition of PTK6. In this work, CCK-8 for cell viability, EdU staining for cell proliferation, terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) staining for cell apoptosis and immunofluorescence staining for LC3 expression were performed. Besides, levels of proliferation-related, apoptosis-related and autophagy-related proteins were detected by western blot analysis. Moreover, molecular docking of trifolirhizin with PTK6 was conducted to seek the compound-protein binding potential. It was demonstrated that trifolirhizin treatment inhibited the proliferation and promoted the apoptosis of NPC cells as well as strengthened autophagy in NPC cells. Furthermore, it was verified that trifolirhizin targeted PTK6 and negatively regulated PTK6 expression. The suppressive effects of trifolirhizin on the malignant behaviors of NPC cells and the enhancing effect of trifolirhizin on autophagy in NPC cells were partly abolished upon upregulation of PTK6. To conclude, findings suggested that trifolirhizin may downregulate PTK6 expression to induce autophagy and exert the antitumor activities in NPC.

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来源期刊
CiteScore
6.40
自引率
2.60%
发文量
104
审稿时长
6-12 weeks
期刊介绍: Drug Development Research focuses on research topics related to the discovery and development of new therapeutic entities. The journal publishes original research articles on medicinal chemistry, pharmacology, biotechnology and biopharmaceuticals, toxicology, and drug delivery, formulation, and pharmacokinetics. The journal welcomes manuscripts on new compounds and technologies in all areas focused on human therapeutics, as well as global management, health care policy, and regulatory issues involving the drug discovery and development process. In addition to full-length articles, Drug Development Research publishes Brief Reports on important and timely new research findings, as well as in-depth review articles. The journal also features periodic special thematic issues devoted to specific compound classes, new technologies, and broad aspects of drug discovery and development.
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