奎尔素作为一种苦味受体激动剂,在头癌细胞中具有抗癌作用
bioRxiv : the preprint server for biology
|September 26, 2025
概括
Quercetin 是一种在植物中发现的化合物,激活了头部和部状细胞癌 (HNSCC) 细胞中的苦味受体 (T2Rs). 这种激活降低了癌细胞的活力,并触发了线粒体脱极化,这表明奎尔在HNSCC中具有潜在的抗癌作用.
科学领域:
- 在瘤学瘤学.
- 细胞生物学 细胞生物学
- 药理学 药理学是指药理学的学科.
背景情况:
- 在临床前的头角状细胞癌 (HNSCC) 模型中,奎尔西显示出抗癌性质.
- 苦味受体 (T2Rs) 在HNSCC细胞中表达,它们被切丁等苦味化合物激活可以诱导亡.
- 在HNSCC中增加T2R表达与改善患者存活率相关.
研究的目的:
- 研究奎尔素作为HNSCC细胞中的抗癌T2R激动剂的作用.
- 评估素对 (Ca2+) 信号传递,细胞活力和线粒体功能在HNSCC中的影响.
主要方法:
- 成像用于评估HNSCC细胞系中素介导的Ca2+反应,有或没有T2R14对手LF1和G蛋白抑制剂YM-254980 (YM).
- 在细胞系和患者衍生瘤切片中使用水晶紫色和MTS测定来评估细胞活力.
- 用TMRE测量了线粒体去极化在T2R途径抑制剂的存在和缺乏的情况下.
主要成果:
- 奎尔赛丁在HNSCC细胞中诱导了显著的Ca2+反应,该反应被LF1和YM减弱.
- 奎尔赛丁在体外减少了细胞活力,并在瘤切片中显示出活力下降的趋势.
- 奎尔丁治疗导致线粒体去极化,这种效应由LF1减少,但不是YM.
结论:
- 奎尔在HNSCC细胞中引起Ca2+反应,可能由T2R14介导.
- 奎尔丁降低了HNSCC细胞活力,并诱导了线粒体去极化.
- 这些发现支持奎尔塞丁作为向HNSCC中的T2Rs的抗癌剂的潜力.
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