来自Psoralea corylifolia的Psoralen和Isopsoralen通过双重机制抑制NSCLC:STAT3抑制和ROS调节
Liwei Bi1,2,3, Guangyi Chen1, Wanfen Liu1
1Department of Pharmacy, Xiamen Medical College, Xiamen 361023, China.
Pharmaceuticals (Basel, Switzerland)
|February 27, 2026
概括
这项研究确定了传统中医药中的psoralen和isopsoralen是新型信号传感器抑制剂和转录3 (STAT3) 激活剂,用于治疗非小细胞肺癌 (NSCLC). 这些化合物通过抑制STAT3和调节活性氧物种 (ROS) 来对抗NSCLC.
科学领域:
- 生物化学和分子生物学
- 药理学和毒理学 药理学和毒理学
- 自然产品化学 自然产品化学
背景情况:
- 非小细胞肺癌 (NSCLC) 的进展与激活的信号传感器和转录3激活器 (STAT3) 有关.
- 传统中国医学为新型抗癌化合物提供了潜在的来源.
- 了解STAT3在NSCLC中的作用,需要确定目标天然产品.
研究的目的:
- 开发使用表面等离子体共振 (SPR) 的STAT3定位识别系统.
- 为了识别Psoralea corylifolia中的天然STAT3抑制剂.
- 评估已识别的化合物的抗NSCLC活动和活性氧物种 (ROS) 调节效应.
主要方法:
- 使用SPR生物传感器对STAT3结合化合物的选和亲和度确定.
- 采用分子对接来分析STAT3和SH2域相互作用.
- 在A549细胞中评估了抗增殖和抗迁移作用;在HUVEC和A549细胞中评估了抗氧化能力和细胞内ROS水平.
主要成果:
- 索拉和异索拉被确定为具有特定亲和力的STAT3结合剂.
- 这两种化合物都抑制了NSCLC细胞的增殖和迁移.
- 松烯和异松烯在正常细胞和癌细胞中表现出不同的抗氧化活性和调节的ROS水平.
结论:
- 松素和异素是具有抗NSCLC潜力的新型双功能STAT3抑制剂.
- 它们的有效性源于联合的STAT3抑制和上下文依赖的ROS调制.
- SPR技术有效地选针对特定蛋白质的生物活性天然产品,如STAT3.
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