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原蛋白调节癌症多药耐药蛋白在非小肺癌细胞系中的表达模式

Khurshid Ahmad Padder¹

¹Department of Endocrinology, Sher-i-Kashmir Institute of Medical Sciences, Soura, J&K, India.

Journal of biochemical and molecular toxicology

|July 14, 2025

概括

原蛋白通过抑制P-glycoprotein (P-gp) 来提高化疗的有效性,P-gp是多药性耐药性 (MDR) 的关键因素. 这种天然化合物通过减少药物流量和降低MDR1基因表达,使癌细胞对像帕克利塔克塞尔 (PTX) 这样的药物敏感.

科学领域:

生物化学生物化学
分子生物学分子生物学
药理学药理学是指药理学的学科.

背景情况:

多种药物耐药性 (MDR) 显著限制了癌症化疗的疗效.
像P-糖蛋白 (P-gp) 这样的ATP结合盒 (ABC) 载体,介导药物排放,导致MDR.
通过抑制ABC载体来逆转MDR对于改善癌症治疗结果至关重要.

研究的目的:

研究阿皮基宁在克服P-gp/ABCB1.1.介导的MDR方面的潜力.
评估阿皮基宁对帕克利塔塞尔 (PTX) 在NCI-H460肺癌细胞中的疗效.
阐明原蛋白对P-gp/ABCB1.1的作用背后的分子机制.

主要方法:

分子对接模拟以评估阿皮金因与P-gp/ABCB1.1的结合亲和力.
使用NCI-H460细胞进行体外研究,以评估apigenin对PTX抗增殖作用的影响.
罗达胺-123 (Rh-123) 药物流量测试测量P-gp运输功能.
定量实时PCR用于分析ABCB1/MDR1mRNA表达水平.

主要成果:

分子对接揭示了阿皮基宁与P-gp/ABCB1.1的跨膜域的强烈结合亲和力.
原蛋白预处理显著增强了PTX在NCI-H460细胞中的抗增殖活性.
原蛋白显著抑制了Rh-123流量,并显著降低了ABCB1/MDR1mRNA表达,表明P-gp抑制.
原蛋白治疗降低了ABCB1/MDR1的表达,进一步支持其在克服MDR中的作用.

结论:

原蛋白显示出作为MDR调节器的显著潜力,增强了NCI-H460细胞中的PTX疗效.
原蛋白的机制包括直接抑制P-gp运输功能和降低ABCB1/MDR1表达的调节.
这些发现表明,阿皮基宁可能是一个有价值的辅助疗法,以改善癌症化疗结果.

关键词:

它们的基因是apigenin.肺癌是一种肺癌.多药性耐药性 (MDR) 是一种多药性耐药性.帕克利塔克塞尔 (paclitaxel) 是一种药物.罗达胺-123 胺-123 胺

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