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卡卡丁衍生物的制备及其抗瘤活性

Yu-Ying Jiang^1,2, Hui-Hua Dong^1,2, Wen-Ting Zhou^1,2

¹Guangxi Technology Innovation Cooperation Base of Prevention and Control Pathogenic Microbes with Drug Resistance, Youjiang Medical University for Nationalities, Baise 533000, Guangxi Zhuang Autonomous Region, China.

World journal of clinical oncology

|August 28, 2024

概括

一种新型的kakkatin衍生品,HK,通过抑制细胞增殖,入侵和转移,对肝细胞癌 (HCC) 具有强大的抗瘤活性. 这种衍生物可以作为治疗HCC的有希望的主要药物,向PDE3B和NFKB1蛋白质.

科学领域:

药理学药理学是指药理学的学科.
药用化学医学化学
在瘤学瘤学.

背景情况:

普埃拉里亚 (PF) 衍生化合物具有显著的抗瘤,抗炎症和肝脏保护性质.
卡卡丁是PF的异黄,具有潜在的抗瘤作用,需要进一步研究.
卡卡丁的衍生物可能提供增强的抗癌疗效.

研究的目的:

为了合成一种新的卡卡丁衍生物,HK (6-(hept-6-yn-1-yloxy) -3-(4-hydroxyphenyl) -7-methoxy-4H-chromen-4-one).
评估HK对肝细胞癌 (HCC) 的抗瘤生物活性.

主要方法:

通过对kakkatin进行修改,合成HK.
在体外测试包括MTT,克隆形成,细胞亡/亡,细胞循环分析,痕和Transwell测试.
网络药理学,分子对接和实时PCR用于机制阐明.

主要成果:

与卡卡丁 (IC50 = 2.5μM) 相比,HK显示了对HCC SMMC-7721细胞的抑制活性增加了30倍.
HK显著抑制了HCC细胞的增殖,入侵和转移,表现优于西斯.
在HCC细胞中,HK诱导的亡和G2/M细胞周期停止.

结论:

香港表现出显著的抗HCC活动.
HK的抗瘤机制涉及cAMP通路,可能向PDE3B和NFKB1蛋白质.
香港代表了一种有前途的化合物,用于开发新的HCC治疗方法.

关键词:

这是一种抗瘤药物.生物活动是生物活动.衍生品是一种衍生品.肝细胞癌是肝细胞癌.在Kakkatin的Kakkatin里

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