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具有细胞毒性活动的类化合物来自Zanthoxylum nitidum

Wei Wei¹, Jing-Hui Yin¹, Bang-Yong Wang¹

¹Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Guilin Medical University, Guilin 541199, PR China.

|October 1, 2025

概括

两种新的类化合物和Zanthoxylum nitidum中已知的化合物显示出强大的抗癌活性. 几种分离物有效抑制了HepG2和SW480癌细胞的增殖,超过了多克索鲁比的疗效.

科学领域:

自然产品化学自然产品化学
药用化学医学化学
药理学药理学是指药理学的学科.

背景情况:

桑托西酸是生物活性化物的一种植物来源.
类化合物具有多种药理性质,包括潜在的抗癌作用.
识别具有卓越疗效的新型化合物对于药物发现至关重要.

研究的目的:

从Zanthoxylum nitidum中分离和描述新的和已知的化物.
为了评估这些化合物对人类癌症细胞系的细胞毒性活性.
为了识别来自自然来源的潜在抗癌药物线索.

主要方法:

使用色谱技术分离类化合物.
通过全面的光谱分析 (NMR,HRESIMS,X射线晶体学,ECD,DP4+) 来阐明结构.
在体外细胞毒性测定对HepG2和SW480细胞,用多克索鲁比作为参考.

主要成果:

分离了两种新型化物 (8-O-demethylmaclekarpine D和zanthonitine) 和一对旋转分子.
确定了35种已知的类化合物,包括类类,类和类.
化合物6,7,18,33显示出对HepG2细胞的强烈抑制 (IC50 7.29-22.90μM),表现优于多克索鲁比辛.
化合物9,16,21显示显著抑制SW480细胞 (IC5021.77-25.13μM),超过了多克索鲁的疗效.

结论:

桑托西酸是结构多样化的类化合物的丰富来源,具有显著的抗癌潜力.
与多克索鲁比相比,一些孤立的类化合物对HepG2和SW480细胞具有更高的细胞毒性.
这些发现突显了Zanthoxylum化物衍生的类化合物在癌症治疗中的治疗前景.

关键词:

类化合物是一种类化合物.细胞毒性细胞毒性黄叶植物 (Rutaceae) 是一个植物.桑托西酸盐化物.

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