Yuan Weihui, Guo Junhui, Wang Xude, Su Guangyue, Zhao Yuqing
School of Functional Food and Wine, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
School of Functional Food and Wine, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
Steroids. 2018 Jan;129:1-8. doi: 10.1016/j.steroids.2017.11.003. Epub 2017 Nov 10.
As active components of ginseng, 25-methoxylprotopanaxadiol and 25-hydroxyprotopanaxadiol exhibited an ability to inhibit the growth and proliferation or to induce the differentiation and apoptosis of tumour cells. We modified 25-OCH-PPD and 25-OH-PPD with non-protein amino acids and a series of derivatives was obtained by chromatographic separation, purification and spectroscopy analysis. Thirteen derivatives of 25-OCH-PPD (compounds 1-13) and 12 derivatives of 25-OH-PPD (compounds 14-25) were synthesised. The anti-cancer activities of the derivatives were evaluated on HCT-116 and BGC-823 cell lines by MTT assay. Compound 9 and compound 14 exhibited considerable anti-tumour activity for HCT-116 and BGC-823 cell lines, exhibited higher cytotoxic activity than 25-OCH-PPD and 25-OH-PPD. Therefore, these ginsenoside derivatives could be used as potential lead for the development of a new type of anticancer agent.
作为人参的活性成分，25-甲氧基原人参二醇和25-羟基原人参二醇具有抑制肿瘤细胞生长和增殖或诱导其分化及凋亡的能力。我们用非蛋白质氨基酸对25-OCH-PPD和25-OH-PPD进行修饰，并通过色谱分离、纯化及光谱分析得到了一系列衍生物。合成了13种25-OCH-PPD的衍生物（化合物1 - 13）和12种25-OH-PPD的衍生物（化合物14 - 25）。采用MTT法在HCT-116和BGC-823细胞系上评估这些衍生物的抗癌活性。化合物9和化合物14对HCT-116和BGC-823细胞系表现出显著的抗肿瘤活性，其细胞毒性活性高于25-OCH-PPD和25-OH-PPD。因此，这些人参皂苷衍生物可作为开发新型抗癌药物的潜在先导化合物。
