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Synthesis and evaluation of new sterol derivatives as potential antitumor agents

机译：新甾醇衍生物作为潜在抗肿瘤剂的合成与评价

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摘要

The current optimization of tetrazanbigen (TNBG) on the C-ring provided a series of new sterol derivatives 2a-2n. All new synthesized compounds were screened for their anti-proliferation activities against five human cancer cell lines (HepG2, QGY-7701, SMMC-7721, A-431 and NCI-H23 cell lines) in vitro. Among them, 2a, 2b, 2c, 2m and 2n exhibited high anti-proliferation activities on SMMC-7721, and their IC50 values approach that of the positive control drug cisplatin. Compound 2a not only showed strong anti-proliferation activities against QGY-7701 and HepG2 cell lines, with IC50 values (IC50: 6.81 +/- 0.24 mu M, 7.69 +/- 0.87 mu M) better than that of cisplatin (IC50: 8.75 mu M, 18.89 +/- 2.01 mu M), but also exhibited good aqueous solubility (0.15-15 mg mL(-1) at pH 7.4 and 2.0). On the most sensitive QGY-7701 cell line, Oil red O staining and western blot analysis were performed. The results suggested that 2a can inhibit the growth of cancer cells possibly by interfering with the lipid metabolism balance of tumor cells, resulting in lipid accumulation and cell apoptosis (lipotoxicity). Moreover, after being treated with 2a, lipid accumulation of QGY-7701 cell was increased in a time and dose dependent manner. Based on these promising results, 2a was selected for drug formulation and further pre-clinical development.
机译：C形环上的Tetrazanbigen（TNBG）的目前优化提供了一系列新的甾醇衍生物2a-2n。将所有新的合成化合物筛选其对五种人癌细胞系（HepG2，QGy-7701，SMMC-7721，A-431和NCI-H23细胞系）的抗增殖活动。其中，2A，2B，2C，2M和2N在SMMC-7721上表现出高抗增殖活性，并且它们的IC 50值接近阳性对照药物顺铂。化合物2A不仅显示出对QGY-7701和HepG2细胞系的强抗增殖活动，具有IC50值（IC50：6.81 +/- 0.24 mu m，7.69 +/- 0.87 mu m），比顺铂更好（IC50：8.75 MU M，18.89 +/- 2.01 mu m），但也表现出良好的水溶性（0.15-15mg ml（-1）pH 7.4和2.0）。在最敏感的QGY-7701细胞系上，进行油红O染色和蛋白质印迹分析。结果表明，通过干扰肿瘤细胞的脂质代谢平衡，2a可以抑制癌细胞的生长，导致脂质积累和细胞凋亡（脂毒性）。此外，在用2A处理后，QGY-7701细胞的脂质积累在时间和剂量依赖性的方式增加。基于这些有前途的结果，选择了2A的药物制剂和进一步的临床开发。

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  • 来源
    《RSC Advances》 |2018年第47期|共10页
  • 作者

    Chen Xiang; Gan Yong Jun; Yu Yu; Zhang Yuan;

  • 作者单位

    Chongqing Med Univ Res Lab Pharmaceut Chem Sch Pharm Chongqing 400016 Peoples R China;

    Chongqing Med Univ Expt Teaching Ctr Chongqing 401331 Peoples R China;

    Chongqing Med Univ Res Lab Pharmaceut Chem Sch Pharm Chongqing 400016 Peoples R China;

    Chongqing Med Univ Dept Pharm Affiliated Hosp 1 Chongqing 40016 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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