College of Pharmacy, Dali University, Dali 671000, PR China.
Shanghai Research Center for Modernization of Traditional Chinese Medicine, National Engineering Laboratory for TCM Standardization Technology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China; University of Chinese Academy of Sciences, Beijing 100049, PR China.
Steroids. 2020 Jul;159:108650. doi: 10.1016/j.steroids.2020.108650. Epub 2020 Apr 28.
A series of oleandrin-4'-yl ester derivatives were designed, synthesized, and evaluated for their proliferation inhibition activities against tumor cell lines. Cytotoxicity data revealed that the C4' moiety had an important influence on cytotoxic activity. Several compounds that we designed and synthesized exhibit significant in vitro antiproliferative activity against the tested tumor cell lines. Among the derivatives of OL, 4b-HCl not only had good anti-tumor activity but also had good water solubility. Furthermore, 4b-HCl can significantly inhibit tumor growth by 96.4% at a dose of 6 mg/kg/d by ip.
我们设计、合成了一系列毛地黄糖苷-4'-基酯衍生物，并评估了它们对肿瘤细胞系的增殖抑制活性。细胞毒性数据表明 C4' 部分对细胞毒性活性有重要影响。我们设计和合成的几种化合物对测试的肿瘤细胞系表现出显著的体外抗增殖活性。在 OL 的衍生物中，4b-HCl 不仅具有良好的抗肿瘤活性，而且具有良好的水溶性。此外，4b-HCl 在 6mg/kg/d 的剂量下通过腹腔注射可显著抑制肿瘤生长，抑制率达 96.4%。
