Tan Cheng-jian, Zhao Yu, Goto Masuo, Hsieh Kan-Yen, Yang Xiao-ming, Morris-Natschke Susan L, Liu Li-na, Zhao Bao-yu, Lee Kuo-Hsiung
Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, United States; College of Chemistry and Environment, Guizhou Minzu University, Guiyang 550025, People's Republic of China.
Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, United States.
Bioorg Med Chem Lett. 2016 Mar 1;26(5):1495-7. doi: 10.1016/j.bmcl.2015.09.010. Epub 2015 Sep 5.
Ten alkaloids (1-10), with sophoridine (1) as the most abundant component, were obtained from the whole plants of Oxytropis ochrocephala Bunge. Furthermore, eight new sophoridine derivatives (11-16, 20, 21), with modification on the C-14 position of 1 were synthesized. All compounds (1-16, 20, 21) were evaluated for antiproliferative activity against five human tumor cell lines. Among them, the newly synthesized derivative 20 exhibited the best inhibitory activity against the tested cell lines. Its activity was increased by more than fourfold as compared with parent compound 1.
从黄花棘豆全草中获得了10种生物碱(1-10),其中槐定碱(1)含量最高。此外,还合成了8种对1的C-14位进行修饰的新槐定碱衍生物(11-16、20、21)。对所有化合物(1-16、20、21)针对5种人类肿瘤细胞系的抗增殖活性进行了评估。其中,新合成的衍生物20对测试的细胞系表现出最佳抑制活性。与母体化合物1相比,其活性提高了四倍多。