Chlorambucil gemcitabine conjugate nanomedicine for cancer therapy
Chlorambucil gemcitabine conjugate nanomedicine for cancer therapy
复制标题
用于癌症治疗的苯丁酸氮芥吉西他滨缀合物纳米药物。
DOI：
10.1016/j.ejps.2015.08.013
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发表时间：
2015-11-15
影响因子：
4.6
通讯作者：
Shi, Bizhi
中科院分区：
文献类型：
--
作者：
Fan, Mingliang;Liang, Xiaofei;Shi, Bizhi
抗癌小分子自组装成纳米结构可能是改善实验性实体肿瘤治疗的一种有吸引力的方法。为了验证这一概念，我们设计并合成了亲水性吉西他滨的共轭前药，通过一个可水解的酯键与疏水性氯氨苄共价偶联。所得到的两亲性偶联物在水中自组装成纳米颗粒，并在体外对多种人类癌细胞表现出显著的抗癌活性。在皮下移植的SMMC-7721肝癌模型上测试了这些纳米颗粒的体内抗癌活性。这种氯布西滨-吉西他滨结合纳米药物在癌症治疗中具有潜在的应用前景。(C) 2015 Elsevier B.V.版权所有
Self-assembly of anticancer small molecules into nanostructures may represent an attractive approach to improve the treatment of experimental solid tumors. As a proof of concept, we designed and synthesized the conjugate prodrug of hydrophilic gemcitabine by its covalent coupling to hydrophobic chlorambucil via a hydrolyzable ester linkage. The resulting amphiphilic conjugates self-assembled into nanoparticles in water and exhibited significant anticancer activity in vitro against a variety of human cancer cells. In vivo anticancer activity of these nanoparticles has been tested on subcutaneous grafted SMMC-7721 hepatocellular carcinoma model. Such chlorambucil gemcitabine conjugate nanomedicine should have potential applications in cancer therapy. (C) 2015 Elsevier B.V. All rights reserved.