Chen Yingyu, Li Cailong, Zheng Yunquan, Gao Yu, Hu Jianda, Chen Haijun
College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China; Fujian Institute of Hematology, Fujian Provincial Key Laboratory of Hematology, Fujian Medical University Union Hospital, Fuzhou, Fujian 350001, China.
College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, China.
Bioorg Med Chem Lett. 2017 Feb 15;27(4):1007-1011. doi: 10.1016/j.bmcl.2016.12.071. Epub 2016 Dec 30.
Recently various drug candidates with excellent anticancer potency have been demonstrated, whereas their clinical application largely suffers from several limitations especially poor solubility. Ursolic acid (UA) as one of ubiquitous pentacyclic triterpenes in plantkingdom exhibited versatile antiproliferative effects in various cancer cell lines. However, the unfavorable pharmaceutical properties became the main obstacle for its clinical development. With the aim of development of novel derivatives with enhanced potency, a series of diversified UA amphiphiles have been designed, synthesized, and pharmacologically evaluated. Amphiphile 10 (FZU-03,010) with significant improved antiproliferative effect can self-assemble into stable nanoparticles in water, which may serve as a promising candidate for further development.
最近，已经证明了各种具有优异抗癌效力的候选药物，然而它们的临床应用在很大程度上受到几个限制，特别是溶解度差。熊果酸（UA）作为植物界中普遍存在的五环三萜之一，在各种癌细胞系中表现出多种抗增殖作用。然而，不利的药物性质成为其临床开发的主要障碍。为了开发具有增强效力的新型衍生物，设计、合成并对一系列多样化的UA两亲物进行了药理学评估。具有显著改善的抗增殖作用的两亲物10（FZU-03010）可以在水中自组装成稳定的纳米颗粒，这可能是进一步开发的有希望的候选物。
