具有增强水溶性和细胞内化作用的N-乙酰葡糖胺共轭阿托伐他汀。
GlcNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization.
作者信息
Zhang Xinfu, Chen Xiaofang, Zhao Weiyu, Zeng Chunxi, Luo Xiao, Li Wenqing, Li Bin, Jiang Justin, Dong Yizhou
机构信息
Division of Pharmaceutics & Pharmaceutical Chemistry, College of Pharmacy, ‡Department of Biomedical Engineering, §The Center for Clinical and Translational Science, ∥The Comprehensive Cancer Center, ⊥Dorothy M. Davis Heart & Lung Research Institute, and ¶Department of Radiation Oncology, The Ohio State University , Columbus, Ohio 43210, United States.
出版信息
Bioconjug Chem. 2017 Aug 16;28(8):2109-2113. doi: 10.1021/acs.bioconjchem.7b00295. Epub 2017 Aug 7.
Targeting ligands facilitate cell specific drug delivery and improve pharmaceutical properties. Herein, we designed two ligand drug conjugates by conjugating GlcNAc (N-acetylglucosamine) with atorvastatin. These two conjugates, termed G-AT and G-K-AT, exhibited enhanced water solubility and cellular uptake. Moreover, both G-AT and G-K-AT were able to release atorvastatin and consequently achieve significant inhibition against 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase.
靶向配体有助于细胞特异性药物递送并改善药物性质。在此，我们通过将N-乙酰葡糖胺（GlcNAc）与阿托伐他汀偶联设计了两种配体-药物偶联物。这两种偶联物，称为G-AT和G-K-AT，表现出增强的水溶性和细胞摄取。此外，G-AT和G-K-AT均能够释放阿托伐他汀，从而对3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶产生显著抑制作用。
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