Synthesis of taurine-fluorescein conjugate and evaluation of its retina-targeted efficiency in vitro

查看全文 作　　者：Meihong [1,2]Huang;Jiaqi [1]Song;Bingzheng [3]Lu;Huizhi [1]Huang;Yizhen [1]Chen;Wei [3]Yin;Wenbo [3]Zhu;Xinwen [3]Su;Chuanbin [1]Wu;Haiyan [1]Hu

机构地区：[1]Laboratory of Pharmaceutics,School of Pharmaceutical Sciences,Sun Yat-sen University,Guangzhou 510006,China;[2]Pharmacy Department of Guangxi Minzu Hospital,Nanning 530001,China;[3]Department of Pharmacology,Zhongshan School of Medicine,Sun Yat-sen University,Guangzhou 510080,China

出　　处：《Acta Pharmaceutica Sinica B》索引2014年第4卷第6期,共7页

摘　　要：In this work, retinal penetration of fluorescein was achieved in vitro by covalent attachment of taurine to fluorescein, yielding the F-Tau conjugate. Nuclear magnetic resonance (NMR) and high resolution mass spectrometry (HRMS) were used to confirm the successful synthesis of F-Tau. The cellular uptake of F-Tau in adult retinal pigment epithelial cells (ARPE-19) and human retinal microvascular endothelial cells (hRMECs) was visualized via confocal scanning microscopy. The results indicated an improvement of solubility and a reduction of logP of F-Tau compared with fluorescein. As compared with fluorescein, F-Tau showed little toxicity, and was retained longer by cells in uptake experiments. F-Tau also displayed higher transepithelial permeabilities than fluorescein in ARPE-19 and hRMECs monolayer cells (Po0.05). These results showed that taurine may be a useful ligand for targeting small-molecule hydrophobic pharmaceuticals into the retina. 关键词：TAURINE Taurine-fluorescein con-jugate Retina-targeting ARPE-19 hRMECs Transepithelial permeability

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Synthesis of taurine-fluorescein conjugate and evaluation of its retina-targeted efficiency in vitro

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