Potential boron delivery agents for Boron Neutron Capture Therapy application: Sodium borocaptate(BSH) conjugated folic acid/biotin via thiol-maleimide "click" reaction

• Main Authors: MINH-TRUNG NGUYEN, 阮明忠
• Other Authors: 謝忠宏
• Format: Others
• Language: en_US
• Published: 2018
• Online Access: http://ndltd.ncl.edu.tw/handle/8c48nx

碩士 === 淡江大學 === 化學學系碩士班 === 106 === Boron neutron capture therapy (BNCT) is a potential approach to treat cancer and Sodium borocaptate (BSH) has been used for BNCT application as a boron delivery agent. Even though, BSH were used in clinical trials, this agent till exhibits some disadvantage in the case of selective targeting of cancer cells and cellular uptake ability. Folic acid and biotin were considered as an excellent targeting ligand which can help to overcome the disadvantage of BSH in BNCT application. In this study, we prepared the natural sodium borocaptate (BSH) from natural abounded starting materials and we also successfully conjugated this potential BNCT agent with folic acid/biotin using 1-(2-Aminoethyl)maleimide as the short crosslinker. Folic acid/biotin-conjugated BSH exhibited the potential boron delivery agent which decreased the cytotoxicity of BSH treatment effects on U2OS cell line. Interestingly, folate-conjugated products which showed two maleimide groups and it also exhibited the high fluorescence emission. Of these, this complex might provide a new strategy to enhance and also detect the boron accumulation. These observations offered two of new BSH delivery platforms which were described as a small molecule weight and highly targeting of cancer cells which could be used as starting material in further investigation.