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    Please use this identifier to cite or link to this item: https://ir.cnu.edu.tw/handle/310902800/23440


    標題: 設計合成B-葡萄糖醛酸酶活化標定之分子探針
    Design and synthesis of activity-based trapping for β-glucuronidase
    作者: 黃義賢
    貢獻者: 呂玉玲
    嘉南藥理科技大學:藥物科技研究所
    關鍵字: B-葡萄糖醛酸酶
    β-glucuronidase
    gene delivery
    日期: 2010
    上傳時間: 2010-12-30 15:34:15 (UTC+8)
    摘要: 在臨床癌症治療過程中,B-glucuronidase (BG) 應用於報告基因和專一性水解前驅藥物上,具有可行性潛在的吸引力,且在影像顯影上,有利於監測報告基因的表現和前驅藥物治療。在本篇研究中,我們發展出一124I tyramine-difluoromethylphenol glucuronide 分子影像探針 (124I-TrapG) ,它能專一性的被β-葡萄糖酸苷酶所活化,而釋出含 fluorodiene 基團具有親電能力的124I-Trap,能夠與BG表現的癌細胞親核 (nucleophile) 部位形成共價鍵結,以微正電子發射型斷層 (PET) 照影,體內外試驗的結果顯示,124I-Trap的影像訊號表現量確實的累積在有表現β-葡萄糖酸苷酶的CT26腫瘤上,而不表現BG的CT26腫瘤則沒有訊號,如此證實124I-TrapG可以於體內外呈現BG分佈位置及表現量。
    綜和以上的結果我們可以知道,利用此分子影像探針及微正電子發射型斷層儀,可以偵測活體內腫瘤表現β-葡萄糖酸苷酶的量,未來也可應用於臨床上,來偵測β-葡萄糖酸苷酶表現量來追蹤腫瘤惡化過程,或者評估抗癌治療的成效。
    B-glucuronidase (BG) is both an attractive reporter gene and a promising prodrug-converting enzyme for cancer therapy.。Imaging of BG activity in living animals would be a convenient method to monitor reporter gene expression and BG prodrug treatments. In this report, we developed a 124I tyramine-difluoromethylphenol glucuronide probe (124I-TrapG) that could be converted by BG to release a trapping 124I-difluoromethylphenol moiety to crosslink any nucleophile moiety on cells. Enhanced signals were shown in CT26/mBG-eB7 tumors in our micro-PET imaging studies, however CT26 tumors are not, indicate 124I-Trap could present the distribution and expression of BG in vitro and in vivo. According to the result, we could use molecular imaging probes and micro-PET to detect the expression of BG in tumor cells. Also application in clinic, we could trace the tumor progression, or estimate the result of anticancer therapy in future.
    關聯: 校內校外均不公開,學年度:98,60頁
    Appears in Collections:[藥學系(所)] 博碩士論文

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