کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10229180 | 509 | 2013 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
[123I]Iodooctyl fenbufen amide as a SPECT tracer for imaging tumors that over-express COX enzymes
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
مهندسی شیمی
بیو مهندسی (مهندسی زیستی)
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
This study is concerned with the development of an agent for single photon emission computer tomography (SPECT) for imaging inflammation and tumor progression. [123I]Iodooctyl fenbufen amide ([123I]IOFA) was prepared from the precursor N-octyl-4-oxo-4-(4â²-(trimethylstannyl)biphenyl-4-yl)butanamide with a radiochemical yield of 15%, specific activity of 37 GBq/μmol, and radiochemical purity of 95%. Analysis of the binding of [123I]IOFA to COX-1 and COX-2 enzymes by using HPLC and a gel filtration column showed a selectivity ratio of 1:1.3. An assay for the competitive inhibition of substrate transfer showed that IOFA exhibited a comparable IC50 value compared to fenbufen. In the normal rat liver, a lower level and homogeneous pattern of [123I]IOFA radioactivity was observed by SPECT. In contrast, in the rat liver with thioacetamide-induced cholangiocarcinoma, a higher uptake and heterogeneous pattern of [123I]IOFA radioactivity was seen as hot spots in tumor lesions by SPECT imaging. Importantly, elevated COX-1 and COX-2 expressions from immunostaining were found in the bile ducts of tumor rats but not of normal rats. Therefore, [123I]IOFA was found to exhibit the potential for imaging tumors that over-express COX.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biomaterials - Volume 34, Issue 13, April 2013, Pages 3355-3365
Journal: Biomaterials - Volume 34, Issue 13, April 2013, Pages 3355-3365
نویسندگان
Ho-Lien Huang, Chun-Nan Yeh, Wei-Yuan Lee, Ying-Cheng Huang, Kang-Wei Chang, Kun-Ju Lin, Shu-Fan Tien, Wen-Chin Su, Ching-Hsiuan Yang, Jenn-Tzong Chen, Wuu-Jyh Lin, Shio-Shio Fan, Chung-Shan Yu,