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This study aims to develop a new folate receptor (FR)-targeting agent for SPECT imaging with improved contrast and evaluate the modification strategies of multimerization and/or PEGylation in the development of new radio-folates. A series of novel folate derivatives have been synthesized and radiolabeled with 99mTc using tricine and TPPTS as coligands. To better investigate their pharmacokinetics, cell uptake, biodistribution, and microSPECT/CT imaging were evaluated. Four radioligands displayed high KB cell uptake after incubation for 2 and 4 h. Presaturated with excess folic acid (FA) resulted in a significant blocking effect in KB cells, indicating specificity of these radioligands toward FR. Biodistribution and microSPECT imaging studies in KB tumor-bearing mice showed that the folate conjugate 99mTc-HYNFA with poly(ethylene glycol) (PEG) and triazole linkage displayed the highest tumor uptake (16.30 ± 2.01 %ID/g at 2 h p.i. and 14.9 ± 0.62 %ID/g at 4 h p.i. in mice biodistribution) and best imaging c...
| Authors: | Zhide Guo; Linyi You; Changrong Shi; Manli Song; Mengna Gao; Duo Xu; Chenyu Peng; Rongqiang Zhuang; Ting Liu; Xinhui Su; Jin Du; Xianzhong Zhang | |
| Journal: | Molecular Pharmaceutics | |
| Year: | 2017 | |
| DOI: | 10.1021/acs.molpharmaceut.7b00536 | |
| Publication date: | 12-Oct-2017 |
Chemokine receptor CXCR4 plays an important role in cancer cell invasion and metastasis. Recent findings suggest that anti-VEGF therapies upregulate CXCR4 expression, which contributes to resistance to antiangiogenic therapies. Here, we report the development of novel derivatives of polyeth ... more
The molecular structures of three parthenolide analogues, (−)-goyazensolide (1), (−)-15-deoxygoyazensolide (2), and (−)-ereglomerulide (3), isolated from the leaves of Piptocoma rufescens in a previous study were determined by X-ray analysis, and the absolute configuration of (−)-goyazensol ... more
Mutual Impact of Phase Separation/Crystallization and Water Sorption in Amorphous Solid Dispersions
The molecular integration of poorly water soluble active pharmaceutical ingredients (APIs) in a suitable polymeric matrix is a possible approach to enhance the dissolution behavior and solubility of these APIs. Like all newly developed pharmaceutical formulations, these formulations (often ... more
Discovery of a biochemical basis for broccoli's cancer-fighting ability
Scientists are reporting discovery of a potential biochemical basis for the apparent cancer-fighting ability of broccoli and its veggie cousins. They found for the first time that certain substances in the vegetables appear to target and block a defective gene associated with cancer. Their ... more
Faster, more cost-effective DNA test for crime scenes, disease diagnosis
Scientists in Japan are reporting development of a faster, less expensive version of the fabled polymerase chain reaction (PCR) a DNA test widely used in criminal investigations, disease diagnosis, biological research and other applications. The new method could lead to expanded use of PCR ... more
'Nanoshells' simultaneously detect and destroy cancerous cells
Researchers at Rice University in Texas have developed a new approach to fighting cancer, based on nanoscale particles that can both detect and destroy cancerous cells. The report appears in the American Chemical Society's journal Nano Letters. Current molecular imaging approaches only dete ... more
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