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Objective:To fulfill the automatic radiolabeling of the norepinephrine transporter (NET) trancer 18F-meta-fluorobenzylguanidine (mFBG), and explore the 18F-mFBG PET/CT imaging effect of pheochromocytoma. Methods:On the basis of the chemical structure of mFBG, a spirocyclic iodonium ylide was used as the precursor to undergo a 3-step reaction sequence (radiofluorination, deprotection and neutralization) on AllinOne synthesis module. Purification by high performance liquid chromatography and formulation were conducted to generate 18F-mFBG. The corresponding quality control tests of 18F-mFBG product was performed. Afterwards, a postoperative patient with pheochromocytoma underwent 18F-mFBG PET/CT imaging. Results:The radiosynthesis was accomplished within 70 min, and 18F-mFBG was obtained in (17.8±2.4)% non-decay-corrected radiochemical yield ( n=5), with radiochemical purity >97% and molar activity >59.2 GBq/μmol. Sterility test, bacterial endotoxins test, abnormal toxicity test and the acetonitrile residue all met the requirements of Pharmacopoeia of the People′ s Republic of China (2020 Volume Ⅳ). The 18F-mFBG PET/CT imaging disclosed high uptake in pheochromocytoma and clear localization of lesions. Conclusions:The automatic radiolabeling of the NET targeted tracer 18F-mFBG is successfully realized by commercially available synthesis module, and the production quality meets all requirements for clinical translation. 18F-mFBG has a potential to image neuroendocrine lesions in clinical setting.
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Objective To investigate the effects,mechanisms,and the optimum doses of Rosuvastatin and Losartan on expression of caveolin-1 in cultured human monocyte-macrophage cells which were induced by oxidized low density lipoprotein(ox-LDL).Methods Human-monocyte cells were separated and changed into the human monocyte-macrophage cells.The model of amerosclerosis was set up.These cells were incubated in different doses of Rosuvastatin(0.1,1.0,5.0 μmol/L) and Losartan (10,50,100 μmol/L),and then cultured in combination of two drags (5.0 μmol/L + 100 μmol/L).Expression of caveolin-1 mRNA was determined with real-time fluorescent quantitative polymerase chain reaction (RT-PCR).Results In ox-LDL group,caveolin-1 mRNA was decreased sharply relative to control group [(0.2533 ±0.00973) vs (0.9410 ±0.03677)] in a concentration-dependent manner (P ＜0.01).Compared to ox-LDL group,expressions of Caveolin-1 mRNA were increased gradually in different doses of Rosuvastatin alone and Losartan alone group [(0.5198 ± 0.04840),(0.6183 ± 0.06740),(0.7257 ± 0.03052) vs (0.2533 ± 0.00973) ; (0.3350 ± 0.04177),(0.4428 ± 0.03804),(0.6049 ± 0.02627) vs (0.2533 ± 0.00973)] in a concentration-dependent manner (P ＜ 0.01) ; the summit expressions of caveolin-1 mRNA were emerged in using Rosuvastatin and Losartan together (F =59.119,P ＜ 0.01).Conclusions Rosuvastatin and Losartan may be responsible for the expression of caveolin-1 in human monocyte-macrophage cells that were induced by ox-LDL.The expressions were up-regulated with dose dependent manner of these drugs,and got the crest stage when using optimum doses of Rosuvastatin and Losartan together.
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Objective To investigate the effects and mechanism of different doses of rosuvastatin on expression of tissue factor(TF) in cultured human monocyte-macrophage cells which were induced by oxidized low density lipoprotein (ox-LDL).Methods The human monocyte-macrophage cells were divided into seven groups:control group,ox-LDL group,poly-insine monophosphate group,different doses of rosuvastatin group(0.01 μmol/L,0.1 μmol/L,1 μmol/L,5 μmol/L).The expression of LOX-1 mRNA and TF mRNA was assayed by RT-PCR.The enzyme-linked immunosorbent assay was performed to determine the protein concentration of TF.Results Effects of different doses of rosuvastatin on expressions of LOX-1mRNA,TF mRNA and TF in cultured human monocyte-macrophage cells induced by ox-LDL:comparison among seven groups,the difference was statistically significant (F =91.334,58.833,103.552,P ＜0.05).Compared with control group,the expressions of LOX-1 mRNA,TF mRNA and TF were increased in the ox-LDL group[(3.25156 ± 0.15772) vs (1 ±0) ;(2.522451 ±0.138967) vs (1 ±0) ;(207.7233± 1.154701)ng/L vs (184.8467 ± 0.871799)ng/L],and they were in a concentration-dependent manner (P ＜ 0.05).Compared with the PolyⅠ group and the different doses of rosuvastatin group,the expressions of LOX-1 mRNA,TF mRNA and TF were in the ox-LDL group,and the different doses of rosuvastatin were decreased by dose-dependent manner.It was in a concentration dependent manner (P ＜ 0.05).Different doses of rosuvastatin were compared between groups (between each group P ＜ 0.05),the difference between each two groups was statistically significant (P ＜ 0.05).Conclusions LOX-1 may be responsible for the expression of TF in Human monocyte-macrophage cells induced by ox-LDL.Rosuvastatin by dose dependent manner and by means of ox-LDL reduced monocyte-macrophage LOX-1 mRNA and TF mRNA expressions,which reduced expression of TF.
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ObjectiveTo investigate the effects and mechanism of rosuvastatin on the expression of tissue factor in cultured human monocyte-macrophages cells which was induced by oxidized low density lipoprotein(ox-LDL).MethodsThe human monocyte-macrophages cells were divided into four groups:control group,ox-LDL group,Poly-inosine monophosphate (Poly Ⅰ) group,rosuvastatin group.The expression of LOX-1mRNA and TF mRNA was assayed by RT-PCR.The ELISA was performed to determine the protein concentration of TF.ResultsCompared with control group,the expression of LOX-1 mRNA and TF mRNA was increased in the ox-LDL group[ (3.25156±0.15772) vs (1±0) ; (2.522451±0.138967) vs (1±0) ],and it was in a concentration-dependent manner (P＜0.01).Compared with the expression of LOX-1 mRNA in the Poly-inosine monophosphate group and rosuvastatin group,TF mRNA were decreased in the ox-LDL group[ (2.95139±0.157253) vs(3.25156±0.15772) ; (2.877343±0.156558) vs(3.25156±0.15772) ; (1.811956±0.169699) vs (2.522451±0.138967) ; (1.687701±0.174647) vs (2.522451±0.138967)],and it was in a concentration-dependent manner(P＜0.05).Compared with control group,the expression of TF in the ox-LDL group was increased [(207.7233±1.154701) vs (184.8467±0.871799) ],and it was in a concentration-dependent manner (P＜0.01).Compared with the Poly-inosine monophosphate group and rosuvastatin group [(197.8733±1.505003) vs (207.7233±1.154701) ;(202.9567±2.722744)vs(207.7233±1.154701) ],the expression of TF in the ox-LDL group were decreased,and it was in a concentration-dependent manner (P＜0.05).ConclusionsLOX-1 may be responsible for the expression of TF in human monocyte-macrophages cells induced by ox-LDL.Rosuvastatin is able to down-regulate the expression of LOX-1mRNA in human monocyte-macrophages cells through oxLDL,and TF mRNA and TF expression can be reduced.