Contrast Media & Molecular Imaging
·
2019
·
IF 1.984
Zi Wang,Liang Cai,Tingting Xu,Dan Tang,Lin Liu,Yue Chen
Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by systemic, symmetrical, and erosive synovitis. RA is one of the most common disabling diseases in the clinic. The main clinical intervention strategies are early diagnosis and early treatment. This study aims to predict the diagnostic value of 68Ga-citrate and 18F-FDG PET/CT in RA by comparing and analyzing the value of 68Ga-citrate and 18F-FDG PET/CT for diagnosing type II collagen-induced arthritis (CIA) in rats. Some CIA models were established. Normal rats were selected as the control group, and 23 days and 40 days were selected as the early and late time points of arthritis, respectively. The semiquantitative analysis of CIA rats was carried out with 68Ga-citrate PET/CT and 18F-FDG PET/CT, and the ratio of the maximum standardized uptake (SUVmax) values in the regions of interest (ROIs) of the hind foot ankle joint and thigh muscle was calculated and statistically analyzed. The distribution of CIA rats in vivo at the 68Ga-citrate 90 min time point was studied, and the ankle tissues were evaluated with hematoxylin and eosin (HE) staining. 68Ga-citrate PET/CT is obviously superior to 18F-FDG PET/CT for CIA imaging, and the statistical results show that the difference between the two examination methods is statistically significant (). The uptake of these two radiopharmaceuticals showed the same trend in arthritis rats with different scores. The distribution of 68Ga-citrate at 90 min is consistent with the trend shown by 68Ga-citrate PET/CT. 68Ga-citrate PET/CT can reflect the inflammatory activity of affected joints in CIA rats earlier and more sensitively than 18F-FDG PET/CT, and this imaging advantage continues until the later stage of inflammation. Therefore, 68Ga-citrate PET/CT is worthy of further promotion and application in the clinical diagnosis of RA.
研究领域:
医学影像学
·
风湿病学
✓ 已验证
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2025
·
IF 8.2
Deyi Zhao,Yongqi Han,Yamei Chen,Zhenyang He,Qian Xia,Ding-Kun Ji,Weihong Tan
Triple-negative breast cancer (TNBC) is one of the most malignant cancer types, characterized by a lack of efficient diagnostic and treatment methods in clinical practice. The development of effective targeted diagnosis and treatment for TNBC has become an important research focus. Here, we report the first proof-of-concept evidence of a glycoaptamer dual-target radionuclide probe (GDRP) for positron emission tomography/computed tomography (PET/CT) imaging of TNBC. The GDRP was created through precise molecular engineering of the aptamer AS1411, combined with three mannose ligands. The GDRP exhibited significantly increased serum stability and a high affinity for TNBC cells through a dual targeting mode. The advantages of our developed GDRP were further demonstrated by its excellent in vivo PET/CT dynamic imaging performance, featuring a long imaging window and high spatiotemporal resolution. This flexible method allows for the preparation of glycosylated functional nucleic acid molecular probes with high serum stability and tumor specificity. We anticipate that this PET/CT molecular probe will expand the development of glycoaptamer-based radioactive drugs and provides molecular tools for the clinical diagnosis of TNBC.
研究领域:
医学影像学
·
分子生物学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Oncology
·
2022
·
IF 5.738
Ren Ya’nan,Liu Chen,Liu Teli,Duan Xiaojiang,Zhang Qian,Liu Jiayue,Wang Pei,Guo Qian,Yang Xing,Du Peng,Zhu Hua,Yang Zhi
Purpose: This study aimed to introduce a novel [18F]AlF-labeled ODAP-Urea-based Prostate-specific membrane antigen (PSMA) probe, named [18F]AlF-PSMA-137, which was derived from the successful modification of glutamate-like functional group. The preclinically physical and biological characteristics of the probe were analyzed. Polit clinical PET/CT translation was performed to analyze its feasibility in clinical diagnosis of prostate cancer.Methods: [18F]AlF-PSMA-137 was maturely labeled with the [18F]AlF2+ labeling technique. It was analyzed by radio-HPLC for radiochemical purity and stability analysis in vitro and in vivo. The PSMA specificity was investigated in PSMA-positive (LNCaP) and PSMA-negative (PC3) cells, and the binding affinity was evaluated in LNCaP cells. Micro-PET/CT imaging was performed in mice bearing LNCaP or PC3 tumors. Thirteen patients with newly diagnosed prostate cancer were included for [18F]AlF-PSMA-137 PET/CT imaging. Physiologic biodistribution and tumor burden were semi-quantitatively evaluated and the radiation dosimetry of [18F]AlF-PSMA-137 was estimated.Results: The radiochemical yield of [18F]AlF-PSMA-137 was 54.2 ± 10.7% (n = 16) with the radiochemical purity over 99% and the specific activity of 26.36 ± 7.33 GBq/μmol. The binding affinity to PSMA was 2.11 ± 0.63 nM. [18F]AlF-PSMA-137 showed high cell/tumor uptake which can be specifically blocked by PSMA inhibitor. According to the biodistribution in patients, [18F]AlF-PSMA-137 was mainly accumulated in kidneys, lacrimal glands, parotid glands, submandibular glands and liver which was similar to the extensive Glu-Ureas based probes. A total of 81 lesions were detected in PET/CT imaging and over 91% of lesions increased between 1 h p.i. (SUVmean: 10.98 ± 18.12) and 2 h p.i. (SUVmean: 14.25 ± 21.28) (p < 0.001). Additionally, the probe showed intensive accumulation in lesions which provided excellent imaging contrast with the high tumor-to-muscle ratio of 15.57 ± 27.21 at 1 h p.i. and 25.42 ± 36.60 at 2 h p.i. (p < 0.001), respectively. The effective dose of [18F]AlF-PSMA-137 was estimated as 0.0119 ± 0.0009 mSv/MBq.Conclusion: An ODAP-Urea-based PSMA probe [18F]AlF-PSMA-137 was successfully prepared with high specificity and binding affinity to PSMA. Micro-PET/CT imaging study demonstrated its feasibility for prostate cancer imaging. Pilot clinical study showed its potential for delay-imaging and prostate cancer detection.
研究领域:
医学影像学
·
肿瘤学
·
放射化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULAR PHARMACEUTICS
·
2018
·
IF 4.556
Hui Liu,Yuxiang Han,Jiyuan Li,Ming Qin,Qunfeng Fu,Chunhong Wang,Zhibo Liu
Amino acids derivative are well established molecular probes for diagnosis of a variety of cancer using positron emission tomography (PET). Recently, boramino acid (BAAs) was found as a prospective molecular platform for developing PET tracer. The objective of this study was to develop a 18F-labeled alanine derivative through displacing its carboxylate by trifluoroborate as a selective ASCT2 marker for cancer imaging. 18F-Ala-BF3 was first evaluated in healthy FVB/N mice in vivo, exhibiting rapid renal clearance with almost negligible uptake in stomach (1.53 ± 0.31%ID/g). Notable uptake was observed in thyroid (3.71 ± 0.49%ID/g, 40 min post injection), of which the uptake was significantly inhibited by co-injection with natural L-alanine. In addition, we further established 18F-Ala-BF3 on a human gastric cancer cell (BGC-823) xenografts bearing mouse model. Dynamic PET-CT scan revealed the optimal time window for tumor imaging, it was between 40 and 60 min post injection, when the BGC-823 xenografts uptake was 5.49 ± 1.47%ID/g (n = 4), and the tumor-to-stomach, tumor-to-blood, tumor-to-muscle, and tumor-to-brain ratios were 3.27 ± 1.53, 3.80 ± 1.48, 3.47 ± 1.48, and 6.20 ± 1.47, respectively.
研究领域:
医学影像学
·
肿瘤学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
·
2021
·Vol. 48
·期 13
·4259-4271
·
IF 9.236
Wang Shuailiang,Zhou Xin,Xu Xiaoxia,Ding Jin,Liu Song,Hou Xingguo,Li Nan,Zhu Hua,Yang Zhi
Purpose In this study, a novel aluminium-[ 18 F]fluoride (Al 18 F)-labelled 1,4,7‑triazacyclononane-N,N′,N″-triacetic acid (NOTA)-conjugated fibroblast activation protein inhibitor (FAPI) probe, named Al 18 F-NOTA-FAPI, was developed for fibroblast activation protein (FAP)-targeted tumour imaging; it could deliver hundreds of millicuries of radioactivity using automated synthesis. The tumour detection efficacy of Al 18 F-NOTA-FAPI was further validated in both preclinical and clinical translational studies. Methods The radiolabelling procedure of Al 18 F-NOTA-FAPI was optimized. Cell uptake and competitive binding assays were completed with the U87MG and A549 cell lines to evaluate the affinity and specificity of the Al 18 F-NOTA-FAPI probe. The biodistribution, pharmacokinetics, radiation dosimetry and tumour imaging efficacy of the Al 18 F-NOTA-FAPI probe were researched in healthy Kunming (KM) and/or U87MG model mice. After the approval of the ethical committee, the Al 18 F-NOTA-FAPI probe was translated into the clinic for PET/CT imaging of the first 10 cancer patients. Results The radiolabelling yield of Al 18 F-NOTA-FAPI was 33.8 ± 3.2% using manual synthesis ( n = 10), with a radiochemical purity over 99% and the specific activity of 9.3–55.5 MBq/nmol. The whole body effective dose of Al 18 F-NOTA-FAPI was estimated to be 1.24E − 02 mSv/MBq, which was lower than several other FAPI probes ( 68 Ga-FAPI-04, 68 Ga-FAPI-46 and 68 Ga-FAPI-74). In U87MG tumour-bearing mice, Al 18 F-NOTA-FAPI showed good tumour detection efficacy based on the results of micro PET/CT imaging and biodistribution studies. In an organ biodistribution study of patients, Al 18 F-NOTA-FAPI showed a lower SUVmean than 2-[ 18 F]-fluoro-2-deoxy-D-glucose (2-[ 18 F]FDG) in most organs, especially in the liver (1.1 ± 0.2 vs. 2.0 ± 0.9), brain (0.1 ± 0.0 vs. 5.9 ± 1.3), and bone marrow (0.9 ± 0.1 vs. 1.7 ± 0.4). Meanwhile, Al 18 F-NOTA-FAPI did not show extensive bone uptake, and was able to detect more lesions than 2-[ 18 F]FDG in the PET/CT imaging of several patients. Conclusion The Al 18 F-NOTA-FAPI probe was successfully fabricated and applied in fibroblast activation protein-targeted tumour PET/CT imaging, which showed excellent imaging quality and tumour detection efficacy in U87MG tumour-bearing mice as well as in cancer patients. Trial registration Chinese Clinical Trial Registry ChiCTR2000038080. Registered 09 September 2020. http://www.chictr.org.cn/showproj.aspx?proj=61192
研究领域:
医学影像学
·
肿瘤学
·
核医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACADEMIC RADIOLOGY
·
2026
·
IF 4.7
Jing Gu,Hui Wang,Yulin He
Rationale and Objective This study utilized micro-positron emission tomography/computed tomography (micro-PET/CT) to track the longitudinal and dynamic progression of cardiac autonomic nerve injury in diabetic rats. Our objective was to map the precise timeline of neural damage relative to disease stages, defining a sensitive imaging window for the early diagnosis of diabetic cardiac autonomic neuropathy (DCAN). Materials and Methods Following streptozotocin induction of type 2 diabetes, rats underwent biweekly micro-PET/CT imaging for up to 17 weeks. Sympathetic and parasympathetic innervations were thoroughly evaluated using [ 11 C]C-MDA and [ 11 C]C-donepezil ([ 11 C]C-DNP), respectively. [ 11 C]C-triphenylmethylphosphonium ([ 11 C]C-TPMP) provided a perfusion baseline to characterize neuro-perfusion mismatches. Quantitative tracer uptake was correlated with histopathological remodeling and the myocardial expression of neurotrophic factors (NGF, GAP-43, CNTF) quantified via quantitative real-time polymerase chain reaction (RT-qPCR). Results Longitudinal PET/CT imaging unveiled a distinct chronological cascade of cardiac deterioration. Parasympathetic denervation ([ 11 C]C-DNP depletion) manifested first at week 6, followed by sympathetic denervation ([ 11 C]C-MDA deficit) at week 8. Conversely, myocardial perfusion deficits ([ 11 C]C-TPMP) remained absent until week 16, escalating to severe metabolic dysfunction by week 17. Histopathology confirmed progressive myocardial inflammation, while RT-qPCR indicated a late-stage, yet insufficient, compensatory upregulation of neurotrophic factors. Conclusion This multi-tracer longitudinal investigation establishes that parasympathetic denervation precedes sympathetic impairment during DCAN development, with both deficits predating microvascular and metabolic crises. These insights offer a critical, noninvasive diagnostic window for early DCAN detection and clinical monitoring.
✓ 已验证
DOI
高影响因子
Pharmaceutics
·
2024
·Vol. 16
·期 12
·1609
·
IF 4.9
Xiaoli Zhang,Tingting Li,Jindong Tong,Meihong Zhou,Zi Wang,Xingdang Liu,Wei Lu,Jingjing Lou,Qingtong Yi
Background/Objectives: The purpose of this study was to develop the gemcitabine-loaded drug-eluting beads (G-DEBs) for transarterial chemoembolization (TACE) in rabbit renal tumors and to evaluate their antitumor effect using 2-deoxy-2-[(18)F]fluoro-D-glucose positron emission tomography/X-ray computed tomography (18F-FDG PET/CT). Methods: DEBs were prepared by polyvinyl alcohol-based macromer crosslinked withN-acryl tyrosine andN,N′-methylenebis(acrylamide). Gemcitabine was loaded through ion change to obtain G-DEBs. Their particle size and drug release profile were characterized. VX2 tumors were implanted in the right kidney of rabbits to establish the renal tumor model. The tumor-bearing rabbits received pre-scan by18F-FDG PET/CT, followed by targeted transarterial injection of G-DEBs under digital subtraction angiography (DSA) guidance. The rabbits received another18F-FDG PET/CT scan 10 or 14 days after the treatment. The therapeutic effect was further validated by histopathological analysis of the dissected tumors. Results: The average particle size of the microspheres was 58.06 ± 0.50 µm, and the polydisperse index was 0.26 ± 0.002. The maximum loading rate of G-DEBs was 18.09 ± 0.35%, with almost 100% encapsulation efficiency. Within 24 h, GEM was eluted from G-DEBs rapidly and completely, and more than 20% was released in different media. DSA illustrated that G-DEBs were delivered to rabbit renal tumors. Compared with the untreated control group with increased tumor volume and intense18F -FDG uptake, the G-DEBs group showed significant reductions in tumor volume and maximum standard uptake value (SUVmax) 10 or 14 days after the treatment. Histopathological analysis confirmed that the proliferating area of tumor cells was significantly reduced in the G-DEBs group. Conclusions: Our results demonstrated that G-DEBs are effective in TACE treatment of rabbit VX2 renal tumors, and18F-FDG PET/CT provides a non-invasive imaging modality to monitor the antitumor effects of TACE in renal tumors.
研究领域:
肿瘤学
·
影像医学
·
药剂学
✓ 已验证
DOI
PubMed
高影响因子
EXPERIMENTAL NEUROLOGY
·
2026
·
IF 4.8
Jiapei Lei,Jie Yu,Xiaotao Zheng,Xiangguo Lai,Junlin Chen,Min Yang,Meng Yu,Yin Wang,Ning Tan
Neonatal bilirubin encephalopathy arises from unconjugated bilirubin deposition in the brain. Conventional tests are limited: serum bilirubin does not reflect intracerebral load, and MRI T1 changes are late and confounded by myelination. We evaluated whether 18 F-FDG PET detects early metabolic abnormalities and monitor progression. Twelve Sprague–Dawley rat were randomly assigned to bilirubin-exposed or control groups. The bilirubin-exposed group received intraperitoneal bilirubin from postnatal day 3. 18 F-FDG PET/CT was performed on days 7 and 21, and regional standardized uptake values and cerebellum-normalized SUV ratios were quantified. Serum bilirubin, histology, immunohistochemistry and qRT-PCR were assessed in parallel. The model showed elevated serum bilirubin ( p < 0.001) and neuronal injury. On day 7, PET revealed regional hypermetabolism in hippocampus and thalamus ( p < 0.01), coinciding with increased IL-6 (cortex, thalamus) and TNF-α (thalamus). By day 21, widespread hypometabolism involved cortex, basal ganglia, hippocampus, thalamus, and brainstem ( p < 0.001), with only residual thalamic IL-6. GFAP indicated persistent astrocytic activation, whereas MAP2 and NeuN were largely preserved. The SUV ratio analysis showed a pattern consistent with the SUV-based findings. 18 F-FDG PET detected age-dependent metabolic alterations in bilirubin encephalopathy and may be useful for early detection and longitudinal monitoring.
✓ 已验证
DOI
PubMed
高影响因子
Molecular Imaging
·
2015
·
IF 1.962
Xinchong Shi,Xiangsong Zhang,Chang Yi,Yubo Liu,Qiao He
The purpose of this study was to investigate the expression of glutamine synthetase (GS) in prostate cancer (PCa) and the utility of [13N]ammonia positron emission tomography/computed tomography (PET/CT) in the imaging of PCa. The uptake ratio of [13N]ammonia and the expression of GS in PC3 and DU145 cells was measured. Thirty-four patients with suspected PCa underwent [13N]ammonia PET/CT imaging, and immunohistochemistry staining of GS was performed. The uptake of [13N]ammonia in PC3 and DU145 cells elevated along with the decrease in glutamine in medium. The expression of GS messenger ribonucleic acid and protein also increased when glutamine was deprived. In biopsy samples, the GS expression scores were significantly higher in PCa tissue than in benign tissues (p < .001), and there was a positive correlation between the maximum GS expression scores and Gleason scores (Spearman r = .52). In 34 patients, [13N]ammonia uptake in PCa segments was significantly higher than that in benign segments (p ≤ .01), and there was a weak correlation between GS expression scores and the uptake of [13N]ammonia (Spearman r = .47). The expression of GS in PCa cells upregulated along with the deprivation of glutamine. GS is the main reason for the uptake of [13N]ammonia, and [13N]ammonia is a useful tracer for PCa imaging.
研究领域:
医学成像
·
肿瘤学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULAR PHARMACEUTICS
·
2023
·
IF 4.9
Pei Wang,Shuailiang Wang,Futao Liu,Ya’nan Ren,Qian Guo,Qian Zhang,XingGuo Hou,Yuan Yao,Hua Zhu,Zhi Yang
Prostate-specific membrane antigen (PSMA) is a prostate cancer target that plays a crucial role in prostate cancer diagnosis and therapy. Herein, a novel dual-targeted imaging probe, [68Ga]Ga-FAPI-PSMA, was prepared by radiolabeling conjugated DOTA-FAPI-PSMA with the short half-life radionuclide gallium-68 (68Ga), which is dedicated to prostate cancer diagnostic imaging. In vitro, [68Ga]Ga-FAPI-PSMA had higher affinity for the PSMA and FAP high-expressing cell lines 22Rv1 and U87 MG with IC50 values of 4.73 and 2.10 nM, respectively, than in the corresponding negative expression cell lines PC3 and A549, and significant differences in cell uptake were also observed. In vivo, [68Ga]Ga-FAPI-PSMA was rapidly cleared from the body, and the estimated radiation dose was relatively low compared with several other FAPI probes. In 22Rv1 and U87 MG tumor xenografts, [68Ga]Ga-FAPI-PSMA rapidly accumulated in tumors after administration, and the best images can be obtained at 1 h postinjection. In conclusion, the dual-targeted probe [68Ga]Ga-FAPI-PSMA was successfully prepared for in vivo prostate cancer PET/CT imaging.
研究领域:
放射学
·
肿瘤学
·
分子影像
·
核医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Oncology
·
2021
·
IF 6.244
Wen Li,Xia Lei,Guo Xiaoyi,Huang Hai-Feng,Wang Feng,Yang Xian-teng,Yang Zhi,Zhu Hua
Trastuzumab is a monoclonal antibody targeting human epidermal growth factor 2 (HER2), which has been successfully used in the treatment of patients with breast cancer and gastric cancer; however, problems concerning its cardiotoxicity, drug resistance, and unpredictable efficacy still remain. Herein, we constructed novel organic dopamine–melanin nanoparticles (dMNs) as a carrier and then surface-loaded them with trastuzumab to construct a multifunctional nanoprobe named Her-PEG-dMNPs. We used micro-PET/CT and PET/MRI multimodality imaging to evaluate the retention effect of the nanoprobe in HER2 expression in gastric cancer patient-derived xenograft (PDX) mice models after labeling of the radionuclides 64Cu or 124I and MRI contrast agent Mn2+. The nanoprobes can specifically target the HER2-expressing SKOV-3 cells in vitro (3.61 ± 0.74 vs. 1.24 ± 0.43 for 2 h, P = 0.002). In vivo, micro-PET/CT and PET/MRI showed that the 124I-labeled nanoprobe had greater contrast and retention effect in PDX models than unloaded dMNPs as carrier (1.63 ± 0.07 vs. 0.90 ± 0.04 at 24 h, P = 0.002), a similarity found in 64Cu-labeled Her-PEG-dMNPs. Because 124I has a longer half-life and matches the pharmacokinetics of the nanoparticles, we focused on the further evaluation of 124I-Her-PEG-dMNPs. Furthermore, immunohistochemistry staining confirmed the overexpression of HER2 in the animal model. This study developed and validated novel HER2-specific multimodality imaging nanoprobes for quantifying HER2 expression in mice. Through the strong retention effect of the tumor site, it can be used for the promotion of monoclonal antibody treatment effect and process monitoring.
研究领域:
肿瘤学
·
分子影像
·
纳米医学
·
癌症治疗
✓ 已验证
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF NUTRITION
·
2017
·Vol. 57
·期 1
·391-403
·
IF 4.37
Hu Tao,Yuan Xiaoxue,Wei Gang,Luo Haoshu,Lee Hyuek Jong,Jin Wanzhu
Purpose Myricetin, a dietary flavonoid, is effective in the treatment of obesity and insulin resistance by increasing glucose transport and lipogenesis in adipocyte and diminishing systemic inflammation in obesity. However, it has not been revealed yet whether myricetin is associated with brown adipose tissue (BAT) activation that tightly mediates systemic energy metabolism. Therefore, this study assessed whether myricetin activated brown adipose tissue in db/db mouse. Methods Myricetin (400 mg/kg) in distilled water was fed daily by oral gavage to leptin receptor-deficient db/db male mice at 4 weeks of age for 14 weeks. Body weight change, glucose intolerance test, blood lipid profile and BAT activation using PET-CT were assessed. Results After myricetin treatment for 14 weeks, systemic insulin resistance and hepatic steatosis were significantly improved in db/db mice with body weight reduction and myricetin led to decreased adipocity, improved plasma lipid profiles and increased energy expenditure. Myricetin activated BAT by upregulating thermogenic protein expression and activating mitochondrial biogenesis, eventually increasing heat dissipation in skin after cold exposure. In iWAT, myricetin induced beige formation, increased thermogenic protein expression and activated mitochondrial biogenesis. Consistently, thermogenic gene expression was upregulated when myricetin was introduced in C 3 H 10 T 1/2 cells during brown adipocytes differentiation. Moreover, the expression level of adiponectin was significantly increased in C 3 H 10 T 1/2 cells, adipose tissues and plasma after myricetin treatment. Conclusions These results highlight that myricetin prevents obesity and systemic insulin resistance by activating BAT and increasing adiponectin expression in BAT.
研究领域:
药理学
·
代谢学
·
内分泌学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）