1.Comparative study on the selectivity differences of 18F-TFQC and 18F-DPA-714 for TSPO gene polymorphisms and their PET imaging in rat neuroinflammation models
Hongxing SU ; Yufei MA ; Qingyu LIN ; Zhequan FU ; Xinyan GAO ; Pengcheng MA ; Dai SHI ; Zonghua LUO ; Dengfeng CHENG
Chinese Journal of Nuclear Medicine and Molecular Imaging 2025;45(8):458-463
Objective:To explore the binding characteristics of N, N-diethyl-2-(2-(4-(2- 18F-fluoroethoxy)phenyl)-5, 7-dimethylpyrazolo[1, 5-a]pyrimidin-3-yl)acetamide ( 18F-DPA-714) and ( R)- N-sec-butyl- N-methyl-4-(3-( 18F-trifluoromethyl)phenyl)quinazoline-2-carboxamide ( 18F-TFQC) to the single nucleotide polymorphisms of the 18×10 3 translocator protein (TSPO), and to evaluate the imaging efficacy and feasibility of those 2 molecular probes in neuroinflammation rat models. Methods:To test the selectivity of 18F-DPA-714 and 18F-TFQC for TSPO polymorphisms, the wild-type (high-affinity binding, HAB) and mutant (low-affinity binding, LAB) sequences of the human TSPO gene were transfected into 293T cells respectively. A competitive inhibition assay was carried out with N-methyl- N-(1-methylpropyl)-1-(2-chlorophenyl)-3-isoquinoline carboxamide (PK11195) as an inhibitor to determine the binding affinities of 2 probes to TSPO polymorphisms. Rat neuroinflammation models ( n=6) were established using lipopolysaccharide. Three days after modeling, small animal PET/CT imaging was performed using 18F-DPA-714 and 18F-TFQC, respectively, to observe and compare the uptake of the tracers, and the ratio of SUV mean of the right striatum to SUV mean of the left striatum (SUVR) was calculated. After the imaging, the expression and distribution of microglia and TSPO were detected by tissue immunofluorescence. Repeated-measures analysis of variance was used to analyze the SUVR data of different groups. Results:The inhibition constants ( Ki) of 18F-TFQC on 293T-LAB and 293T-HAB cells were 23.51 and 14.60 nmol/L, respectively, with a Ki LAB/ Ki HAB ratio of 1.61, indicating low sensitivity to TSPO single nucleotide polymorphisms. The Ki of 18F-DPA-714 for binding to 293T-LAB and 293T-HAB cells were 45.23 and 6.47 nmol/L, respectively, with a Ki LAB/ Ki HAB ratio of 6.99. Small animal PET/CT imaging demonstrated that specifically uptake of both probes could be found in neuroinflammatory lesions. The overall SUVR of 18F-DPA-714 in the lesions within 60minutes was slightly higher than that of 18F-TFQC, but no significant difference was observed ( F values: inter-group 0.40, time effect 0.30, cross-effect 0.03; all P>0.05). Conclusions:Compared with 18F-DPA-714, 18F-TFQC is less sensitive to TSPO gene polymorphisms, thus being more suitable for clinical application and promotion. It holds promise for the early identification of neuroinflammation and the efficacy monitoring of anti-inflammatory drug treatments.
2.Synthesis and evaluation of TSPO-targeting radioligand 18FF-TFQC for PET neuroimaging in epileptic rats.
Wenhui FU ; Qingyu LIN ; Zhequan FU ; Tingting YANG ; Dai SHI ; Pengcheng MA ; Hongxing SU ; Yunze WANG ; Guobing LIU ; Jing DING ; Hongcheng SHI ; Dengfeng CHENG
Acta Pharmaceutica Sinica B 2025;15(2):722-736
The translocator protein (TSPO) positron emission tomography (PET) can noninvasively detect neuroinflammation associated with epileptogenesis and epilepsy. This study explored the role of the TSPO-targeting radioligand [18F]F-TFQC, an m-trifluoromethyl ER176 analog, in the PET neuroimaging of epileptic rats. Initially, [18F]F-TFQC was synthesized with a radiochemical yield of 8%-10% (EOS), a radiochemical purity of over 99%, and a specific activity of 38.21 ± 1.73 MBq/nmol (EOS). After determining that [18F]F-TFQC exhibited good biochemical properties, [18F]F-TFQC PET neuroimaging was performed in epileptic rats at multiple time points in various stages of disease progression. PET imaging showed specific [18F]F-TFQC uptake in the right hippocampus (KA-injected site, i.e., epileptogenic zone), which was most pronounced at 1 week (T/NT 1.63 ± 0.21) and 1 month (T/NT 1.66 ± 0.20). The PET results were further validated using autoradiography and pathological analysis. Thus, [18F]F-TFQC can reflect the TSPO levels and localize the epileptogenic zone, thereby offering the potential for monitoring neuroinflammation and guiding anti-inflammatory treatment in patients with epilepsy.
3.Comparative study on the selectivity differences of 18F-TFQC and 18F-DPA-714 for TSPO gene polymorphisms and their PET imaging in rat neuroinflammation models
Hongxing SU ; Yufei MA ; Qingyu LIN ; Zhequan FU ; Xinyan GAO ; Pengcheng MA ; Dai SHI ; Zonghua LUO ; Dengfeng CHENG
Chinese Journal of Nuclear Medicine and Molecular Imaging 2025;45(8):458-463
Objective:To explore the binding characteristics of N, N-diethyl-2-(2-(4-(2- 18F-fluoroethoxy)phenyl)-5, 7-dimethylpyrazolo[1, 5-a]pyrimidin-3-yl)acetamide ( 18F-DPA-714) and ( R)- N-sec-butyl- N-methyl-4-(3-( 18F-trifluoromethyl)phenyl)quinazoline-2-carboxamide ( 18F-TFQC) to the single nucleotide polymorphisms of the 18×10 3 translocator protein (TSPO), and to evaluate the imaging efficacy and feasibility of those 2 molecular probes in neuroinflammation rat models. Methods:To test the selectivity of 18F-DPA-714 and 18F-TFQC for TSPO polymorphisms, the wild-type (high-affinity binding, HAB) and mutant (low-affinity binding, LAB) sequences of the human TSPO gene were transfected into 293T cells respectively. A competitive inhibition assay was carried out with N-methyl- N-(1-methylpropyl)-1-(2-chlorophenyl)-3-isoquinoline carboxamide (PK11195) as an inhibitor to determine the binding affinities of 2 probes to TSPO polymorphisms. Rat neuroinflammation models ( n=6) were established using lipopolysaccharide. Three days after modeling, small animal PET/CT imaging was performed using 18F-DPA-714 and 18F-TFQC, respectively, to observe and compare the uptake of the tracers, and the ratio of SUV mean of the right striatum to SUV mean of the left striatum (SUVR) was calculated. After the imaging, the expression and distribution of microglia and TSPO were detected by tissue immunofluorescence. Repeated-measures analysis of variance was used to analyze the SUVR data of different groups. Results:The inhibition constants ( Ki) of 18F-TFQC on 293T-LAB and 293T-HAB cells were 23.51 and 14.60 nmol/L, respectively, with a Ki LAB/ Ki HAB ratio of 1.61, indicating low sensitivity to TSPO single nucleotide polymorphisms. The Ki of 18F-DPA-714 for binding to 293T-LAB and 293T-HAB cells were 45.23 and 6.47 nmol/L, respectively, with a Ki LAB/ Ki HAB ratio of 6.99. Small animal PET/CT imaging demonstrated that specifically uptake of both probes could be found in neuroinflammatory lesions. The overall SUVR of 18F-DPA-714 in the lesions within 60minutes was slightly higher than that of 18F-TFQC, but no significant difference was observed ( F values: inter-group 0.40, time effect 0.30, cross-effect 0.03; all P>0.05). Conclusions:Compared with 18F-DPA-714, 18F-TFQC is less sensitive to TSPO gene polymorphisms, thus being more suitable for clinical application and promotion. It holds promise for the early identification of neuroinflammation and the efficacy monitoring of anti-inflammatory drug treatments.
4.Expert consensus on the diagnosis and treatment of osteoporotic proximal humeral fracture with integrated traditional Chinese and Western medicine (version 2024)
Xiao CHEN ; Hao ZHANG ; Man WANG ; Guangchao WANG ; Jin CUI ; Wencai ZHANG ; Fengjin ZHOU ; Qiang YANG ; Guohui LIU ; Zhongmin SHI ; Lili YANG ; Zhiwei WANG ; Guixin SUN ; Biao CHENG ; Ming CAI ; Haodong LIN ; Hongxing SHEN ; Hao SHEN ; Yunfei ZHANG ; Fuxin WEI ; Feng NIU ; Chao FANG ; Huiwen CHEN ; Shaojun SONG ; Yong WANG ; Jun LIN ; Yuhai MA ; Wei CHEN ; Nan CHEN ; Zhiyong HOU ; Xin WANG ; Aiyuan WANG ; Zhen GENG ; Kainan LI ; Dongliang WANG ; Fanfu FANG ; Jiacan SU
Chinese Journal of Trauma 2024;40(3):193-205
Osteoporotic proximal humeral fracture (OPHF) is one of the common osteoporotic fractures in the aged, with an incidence only lower than vertebral compression fracture, hip fracture, and distal radius fracture. OPHF, secondary to osteoporosis and characterized by poor bone quality, comminuted fracture pattern, slow healing, and severely impaired shoulder joint function, poses a big challenge to the current clinical diagnosis and treatment. In the field of diagnosis, treatment, and rehabilitation of OPHF, traditional Chinese and Western medicine have accumulated rich experience and evidence from evidence-based medicine and achieved favorable outcomes. However, there is still a lack of guidance from a relevant consensus as to how to integrate the advantages of the two medical systems and achieve the integrated diagnosis and treatment. To promote the diagnosis and treatment of OPHF with integrated traditional Chinese and Western medicine, relevant experts from Orthopedic Expert Committee of Geriatric Branch of Chinese Association of Gerontology and Geriatrics, Youth Osteoporosis Group of Orthopedic Branch of Chinese Medical Association, Osteoporosis Group of Orthopedic Surgeon Branch of Chinese Medical Doctor Association, and Osteoporosis Committee of Shanghai Association of Integrated Traditional Chinese and Western Medicine have been organized to formulate Expert consensus on the diagnosis and treatment of osteoporotic proximal humeral fracture with integrated traditional Chinese and Western medicine ( version 2024) by searching related literatures and based on the evidences from evidence-based medicine. This consensus consists of 13 recommendations about the diagnosis, treatment and rehabilitation of OPHF with integrated traditional Chinese medicine and Western medicine, aimed at standardizing, systematizing, and personalizing the diagnosis and treatment of OPHF with integrated traditional Chinse and Western medicine to improve the patients ′ function.
5.Indoor Radon Survey in 31 Provincial Capital Cities and Estimation of Lung Cancer Risk in Urban Areas of China.
Xiaoxiang MIAO ; Yinping SU ; Changsong HOU ; Yanchao SONG ; Bowei DING ; Hongxing CUI ; Yunyun WU ; Quanfu SUN
Biomedical and Environmental Sciences 2024;37(11):1294-1302
OBJECTIVE:
We aimed to analyze the current indoor radon level and estimate the population risk of radon-induced lung cancer in urban areas of China.
METHODS:
Using the passive monitoring method, a new survey on indoor radon concentrations was conducted in 2,875 dwellings across 31 provincial capital cities in Chinese mainland from 2018 to 2023. The attributable risk of lung cancer induced by indoor radon exposure was estimated based on the risk assessment model.
RESULTS:
The arithmetic mean (AM) and geometric mean (GM) of indoor radon concentrations were 65 Bq/m³ and 55 Bq/m³, respectively, with 13.6% of measured dwellings exceeding 100 Bq/m³ and 0.6% exceeding 300 Bq/m³. The estimated number of lung cancer deaths induced by indoor radon exposure was 150,795, accounting for 20.30% (95% CI: 20.21%-20.49%) of the lung cancer death toll.
CONCLUSION
This study provided the most recent data on national indoor radon levels in urban areas and the attributable risk of lung cancer. These results served as an important foundation for further research on the disease burden of indoor radon exposure and radon mitigation efforts.
Radon/analysis*
;
China/epidemiology*
;
Air Pollution, Indoor/analysis*
;
Lung Neoplasms/etiology*
;
Humans
;
Cities/epidemiology*
;
Air Pollutants, Radioactive/adverse effects*
;
Neoplasms, Radiation-Induced/etiology*
;
Risk Assessment
;
Radiation Monitoring
6.Efficacy of microsurgical treatment in 58 patients with primary jugular foramen schwannomas
Guochen YANG ; Xixi LI ; Weijie SU ; Honglin WU ; Hongxing TANG ; Zhong DENG ; Yibin YANG ; Lixuan YANG
Chinese Journal of Neuromedicine 2022;21(11):1138-1142
Objective:To investigate the clinical efficacy of microsurgical resection in primary jugular foramen schwannomas (JFSs).Methods:A retrospective analysis was performed; the clinical data of 58 patients with JFSs treated by microsurgery in Department of Neurosurgery, First Affiliated Hospital of Sun Yat-sen University from May 2012 to June 2021 were collected. Seven patients accepted microsurgery via suboccipital retrosigmoid approach, and 51 patients accepted microsurgery via jugular foramen approach. Fifty-three patients were followed up for 4.5 years (ranged from 0.5-8.5 years); follow-ups included Karnofsky performance status (KPS) scores, postoperative complications, and imaging reexaminations. Results:Fifty patients (86.2%) achieved total tumor resection and 8 (13.8%) subtotal resection. The KPS scores at discharge were 68.6±14.9, which were significantly lower than the preoperative KPS scores (77.6±13.5, t=2.452, P=0.017). During the follow-up, 5 patients(9.4%) had tumor recurrence, and 39 patients (73.6%) had improved symptoms after surgery. One patient (1.9%, modified Samii D type) died of cerebellar hemorrhage and swelling after surgery. The main complications included new/aggravated hoarseness (11/53), cerebrospinal fluid leakage (7/53), new/aggravated dysphagia (5/53), and new facial paralysis (4/53). Conclusion:In microsurgical resection of JFSs, short-term symptoms of the lower cranial nerves may be exacerbated, but long-term results are good.
7.Mixed鄄phenotypic acute leukemia with SET鄄NUP214 fusion gene positive and extramedullary infiltration: report of one case and review of literature
Xiaoli MA ; Xian ZHANG ; Fang WANG ; Yunchao SU ; Xue CHEN ; Yang ZHANG ; Yu ZHANG ; Mingyu WANG ; Wei ZHANG ; Jing ZHANG ; Daijing NIE ; Jiaqi CHEN ; Mingyue LIU ; Ming LIU ; Hongxing LIU
Journal of Leukemia & Lymphoma 2019;28(4):219-222
Objective To investigate the clinical and molecular biological characteristics of mixed_phenotypic acute leukemia (MPAL) with SET_NUP214 fusion gene positive and extramedullary infiltration. Methods The clinical characteristics, diagnosis and treatment of one MPAL patient with SET_NUP214 and extramedullary infiltration who was admitted to Hebei Yanda Ludaopei Hospital in November 2017 were analyzed, and the literature was reviewed. Results The patient was diagnosed as MPAL with extramedullary infiltration. Gene detection found SET exon7_NUP214 exon17 fusion positive accompanied with PHF6, SRSF2 and NRAS mutations. After intensive chemotherapy, the patient achieved complete remission, and then received hematopoietic stem cell transplantation (HSCT), followed by early extramedullary relapse after transplantation, and achieved secondary remission after consolidation chemotherapy. Conclusions MPAL with SET_NUP214 fusion gene positive and extramedullary infiltration has a poor prognosis, and it is easy to relapse. Currently, HSCT is the best available treatment strategy for such patients.
8.Serum galactomannan test for diagnosis of invasive pulmonary aspergillosis in patients with chronic obstructive pulmonary disease
Qian HE ; Simei SHEN ; Wei ZHOU ; Yuwen RUI ; Hongxing LI ; Pei LI ; Fang ZHANG ; Xin SU ; Yi SHI
Journal of Medical Postgraduates 2017;30(4):380-383
Objective The purpose of this study was to investigate the value of serum galactomannan (GM) in the diagnosis of invasive pulmonary aspergillosis (IPA) in patients with chronic obstructive pulmonary disease (COPD).Methods We enrolled 60 COPD patients in the study, including 19 IPA and 41 non-IPA cases.We examined serum GM of the patients by ELISA, evaluate the value of serum GM test for the diagnosis of IPA in patients with COPD, and compared the GM values before and after treatment.Results With 0.5 as the positive cutoff value, the sensitivity, specificity, positive predictive value, and negative predictive value of serum GM were 57.9%, 95.3%, 84.6%, and 83.0%, respectively, with a high specificity and a low sensitivity.The 7 IPA cases showed a significantly decreased GM value after treatment as compared with the baseline (0.30±0.21 vs 1.48±1.37, P=0.004).Conclusion The serum GM test has a limited value in the diagnosis of IPA in patients with COPD, but dynamic monitoring of the changes of the serum GM value may help evaluate the patient's condition.
9.Effect of quantitative assessment of grading nursing model on nursing quality and satisfaction of psychiatric inpatients
Sha NIE ; Xiashu YAN ; Hongxing LI ; Xiaozhen SU ; Xiuqun MEI
Chinese Journal of Modern Nursing 2017;23(31):3969-3972
Objective To explore the effect of quantitative assessment of grading nursing model on nursing quality and satisfaction of psychiatric inpatients. Methods From September to December 2016, 77 psychiatric inpatients from a class Ⅲ grade A psychiatric hospital of Guangzhou were selected as the research object. The patients were randomly divided into two groups according to the order of hospitalization, 47 cases in the study group and 30 cases in the control group. The study group was the quantitative evaluation group, and the nurses grouped with the doctor. The medical team consisted of 2 nurses (1 nurse-in-charge or over and 1 senior nurse) and 1 doctor. The control group, that was, the traditional routine group, the doctor in charge was responsible for delivering the order, and the nursing staff was responsible for the implementation. After 6 weeks of the intervention of quantitative evaluation and classified nursing mode in psychiatric department, two groups of patients were investigated by using self-made general information questionnaire, grading nursing quality evaluation table and patient satisfaction questionnaire. Results The total average score of nursing quality of the study group was (97.61±2.19) points, the hospital satisfaction was (33.28±1.79) points, while in the control group the total average score of nursing quality was (96.48±1.37) points, the satisfaction score was (28.83±4.71) points. There was a significant difference in the score of nursing quality between the two groups (t=2.515, 5.802;P<0.05). Conclusions The preliminary results show that quantitative assessment of grading nursing model can improve nursing quality and hospitalization satisfaction of psychiatric hospitalized patients.
10.Study on groundwater radon concentrations and its dose contribution in some cities in China
Yunyun WU ; Hongxing CUI ; Bing SHANG ; Jianxiang LIU ; Xu SU
Chinese Journal of Radiological Medicine and Protection 2016;36(2):129-132,148
Objective To investigate the levels and distribution of radon concentrations in groundwater in some representative cities in China,and estimate the effective dose from inhaled radon released from domestic groundwater.Methods A total of 12 cities in 7 provinces (municipalities) were selected,including Beijing,Inner Mongolia,Ningxia,Shaanxi,Henan,Liaoning and Heilongjiang.In total,73 water samples from groundwater supply were taken.Radon concentrations in water samples were determined by using a continuous radon monitor with air-water exchanger.Results The average radon content in groundwater for drinking was 11.8 Bq/L in 12 cities in 7 provinces,ranging from 1.0 to 63.8 Bq/L.The radon concentrations in 37% water samples exceeded 1 1.1 Bq/L,the safe limit recommended for drinking water by the United States Environmental Protection Agency (EPA).The radon contents in all of the water samples was lower than the reference level 100 Bq/L recommended by World Health Organization (WHO).The average annual effective dose arising from inhaled radon released from groundwater was 29 μSv (2.4 to 160 μSv).Conclusions Generally,the effective dose from inhaled radon released from groundwater is negligibly low.However,in some areas dominated by granite bedrock,the dose contribution from radon released from groundwater to residents should be routinely monitored.

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