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.Research progress on the chemical composition and antidepressant mechanism of volatile oils of traditional Chinese medicine
Yifei ZHANG ; Lu CHENG ; Mingshi REN ; Dao GUO ; Fengjiao KUANG ; Zonghua KANG ; Jianguang LUO ; Feihua WU
Journal of China Pharmaceutical University 2025;56(1):22-30
Depressive disorder is a mental illness characterized by poor mood and cognitive dysfunction caused by a range of complicated factors. Antidepressants have strong short-term efficacy in clinical application, yet with significant adverse effects and resistance in long-term use. Essential oils are small molecular compounds mainly composed of monoterpenes and sesquiterpenes, most of which are characterized by aromatic odors, easy permeability through the blood-brain barrier, and low toxic side effects. Volatile oil from traditional Chinese medicine can regulate neurotransmitter monoamine, hypothalamic-pituitary-adrenal axis, brain-derived neurotrophic factor, neuroinflammation and oxidative stress, and intestinal microbiota-gut-brain axis to exert an antidepressant effect through multiple pathways and targets. This review summarizes the main antidepressant chemical components of essential oil of traditional Chinese medicine, their pharmacological mechanisms and clinical application, aiming to provide some reference for further development and clinical application of essential oil of traditional Chinese medicine.
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.Construction of an index system of ideological and political education elements of Health Assessment course based on consensus methods
Zonghua WANG ; Li LIN ; Jiangshan FAN ; Lingfang HUANG ; Weiwei LIU ; Yu LUO
Chinese Journal of Medical Education Research 2024;23(4):449-454
Objective:To construct an index system for including ideological and political education elements and cases in the Health Assessment course, and to provide a reference for the evaluation of ideological and political teaching of the Health Assessment course.Methods:By using literature analysis, the nominal group method, and the Delphi expert consultation method, we determined indicators for ideological and political elements and case inclusion criteria for the undergraduate nursing course Health Assessment. The analytic hierarchy method was applied to quantify the items and determine the final weights of the indicators at each level.Results:The response rates of two rounds of expert consultation were both 100%. The authority coefficient of the experts was 0.880. For the second-round consultation on the system of ideological and political elements, the coefficient of variation was 0.078, and the Kendall's coefficient of concordance was 0.334. For the second-round consultation on the inclusion criteria for ideological and political cases, the coefficient of variation was 0.075, and the Kendall's coefficient of concordance was 0.312. Finally, we determined 6 first-level indicators and 30 second-level indicators for the ideological and political elements of the Health Assessment course, and 9 indicators for the inclusion of ideological and political cases for the Health Assessment course.Conclusions:The established index system for the ideological and political elements and cases of the Health Assessment course for nursing undergraduates is reasonable, scientific, and reliable, which can provide a reference for subsequent construction of the ideological and political teaching system for the Health Assessment course.
5.Coping ways and influence factors of the migrant workers of the generation after 90s in Shenzhen
Suwen CHEN ; He WU ; Shike LUO ; Xiuling HUANG ; Jing GAN ; Zonghua XIANG ; Jiarong LIU
Chinese Journal of Modern Nursing 2014;20(21):2617-2620
Objective To analyze the coping ways and influence factors of the migrant workers of the generation after 90s in Shenzhen.Methods By cluster sampling, 614 migrant workers of the generation after 90 s were surveyed with demographic data and the Simplified Coping Style questionnaire ( SCSQ ) .Results Among 614 participants the score of coping ways was (1.85 ±0.44), higher than the norm, and the negative coping score was (1.14 ±0.52), lower than the norm.The differences were statistical significant (t =-3.87,-21.34, respectively;P<0.01).There were 487 participants (79.3%) in the normal state of positive coping ways,and 376 participants (61.2%) in the normal state of negative coping ways .The education level and gender were the influence factors of coping ways , within which the education level had a significant positive effect on the coping ways (F=4.015, P=0.019), and the influence factors had a significant negative effect on the coping ways (t=3.230, P=0.001).Conclusions Most of the employee of the generation after 90 s are at a normal state of coping , and have preferable coping ways .The education level and gender are the factors that influence the ways of the behavior and reaction .The inferiority, timidity, atresia and loneliness were found among these employee during the investigation .

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