1.Preparation and biological evaluation of 111 In-triphenylphosphonium cations
Liqiang LI ; Chengyan DONG ; Zhi YANG ; Bing JIA ; Fan WANG
Chinese Journal of Nuclear Medicine and Molecular Imaging 2017;37(1):20-24
Objective To synthesize 4 kinds of 111 In?TPP cations and evaluate their properties as tumor cationic radiotracers in vivo and in vitro. Methods DO3A?xy?TPP, DO3A?xy?mTPP, DO3A?xy?dmTPP and DO3A?xy?tmTPP were radiolabeled with 111 In;their lipid?water partition coefficients and in vivo and in vitro stability were evaluated. The binding affinities of 4 kinds of 111 In?radiotracers were determined in cell uptake and cell efflux assay using U87MG tumor cells. Biodistribution studies and γ imaging studies were performed using the athymic nude mice bearing U87MG human glioma xenografts to explore the biologi?cal properties of 4 kinds of 111 In?radiotracers. One?way analysis of variance was used. Results The labeling yields of 4 kinds of 111 In?radiotracers were all above 85%, and the radiochemical purity were all greater than 99% after purification. Binding assay in U87MG cells showed that 4 kinds of radiotracers had great binding affinity and cell retention ability, and 111In?DO3A?xy?mTPP had the best binding ratio (1?49%;F=177.8, P<0.05) . Gamma imaging and biodistribution results showed that the U87MG tumors could be clearly visualized by 111In?DO3A?xy?mTPP, 111In?DO3A?xy?dmTPP and 111In?DO3A?xy?tmTPP, and the liver uptake of the 3 tracers was lower than that of 111In?DO3A?xy?TPP. In particular, 111In?DO3A?xy?mTPP had the best tumor/liver ratio (0.13±0.05, 2 h postinjection;F=9.4, P<0?05). Conclusions The tumor?targeted ability of 111In?DO3A?xy?mTPP is better than those of 111In?DO3A?xy?dmTPP, 111In?DO3A?xy?tmTPP and 111In?DO3A?xy?TPP, suggesting that it has the potential to be a promising tumor cationic radiotracer.
2.The effect of mild hypothermia on the content of Ca~(2+)、Mg~(2+)、EAA in rat brain tissue and ET in plasma after acute cerebral infarction
Zhichao LIU ; Chengyan LI ; Hongjuan DONG ; Shanping MAO
Chinese Journal of Physical Medicine and Rehabilitation 2003;0(11):-
Objective To investigate the effect of m il d hypothermia on the content of Ca 2+、Mg 2+、EAA in rat brain tissue and ET in plasma after acute cerebral infarction. Methods Forty-eight Sprague-Dawley rats were randomly assigned into trial group and control group. Using the method of reformed line-thrombosis,the cerebral in farction models were established. The rats in the trial-group were cooled by mi ld hypothermia for half an hour, while those in the control group were subjected to no disposal. Every group was divided into 4 sub-groups according to the pos t-infarction disposal time. Every sub-group was composed of 6 SD rats and kill ed at the time points of 1 hour,2 hour,4 hour and 8 hour after infarction, respe ctively. Then the content of Ca 2+、Mg 2+、EAA in rat brain tissue an d ET in plasma were measured. ResultsThe post-infar ction content of Ca 2+、EAA and ET of trial-group increased mildly and Mg 2+ reduced very little. There was a significant statistical difference bet ween the trial group and the control group. Conclusion Mild hypothermia may significantly reverse the increase of the content of Ca 2+ and EAA and the fall of Mg 2+ and the increment of ET in plasma as well after acute cerebral infarction in experimental animals. So as a result, m ild hypothermia possesses protective effect on brain.
3.Radiation dosimetry and biodistribution of 68Ga-FAPI-04 PET in patients with hepatobiliary tumor
Haiqun XING ; Wenjia ZHU ; Chengyan DONG ; Jingnan WANG ; Ximin SHI ; Meiqi WU ; Shaobo YAO ; Fang LI ; Li HUO
Chinese Journal of Radiological Medicine and Protection 2021;41(4):293-298
Objective:To investigate the radiation dosimetry and biodistribution of 68Ga-FAPI-04 PET/CT in patients with hepatobiliary tumor. Methods:A total of six patients with hepatic lesions who underwent PET/CT examination in Peking Union Medical College Hospital were enrolled. After intravenous injection of radiotracer 68Ga-FAPI-04 at (170.57 ± 14.43) MBq, whole-body imaging were performed at the time points of 3, 10, 15, 20, 30 and 60 min, respectively. Biodistribution pattern was observed. Regions of interest were manually delineated. Radiation dosimetry of all target organs were calculated by Olinda/EXM software. Results:The radioactive uptake dissipated gradually in liver whereas it was relatively stable in tumor lesions. The average SUV max of tumor lesions reached the maximum value (13.87± 2.55) at 20 min after injection. The target-to-background ratio increased with time, reaching the maximum value (10.09 ± 8.17) at 30 min after injection. The average effective dose in total body was (0.020 ± 0.002) mSv/MBq and organ with the highest effective dose was bladder wall at (0.146 ± 0.035) mSv/MBq. Conclusions:The effective dose in total body of 68Ga-FAPI-04 was similar to that of 18F-FDG. 68Ga-FAPI-04 is expected to be a PET/CT radiotracer for hepatobiliary tumors in consideration of rapid tumor uptake, low accumulation of liver background, and no influence of blood sugar levels.
4.Preclinical and clinical translation research of 68Ga-labeled fibroblast activation protein inhibitor for PET imaging
Haiqun XING ; Ximin SHI ; Chengyan DONG ; Xuezhu WANG ; Xiaona JIN ; Yonghong DANG ; Wenjia ZHU ; Shaobo YAO ; Fang LI ; Li HUO
Chinese Journal of Nuclear Medicine and Molecular Imaging 2020;40(8):480-485
Objective:To prepare 68Ga-fibroblast activation protein inhibitor (FAPI)-04, and evaluate its biodistribution and imaging characteristics in animals and healthy volunteers, in order to investigate the clinical translation potential. Methods:68Ga-FAPI-04 was synthesized by a manual method and its radiolabeling yield, radiochemical purity, and stability ( in vivo and in vitro) were analyzed. ICR mice ( n=16) were scarified at 5, 30, 60 and 120 min postinjection of 68Ga-FAPI-04 (1.11 MBq) to measure radioactive counts in main organs. The dynamic mircoPET imaging was acquired for 60 min on 3 ICR mice, and tumor imaging capabilities were examined with nude mice bearing HepG2 tumors. Furthermore, 2 healthy volunteers (1 male with age of 64 years, 1 female with age of 56 years) were recruited for the investigation of probe biodistribution in humans. A serial whole-body dynamic PET/CT scan was performed immediately following injection. Results:68Ga-FAPI-04 was synthesized within 20 min with the radiochemical yield of (68.7±4.0)% (decay corrected). The radiochemical purities of 68Ga-FAPI-04 were over 99% and the products were stable for 180 min in vitro and for 90 min in blood. 68Ga-FAPI-04 was mainly cleared through urinary tracts, while other organs only showed mild tracer accumulation. MicroPET imaging showed high uptake of 68Ga-FAPI-04 in the tumor tissue of mice, and the ratio of tumor/liver was 2.14±0.01 (35 min). The PET/CT imaging results of healthy volunteers revealed 68Ga-FAPI-04 could be quickly cleared. Conclusion:68Ga-FAPI-04 has many advantages for PET imaging, such as easy labeling, good stability, quick clearance and low background signals in the liver, which can be used as an attractive PET tracer for detection hepatocellular carcinoma.
5.Guideline for the diagnosis and treatment of chronic refractory wounds in orthopedic trauma patients (version 2023)
Yuan XIONG ; Bobin MI ; Chenchen YAN ; Hui LI ; Wu ZHOU ; Yun SUN ; Tian XIA ; Faqi CAO ; Zhiyong HOU ; Tengbo YU ; Aixi YU ; Meng ZHAO ; Zhao XIE ; Jinmin ZHAO ; Xinbao WU ; Xieyuan JIANG ; Bin YU ; Dianying ZHANG ; Dankai WU ; Guangyao LIU ; Guodong LIU ; Qikai HUA ; Mengfei LIU ; Yiqiang HU ; Peng CHENG ; Hang XUE ; Li LU ; Xiangyu CHU ; Liangcong HU ; Lang CHEN ; Kangkang ZHA ; Chuanlu LIN ; Chengyan YU ; Ranyang TAO ; Ze LIN ; Xudong XIE ; Yanjiu HAN ; Xiaodong GUO ; Zhewei YE ; Qisheng ZHOU ; Yong LIU ; Junwen WANG ; Ping XIA ; Biao CHE ; Bing HU ; Chengjian HE ; Guanglin WANG ; Dongliang WANG ; Fengfei LIN ; Jiangdong NI ; Aiguo WANG ; Dehao FU ; Shiwu DONG ; Lin CHEN ; Xinzhong XU ; Jiacan SU ; Peifu TANG ; Baoguo JIANG ; Yingze ZHANG ; Xiaobing FU ; Guohui LIU
Chinese Journal of Trauma 2023;39(6):481-493
Chronic refractory wound (CRW) is one of the most challengeable issues in clinic due to complex pathogenesis, long course of disease and poor prognosis. Experts need to conduct systematic summary for the diagnosis and treatment of CRW due to complex pathogenesis and poor prognosis, and standard guidelines for the diagnosis and treatment of CRW should be created. The Guideline forthe diagnosis and treatment of chronic refractory wounds in orthopedic trauma patients ( version 2023) was created by the expert group organized by the Chinese Association of Orthopedic Surgeons, Chinese Orthopedic Association, Chinese Society of Traumatology, and Trauma Orthopedics and Multiple Traumatology Group of Emergency Resuscitation Committee of Chinese Medical Doctor Association after the clinical problems were chosen based on demand-driven principles and principles of evidence-based medicine. The guideline systematically elaborated CRW from aspects of the epidemiology, diagnosis, treatment, postoperative management, complication prevention and comorbidity management, and rehabilitation and health education, and 9 recommendations were finally proposed to provide a reliable clinical reference for the diagnosis and treatment of CRW.