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.

Objective To assess the efficacy and safety of dl-3-butylphthalide on the treatment of acute ischemic stroke. Methods A total of 197 patients who were in the period of 72 hours of first attack of ischemic stroke of internal carotid artery with NIHSS from 5 to 25 scores were enrolled in this multi-center, randomized, double-blind and aspirin-control study. Compound " Dan Shen" was used as a baseline therapy. Results Basical recovery plus significant improvement was seen in 74.7% of the patients in dl-3-butylphthalide group and 60.9% in aspirin group (CMH value 4.0,P=0.047);There was a significant improvement for dl-3-butylphthalide group regarding NIHSS total score, total score difference value and Barthel index on the day 11th and 21st after treatment compared with control group. The main adverse reaction of dl-3-butylphthalide was increased aminotransferase and mainly the slight increase of aspartate aminotransferase, by 4.34% and 0 respectively. Conclusion dl-3-butyiphthalide should be regarded as an effective and safe treatment for ischemic stroke and a treatment without severe side effects.

Objective:To investigate the effect of S14G-humanin (HNG) on spatial learning and memory abilities and hippocampal neuron autophagy in amyloid precursor protein (APP)/presenolin-1 (PS1) double-transgenic mice.Methods:The APP/PSl transgenic mice were randomly divided into model group and HNG treatment group ( n=8). Another 8 C57BL/6J mice were chosen as controls; 0.5 mL double-steamed water was intraperitoneally injected into mice in the control group and model group every day, and 0.5 mL of HNG (50 μg/kg) was intraperitoneally injected into mice in the HNG treatment group every day; after 4 weeks of continuous injection, Morris water maze test was used to test the spatial learning and memory abilities of mice in each group. Western blotting and reverse transcription-PCR were used to detect the protein and mRNA expressions of ubiquitin like kinase1 (ULK1), P62, anti-microtubule associated protein 1 light chain 3 (LC3) II/LC3 I and cathepsin D in the hippocampus. Immunohistochemical staining was used to detect the deposition of amyloid β protein (Aβ) in the hippocampus of mice in each group. Results:Morris water maze test showed that the escape latency of mice in the control group, HNG treatment group and model group was statistically prolonged in turn, and the number of times traversing through the quadrant of the original platform was significantly smaller in turn ( P<0.05). Western blotting and reverse transcription-PCR showed that the ULK1 protein and mRNA expressions in the hippocampus decreased successively, P62 protein and mRNA expressions increased successively, LC3 II protein/LC3 I protein and LC3 II mRNA/ LC3 I mRNA ratio increased successively, and cathepsin D protein and mRNA expressions decreased successively in the control group, HNG treatment group and model group, with significant differences ( P<0.05). Immunohistochemical staining showed that the Aβ positive expressions in the hippocampal neurons of the control group, HNG treatment group and model group increased successively, with statistical differences ( P<0.05). Conclusion:HNG treatment can improve the spatial learning and memory abilities, which may be attributed to ameliorate autophagic network dysfunction and reduce Aβ plaques in the hippocampi of APP/PSl transgenic mice.

Objective : To explore the changes of tryptophan-2,3-dioxygenase 2(TDO2) expression and its mediated kynurenine(Kyn) pathway in different inflammatory stages(initial period, peak period and remission period) of adjuvant arthritis in rats. Methods: A rat model of AA was established.AA rats were sacrificed at different stages of inflammation.The pathological changes of joint synovium and liver were observed by HE staining; TDO2 expression in joint synovial tissue and liver tissue was detected by immunohistochemistry; High performance liquid chromatography was used to detect tryptophan(Trp) and Kyn levels in serum and liver. Results : Compared with the normal group, AA rats showed similar clinical and pathological features to RA.The expression of TDO2 in rat joint synovium and liver tissue increased during the peak period and remission period(P<0.05).Trp levels in serum of AA rats at each inflammation stage decreased, and Kyn levels increased in the initial stage(P<0.01);Trp levels in the liver tissues of rats at the peak period decreased, Kyn levels increased, and Kyn/Trp ratio increased(P<0.01). Conclusion TDO2 may play an important role in the peak period of AA,and mediate Kyn metabolism to participate in the occurrence and development of RA.