Automatic synthesis of 18F-fallypride and evaluation of microPET/CT imaging effect / 中华核医学与分子影像杂志

Objective:To establish an optimized automatic synthesis method of 18F-fallypride, and evaluate its biodistribution and microPET/CT characteristics. Methods:18F-fallypride was automatically prepared by AIO synthesis module and disposable cassette & reagents kit. The crude product was purified by a dedicated coupled column (HLB+ Alumin-N) to obtain the final product. Radiochemical purity and radiolabeling yield were determined. Parkinson′s disease (PD) model mice and rats were established. The radioactive distribution of different organs of PD model mice ( n=24) were monitored. The distribution process of the agent in the SD rat brain (PD model, n=6; normal rat, n=6) were evaluated by microPET/CT imaging. Results:The radiochemical yield of 18F-fallypride synthesized by automatic synthesis module was stable at (10±1)% ( n=5, no decay corrected). The total synthesis time was about 40 min. The radiochemical purity of 18F-fallypride was more than 95%, and the radiochemical purities were also over 95% after being stored in saline and serum for 120 min at room temperature. 18F-fallypride was mainly excreted by the kidneys, and it was less radioactive intake in the liver and spleen in PD mice. MicroPET/CT imaging showed that higher accumulation of 18F-fallypride was noted in corpus striatum and the SUV ratio of PD group was lower than that of control group (5.00±0.93 vs 6.53±1.96). Conclusion:18F-fallypride can be successfully prepared automatically by improved multifunctional module, with the advantages of convenient preparation, stable radiochemical yield, satisfying purity and quality control, so it can be used in the follow-up standardized production of Good Manufacture Practice (GMP) system.

Influence of sildenafil and buflomedil on survival of randomized flaps in rats: an experimental study / Influência do buflomedil e do sildenafil na sobrevivência de retalhos randomizados em ratos: estudo experimental

BACKGROUND: Microcirculation dysfunction, as a consequence of localized vascular insufficiency, is considered to be one of the dominant causes of surgical flap necrosis. Several vasoactive drugs have been tested for the pharmacological treatment of tissue ischemia, with varying degrees of success. This study aimed to assess the impact of buflomedil and sildenafil on the viability of random skin flaps in rats. METHODS: Caudally pedicled skin flaps (10 x 3 cm) were created on the backs of rats. The animals were randomly assigned, in groups of 10, to three treatment groups: one group served as the vehicle control group, one group received buflomedil (10 mg/kg/d, orally), and a third group received the same dosage of sildenafil. Following seven days of dosing, the animals were sacrificed, and the viable flap area was determined. RESULTS: The average viable flap area for each group was: 16.2 ± 3.56 cm² (control group), 17.69 ± 2.54 cm² (buflomedil group), and 18.28 ± 3.74 cm² (sildenafil group). Data analysis by the Kruskal-Wallis test failed to show a statistically significant difference between the three groups. CONCLUSIONS: Neither buflomedil nor sildenafil showed a reduction in the necrotic area of random skin flaps in rats.

INTRODUÇÃO: A insuficiência no aporte sanguíneo e a consequente disfunção gerada no fluxo da microcirculação são consideradas causas dominantes de sofrimento de um retalho cirúrgico. Várias drogas vasoativas têm sido testadas para o tratamento farmacológico da isquemia tecidual, porém com graus variáveis de sucesso. Este estudo teve como objetivo avaliar a influência do buflomedil e do sildenafil na viabilidade de retalhos cutâneos ao acaso, em ratos. MÉTODO: Foram confeccionados retalhos cutâneos no dorso de ratos, com dimensões de 10 x 3 cm e base caudal. Foram utilizados 30 ratos, divididos em três grupos de 10 ratos cada: um grupo que recebeu apenas o veículo da solução (grupo controle); um grupo que recebeu buflomedil (grupo buflomedil); e um terceiro grupo que recebeu sildenafil (grupo sildenafil). A via de administração foi a oral e a dose foi de 10 mg/kg/dia para cada droga, durante sete dias. Ao final desse período, os animais foram sacrificados, sendo realizada a determinação das áreas viáveis dos retalhos. RESULTADOS: A média das áreas viáveis dos retalhos foi de 16,2 ± 3,56 cm² para o grupo controle, de 17,69 ± 2,54 cm² para o grupo buflomedil, e de 18,28 ± 3,74 cm² para o grupo sildenafil. A análise dos dados pelo teste de Kruskal-Wallis não demonstrou significância estatística entre os três grupos. CONCLUSÕES: A utilização do buflomedil e do sildenafil demonstrou não diminuir a área de necrose de retalhos randomizados em ratos.

Protective effect of pyrrolidine dithiocarbamate pretreatment on lung against LPS-induced injury in rats / 中华麻醉学杂志

Objective To investigate the protective effect of pyrrolidine dithiocarbamate (PDTC) pretreatment on lung agaillst LPS-indueed injury in rats.Methods Fifty-four Wistar rats of both sexes weighing 180-220 g were randomly idivided into 3 groups:group I normal control(group C,n=6);group Ⅱ LPS (group L,n=24)and group Ⅲ PDTC(group P,n=24).Endotoxemia was induced by intraperitoneal LPS 8 mg/kg in group Ⅱ and Ⅲ.In group Ⅲ PDTC 120 mg/kg was injected iv at 30 min before IP LPS.Venous blood samples were collected at 1,3,6 and 12 h after LPS administration in group L and P and after normal saline administration in group C for determination of serum IL-6 concentration by ELISA.Six animals were killed at each time point after blood sample collection.The lungs were removed for microscopic examination and determination of W/D lung weight ratio,HSP70 expression and NF-κB activity.Results Intraperitoneal LPS significantly increased serum IL-6 concentration and W/D lung weight ratio,HSP70 expression and NF-κB activity in group Ⅱ.PDTC pretreatment significantly attenuated LPS-induced increase in serum IL-6 concentration,W/D lung weight ratio andNF-κB activity.The lung histologic dalnage induced by LPS Wag also ameliorated by pretreatment with PDTC.Conclusion Pyrrolidine dithiocarbamate pretreatment Can protect lung against LPS-induced injury through inhibition of activation of lung tissue NF-κB and up-regulation of expression of HSP70.

Effect of the NF-?B inhibitor pyrrolidine dithiocarbamate on the apoptosis and proliferation of mesangial cells in the rat with anti-thymocyte serum nephritis / 中国病理生理杂志

AIM: To explore the effect of pyrrolidine dithiocarbamate (PDTC), the specific inhibitor of NF-?B, on anti-thymocyte serum nephritis (ATSN) in rats. METHODS: The rat model of ATSN was reproduced with rabbit anti-thymocyte serum (ATS). The rats were divided into ATSN group, ATSN+PDTC group and control group. The expression of NF-?B p65 and the apoptosis, lysis as well as proliferation of mesangial cells (MC) were examined by immunohistochemical staining, Tdt-mediated X-dUTP nick end labeling (TUNEL), light microscope and electron microscope at 40 minutes, 24 hours and 7 days after injection of ATS or normal serum. RESULTS: The expression of glomerular NF-?B p65 in the ATSN group was observed with significant difference compared to controls at 40 min (P