To screen potential hamster chymase 2 inhibitors, a high-throughput screening (HTS) model was established. Recombinant hamster chymase 2 with active form was cloned and expressed in E. coli. The HTS model with total volume of 50 microL in 384-well microplate was based on fluorescence analysis and was proved sensitive as well as specific (Z' = 0.84). A total of 40 080 samples (including 28 060 compounds and 12 020 natural products) were screened, and 613 samples with inhibition greater than 90% were selected for further rescreening. Finally, compounds J16647 and J16648 were identified with high inhibitory activity on chymase 2, and whose IC50 values were 0.823 and 0.690 micromol x L(-1), respectively.

To screen potential human soluble protein tyrosine phosphatase 1B (PTP1B) inhibitors, a high-throughput screening (HTS) model in 384-well microplate with total volume of 50 microL was established. Recombinant PTP1B was cloned and expressed in E. coli. with its specific substrate 4-nitrophenyl phosphate disodium salt hexahydrate (PNPP). The HTS model was based on enzyme reaction rate with enhanced sensitivity and specificity (Z' = 0.78). A total of 24,240 samples were screened, among them 80 samples with inhibition greater than 70% were selected for further rescreening. Finally, six compounds with high inhibitory activity were identified, whose IC50 values were 21.58, 18.39, 15.37, 11.92, 37.27, and 36.61 microg x mL(-1), separately. The results indicated that the method was stable, sensitive, reproducible and also suitable for high-throughput screening.

Objective To investigate the clinical application of 3.0 T mobile iMRI and neuronavigation in the microsurgical operation for the high grade gliomas in brain functional area.Methods The clinical data of 47 cases which were operated from April,2012 to August,2014 assisted by intraoperative magnetic resonance and neruonavigation system were analyzed retrospectively,including 19 cases of near the frontal motor areas,21 cases of closed to the dominant hemisphere language areas,and 7 cases of involved multiple lobes of the brain.The operative plans were made before the operative day using 3.0 T iMRI for T1-MPRAGE plain and enhancement magnetic resonance imaging sequence,diffusion tensor imaging (DTI) sequence and blood oxygenation level dependent functional MRI (BOLD-fMRI) sequence scanning.Before the start of operation,the margin of the tumor was marked on the scalp,and removed the tumor under the microscopy,according to the need 1-4 iMRI plain scan and enhanced scan were applied to reconstruct the real-time imaging of the residual tumors and corticospinal tract,and gained once more chances to remove the tumor repeatedly,until the tumor was removed totally,accurately and safely.Results The total resection rate increased from 63.8％ (30/47) to 95.7％ (45/47) by repeated resection,and 2 cases (4.3％ lesions) with subtotal resection.The dysfunction of motion and the language barrier got worse in 4 patients (8.5％).No cases with sever complication such as death and severe disability after operation.There were no intracranial hemorrhage,infection and other adverse events.Patients were followed up with nervous system symptoms and head MRI,the follow-up period was 3 months-2 years.Twenty-eight cases (59.6％) ob-tained good clinical efficacy;the dysfunction of motion and the language barrier got worse in 4 cases (8.5％);the symptoms and tumors recurrenced in 15 cases (31.9％).Conclusion The 3.0 T mobile iMRI system combined with functional neuronavigation can accurately display the relationships among the motor and language cortex,tumors and white matter fiber bundles real-timely.The extent of the tumor resection can be assessed accurately by real-time images provided by iMRI,and the residual tumor have chames to be resected repeatedly,until the tumors were resected totally before operation finished.The iMRI system can correct intraoperative brain shift timely.The total resection rate can be improved safely and accurately by one or more times resection.

[ ABSTRACT] AIM:To explore the regulatory effect of intermedin ( IMD) on pulmonary collagen synthesis and ac-cumulation in rats with pulmonary hypertension induced by high pulmonary blood flow.METHODS: Healthy male SD rats (n=20) were randomly divided into control group (n=7), shunt group (n=7) and shunt with IMD group (n=6).The shunting of abdominal aorta and inferior vena cava was produced in rats of shunt group and shunt with IMD group.After 8 weeks, IMD was administered into the rats of shunt with IMD group subcutaneously by mini-osmotic pump for 2 weeks.Mean pulmonary artery pressure (mPAP), relative medial thickness (RMT) of pulmonary arteries, contents of hydroxyproline, collagen type I and III, bone morphogenetic protein-2 (BMP-2), and the mRNA expression of procollagen I and III in lung tissues were measured and compared.RESULTS:Compared with control group, mPAP and RMT of medium and small pul-monary arteries in the rats of shunt group were significantly increased.Meanwhile, the lung hydroxyproline, collagens I and III and BMP-2 contents, and the mRNA expression of lung procollagen I and III were all significantly increased compared with control group.However, IMD significantly decreased mPAP, alleviated the changes of pulmonary vascular micro-struc-ture, decreased the collagen accumulation and pulmonary tissue homogenate BMP-2 contents, and inhibited the mRNA ex-pression of procollagen I and III in the lung tissue of shunting rats.CONCLUSION:IMD plays a protective role in the de-velopment of pulmonary hypertension and pulmonary vascular structural remodeling induced by high blood flow by inhibiting pulmonary collagen synthesis and accumulation, possibly in association with the BMP-2 pathway.

[ ABSTRACT] AIM:To illustrate the effect of methylene blue ( MB) on T-lymphocyte subsets and oxidative stress of the thymus in rats with paraquat ( PQ) poisoning.METHODS: Male SD rats ( n=40) were randomly assigned to 4 groups:normal group, control group, low-dose (2 mg? kg-1? d-1 ) MB group and high-dose (4 mg? kg-1? d-1 ) MB group.After 72 h, the pathological morphological changes of the thymus were observed under microscope with HE staining. The SOD activity and MDA content were measured by colorimetry method.The expression of Bcl-2, Bax, CD4 and CD8 was determined by immunohistochemical method.RESULTS:In MB group, the thymus tissue showed good corticomedul-lary demarcation.MDA content decreased and SOD activity increased, indicating that the ability of antioxidation enhanced. Bcl-2 and Bax expression was down-regulated, Bcl-2/Bax ratio increased, and CD4 positive cells increased.CONCLU-SION:MB protects against oxidative damage induced by PQ, and regulates the distribution of T-lymphocyte subsets in the cortex and medulla, thus relieving the persistent body damage.

Micro-droplets are widely used in the fields of drug controlled release,virus detection,synthetic of particulate materials,catalysts and so on due to their small size,large surface area,high speed,high throughput,uniform size,closed system,internal stability and other characteristics.The emergence and development of microfluidics technology provide a new platform for the generation and precise manipulation of size-controlled microdroplets with different structures and functional characteristics.The fundamentals,generation and manipulation of droplet-based microfluidics technology are introduced.Similarities and differences of droplets'conventional preparation methods and droplet-based microfluidics technology are compared and analyzed.Finally,the applications of droplet-based microfluidics for the synthesis of functional materials,bio-medicine and design of food structure etc.are comprehensively presented.In addition,the potential value and development direction of drop-based microfluidics are discussed and forecasted.

Objective To develop a lower limbs rehabilitative apparatus and explore its effects. Methods From January to September, 2016, 28 children with spastic cerebral palsy were divided into control group (n=14) and observation group (n=14) randomly. The control group received routine rehabilitation, while the observation group received self-made lower limbs rehabilitative apparatus training addition-ally. They were assessed with Gross Motor Function Measure (GMFM)-88 and Berg Balance Scale (BBS) before and three months after treatment. Results There was no significant difference in the scores of GMFM-88 and BBS between two groups before treatment (P>0.05), while they increased after treatment (t>6.124, P<0.001), and were higher in the observation group than in the control group (t>2.329, P<0.05). Conclusion Self-made lower limbs rehabilitative apparatus could help to improve the gross motor function and balance function in children with spastic cerebral palsy.

AIM: Metallothioneins (MTs) are cysteine-rich metal-binding proteins that exert cytoprotection during metal exposure and oxidative stress. The present study was designed to investigate whether MT can directly protect NTPase on nuclear envelope from damage induced by hydroxyl radical.METHODS: Isolated hepatic nuclei from rat liver were exposed to Fe 2+ /H 2O 2 with or without MT, and the NTPase activity on nuclei was assayed using ATP and GTP as substrate, respectively. RESULTS: Incubation of rat hepatic nuclei with the Fe 2+ /H 2O 2 (in ?mol?L -1 / ?mol?L -1 : 0 1/0 5, 0 5/2 5, 1/5, 5/25) resulted in a concentration-dependent decrease in nuclear NTPase activities ( P0 05 ). In addition, incubation of hepatic nuclei with only MT had no effect on nuclear NTPase activity. CONCLUSION: These data demonstrate that hydroxyl radical generated from Fe 2+ /H 2O 2 might attack nuclear NTPase. MT antagonistically reduces toxicity of Fe 2+ /H 2O 2 system to the NTPase.

AIM: To observe the effect of hydrogen sulfide (H_2S) on the rat cardiac function in vitro, to explorer the physiological regulation of endogenous H_2S on myocardial action. METHODS: H_2S concentration and production in the rat myocardial tissues were detected. The expression of CSE (a kind of key enzyme of endogenous H_2S production) mRNA in myocardial tissues was screened by RT-PCR. Langendorff apparatus was used to perfuse the rat heart in vitro. After 20 minutes of stabilization, NaHS (10~-6 -10~-3 mol/L) were added cumulatively in order to the perfusive fluid, and another group applied physiological concentration NaHS (4?10~-4 mol/L), continuously perfusion for 20 min, heart rate (HR), difference of left ventricular pressure (△LVP), left ventricular peak rate of contraction (+LV dp/dt_~max ), peak rate of relaxation (-LV dp/dt_~max ) and coronary perfusive flow (CPF) were measured at the times. Finally, glibenclamide was applied to block the K_~ATP channel of heart, to observe the effect of NaHS at physiological concentration on cardiac function. RESULTS: NaHS concentration-dependently inhibited left ventricular ?dp/dt_~max and △LVP (P

The low-risk mild hypertension constitutes a considerable proportion in hypertension. Through searching CNKI, Wanfang database, VIP database and PubMed database, literature during the last 10 years was collected and reviewed. It was indicated that excessive diagnosis, insufficient evidence of drug treatment, and poor drug adherence existed in low-risk mild hypertension, however, acupuncture at Renying (ST 9) and other therapies had remarkable effects. This paper mainly expounded the diagnosis and treatment status of low-risk mild hypertension as well as the research summary of acupuncture for low-risk mild hypertension.
Acupuncture Points ; Acupuncture Therapy ; trends ; Humans ; Hypertension ; therapy ; PubMed ; statistics & numerical data