Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. We have previously identified the benzoyl sulfathiazole derivative II as a non-competitive PTP1B inhibitor with in vivo insulin sensitizing effects. Preliminary SAR study on this compound series has been carried out herein, and thirteen new compounds have been designed and synthesized. Among them, compound 10 exhibited potent inhibition against human recombinant PTP1B with the IC50 value of 3.97 micromol x L(-1), and is comparable to that of compound II.
Humans ; Protein Tyrosine Phosphatase, Non-Receptor Type 1 ; antagonists & inhibitors ; Structure-Activity Relationship ; Sulfathiazoles ; chemistry ; pharmacology

Objective To evaluate the efficacy and safety of 308-nm excimer light in the treatment of stable vitiligo. Methods Thirty patients with stable vitiligo were enrolled in this clinical trial. All the subjects received the treatment with 308-nm excimer light on a twice-weekly schedule for 3 months. Results The repigmentation rate was 95.0%, 75.0% and 66.7% for lesions in the face and neck, trunk and limbs, with the treatment sessions averaging 10.22 ± 1.60, 19.10 ± 2.38, 37.74 ± 3.06, respectively, and accumulative irradiation dose averaging 7.50 ± 3.45, 10.60 ± 1.01, 18.56 ± 3.05 J/cm2 respectively. Significant differences were observed in the repigmentation rate and treatment sessions between the lesions in the face and neck, trunk and limbs (all P ＜ 0.05). No severe side effects were seen during the treatment. Conclusion 308-nm excimer light is effective and safe for the treatment of vitiligo.

Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. We have previously identified the benzoyl sulfathiazole derivative II as a non-competitive PTP1B inhibitor with in vivo insulin sensitizing effects. Preliminary SAR study on this compound series has been carried out herein, and thirteen new compounds have been designed and synthesized. Among them, compound 10 exhibited potent inhibition against human recombinant PTP1B with the IC50 value of 3.97 micromol x L(-1), and is comparable to that of compound II.

The purpose of this article was to investigate the application of Google Earth (GE)in the Three Dimensional Visualization(TDV)of the warnings signaled by early warning system of infectious disease.As an example.the prospective space-time scan statistics was used by mimicking daily prospective analyses of bacillary dysentery data from Shanghai municipality,Zhejiang province and Jiangsu province in 2005.Then one of the warnings was picked to illustrate the visualization of GE.GE could vividly display the results in three dimensions containing the complex information including date,areas,observed numbers,expected numbers ere.GE seemed a useful tool for infectious disease surveillance and had potential important values in reflecting the emergency response situation.The development of integrated system which consisted of GE,the infectious disease reporting system and cluster detection methods need to be emphasized for further research.

Objective To investigate the diagnostic significance of endoscopic findings in Henoch-Schonlein purpura(HSP),especially when abdominal pain preceded the cutaneous lesions.Methods The clinical data and gastroscopic findings in 37 cases of children with HSP were studied and analysed retrospectively in order to detect the pathological changes in the stomach and duodenum mucosa.The biopsy was taken in the pathological changeing place,and the relationship between clinical and endoscopic findings was analyzed.Results Detection rate of the pathological changes in the stomach and duodenum mucosa was 62.2%,31.3% of which experienced only cutaneous lesions,100% of which presented the acute abdominal pain.Three patients were not checked up the pathological changes.Of them,1 had arthritis,2 had Henoch-Schonlein nephritis.Characteristically endoscopic findings in the stomach and duodenum mucosa were found.The endoscopic findings included anabrosis,hyperemia,edema and hemorrhage.Conclusions Detection rate of the pathological changes in the stomach and duodenum mucosa is higher.Endoscopy is very helpful to the early diagnosis of HSP in children,especially abdominal pain presented firstly.

Humans ; Acupuncture Therapy ; Neck Injuries ; Vertigo

Background The sex hormones plays an important role in the incidence of dry eye,especially for the regulation of function.However,the effects of sex hormones on lacrimal gland epithelial cells are below understand.Objective This study was to investgate the effects of estradiol and testosterone on the apoptosis of lacrimal gland cells induced by H2O2.Methods The lacrimal gland tissue was obtained from 2- or 3-month-old clean male New Zealand rabbits and the lacrimal gland epithelial cells were cultured in vitro using esplant culture method.The cells were identified by pan cytokeratin antibodies with immunocytochemistry.lacrimal gland epithelial cells were incubated in the 96 well plate at the density of 5 × l04 cells/ml for 44 hours.Estradiol or testosterone with the concentrations of 1 × 10-5,1 × 10-6,1 × 10-7,1 × 10-8 mol/L were added into the medium for 24 hours respectively and 1× 10-4 mol/L H2O2 treated the cells for 1 hour to induce the apoptosis in experimental groups.The cells treated by only 1 × 10-4 mol/L H2O2 were used as apoptotic control group,and the cells cultured by regular method were used as blank control group.The cell viability in different groups was detected using MTT at 570 nm ( A570 ),and the apoptotic rates of the cells were assayed using Annexin V/PI double staining.This use and maintain of experimental animals followed the Regulation for the Administration of Affairs Concerning Experimental Animals by State Science and Technology Commission.Results The cultured cells showed the irregular polygon in shape,and about 80％ cells was positive response for cytokeratin.MTT assay showed that the lower A570 values were detected in the H2O2-induced group,various concentrations of estradiol or testosterone groups compared with blank control group (P＜0.01 ).The A570 values in 1 × 10-5,1 × 10-6,1 × 10-7 mol/L estradiol groups or 1 × 10-6 mol/L testosterone group were significantly higher than ones of H2 O2-induced group (P＜0.01 ).Compared with corresponding concentrations of testosterone groups,the A570values in various concentrations of estradiol groups were elevated( P＜0.01 ).The apoptosis rates at the early and later phase were significantly declined in both estradiol group and testosterone group in comparison with H2 O2-induced group (P ＜ 0.01,P＜ 0.05 ),and those in estradiol group were lower than the testosterone group( P＜0.01,P＜0.05 ).Conclusions Estradiol and testosterone suppress the apoptosis of lacrimal gland cells induced by H2O2,and the stronger effect is found in estrogen.The inhibition of estrogen on lacrimal gland cell apoptosis show a dose-dependent manner to some extent.

Objective To evaluate the effect of electroacupuncture (EA) preconditioning on the activity of dynamin-related protein 1 (Drp1) in brain tissues during cerebral ischemia-reperfusion (I/R) in rats.Methods A total of 126 pathogen-free healthy adult male Wistar rats,weighing 250-300 g,were divided into 3 groups (n =42 each) using a random number table:sham operation group (group S),group I/R and EA preconditioning group (group EA).In group S,the blood vessels were only separated but not occluded.In group I/R,a nylon thread with rounded tip was inserted into the left middle cerebral artery advanced cranially until resistance was met,and middle cerebral artery occlusion was maintained for 2 h followed by reperfusion.In group EA,Baihui acupoints were stimulated with an electric stimulator (2/ 15 Hz disperse-dense waves,intensity 1 mA) for 30 min,lasting for 5 consecutive days,and the model of focal cerebral I/R was established at 24 h after the last stimulation.At 6,24 and 48 h of reperfusion,the neurologic deficit was assessed and scored,the mitochondria in the cerebral cortex on the ischemic side were extracted,the expression of Drpl in mitochondria was detected using Western blot,the mitochondrial uhrastructure was examined with an electron microscope,and neuroapoptosis was measured using TUNEL.The apoptosis rate was calculated.Results Compared with group S,the neurological deficit score and apoptosis rate were significantly increased,and the expression of Drpl in mitochondria was up-regulated at each time point in I/R and EA groups (P＜0.05).Compared with group I/R,the neurological deficit score and apoptosis rate were significantly decreased,and the expression of Drpl in mitochondria was down-regulated at each time point in group EA (P＜0.05).Conclusion The mechanism by which EA preconditioning reduces cerebral I/R injury may be related to inhibiting the activity of Drpl and thus inhibiting the excessive fission of mitochondria in rats.

Objective To evaluate the effect of electroacupuncture (EA) preconditioning on inositol-requiring kinase 1 (IRE1)-X-box binding protein 1 (XBP1) signaling pathway in endoplasmic reticulum in the cortex in a rat model of cerebral ischemia-reperfusion (I/R).Methods One hundred and eight pathogen-free healthy male Sprague-Dawley rats,aged 8-12 weeks,weighing 200-250 g,were assigned into 3 groups (n =36 each) using a random number table:sham operation group (group S),group I/R and EA preconditioning group (group EA).Focal cerebral I/R was induced by occlusion of right middle cerebral arteries for 2 h followed by reperfusion in rats anesthetized with chloral hydrate.In group EA,Baihui acupoints were stimulated with an electric stimulator for 30 min once a day for 5 consecutive days starting from 5 days before ischemia,and the model was established at 24 h after the last preconditioning.Rats were sacrificed after neurological deficit was scored at 6,12 and 24 h of reperfusion,brains were removed,and the ischemic area in cerebral cortex was isolated for examination of the cell ultrastructure (with an electronic microscope) and for determination of the expression of IRE1 and XBP1 (by Western blot).Results Compared with group S,the neurological deficit scores were significantly increased,and the expression of IRE1 and XBP1 in the ischemic area was up-regulated at each time point in I/R and EA groups (P＜0.01).Compared with group I/R,the neurological deficit scores were significantly decreased,and the expression of IRE1 and XBP1 was up-regulated at each time point in group EA (P＜0.05).The cell damage in the ischemic area in cerebral cortex was significantly attenuated in group EA when compared with group I/R.Conclusion The mechanism by which EA preconditioning attenuates cerebral I/R injury is related to activating IRE1-XBP 1 signaling pathway and relieving endoplasmic reticulum stress in rats.

OBJECTIVETo observe the characteristics of uterine contraction and stages of labor during delivery under continuous epidural block anesthesia.

METHODSTotaling 213 parturients in spontaneous labor under epidural block anesthesia with dilated cervical orifice of 3 cm were monitored for the contraction cycle, duration, intensity and curve types of uterine contraction, and recordings were made for 30 min before and 30, 60 and 120 min after the anesthesia took effect, respectively. The duration of the active phase in the first, second and third stages of labor was compared between 421 cases with anesthesia and 237 without anesthesia.

RESULTSSignificant difference was noted in the objective indexes of uterine contraction recorded after anesthesia had taken effect (P<0.05) in comparison with those before anesthesia, suggesting significantly attenuated uterine contraction after anesthesia, whereas these indexes underwent no significant further variation as compared between different time points after anesthesia (P>0.05). The average active phase in the first stage was significantly shorter in anesthesia group than that in the control group (P<0.05), but the average duration of the second and third stages of labor differed little between the two groups with appropriate use of oxytocin under strict monitoring (P>0.05). The rates of obstetric forceps utilization and use of oxytocin were higher in anesthesia group than in the control group (P<0.05).

CONCLUSIONEpidural block anesthesia produces certain influences on uterine contraction and stages of labor during delivery, for which appropriate treatment measures may prove beneficial.

Adult ; Anesthesia, Epidural ; methods ; Anesthesia, Obstetrical ; methods ; Female ; Humans ; Labor, Obstetric ; physiology ; Pregnancy ; Time Factors ; Uterine Contraction ; drug effects ; Uterus ; drug effects ; physiology