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@#In order to improve the yield and simplify the operation, the synthesizing process of JAK3 inhibitor tofacitinib citrate was improved based on the analysis of the methods previously published.Using 2, 4-dichloro-7H-pyrrolo [2, 3-d] pyrimidine and (3R, 4R)-1-benzyl-N, 4-dimethylpiperidin-3-amine dihydrochloride as starting materials, tofacitinib citrate was obtained through four steps of nucleophilic substitution, catalytic transfer hydrogenation, cyanide acetylation and citrate salt, and its crystal form was consistent with the original research.After optimization, the yield was better than those reported in literature, and the mild reaction conditions were suitable for industrial production.
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Objective:To explore the risk factors for hyperlipidemic acute pancreatitis (HTGP).Methods:The clincial data of 169 HTGP cases admitted in Capital Medical University Attached Xuanwu Hospital from September 2012 to December 2018 were retrospectively analyzed. Patients were divided into severe HTGP group ( n=63) and mild or moderately severe HTGP group ( n=106). Clinical data were compared between two groups and variables with statistically significance and clinical values were chosen and included for binary logistic regression to explore the independent risk factors for severe HTGP. Results:Severe HTGP patients′ heart beat and respiratory rate were significantly higher than moderately severe or mild HTGP cases, while the percentage of patients with previous AP history in severe HTGP group was obviously lower than moderately severe or mild HTGP cases. There were no statistically significant differences on other baseline data and previous history. Severe HTGP patients had significantly higher white blood cell, mean platelet volume, erythrocyte sedimentation rate, total protein, C-reaction protein on first day, C-reaction protein on third day, amylase, lipase, triacylglycerol, prothrombin time, D-dimer, fibrinogen, CTSI, APACHEⅡ score and Ranson score than those in moderately severe or mild HTGP cases; the lymphocyte count, albumin-globulin ratio, uric acid, apolipoprotein-A1, blood calcium, prothrombin activity were obviously lower than those in moderately severe or mild HTGP cases; and all the differences were statistically significant. Triglyceride and CRP on the first and third day, CTSI, APACHEⅡ score and Ranson score were included for binary logistic regression model, and the results showed that triglyceride on the first day ( OR=1.08, 95% CI 1.02-1.14, P=0.01), C-reaction protein on the third day ( OR=1.01, 95% CI 1.00-1.01, P<0.01), CTSI score( OR=1.51, 95% CI 1.06-2.13, P=0.02), APACHEⅡ score( OR=1.22, 95% CI 1.07-1.40, P<0.01)were the risk factors of severe HTGP, while triglyceride on the third day ( OR=0.8, 95% CI 0.69-0.91, P=0.00)was the protective factor of severe HTGP. Conclusions:Triglyceride on the first day, C-reaction protein on the third day, CTSI score and APACHEⅡ score were the risk factors of severe HTGP, which deserve special attention.
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Objective@#To explore the risk factors for hyperlipidemic acute pancreatitis (HTGP).@*Methods@#The clincial data of 169 HTGP cases admitted in Capital Medical University Attached Xuanwu Hospital from September 2012 to December 2018 were retrospectively analyzed. Patients were divided into severe HTGP group (n=63) and mild or moderately severe HTGP group (n=106). Clinical data were compared between two groups and variables with statistically significance and clinical values were chosen and included for binary logistic regression to explore the independent risk factors for severe HTGP.@*Results@#Severe HTGP patients′ heart beat and respiratory rate were significantly higher than moderately severe or mild HTGP cases, while the percentage of patients with previous AP history in severe HTGP group was obviously lower than moderately severe or mild HTGP cases. There were no statistically significant differences on other baseline data and previous history. Severe HTGP patients had significantly higher white blood cell, mean platelet volume, erythrocyte sedimentation rate, total protein, C-reaction protein on first day, C-reaction protein on third day, amylase, lipase, triacylglycerol, prothrombin time, D-dimer, fibrinogen, CTSI, APACHEⅡ score and Ranson score than those in moderately severe or mild HTGP cases; the lymphocyte count, albumin-globulin ratio, uric acid, apolipoprotein-A1, blood calcium, prothrombin activity were obviously lower than those in moderately severe or mild HTGP cases; and all the differences were statistically significant. Triglyceride and CRP on the first and third day, CTSI, APACHEⅡ score and Ranson score were included for binary logistic regression model, and the results showed that triglyceride on the first day (OR=1.08, 95% CI 1.02-1.14, P=0.01), C-reaction protein on the third day (OR=1.01, 95% CI 1.00-1.01, P<0.01), CTSI score(OR=1.51, 95% CI 1.06-2.13, P=0.02), APACHEⅡ score(OR=1.22, 95% CI 1.07-1.40, P<0.01)were the risk factors of severe HTGP, while triglyceride on the third day (OR=0.8, 95% CI 0.69-0.91, P=0.00)was the protective factor of severe HTGP.@*Conclusions@#Triglyceride on the first day, C-reaction protein on the third day, CTSI score and APACHEⅡ score were the risk factors of severe HTGP, which deserve special attention.
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ETS-1 is a transcription factor that is a member of the E26 transformation-specific (ETS) family. Galanin receptor 2 (GalR2), a subtype of receptors of the neuropeptide galanin, has been shown to have an antidepressant-like effect after activation in rodents. Our previous study has shown that overexpression of ETS-1 increases the expression of GalR2 in PC12 phaeochromocytoma cells. However, whether ETS-1 has an antidepressant-like effect is still unclear. In this study, we found that chronic mild stress (CMS) decreased the expression of both ETS-1 and GalR2 in the ventral hippocampus of rats. Meanwhile, we demonstrated that overexpression of ETS-1 increased the expression of GalR2 in primary hippocampal neurons. Importantly, we showed that overexpression of ETS-1 in the ventral hippocampus counteracted the depression-like behaviors of CMS rats. Furthermore, we found that overexpression of ETS-1 increased the level of downstream phosphorylated extracellular signal-regulated protein kinases 1 and 2 (p-ERK1/2) of GalR2 in the ventral hippocampus of CMS rats. Taken together, our findings suggest that ETS-1 has an antidepressant-like effect in rats, which might be mediated by increasing the level of GalR2 and its downstream p-ERK1/2 in the ventral hippocampus.
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Objective@#To explore the correlation of apolipoprotein levels with the severity of hyperlipidemic acute pancreatitis.@*Methods@#Clinical date of 169 patients with hyperlipidemic acute pancreatitis (AP) admitted in our hospital from September 2012 to December 2018 were retrospectively analyzed. Apolipoprotein (Apo) AⅠ, Apo B, Apo B/Apo AⅠ ratio were compared among hyperlipidemic AP patients with different severity. Pearson correlation analysis was conducted to explore the correlation of Apo AⅠ, Apo B, Apo B/Apo AⅠ with Atlanta classification, CTSI score, APACHE-Ⅱscore, RANSON score and C-reaction protein level. The optimal cut-off point of apolipoproteins for predict the severe hyperlipidemic AP was determined by ROC curve. The local and systemic complications of pancreatitis patients with different Apo levels were compared with chi-square test.@*Results@#There were no significant differences in general conditions among patients with severe AP (SAP), median-severe AP (MSAP) and mild AP (MAP). The Apo AⅠ levels of SAP [ (0.89±0.36) g/L] were lower than those of MSAP [(1.07±0.40)g/L, t=2.07, P=0.04] and MAP [(1.14±0.70) g/L, t=2.55, P=0.01]. Apo AⅠ was negatively correlated with Atlanta classification (r=-0.24, P<0.01). The optimal cut-off point of Apo A Ⅰ to predict SAP was 0.8 g/L, with the sensitivity of 0.877, specificity of 0.674 and Youden index of 0.55. The area under curve (AUC) was 0.623 (P<0.01). The proportions of SAP patients [52.94% (27/51) vs. 30.51%(36/118), χ2=7.66, P<0.01] and the patients of APACHE-Ⅱscore>8 [70.59%(36/51) vs. 55.08%(65/118), χ2=3.56, P=0.04] in patients with Apo AⅠ≤0.8 g/L were higher than those in patients with Apo AⅠ>0.8 g/L.@*Conclusion@#Apolipoprotein AⅠ level is negatively correlated with Atlanta classification and Apo AⅠ level can be used to predict severity of hyperlipidemic acute pancreatitis.
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Objective To analyze death causes in patients with acute myocardial infarction complicated by cardiac rupture.Methods The patients who were admitted with cardiac rupture after acute myocardial infarction in Beijing Anzhen Hospital Affiliated to Capital Medical University from January 2012 to December 2014 were enrolled.These patients were divided into death group and survival group.Then statistical analysis was performed for the clinical data of these patients in two groups,Logistic regression analysis was used to analyze the risk factors with statistical significance.Results A total of 59 patients diagnosed cardiac rupture after acute myocardial infarction were enrolled in this study,including 50 patients died,and 9 patients survived.There were significant differences between the two groups of patients with clinical baseline data.Compared with the survival group,death group had higher age ((69.94 ± 9.24) years old vs.(61.56 ± 9.14) years old,t =2.511,P =0.015),the higher incidence of malignant arrhythmia (22.0％ vs.0,x2 =4.070,P =0.044),the lower proportion of alcohol abuse (12.0％ vs.44.4％,x2 =5.704,P =0.017),higher fasting blood glucose ((8.97 ±3.98) mmol/L vs.(6.06± 1.25) mmol/L,t =4.153,P＜0.01) and triglycerides ((1.78±0.50) mmol/L vs.(1.39±0.20) mmol/L,t =4.146,P＜0.01),higher proportion of pulmonary arterial hypertension(22.0％ vs.0,x2 =4.070,P =0.044) and brain natriuretic peptide (406.50 (110.00,570.28) ng/L vs.33.00 (20.00,176.00) ng/L,P=0.004),smaller the left ventricular end diastolic diameter((47.76±5.13) mm vs.(52.22 ±4.66) mm,t =-2.434,P =0.018).The use of fondaparinux sodium (26.0％ vs.0,x2 =4.920,P =0.027),heparin (48.0％ vs.88.9％,x2 =5.138,P =0.023) and nitrates (72.0％ vs.100.0％,x2 =5.361,P =0.021)were significantly differences.The occurrence of acute heart failure in patients in death group was significantly higher than the survival group (11.0％ vs.0,x2 =3.258,P =0.071),but the difference was not significant.Logistic regression analysis showed that old age (OR =1.151),fasting blood glucose (OR =1.974)and heart rupture were significandy correlated (P＜ 0.05).Conclusion Cardiac rupture patients have a high mortality rate after myocardial infarction.Advanced age and fasting blood glucose were risk factors,while the use of common heparin is protective factor.Patients should be evaluated in a timely manner to assess the prognosis and to take targeted measures.
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Objective To analyze the clinical features and prognosis of patients with acute myocardial infarction (AMI) complicated with different parts of heart rupture. Methods Patients diagnosed for AMI complicated with cardiac rupture from January 2010 to December 2015 in Beijing Anzhen Hospital were collected. All of them were divided into free wall rupture group and ventricular septal perforation group according to the rupture site. Clinical features, hospital related examination results, treatment and prognosis of these two groups were analyzed statistically. Results A total of 120 patients with AMI complicated with cardiac rupture were included in the study, including 64 patients with free wall rupture, and 56 patients with ventricular septal perforation. Compared with the ventricular septal perforation group by the single factor analysis, the patients in free wall rupture group had higher age (year: 68.88±9.31 vs. 63.86±8.68, t = 3.039, P = 0.003), lower body mass index [BMI (kg/m2): 22.74±2.07 vs. 25.21±2.99, t = -5.203, P = 0.000], higher rate of history of renal insufficiency (12.5% vs. 1.8%, χ2 = 4.942, P = 0.026), higher level of aspartate transaminase [AST (U/L): 76.00 (38.33, 197.50) vs. 33.50 (19.00, 137.50), Z = -2.788, P = 0.005], triglyceride [TG (mmol/L): 1.68±0.50 vs. 1.36±0.70, t = 2.903, P = 0.005], total cholesterol [TC (mmol/L): 4.21±0.74 vs. 3.87±1.01, t = 2.081, P = 0.040], high density lipoprotein cholesterol [HDL-C (mmol/L): 1.12±0.91 vs. 0.91±0.32, t = 2.910, P = 0.004] and cardiac troponin I [cTnI (μg/L): 18.83 (4.48, 81.68) vs. 0.82 (0.08, 8.50), Z =-5.011, P = 0.000], lower level of blood urea nitrogen [BUN (mmol/L): 7.11±3.11 vs. 10.14±6.97, t = -2.999, P = 0.004], brain natriuretic peptide [BNP (ng/L): 169.00 (98.50, 485.75) vs. 793.00 (478.75, 1 426.25), Z = -5.739, P = 0.000], and D-dimer [μg/L: 219.00 (141.00, 315.75) vs. 310.50 (188.75, 532.00), Z = -2.607, P = 0.009], smaller left ventricular end diastolic diameter [LVEDD (mm): 48.58±5.17 vs. 53.65±6.63, t = -4.631, P = 0.000] and left ventricular end systolic diameter [LVESD (mm): 33.54±5.40 vs. 37.24±6.53, t = -3.397, P = 0.001], lower proportion of left ventricular aneurysm formation [14.1% (9/64) vs. 76.8% (43/56), χ2 = 47.851, P = 0.000] and pulmonary arterial hypertension [20.3% (13/64) vs. 53.6% (30/56), χ2 = 14.368, P = 0.000], higher usage rate of aspirin [100% (64/64) vs. 75.0% (42/56), χ2 = 18.113, P = 0.000], clopidogrel usage rate [82.8% (53/6) vs. 46.4% (26/56), χ2 = 17.578, P = 0.000], ticagrelor usage rate [12.5% (8/64) vs. 1.8% (1/56), χ2 = 4.924, P = 0.026], and common heparin usage rate [53.1% (34/64) vs. 10.7% (6/56), χ2 = 24.174, P = 0.000], lower usage rate of nitrates [70.3% (45/64) vs. 85.7% (48/56), χ2 = 4.063, P = 0.044], higher percutaneous coronary intervention (PCI) operation rate [42.9% (27/64) vs. 12.5% (7/56), χ2 = 13.388, P = 0.000], lower coronary artery bypass graft (CABG) surgery rate [7.8% (5/64) vs. 48.2% (27/56), χ2 = 24.930, P = 0.000], success rate of CABG surgery [60.0% (3/5) vs. 100% (27/27), χ2 = 8.233, P = 0.004], and incidence rate of cerebral infarction in hospital [1.6% (1/64) vs. 10.7% (6/56), χ2 = 4.554, P = 0.033], higher hospital all-cause mortality [85.9% (55/64) vs. 23.2% (13/56), χ2 = 47.851, P = 0.000]. The differences of other indicators were not statistically sig nificant. Conclusions Patients with AMI complicated with free wall rupture usually have more risk factors and worse prognosis. These two types of patients should be treated with target.
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This study was aimed to establish a HPLC method for the determination of isogarcinol. Daojin Inertsil WP300 C18 (4.6 mm× 150 mm, 5μm) was employed with methanol and water (75?25) as the mobile phase. The flow rate was 1.0 mL·min-1. The column temperature was set at 40°C. The detection wavelengthγ was set at 277 nm. The results showed that the linear range of isogarcinol was 0.005 7-0.039 9μg. The average recovery rate was 99.58%. The relative standard deviation (RSD) was 1.25%. The contents of isogarcinol inGarcinia mangostana,Garcinia oblongifolia,Garcinia oligantha,Cratoxylum cochinchinense andCalophyllum membranaceum were 0.285%, 0.199%, 0.857%, 0.161% and 0.006%, respectively. Isogarcinol was not detected inCratoxylum formosum orCalophyllum inophyllum. It was concluded that the method was convenient, accurate with high sensitivity, good stability and repeatability. It can be used for determination of isogarcinol content in Chinese herbal medicine.
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Objectives To analyze the characteristics of serum protein electrophoresis(SPE)in chronic heart failure(CHF) patients,evaluate prognostic value and explore the reason of it preliminarily.Methods Retrospective exploration of 6 1 8 chronic heart failure patients in study cohort (CHF cohort)and 70 patients with normal cardiac function in control cohort was made to comp are the difference of serum protein electrophoresis.Then,CHF Patients were tracked down by phone to discuss the correlation between adverse event rate (re-hospitalization rate or mortality rate)and their SPE.Last,the multiple linear regression analysis of SPE and biochemical indicators was made to explore the reason of the abnormality.Results Pa-tients of CHF cohort appeared to have significantly rising beta 1-gobulin(6.01±1.06)%,compared with control cohort(t=3.417,P<0.001).Post-discharge adverse event rate displayed by the curve demonstrated that patients with beta 1-gobulin higher than or equal to 6% had much more adverse event rate than those with beta 1-gobulin less than 6%,in 7 to 24 months after discharged from the hospital,which had been proved by the Chi-square test of 0.031(P<0.05).Multiple linear regres-sion analysis showed that beta 1-globulin and serum creatinine,uric acid,and sodium were significantly correlated.Conclusion CHF patients had higher beta 1-gobulin of SPE probably because of immunoactivation,which may increase their re-hospi-talization rate ormortality rate after hospital discharge.Meanwhile,growing beta 1-gobulin is closely correlated with blood creatinine,uric acid and blood natrium and becomesa risk of kidney dysfunction due to hypoperfusion and accumulation of se-rum immunoglobulin.
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Objective To measure the levels of interleukin-6 (IL-6) and tumor necrosis factor-a( TNF-a) in the cervical intervertebral disk of patients with cervical spondylotic myelopathy ( CSM) ,study the role of IL-6 and TNF-a in the pathogenesis of CSM.Methods 40 degenerative cervical vertebral disk tissues were collected from CSM cases;20 normal tissues of vertebral disk were taken as control.The contents of IL-6 and TNF-a were detected by ELISA.Results The contents of IL-6 and TNF-a in disk of CSM sufferers increased significantly compared with the control group (P<0.01).Conclusion The results of the present study indicated that IL-6 and TNF-a may be involved in the pathogenesis of CSM.