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Objective: To investigate the level of nucleic acid oxidation in myocardial tissue of patients aged over 85 with heart failure with preserved ejection fraction (HFpEF) and the correlation with myocardial amyloid deposition. Methods: This was a retrospective case-control study. Data of patients≥85 years old who underwent systematic pathological autopsy in Beijing Hospital from 2003 to 2017 were retrospectively collected. Twenty-six patients were included in the HFpEF group and 13 age-and sex-matched patients who had not been diagnosed with heart failure and died of non-cardiovascular diseases served as the control group. The left ventricular myocardium slices of both groups were semi-quantitatively analyzed using immunohistochemical staining of 8-oxidized guanine riboside (8-oxo-G) and 8-oxidized guanine deoxyriboside (8-oxo-dG) to evaluate the oxidation of RNA and DNA in cardiomyocytes. Using the median of the mean absorbance value of 8-oxo-G immunohistochemical staining as the cut-off value, patients were divided into high-absorbance group and low-absorbance group. Congo red staining was used to compare myocardial amyloid deposition between the two groups. Results: The mean age of patients in HFpEF group was (91.8±3.7) years, 24 (92.3%) were males. The mean age of patients in control group was (91.7±3.7) years old, 11 (84.6%) were males. The median mean optical absorbance value of 8-oxo-G immunohistochemical staining of myocardium was significantly higher in HFpEF patients than in control group (0.313 8 (0.302 2, 0.340 6) vs. 0.289 2 (0.276 7, 0.299 4), Z=-3.245, P=0.001). The median mean absorbance value of 8-oxo-dG immunohistochemical staining of myocardial tissue was similar between the two groups (0.300 0 (0.290 0, 0.322 5) vs. 0.300 0 (0.290 0, 0.320 0), Z=-0.454, P=0.661). Proportion of patients with moderate and severe cardiac amyloid deposition was significantly higher in the high-absorbance group than in the low-absorbance group ((85.0%, 17/20) vs. (31.6%, 6/19), P=0.001). Conclusion: The RNA oxidation degree of myocardium in HFpEF patients is higher than that in elderly people without heart failure. Degree of myocardial amyloid deposits is higher in patients with high levels of RNA oxidation.
Subject(s)
Aged , Male , Humans , Aged, 80 and over , Female , Heart Failure/pathology , Retrospective Studies , Stroke Volume , Case-Control Studies , Nucleic Acids , 8-Hydroxy-2'-Deoxyguanosine , Myocytes, Cardiac/pathology , RNA , Oxidative Stress , Guanine , Ventricular Function, LeftABSTRACT
Objective: To investigate the level of nucleic acid oxidation in myocardial tissue of patients aged over 85 with heart failure with preserved ejection fraction (HFpEF) and the correlation with myocardial amyloid deposition. Methods: This was a retrospective case-control study. Data of patients≥85 years old who underwent systematic pathological autopsy in Beijing Hospital from 2003 to 2017 were retrospectively collected. Twenty-six patients were included in the HFpEF group and 13 age-and sex-matched patients who had not been diagnosed with heart failure and died of non-cardiovascular diseases served as the control group. The left ventricular myocardium slices of both groups were semi-quantitatively analyzed using immunohistochemical staining of 8-oxidized guanine riboside (8-oxo-G) and 8-oxidized guanine deoxyriboside (8-oxo-dG) to evaluate the oxidation of RNA and DNA in cardiomyocytes. Using the median of the mean absorbance value of 8-oxo-G immunohistochemical staining as the cut-off value, patients were divided into high-absorbance group and low-absorbance group. Congo red staining was used to compare myocardial amyloid deposition between the two groups. Results: The mean age of patients in HFpEF group was (91.8±3.7) years, 24 (92.3%) were males. The mean age of patients in control group was (91.7±3.7) years old, 11 (84.6%) were males. The median mean optical absorbance value of 8-oxo-G immunohistochemical staining of myocardium was significantly higher in HFpEF patients than in control group (0.313 8 (0.302 2, 0.340 6) vs. 0.289 2 (0.276 7, 0.299 4), Z=-3.245, P=0.001). The median mean absorbance value of 8-oxo-dG immunohistochemical staining of myocardial tissue was similar between the two groups (0.300 0 (0.290 0, 0.322 5) vs. 0.300 0 (0.290 0, 0.320 0), Z=-0.454, P=0.661). Proportion of patients with moderate and severe cardiac amyloid deposition was significantly higher in the high-absorbance group than in the low-absorbance group ((85.0%, 17/20) vs. (31.6%, 6/19), P=0.001). Conclusion: The RNA oxidation degree of myocardium in HFpEF patients is higher than that in elderly people without heart failure. Degree of myocardial amyloid deposits is higher in patients with high levels of RNA oxidation.
Subject(s)
Aged , Male , Humans , Aged, 80 and over , Female , Heart Failure/pathology , Retrospective Studies , Stroke Volume , Case-Control Studies , Nucleic Acids , 8-Hydroxy-2'-Deoxyguanosine , Myocytes, Cardiac/pathology , RNA , Oxidative Stress , Guanine , Ventricular Function, LeftABSTRACT
OBJECTIVE@#To investigate the clinical significance and related factors of drainage tube after percutaneous endoscopic lumbar discectomy(PELD).@*METHODS@#The clinical data of 151 patients with lumbar disc herniation who underwent PELD from January 2019 to September 2019 was retrospectively analyzed. According to whether the drainage tube was used after operation, the patients were divided into drainage tube group and non drainage tube group. The placement time and total drainage volume were recorded. The characteristics of patients, such as age, gender, body mass index, lumbar disc herniation segment, smoking history, basic diseases and whether taking anticoagulants, were analyzed by single factor and multiple factor.@*RESULTS@#Drainage tubes were used in 32 patients after PELD. There were statistical differences in visual analogue scale(VAS) and Japanese Orthopaedic Assiciation(JOA) scores between postoperative and preoperative of that in two groups(P<0.05). There were statistical differences in VAS and JOA scores at discharge between two groups(P<0.05), while there were no statistical differences at other time points(P>0.05). Univariate analysis showed that age, basic diseases and whether taking anticoagulants were related to the use of drainage tube, but gender, body mass index, lumbar disc herniation segment and smoking history were not significantly related to the use of drainage tube. Multivariate analysis showed that elderly patients, complicated with hypertension and diabetes, taking anticoagulants were related to the use of drainage tube.@*CONCLUSION@#The use of drainage tube after percutaneous endoscopic lumbar discectomy can improve the symptoms of lumbar and leg pain in early stage. For elderly patients with hypertension, diabetes and taking anticoagulants drugs, drainage tube can be considered after transforaminal endoscopy.
Subject(s)
Aged , Humans , Diskectomy/adverse effects , Diskectomy, Percutaneous/adverse effects , Drainage , Endoscopy , Intervertebral Disc Displacement/surgery , Lumbar Vertebrae/surgery , Retrospective Studies , Treatment OutcomeABSTRACT
Objective:To investigate the antitumor effect and the mechanism of Dunhuang Pingweiwan and its decomposed recipes based on phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt)/mammalian target of rapamycin (mTOR) signaling pathway in SCG-7901 gastric cancer-mice. Method:The subcutaneous tumor bearing model of SCG-7901 gastric cancer in mice was established, and the the mice were randomized into model group, Dunhuang Pingweiwan group (14.04 g·kg<sup>-1</sup>·d<sup>-1</sup>), Huoxue Jiedu group (6.50 g·kg<sup>-1</sup>·d<sup>-1</sup>), Wenzhong Sanhan group (3.64 g·kg<sup>-1</sup>·d<sup>-1</sup>) and cisplatin group (2 mg·kg<sup>-1</sup>·d<sup>-1</sup>), with 8 mice in each group. From the 8<sup>th</sup> day of inoculation, the mice were administered for 10 consecutive days. The mice were weighed and the general conditions were observed every other day. On the next day of the last administration, the mice were sacrificed, and the tumor was removed and weighed to calculate the anti-tumor rate. The histopathological changes were observed by hematoxylin-eosin (HE) staining, and the mRNA and protein expressions of PI3K, Akt, and mTOR in tumor tissues were detected by real-time polymerase chain reaction(Real-time PCR) and immunohistochemistry (IHC), respectively. Result:From the 10<sup>th</sup> day of inoculation, the mice in cisplatin group were generally in poor condition and their body mass decreased. The mice in model group, Dunhuang Pingweiwan group, Huoxue Jiedu group and Wenzhong Sanhan group were generally fair, and their body mass increased without significant difference among groups. The tumor inhibition rates of Dunhuang Pingweiwan, Huoxue Jiedu, Wenzhong Sanhan and cisplatin groups were 30.74%, 24.80%, 4.19% and 63.84%, respectively. Except for Wenzhong Sanhan group, tumor weight of the other treatment groups was significantly lower than that of the model group (<italic>P</italic><0.01), and there was no significant difference between the Dunhuang Pingweiwan and Huoxue Jiedu group. Dunhuang Pingweiwan and Huoxue Jiedu group could significantly reduce tumor cell density and cause tumor cell necrosis. Compared with the model group, the expressions of PI3K, Akt, and mTOR mRNA and protein in the Dunhuang Pingweiwan, Huoxue Jiedu and cisplatin groups significantly decreased (<italic>P</italic><0.05, <italic>P</italic><0.01), and there was no significant difference between the Dunhuang Pingweiwan group and Huoxue Jiedu group. Conclusion:Dunhuang Pingweiwan and its decomposed recipes (Huoxue Jiedu) have a certain anti-tumor effect on the SCG-7901 gastric cancer-mice, and the mechanism may be related to the down-regulation of key molecules in the PI3K/Akt/mTOR signaling pathway.
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OBJECTIVE@#To quantitatively study the biomechanical parameters of Bachuorounian manipulation in the treatment of humeral epicondylitis, and discuss the effects of individual characteristics on the biomechanical parameters were discussed.@*METHODS@#From July 2019 to February 2020, 40 patients with external humeral epicondylitis were selected, including 18 males and 22 females, ranging in age from 20 to 50 years old, with an average of (34.37±8.41) years old;and the course of disease ranged from 1 to 11 months, with a mean of (6.05±2.71) months. The biomechanical parameters of the elbow joint of the affected side were measured by using the biomechanical sensor. At thesame time, the individual characteristic parameters of patients were collected to analyze the influence of different individual characteristics of patients on biomechanical parameters.@*RESULTS@#The results of mechanical analysis in each stage of the bachuorounian manipulation were as follows:the rolling back rotation force was (31.17±2.99) N;the buckling bending drawing force was (44.99±2.38) N;the rolling pre rotation force was (31.03±2.75) N;and stretching drawing force was (48.75±2.09) N. The correlation analysis between the parameters showed that there was a significant positive correlation between the buckling bending drawing force and the stretching drawing force parameters, and a significant positive correlation between the rolling force back-rotation force and the rolling pre-rotation force parameters. The multivariate linear regression analysis on the parameters of influencing factors and manipulative biomechanics showed that there was a significant correlation between body weight and rolling back-rotation force, significant correlation between elbow tenderness and the buckling bending drawing force, and significant correlation between disease duration and the stretching drawing force.@*CONCLUSION@#The bachuorounian manipulation of humeral epicondylitis has a certain range of operating force. Manipulation of each stage has a correlation and systematic. The patient's weight, elbow tenderness and disease course are important factors affecting the bachuorounian manipulation.
Subject(s)
Female , Humans , Infant , Male , Biomechanical Phenomena , Elbow , Elbow Joint , Humerus , Tennis ElbowABSTRACT
The pathological anatomical results of coronavirus disease-2019 (COVID-19) patients showed that excessive inflammatory reaction in the lungs is one of the important causes for such complications as acute lung injury or acute respiratory distress syndrome. Therefore, regulation of immune response may be an effective measure for COVID-19. Alveolar macrophages have a high heterogeneity and plasticity. The dynamic changes of subsets balance and function of M1/M2 alveolar macrophages have a significant effect on pulmonary inflammatory response during the early and late stages of infection. This paper reviews the classification and function of macrophages and explores the mechanism of alveolar macrophage in the pathological process of COVID-19 at different stages and the pharmacodynamic mechanism of traditional Chinese medicine. Besides, it provides ideas for the treatment of COVID-19 with traditional Chinese medicine and other drugs' research and development based on the regulation of macrophage polarization.
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Objective: To assess the efficacy and long-term outcome of percutaneous balloon aortic valvuloplasty (PBAV) for children with congenital aortic stenosis (CAS) and to explore risk factors for significant aortic regurgitation (AR) and reintervention after PBAV during follow up. Methods: This was a retrospective study. Children (≤18 years old) with CAS, who underwent PBAV in Guangdong Provincial Hospital from January 2004 to December 2018, were included in this study. Demographic, preoperative transthoracic echocardiography (TTE) and surgical data were collected. Postoperative complications were closely observed, and the patients were followed up at 1, 6, 12 months after the operation, and then at one year interval thereafter. Endpoint events included significant AR and reintervention. Reintervention was defined as any intervention that needed to be performed on the valve for various reasons, including re-PBAV, surgical valvuloplasty and valve replacement. Significant AR was defined as AR grade≥3 by TTE criteria. The results of the last TTE examination before the end of the study were collected. The Kaplan-Meier curve for long-term AR-free and intervention-free survival was plotted. Cox regression model was used to further analyze the risk factors for significant AR and reintervention after PBAV in CAS patients. Results: A total of 55 patients were enrolled in this study, and the age was 4.6(1.6, 6.5) years, with 37(67.3%) males. The peak systolic valve gradient fell from (80.3±30.6)mmHg to (38.5±18.5)mmHg(P<0.001, 1 mmHg=0.133 kPa). Surgical success rate was 89% (49/55). Acute post-PBAV AR occurred in 18 patients, including 3 patients with RA≥3 grade. In-hospital complications occurred in 6 patients (2 deaths, 2 cases of transient arrhythmia, and 2 cases of femoral artery embolization). Fifty patients accomplished the follow-up and the follow-up time was 6.2(3.4, 8.5) years. Significant AR was found in 20 patients. Significant AR-free survival rate was 53% at 5 years and 19% at 10 years. Reintervention was performed in 11 patients (4 with valvuloplasty and 7 with valve replacement), and the 5-year and 10-year intervention-free survival rates were 87% and 62%, respectively. Multivariate Cox regression analysis showed that acute post-PBAV AR was a risk factor for long-term significant AR (HR=2.398, 95%CI 1.007-5.712, P=0.048). Post-PBAV residual pressure gradient ≥ 35 mmHg (HR=4.747, 95%CI 1.116-19.329, P=0.030)and acute post-PBAV AR (HR=5.104, 95%CI 1.083-24.065, P=0.039)were risk factors for re-intervention. Conclusions: PBAV is safe and effective in the treatment of CAS in children, but attention should be paid on significant AR post procedure. Acute post-PBAV AR is a risk factor for re-intervention and significant AR post PBAV, and high post-PBAV residual pressure gradient is a risk factor for re-intervention.
Subject(s)
Child , Humans , Male , Aorta , Aortic Valve Insufficiency , Aortic Valve Stenosis/surgery , Cardiac Surgical Procedures , Retrospective StudiesABSTRACT
BACKGROUND@#Pulmonary artery hypertension associated with congenital heart disease (PAH-CHD) occurs predominantly among patients with uncorrected CHD. Treatment of severe pediatric PAH-CHD remains a major intractability. This study evaluated the predictors and prognoses of children with PAH-CHD who underwent surgical correction.@*METHODS@#The data for 59 children with severe PAH-CHD who underwent surgical correction, with or without postoperative medication, between May 2011 and June 2015 at the Guangdong Provincial People's Hospital were analyzed retrospectively. A regression analysis, receiver-operating characteristic (ROC) curves, and Kaplan-Meier curves were used for survival analysis.@*RESULTS@#Fifty-nine children with severe PAH-CHD underwent heart catheterization and correction, with or without specific anti-PAH drugs postoperatively, were included in this study. The pulmonary pressure, heart function, and ending events were observed and median observation period was 49 ± 20 months. Twenty-eight patients (50%) received at least one additional anti-PAH drug after correction. The survival rate after 2 years was 91.5% (54/59); two patients were in a critical condition, and three were lost to follow-up. Twelve patients (29%) still received over one additional PAH-specific therapy at follow-up, whereas 42 (75%) had successfully stopped drug treatment. Two patients (3.5%) died and one underwent a second thoracotomy to remove the ventricular septal defect patch. Acute vasoreactivity test (AVT) criteria had limited efficacy in predicting pediatric PAH-CHD, whereas pulmonary vascular resistance (PVR) ≤ 6.65 Wood units (WU)/m or PVR/systemic vascular resistance (SVR) ≤ 0.39 during AVT indicated a good prognosis after surgical correction with an AUC of 98.3% (95% confidence interval [CI]: 96.0-100%), 98.4% (95% CI: 96.0-100%) sensitivity of 100%, 100% and specificity of 82.1%, 92.9%, respectively.@*CONCLUSIONS@#Although the criteria for positive AVT currently used are unsuitable for pediatric patients with PAH-CHD, PVR and PVR/SVR during AVT are excellent predictors of outcome in pediatric PAH-CHD. Surgery aided by anti-PAH drugs is an effective strategy and should be recommended for severe pediatric PAH-CHD with PVR ≤ 6.65 WU/m and PVR/SVR ≤ 0.39 after iloprost aerosol inhalation.
Subject(s)
Adolescent , Child , Child, Preschool , Female , Humans , Male , Echocardiography , Heart Defects, Congenital , Pathology , General Surgery , Hypertension, Pulmonary , Pathology , General Surgery , Kaplan-Meier Estimate , Prognosis , ROC Curve , Retrospective Studies , Risk FactorsABSTRACT
Objective To explore the clinical effect of non-invasive positive pressure ventilation(NPPV)for treatment of acute left heart failure after mitral valve replacement. Methods Sixty patients with acute left heart failure after mitral valve replacement in Xinxiang Central Hospital from April 2009 to August 2017 were selected. The patients were divided into control group and NPPV group,with 30 patients in each group. The patients in the control group were treated with double oxygen ab-sorption (mask and nasal catheter),strong heart,diuresis and dilated blood vessels. Based on the treatment of control group, the patients in NPPV group were treated with NPPV therapy. The plasma N-terminal pro-B-type natriuretic peptide(NT-proB-NP)level of patients in the two groups was monitored by rapid determination of immunofluorescence before treatment and 6,24 hours after treatment. The respiratory frequency,blood oxygen saturation,heart rate and oxygen partial pressure monitoring of patients in the two groups was monitored before treatment and 2,6 and 24 hours after treatment. Results The total effective rate of patients in the control group and NPPV group was 92. 4%(26 / 28)and 96. 6%(28 / 29)respectively;there was no sig-nificant difference in the total effective rate between the two groups(χ2 = 1. 25,P > 0. 05). There was no significant difference in the plasma NT-proBNP level between the two groups before treatment (P > 0. 05);the level of NT-proBNP at 6,24 h after treatment was significantly lower than that before treatment in the two groups (P < 0. 05);the level of NT-proBNP of patients in the NPPV group was significantly lower than that in the control group at 6,24 h after treatment (P < 0. 05). There was no significant difference in the respiratory frequency,blood oxygen saturation,heart rate and oxygen partial pressure between the two groups before treatment(P > 0. 05). Compared with before treatment,the respiratory frequency and heart rate of patients were decreased and the blood oxygen saturation,oxygen partial pressure were increased at 2,6,24 h after treatment in the two groups (P < 0. 05). There was no significant difference in the oxygen partial pressure between the two groups at 2 h after treat-ment(P > 0. 05);the oxygen partial pressure of patients in the NPPV group was significantly higher than that in the control group at 6,24 h after treatment(P < 0. 05);there was no significant difference in the respiratory frequency,blood oxygen satu-ration and heart rate between the two groups at each time piont after treatment(P > 0. 05). Conclusion NPPV is an effective treatment for acute left heart failure after mitral valve replacement.
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Objective To investigate the clinical effect of endoscopic treatment of carpal tunnel syndrome (CTS) with subsynovial hyperplasia. Methods 37 cases (total 41 wrists) of CTS with subsynovial hyperplasia who accepted endoscopic treatment in our hospital were retrospectively analysised, all the transverse ligament of wrist were cutted off under endoscope and the hyperplastic subsynovial membrane arounding the superficial flexor tendon of finger. The changes of clinical symptoms and signs before and after operation were compared. Results According to Kelly classification, the overall excellent and good rate was 95.12%. After operation, the feel of numb and pain during night disappeared in all patients, the positive rate of Tinel and Phalen sign was both reduced to 2.44% (P < 0.05), and the mean value of two-point discrimination was reduced to (3.5 ± 0.9) mm. No serious complication occurred during treatment. Conclusion For the patients of CTS with subsynovial hyperplasia, to cut the transverse ligament tendon under endoscope and remove the subsynovial around the flexor tendon at the same time is a new and feasible surgical procedure with notable curative effect, which deserves clinical popularization.
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<p><b>BACKGROUND</b>Percutaneous balloon pulmonary valvuloplasty (PBPV) is the preferred therapy for pulmonary valve stenosis (PVS). This study retrospectively reviewed recent PBPV outcomes in infants with PVS. The aim of this study was to evaluate factors associated with immediate therapeutic outcomes and restenosis during medium-term follow-up.</p><p><b>METHODS</b>The study included 158 infants with PVS who underwent PBPV from January 2009 to July 2015. Demographic characteristics and patient records were reviewed, including detailed hospitalization parameters, hemodynamic data before and immediately after balloon dilation, cineangiograms, and echocardiograms before PBPV and at each follow-up. All procedures were performed by more than two experienced operators.</p><p><b>RESULTS</b>Immediately after balloon dilation, the pressure gradient across the pulmonary valve decreased from 73.09 ± 21.89 mmHg (range: 43-151 mmHg) to 24.49 ± 17.00 mmHg (range: 3-92 mmHg; P < 0.001) and the right ventricular systolic pressure decreased from 95.34 ± 23.44 mmHg (range: 60-174 mmHg) to 52.07 ± 18.89 mmHg (range: 22-134 mmHg; P < 0.001). Residual transvalvular pressure gradients of 67.31 ± 15.19 mmHg (range: 50-92 mmHg) were found in 8.2% of patients, indicating poor therapeutic effects; 6.4% of patients had variable-staged restenosis at follow-up and 3.8% underwent reintervention by balloon dilation or surgical repairs. Further analysis demonstrated that the balloon/annulus ratio showed statistically significant differences (P < 0.05) among groups with different therapeutic effects and between the restenosis and no-stenosis groups. Binary logistic regression analysis further revealed that higher balloon/annulus ratio (odds ratio: 0.005, 95% confidence interval: 0-0.39) was an independent protective factor for restenosis. The rate of severe complications was 1.9%.</p><p><b>CONCLUSIONS</b>PBPV is a definitive therapy for infants with PVS based on its effectiveness, feasibility, and safety. Restenosis upon medium-term follow-up is relatively rare.</p>
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?AIM:To investigate the correlation between dry eye and different degrees of diabetic retinopathy ( DR ) in type 2 diabetic patients.?METHODS: In the cross-sectional study, 340 patients (340 eyes) with type 2 diabetes were enrolled. Tear film function tests including tear meniscus height, tear film breakup time ( BUT ) , fluorescein staining, Schirmer Ⅰtest were performed followed by surveying questionnaires about dry eye. Retinal status was evaluated by retinal color photography and indirect ophthalmoscopy exam with dilated pupils to evaluate DR and whether companied by macular edema.?RESULTS:The prevalence of dry eye was 49. 41%. The mean duration of diabetes in patients with dry eye was 11.15±7.07a, while 6.92±5.45a without dry eye(P<0.01). Dry eye had the positive correlation to the development of DR. The incidence of dry eye in people with mild nonproliferative diabetic retinopathy ( NPDR ) , moderate NPDR, severe NPDR and proliferative diabetic retinopathy (PDR) was 1. 097 times, 1. 724 times, 2. 86 times and 5. 43 times respectively, compared with people without DR. The occurrence of dry eye in people with macular edema increased by 3. 697 times compared with people without macular edema.?CONCLUSION: Dry eye was more prevalent in people with type 2 diabetes. The incidence of dry eye increased gradually with the occurrence and development of diabetic retinopathy.
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In this paper, fourteen new L-proline derivatives were designed and synthesized, and their acetlcholinesterase (AChE) inhibitory activities were also investigated in vitro. New L-proline derivatives were prepared from substituted 2-bromo-1-acetophenones through four-step reaction; and their bioactivities as AChE inhibitors were measured by Ellman spectrophotometry. The results showed that the target compounds had a certain AChE inhibitory activity to in vitro. The bioactivity of compound 8b was the best of them, and its IC50 value was 5.45 µmol.L-1, which was better than that of rivastigmine. So the acetylcholinesterase inhibitory activities of new L-proline derivatives were worth to be further studied.
Subject(s)
Acetylcholinesterase , Cholinesterase Inhibitors , Chemistry , Drug Design , Proline , Rivastigmine , Chemistry , Structure-Activity RelationshipABSTRACT
The target compounds were prepared from 5-aminobenzimidazolone by two steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The AChE inhibitory activity of compound 4d is the best of them, and its IC50 value is equal to 7.2 μmol·L(-1), which is better than that of rivastigmine; moreover the 4d had no inhibitory activities to BuChE. Therefore, the inhibitory activities of 5-aminobenzimidazolone derivatives to acetylcholinesterase are worth further researching.
Subject(s)
Acetylcholinesterase , Metabolism , Benzimidazoles , Chemistry , Cholinesterase Inhibitors , Chemistry , Drug Design , Phenylcarbamates , Chemistry , Rivastigmine , Structure-Activity RelationshipABSTRACT
To assess the efficacy of fluorine-18 fluorodeoxyglucose positron emission tomography [[18]F-FDG PET]/computed tomography [CT] in the diagnosis of patients with fever of unknown origin [FUO], who were finally diagnosed as lymphoma. A retrospective study was performed in the First Affiliated Hospital, School of Medicine of Zhejiang University, China, from March 2009 to March 2012. The PET/CT images of consecutive patients with FUO were analyzed. Within 1 week of PET/CT scanning, additional histological tests were also performed if clinically needed. A total of 73 consecutive patients were included. Of these, 34 [47%] had a PET/CT finding suggestive of the presence of lymphoma and 29 [85%] had a diagnosis of confirmed lymphoma; 39 [53%] had a PET/CT result revealing the absence of lymphoma and 4 [10%] were diagnosed by biopsy as having lymphoma. The most frequent lymphoma diagnosis was peripheral T cell lymphoma [n = 16; 55%], followed by diffuse large B cell lymphoma [n = 9; 31%]. The accuracy of PET/CT was 88%. In this study, PET/CT had high diagnostic accuracy in patients with FUO resulting from lymphoma, which indicated that PET/CT scanning was a valuable diagnostic tool for these groups of patients with FUO
Subject(s)
Humans , Male , Female , Positron-Emission Tomography , Fluorodeoxyglucose F18 , Tomography, X-Ray Computed , Lymphoma , Retrospective StudiesABSTRACT
N-Acyl-4-phenylthiazole-2-amines were designed and synthesized, moreover their effects on acetylcholinesterase activities were tested. N-Acyl-4-phenylthiazole-2-amines were prepared from substituted 2-bromo-1-acetophenones by three steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The results showed that the target compounds had a certain inhibitory activity on AChE in vitro. Among them, 8c was the best, and IC50 of 8c was 0.51 micromol x L(-1), better than that of rivastigmine and Huperzine-A. The inhibitory activities of N-acyl-4-phenylthiazole-2-amines on acetylcholinesterase are worth while to be further studied.
Subject(s)
Acetylcholinesterase , Metabolism , Alkaloids , Pharmacology , Amines , Pharmacology , Cholinesterase Inhibitors , Pharmacology , Drug Design , Rivastigmine , Pharmacology , Sesquiterpenes , Pharmacology , Structure-Activity Relationship , Thiazoles , PharmacologyABSTRACT
A series of novel 2-amino-4-phenylthiazole derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase were investigated. 2-Amino-4-phenylthiazoles were prepared from alpha-bromoacetophenones by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 8a was the best of them. The IC50 of 8a to AChE is 3.54 micromol x L(-1), and the value was better than that of rivastigmine. 2-Amino-4-phenylthiazole derivatives showed a certain bioactivity in vitro, which were worth further investigation.
Subject(s)
Acetylcholinesterase , Metabolism , Cholinesterase Inhibitors , Chemistry , Pharmacology , Drug Design , Inhibitory Concentration 50 , Molecular Structure , Thiazoles , Chemistry , PharmacologyABSTRACT
A series of novel N-acyl-thiochromenothiazol-2-amine derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase was investigated. N-Acyl-thiochromenothiazol-2-amines were prepared from thiophenol by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 10a was the best in them. The IC50 of 10a to AChE is 7.92 μmol x L(-1), and the value is better than that of rivastigmine. N-Acyl-thiochromenothiazol-2-amine derivatives showed a certain bioactivity in vitro, which were worth further investigation.
Subject(s)
Acetylcholinesterase , Metabolism , Amines , Pharmacology , Benzopyrans , Pharmacology , Cholinesterase Inhibitors , Pharmacology , Rivastigmine , Structure-Activity Relationship , Thiazoles , PharmacologyABSTRACT
<p><b>OBJECTIVE</b>To timely identify the HIV-1 infection in window-period and to estimate the HIV-1 incidence among people who came for voluntary counseling and testing (VCT) service as well as men who have sex with men (MSM), respectively.</p><p><b>METHODS</b>HIV antibody negative samples that were determined by screening tests between January and October 2012, were collected and tested with pooling HIV-1 RNA testing technique (2-staged pooling by 50:1, 10:1). Positive cases were followed-up for HIV antibody testing while HIV incidence was calculated under Ron Brookmeyer' s method, among VCT and MSM populations.</p><p><b>RESULTS</b>Among 1400 HIV antibody negative samples of VCT, two showed HIV-1 RNA positive during the antibody window period with the HIV-1 incidence as 1.87% per year (95% CI: 1.23%-2.65% ). Among 500 HIV antibody negative samples from MSM population, two showed HIV-1 RNA positive in the antibody window period, with HIV-1 incidence as 5.31% per year (95% CI: 3.52%-7.45% ).</p><p><b>CONCLUSION</b>Pooling HIV-1 RNA testing seemed a powerful tool for HIV antibody testing in the window-period. Measures should be taken to strengthen the HIV diagnostic programs among MSM and other high risk groups,during the HIV antibody window-period. More frequent detection approach as pooling HIV-1 RNA testing might be a good choice.</p>
Subject(s)
Humans , Male , Counseling , HIV Infections , Epidemiology , HIV-1 , Genetics , Homosexuality, Male , Incidence , Mass Screening , RNA, Viral , BloodABSTRACT
To report a rare case of brucellosis with myelo-dysplastic syndrome [MDS]. A 70-year-old woman presented with pancytopenia and fever of unknown origin [FUO]. The initial diagnosis was brucellosis; the woman was treated with doxycycline and rifampin against Brucella melitensis but was later diagnosed as suffering from MDS. She was immediately transferred to the Department of Hematology for further evaluation. This study highlights the rarity of brucellosis with MDS, and we recommend that brucellosis with MDS be considered in patients presenting with pancytopenia and FUO