1.Synthesis, biological activity and molecular docking research of N-{(4-oxo-thiochroman-3-yl)phenyl-methyl}acetamide derivatives as α-glucosidase inhibitors.
Guan ZHOU ; Guochao LIANG ; Xiaoyan HAN ; Yifan ZHONG ; Yunfang DONG ; Xiaocong LUO ; Hongwei JIN ; Yali SONG
Acta Pharmaceutica Sinica 2016;51(1):93-9
In order to develop potent antidiabetic agents that have inhibitory effect to a-glucosidase, twelve β-acetamido ketone derivatives such as N-{[(substituted-4-oxo-thiochroman-3-yl)phenyl]-methyl}acetamide are designed and synthesized through one-pot Dakin-West reaction. Their chemical structures are confirmed by 1H NMR, 13C NMR, IR and HR-MS. In vitro α-glucosidase inhibition assays of compounds 4a-41 were carried out using glucose oxidase method. The result indicated that most of them possess inhibitory activity in vitro. Compound 4k showed the most potent inhibitory activity with 87.3% inhibition of α-glucosidase at the concentration of 5.39 mmol x L(-1). The structure-activity relationship of these β-acetamido ketone derivatives was discussed preliminarily. Moreover, the molecular docking method was used to study the interaction mode of compound 4k and α-glucosidase. Our results will be helpful for designing of α-glucosidase inhibitors in the future.
2.Evaluation of adequate surgery for papillary thyroid microcarcinoma
Qingqing HE ; Dayong ZHUANG ; Luming ZHENG ; Yuhong CUI ; Ziyi FAN ; Jinxiang WEI ; Yinggang SUN ; Xueliang LI ; Peng ZHOU ; Yifan GUAN
International Journal of Surgery 2012;39(10):671-676
Objective To explore the best operation method in the patients with papillary thyroid microcarcinoma.Methods A total of 139 patients with papillary thjroid microcarcinoma were treated at our institute between Jan.2000 and Jan.2010.The data on the clinicopathological characteristics of patients and treatment were collected.Results The mean tumor size was (0.45 ± 0.24) cm.Of the 139 patients,30.2% had multifocal tumors,19.4% had bilateral tumors,42.4% neck lymph node metastases.The number of eases of lymph node metastasis in level Ⅵ,Ⅱa,Ⅲ and Ⅳ was 58(41.7%),3(2.2%),10(7.9%),5(3.6%),respectively.Only one had lymph node metastasis in Level Ⅲ Microscopic extrathyroid extension was associated with neck lymph node metastases in papillary thyroid microcareinoma patients (x2 =38.39,P <0.001).No one developed permanent hypoparathyroidism.The median follow-up time was 103 (range,30-154) months,and local recurrence in the thyoid was diagnosed in 2 patients who underwent hemi-or subtotal thyroidectomy.Follow-up of 10 years was done in 16 cases,and the survival rate of 139 patients for 10-year was 100%.Conclusions It suggested that patients with papillary thyroid microcarcinoma has uniform clinicopathologic characteristics and the pattern of lymph node metastasis from those with papillary thyroid carcinoma.Total thyroidectomy plus level Ⅵ dissection is the optimal surgical treatment of papillary thyroid microcarcinoma.
3.Prognostic factors of patients with T2N0M0 upper tract urothelial carcinoma:a single-center retrospective study of 235 patients
Bao GUAN ; Zhenpeng CAO ; Ding PENG ; Yifan LI ; Yonghao ZHAN ; Libo LIU ; Shiming HE ; Gengyan XIONG ; Xuesong LI ; Liqun ZHOU
Journal of Peking University(Health Sciences) 2017;49(4):603-607
Objective: To evaluate the impacts of the prognostic factors of T2N0M0 upper tract urothelial carcinoma (UTUC) for Chinese patients.Methods: A retrospective study was conducted including 235 patients who were diagnosed with T2N0M0 UTUC in our hospital and received radical nephroureterectomy (RNU) or partial ureterectomy during January 2000 and December 2013.The 3 and 5-year can-cer-specific survival rates and bladder recurrence-free survival rates of all the patients were valued using Kaplan-Meier method, and the survival curves with statistical significance between the two were compared using the Log-rank test.Variables with significant differences in the univariate analysis were subjected to the multivariate analysis by Cox regression model.Results: A total of 235 patients were included in this study, including 95 (40.4%) male patients and 140 (59.6%) female patients.The mean age was 66.73±10.49 years.The median follow-up time was 53 (rang: 3-142) months, and during the follow-up, 74 (31.5%) patients died of UTUC after a median of 35 months,and 96 (40.9%) patients developed intravesical recurrence after a median of 19.5 months.The 3 and 5-year cancer-specific survival rates of all the patients were 89.1% and 85.9%, respectively;the bladder recurrence-free survival rates were 85.5% and 80.2%, respectively.The independent prognostic factors of cancer-specific mortality were tumor age elder than 55 years (HR=3.138, 95%CI: 1.348-7.306, P=0.008) and diameter larger than 5 cm (HR=3.320, 95%CI: 1.882-5.857, P<0.001).The independent prognostic factors of bladder recurrence-free survival were ureter tumor (HR=1.757, 95%CI: 1.159-2.664, P=0.008) and lower tumor grade (HR=1.760, 95% CI: 1.151-2.692, P=0.009).Conclusion: T2N0M0 UTUC has a better cancer-specific survival.The intravesical recurrence was equivalent to non-muscle invasive UTUC but earlier.The tumor diameter larger than 5 cm and the patient age elder than 55 years were independently associated with cancer-specific mortality;the primary tumor located in ureter and lower tumor grade were more likely to develop intravesical recurrence.
4.Effectiveness of exercise intervention on sleep quality and negative emotion among female college students with anxiety
GONG Yujing, ZHANG Yifan, YANG Xinyi, GUAN Yuan, TANG Donghui
Chinese Journal of School Health 2019;40(4):542-545
Objective:
To investigate the effect of exercise intervention on sleep quality of female college students with anxiety, and to further explore the mediating effect of negative emotions in this association.
Methods:
Seventy female college students were randomly divided into experimental group (34 patients) and control group(36 patients). The experimental group received eight-week aerobic exercise and yoga training. The control group received no training. Sleep Quality Scale, Negative Emotion Scale and Anxiety Self-rating Scale were used to assess the level of sleep and negative emotion before and after exercise intervention.
Results:
After exercise intervention, sleep quality (4.31±1.26), anxiety (36.41±7.32) and negative emotion (2.37±0.50) in the experimental group significantly improved(P<0.01), no similar changes were found in the control group(P<0.05). By examining the mediating effects, negative emotions played a partial mediating role in the association between exercise and sleep quality(t=6.77, P<0.01).
Conclusion
Exercise intervention significantly improved the quality of sleep and negative emotion among female college students with anxiety. Negative emotions play a partial role in the positive effect of exercise on sleep quality.
5.Autologous peripheral blood CD34+ stem cells transplanted into 100 patients with advanced cirrhosis.
Yutong YAO ; Lanyun LUO ; Hua XUE ; Le LUO ; Haibo ZOU ; Guan WANG ; Zhiming AN ; Ming ZHONG ; Xiaobing HUANG ; Yifan ZHU ; Lingling WEI ; Maozhu YANG ; Tian ZHANG ; Ping XIE ; Gang XU ; Shaoping DENG ; Xiaolun HUANG
Chinese Journal of Hepatology 2014;22(9):667-670
OBJECTIVETo investigate whether transplantation of autologous peripheral blood CD34+ stem cells is a viable approach for treating patients with advanced cirrhosis,which is currently hindered by a shortage in liver donors.
METHODSA total of 100 patients with advanced cirrhosis and who had failed to respond to conservative therapy were recruited for transplantation of autologous peripheral blood CD34+ stem cells.The success of transplantation was investigated 6-and 12-months later by measuring markers of liver biosynthesis function (coagulation,albumin level,indocyanine green clearance,Child-Pugh score) and assessing pathological changes (Knodell score) and morphologic changes in the liver tissue.Complications were also recorded during follow-up.
RESULTSThe 1-year cumulative survival rate was 100%. Fifty-two patients with massive ascites showed gradual reduction and disappearance of the ascites.Four patients experienced upper gastrointestinal bleeding and three patients developed with hepatic encephalopathy (I-II degree) at 3 months post-transplantation.All patients showed significantly improved liver biosynthesis function,liver elasticity and Knodell score after transplantation (P less than 0.05).
CONCLUSIONAutologous peripheral blood CD34+ stem cell transplantation is a safe and effective treatment for advanced cirrhosis,and has high cost-benefit since it improves liver function,liver histology,and quality of life.
Ascites ; Humans ; Liver Cirrhosis ; therapy ; Quality of Life ; Stem Cell Transplantation ; Transplantation, Autologous ; Treatment Outcome
6.Muscle-invasive upper tract urothelial carcinoma predicts invasive bladder recurrence tumor
Bao GUAN ; Zhenpeng CAO ; Ding PENG ; Yifan LI ; Yonghao ZHAN ; Shiming HE ; Yanqing GONG ; Dong FANG ; Lei ZHANG
Chinese Journal of Urology 2017;38(12):896-900
Objective To evaluate the risk factors and prognosis of high risk bladder recurrence developing after radical nephroureterectomy(RNU) for upper tract urothelial carcinoma (UTUC).Methods The data of 148 UTUC patients who developed bladder tumor after RNU between January 2000 and December 2013 was retrospectively studied.There were 69 males and 79 females,aged from 34 to 82 years old (average 68 years old).83 patients were accompanied with hydronephrosis.80 patients were renal pelvic carcinoma.32 patients had the history of smoking.24 patients had the history of ureteroscope.68 patients had the tumor larger than 3 cm.Logistic regression model was used to analyze the risk factors of muscle invasive and high grade bladder recurrence lesions.We compared the clinocopathologic characteristics between primary UTUC and bladder cancer recurrence by using Fisher' s exact test.Cancer specific survival was analyzed using the Kaplan-Meier method,with the log-rank test used to assess significance.A Cox proportional hazard model was used for multivariate analysis.Results Of the 148 patients,non-muscle invasive (Tis、Ta and T1) tumors of primary UTUC and bladder recurrence were 51 (34.5%) and 119 (80.4%),respectively.High grade (G3) tumors of primary UTUC and bladder recurrence were 41 (27.7%) and 53(35.8%),respectively.During follow-up,94 (63.5%) experienced bladder recurrence once and 54 (36.5%) experienced multiple bladder recurrence.The median follow-up time was 59.5 (rang 8-142) months,48 (32.4%) patients died of UTUC.The grade of bladder cancer recurrence correlated with the grade (P =0.046),muscle-invasion (P =0.002) and tumor architecture (P =0.034) of the primary UTUC;muscle-invasive bladder cancer recurrence associated with that of the primary UTUC (P =0.009);bladder multiple recurrence related to gender (P =0.007).On multivariate logistic regression analysis,the muscle-invasion of primary UTUC was an independent risk factor for muscle-invasive (HR =5.512,95% CI 1.654-18.37,P =0.004) and high grade (HR =3.948,95% CI 1.589-9.813,P =0.004) bladder recurrence tumor.The muscle invasion of primary UTUC (HR =3.498,95% CI 1.569-7.803,P =0.002) was a prognostic factor for cancer specific survival on multivariate Cox regression analysis.Conclusions Muscle-invasive UTUC tend to predict high risk bladder recurrence tumor,and the female could be more likely to appear multiple recurrence tumor.The muscle invasion of primary UTUC could be an independent prognostic factor for cancer specific survival.
7.Spectrum change of rheumatic diseases in hospitalized children: a 12-year single-center experience of Shanghai
Tao ZHANG ; Haimei LIU ; Guomin LI ; Yu SHI ; Wen YAO ; Yifan LI ; Wanzhen GUAN ; Lijun ZHOU ; Fang LIU ; Hong XU ; Li SUN
Chinese Journal of Rheumatology 2020;24(2):120-124
Objective:To gain insight into the constitution of juvenile rheumatic diseases, treatment outcome and trends of rheumatic inpatients in past 12 years, and to improve awareness of juvenile rheumatic diseases.Methods:The clinical data of 5 950 patients in rheumatology department of the affiliated pediatric hospital of Fudan University (from 2005 to 2016) were analyzed retrospectively, and the chi-square test was used to compare and analyze the incidence.Results:Disease changes: ① The top three rheumatic diseases were Kawasaki disease (KD) (44.3%), Henoch-schoniein purpura (HSP) (35.4%), juvenile idiopathic arthritis (JIA)(9.6%). ② The number of all constitution of juvenile rheumatic diseases in hospital increased other than HSP. ③ The rheumatic diseases were increased from 17 to 37 kinds in the past 6 years. ④ The number of systemic lupus erythematosus (SLE) increased year by year (112/2 348 vs 197/3 602, χ2=1.41, P=0.235), as well as the severe SLE (35/112 vs 55/197, χ2=0.38, P=0.536). ⑤ The rate of rheumatic diseases complicated with macrophage activation (MAS) was 7.2‰(43/5 950). 12.9%(26/201) of systemic juvenile idiopathic arthritis(sJIA) were complicated with MAS, which was accounted for 60.5%(26/43) of total number of MAS in rheumatic diseases. In the last 6 years, there was a significant increase in the number of patients with MAS in patients with rheumatic diseases ( χ2=14.1, P<0.01) and sJIA( χ2=11.2, P<0.01). ⑥ 1.1%(64/5 950) of rheumatic diseases patients had lung lesions, juvenile dermatomyositis (JDM) accounted for 24.4%(20/82). In the last 6 years, the number of patients with lung lesions associated with rheumatic diseases increased significantly ( χ2=5.66, P=0.017). ⑦ The mortality rate of juvenile rheumatic diseases was only 3.7‰(22/5 950), and 45.5% occurred in SLE (10/22). The mortality rate of SLE decreased in last 6 years (5/112 vs 5/197, χ2=0.34, P=0.558). Conclusion:The constitution of juvenile rheumatic diseases in our center is decreasing for systemic vasculitis (KD, HSP), JIA, SLE, JDM in last 6 years. The annual total number of patients is relatively stable. But rare, difficult and critically illed cases increase year by year. Although SLE is still the primary cause of death in juvenile rheumatic diseases in recent 6 years, the mortality rate has decreased year by year.