2.SAR of benzoyl sulfathiazole derivatives as PTP1B inhibitors.
Wen-Wen YIN ; Zheng CHEN ; Yan-Bo TANG ; Fei YE ; Jin-Ying TIAN ; Zhi-Yan XIAO
Acta Pharmaceutica Sinica 2014;49(5):632-638
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
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Protein Tyrosine Phosphatase, Non-Receptor Type 1
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antagonists & inhibitors
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Structure-Activity Relationship
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Sulfathiazoles
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chemistry
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pharmacology
3.Changes of Transforming Growth Factor-?_1 and Vascular Endothelial Growth Factor in Children with Primary Nephrotic Syndrome
xue, ZHAO ; xiu-qiao, TIAN ; hui-feng, ZHANG ; zhi-yan, DOU
Journal of Applied Clinical Pediatrics 1992;0(05):-
Objective To investigate the change of serum transforming growth factor(TGF)-?1 and vascular endothelial growth facter( VEGF) in children with different types of primary nephrotic syndrome( PNS). Methods Children involved in the experiments were divided into simple type group, 16 cases; nephrit was type group, 16 cases, collecting blood sample in prednison - pretreated stage and in prednison- treated stage;control group, 14 cases. Monoclonal EUISA detected TGF-?1 and VEGF. Results Serum level of TGF-?1 and VKGF in active stage of simple type were higher than those of remission stage. The level in nephritis type was no signifi cant difference between prednison- treated stage and prednison - pretreated stage. The level in nephritis type was significantly higher than that in simple type. Conclusion Monitoring the dynamic change of serum TGF-?1 and VEGF can assess the effect of prednison treatment,and evaluate the prognosis of nephrotic syndrome.
4.Evaluation of long term effects of arthroscopic knee debridement and reconstructing for treating osteoarthritis in patients with Kaschin-Beck disease
Ming, LING ; Xiang-hui, HUANG ; Zhi, YI ; Yan-hai, CHANG ; Jun, LIU ; Jie, QI ; Xin, TIAN
Chinese Journal of Endemiology 2010;29(5):559-561
Objective To observe the long term effects of arthroscopic knee debridement and reconstructing operation for treating osteoarthritis in patients with Kaschin-Beck disease. Methods Thirty-one cases of patients with Kaschin-Beck disease were followed for 6 years after operation of articular clearing by arthroscope. Index of pain, symptoms of self-evaluation, range of motion, walking distance, standing test by affected leg when bending at 30° or 60° were recorded and compared with the preoperative results. Results Twenty-four cases were followed up for 6 years. Six years after operation the pain index(3.38 ± 2.87) was dramatically decreased compared to that before operation (6.88 ± 1.45, t = 5.30, P < 0.05). Patients symptoms markedly improved by subjective self-evaluation was 70.83% (17/24), the effective rate was 100% (24/24). The number of cases that could stand up when leg bending at 30° or 60° were 21,18 cases, respectively, compared with that of preoperative of 14, 11 cases, respectively, the difference was statistically significant(x2 = 5.17,4.27, all P < 0.05). Six years after operation the walking distance(3 cases < 1 km, 11 cases 1 - 5 km and 10 cases > 5 km) were greatly improved compared to the results before operation (12 cases < 1 km, 9 cases 1 - 5 km and 3 cases > 5 km, U = 2.88, P <0.05). Six years after operation the knee activity[(132.25 ± 14.52)°] remained at the same level, compared with that of preoperative [(131 .58 ± 14.68) °], the difference was not statistically significant (t = 0.16, P > 0.05) .Conclusions The method of arthroscopic joint debridement to cure Kaschin-Beck disease knee osteoarthritis can significantly reduce pain, improve function and walking distance, with more stable long-term satisfactory outcome.
5.Design of the wireless medical information system based on PDA.
Tian-Long SHEN ; Jun SHI ; Zhuang-Zhi YAN
Chinese Journal of Medical Instrumentation 2007;31(5):344-347
This paper introduces the design of the wireless medical information management system based on PDA and its model whose experiment results show that it can realize the functional requirements of the design.
Computers, Handheld
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Information Systems
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instrumentation
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organization & administration
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Medical Informatics Applications
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Signal Processing, Computer-Assisted
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Software Design
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Wireless Technology
6.Research and practice about risk control of shenfu injection.
Zhi-Fei WANG ; Da-Li TIAN ; Wen ZHANG ; Yan-Ming XIE
China Journal of Chinese Materia Medica 2014;39(18):3641-3644
Shenfu injection is developed by improving dosage form of ancient prescription "Shenfu Tang" and is mainly derived from extracts of both traditional Chinese medicine red ginseng and prepared lateral root of monkshood with polysorbate 80 as auxiliary material. Shenfu injection may be administered through intramuscular injection, intravenous drip or intravenous injection. It produces good effects in restoring Yang and rescuing patients from collapse, tonifying Qi and preventing exhaustion. It is mainly used to treat not only syncope and prostration resulting from sudden Yang collapse (infectious, hemorrhagic and water depletion shock etc), but also pavor, palpitation, dyspnea with cough, stomachache, diarrhea and arthralgia etc caused by deficiency of Yang (deficiency of vital energy). Research group has audited the monitored hospitals and has carried out postmarketing study of Shenfu solution from many aspects including literature review, spontaneous reporting system (SRS) and hospital information system (HIS) data analysis etc. A summary is shown below.
Drugs, Chinese Herbal
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administration & dosage
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adverse effects
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Humans
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Injections
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Medicine, Chinese Traditional
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methods
7.Effect of Chinese herb Yiyanheji on intestinal mucosa barrier in rats with severe acute pancreatitis
Jun-Shan YANG ; Yan ZUO ; Li-Ming HAN ; Yu-Zhi TIAN ; Yu HOU ;
Chinese Journal of Primary Medicine and Pharmacy 2005;0(11):-
Objective To study the effects of Chinese herbs Yiyanheji on intestinal mucosa barrier in rats with SAP.Methods Animal models of SAP were induced by retrograde injection of 5% sodium taurocholate (0.1ml/100g) into the common biliopancreatic duct.90 healthy Wistar rats weighing (250?30)g were randomly divided into 3 groups:sham operation group (SO,n=30),SAP group (SAP,n=30) and Chinese herbs Yiyanheji treated group(SAP+YH,n=30).Treated group was treated with Yiyanheji after operation.The SAP group was treated with physiological saline.Three groups of rats were killed at 72 hours after operation or treatment.Bacterial cultures were performed in all animals.The changes of terminal ileum' tissue were observed by optical electron mi- croscopy.The data of test were analyzed by statistic software.Results The incidence of bacterial translocation was 22.5% in Yiyanheji treated group,and it was lower than that in SAP group which was 90.0 %.The difference was significant(P
8.Significance of Computed Tomography in Diagnosis of Bronchial Foreign Body in Children
yan, SUN ; shao-hua, WANG ; rong-jun, LIN ; guang-feng, JIANG ; ying, TIAN ; zhi-jun, CHEN
Journal of Applied Clinical Pediatrics 2006;0(16):-
Objective To investigate clinical significance of computed tomography (CT) scan in diagnosis of bronchial foreign body in children.Methods Twenty-one suspected children with bronchial foreign body were studied with spiral CT cross-section scan and coronal reconstruction and diagnosis was confirmed with bronchoscopy.Results The foreign body was displayed in all of 21 cases. CT scan showed foreign body was located in right main bronchial 12 cases, right middle bronchial 1 case, right inferior lobar bronchial 2 cases and left main bronchial 6 cases. Foreign bodies were extracted with bronchoscopy.Conclusion CT scan can display and locate accurately foreign body in bronchial of children,and has very important diagnostic value in patients having atypical histories, clinical and radiological findings.
9.Angiotensin Ⅱ Stimulate the Expression of Integrin-Linked Kinase in Rat Glomerular Mesangial Cell
zhi-hui, LI ; tian-hui, WU ; cui-rong, DUAN ; jin-hua, HE ; yan, YIN
Journal of Applied Clinical Pediatrics 1992;0(05):-
Objective To investigate the effect of angiotensin Ⅱ(Ang Ⅱ)on the expression of integrin-linked kinase(ILK)in rat glomerular mesangial cells.Methods SD rat glomerular mesangial cells were separated and cultured.They were treated with 10-7 mol/L Ang Ⅱ in various time-point(0,12,24,48,72 h),and then cultured rat glomerular mesangial cells were treated 48 h with Ang Ⅱ in various concentration(0,10-11,10-9,10-7,10-5 mol/L).Then total protein expression in rat glomerular mesangial cells stimulated by Ang Ⅱ at every time-point and every concentration-point was extracted.The expression of ILK protein was measured by Western blot.Results 1.Expression of ILK protein in rat glomerular cells stimulated by Ang Ⅱ in various time-point,or various concentration was significantly increased.In group of 10-7 mol/L Ang Ⅱstimulated cells,the protein semiquantity of ILK at 0,12,24,48,72 h respectively was 0.18?0.02,0.37?0.07,0.90?0.10,1.73?0.12,and 1.72?0.13(F=166.78 P
10.Literature search of TCM syndrome elements of common diseases
Tian-Fang WANG ; Xiu-Yan WU ; Yan ZHAO ; Chun-Guang YU ; Zhi-Geng LI ; Wen-Jie XU ; Cai-Feng DU ; Li LI ; Zhi-Yu WANG ; Qing-Guo WANG
China Journal of Traditional Chinese Medicine and Pharmacy 2006;0(09):-
Objective: To summarize the distributing rule of TCM syndrome elements of common diseases by analyzing the literature of Depression,Chronic Hepatitis B,Chronic Renal Failure,Chronic Obstructive Pulmonary Disease,Menopausal Syndrome.Methods: We selected eligible literatures,then established database with EpiData 3.0 software and computed the frequency of TCM syndrome elements with SPSS 12.0 software.Results: ①Liver,heart,spleen,lung and kidney are common TCM syndrome elements of location of disease.②Yin deficiency,yang deficiency,heat,qi stasis,qi deficiency,blood stasis,damp and phlegm are common TCM syndrome elements of nature of disease.③There are TCM syndrome types between 62 and 148,but the sum of frequency of leading syndrome types which includes disease information is mostly no more than 50%.There are TCM syndrome elements between 19 and 47,but the sum of frequency of leading syndrome elements which includes disease information is mostly above 80%.Conclusion: It is convenient to study TCM syndrome from the aspect of TCM syndrome elements,so we should thoroughly keep on studying TCM syndrome elements.