3.Diversity-oriented synthesis and its application in drug discovery.
Lei ZHANG ; Ming-yue ZHENG ; Hong LIU
Acta Pharmaceutica Sinica 2015;50(4):419-433
Diversity-oriented synthesis (DOS) aims to efficiently generate collections of small molecules with diverse appendages, functional groups, stereochemistry and skeletons, thus yielding diverse biological activities capable of modulating a wide variety of biological processes. In this review, we discussed the common strategies employed in DOS with specific examples from recent literature, including reagent-based approach, substrate-based approach, build-couple-pair strategy and privileged substructure-based DOS. The application of some DOS libraries in drug discovery is also presented.
Drug Design
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Drug Discovery
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Small Molecule Libraries
4.The applying Diver CE thrombus-aspirating device in acute myocardial infarction
Lili ZHANG ; Yanhua LI ; Hong ZHENG
Chinese Journal of Practical Internal Medicine 2006;0(22):-
Objective To assess the effect and safety of applying Diver CE thrombus-aspirating device during direct percutaneous coronary intervention(PCI)in pations with ST-segment elevation myocardial infarction(STEMI). Methods Select 46 patients with STEMI who underwent direct PCI between July,2006 and June,2007 in Fushun Central Hospital. Dividing these patients into thrombus-aspirating group and direct PCI group,comparing the difference in chest pain relieving.magnitude of ST-segment declining in 2h,TIMI flow grade 3,the maximum value of CK and CK-MB,EF and MACE outcome(death、myocardial infarction and targert vessel revascularization).Results The percent of chest pain relieving、magnitude of ST-segment declining 、TIMI flow grade 3、the maximum value of CK and CK-MB,and EF in thrombus-aspirating group are piror to the direct PCI group(P0.05).Conclusion applying Diver CE thrombus-aspirating device during PCI can obviously reduce thrombus in coronaty artery and distal embolization,improve myocardial reperfusion more effectively.
5.Radiotherapy for 71 patients with tonsillar carcinoma
Jidong HONG ; Qingsong TU ; Zheng ZHANG
Chinese Journal of Radiation Oncology 1993;0(03):-
0.05). Conclusion Brachytherapy ,when used to increase the dose effect,may enhance the local effect without any change in the overall survival.
6.Clinical efficacy analysis of methotrexate and mifepristone in treatment of ectopic pregnancy
Jinhong ZHENG ; Hong ZHANG ; Jinxiang JIANG
Chinese Journal of Biochemical Pharmaceutics 2014;(3):130-131,134
Objective To investigate the clinical efficacy of methotrexate and mifepristone in treatment of ectopic pregnancy. Methods 58 cases with ectopic pregnancy admitted in the Second People's Hospital in Putuo district of Zhoushan city from February 2010 to February 2012 were randomly divided into observation group and control group,each had 29 cases. Control group were received methotrexate 1 mg/kg or 50 mg/m2 once a day by intramuscular injection,observation group were given both methotrexate and mifepristone treatment,the mifepristone was given one piece a day and each piece is 75 mg. the treatment success,b-HCG returned to normal time,normal pregnancy and the occurrence of complications were compared between two groups. Results The treatment success and normal pregnancy rate in observation group were significantly higher than control group(P<0.05),b-HCG returned to normal time was significantly shorter than control group (P<0.05 ). There were no obvious adverse reactions in both two groups, observation group had one light nausea,and control group had one light nausea and one case with alanine aminotransferase (ALT)slightly increased phenomenon,those patients were all back to normal on their own without treatment,the difference of adverse reaction rate between two groups was not significant. Conclusions Methotrexate and mifepristone has good efficacy and are safe and reliable in,treatment of ectopic pregnancy.
7.Anesthetic efficacy of epidural ropivacaine mixed with different doses of snfentanil for hysterectomy
Hong ZHENG ; Zhiqun XIA ; Qing ZHANG
Chinese Journal of Anesthesiology 1994;0(04):-
Objective To assess the efficacy of ropivacaine in combination with different doses of sufentanil for epidural anesthesia in patients undergoing hysterectomy. Methods Eighty ASA Ⅰ or Ⅱ patients aged 30-55 yrs weighing 40-70 kg undergoing elective hysterectomy were randomly divided into 4 groups ( n = 20 each) : ropivacaine group (R) and 3 ropivacaine-sufentanil groups (R-S1-3). The patients were unpremedicated. ECG, BP, HR and SpO2 were monitored during ansthesia. Each patient received an epidural catheter placed at L2,3 interspace. After correct placement of epidural catheter was confirmed 0.75% ropivacaine 13 ml and normal saline (NS) 2 ml were given through epidural catheter in group R whereas in the 3 R-S groups 0.75% ropivacaine 13 ml and sufentanil 10 (R-S1), 20 (R-S2) or 30 (R-S3) ?g in NS 2 ml were injected into epidural space. BP, HR and SpO2 were recorded every 3 min. The onset time, upper spread and duration of sensory block; onset and duration of motor block (Bromage scale); degree of abdominal muscle relaxation; level of sedation (OAA/S scale); anesthetic efficacy and side-effects were recorded. The dose-response curve constructed by probit regression analysis was established to calculate ED50 and ED95. Results The onset time, the time needed to reach the highest sensory level were significantly shorter and the duration of sensory block was significantly longer in the 3 R-S groups than in R group ( P
8.Research progress of surgery for age-related macular degeneration with cataract
Xiao-Liang, ZHENG ; Jie, ZHANG ; Hong, YAN
International Eye Science 2017;17(9):1678-1681
Age-related macular degeneration (AMD) and cataract are the most common causes of low vision worldwide.Nowadays, there is still a controversy about whether cataract surgery should be taken in patients combined with AMD and when should the surgery be taken.The aim of this review is to assess the influence of cataract surgery on the occurrence and development of AMD, to analyze the risk factors, to explore the occasion of cataract surgery in patients with AMD, and joint with anti-vascular endothelial growth factor (VEGF) treatment, also including the development and application of intraocular lens.It helps to avoid and postpone the development and progression of macular degeneration after cataract surgery and get good visual outcome.
9.Clinical observation of Chinese medical gargle on gingivitis of the patients during fixed orthodontic treat-ment
Caihong LIU ; Hong ZHENG ; Lurong ZHANG
Journal of Practical Stomatology 2016;32(6):865-867
Objective:To observe the clinical efficacy of Chinese medical gargle on gingivitis of the patients wearing fixed appliance. Methods:60 gingivitis patients with fixed orthodontic treatment were randomly divided into chlorhexidine gargle group( CG group) and Chinese medical gargle group(CMG group)(n=30). Gingival index(GI) and sulcus bleeding index(SBI) in all patients were tested, then the patients were treated by scaling and curettage, and guided to use gargling with corresponding gargle 3 times a day for 14 d. GI and SBI were tested after 7 and 14 days respectively. Data were analysed. Results:After 7 d treatment, GI and SBI were decreased( P<0. 05) and there was no obvious difference between the 2 groups(P<0. 05). After 14 d treatment GI and SBI in CMG group de-creased more than those in CG group(P<0. 05). Conclusion:Chinese medical gargle is effective in the treatment of gingivitis of the patients during fixed orthodontic treatment.
10.Effects of Icariin of experimental IgA nephropathy in rats
Hong ZHANG ; Nian LIU ; Zheng LI
Chinese Journal of Comparative Medicine 2017;27(1):73-78
Objective To investigate the effect of Icariin ( ICA) experimental IgA nephropathy in rats and to explore related mechanisms .Methods Experimental IgA nephropathy rat model was established and then model rat were treated with or without different doses of ICA .Then, urine RBC, Urine protein and urine NAG were analyzed; IgA precipitation was detected with immunofluorescence staining;the protein level of NF-κBp65 and MCP-1 were examined by immunohistochemical staining;the mRNA level of IL-4, IL-10 and IL-13 were determined by quantitative PCR .Results The concentrations of urine RBC, Urine protein and urine NAG were reduced after ICA treatment , as companied by a decrease of IgA precipitation .Moreover, ICA treatment also decreased the protein level of NF-κBp65 and MCP-1, and the mRNA level of IL-4, IL-10 and IL-13.Conclusions ICA exerts a certain degree of efficacy on the treatment of experimental IgA nephropathy through regulating NF-κBp65 and MCP-1 expression and the immunoregulation mechanism .