2.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
5.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.
6.Research strategy of the case-control post-genome-wide association study
Jiayu LIU ; Lina ZHANG ; Hong ZHENG
Tianjin Medical Journal 2015;(7):810-812,813
Since the first paper reported the finding of genetic variation contributing to human age-related macular de?generation by genome-wide association study (GWAS) in 2005, large number of human complex diseases associated genetic variants have been identified through GWAS method. However, the biological function of these genetic variants is not very clear. The present paper reviewed the methods of fine-mapping and the progress of the functional studies for these suscepti?bility variants. In the post GWAS Era, the study of genetic mechanisms can help us to understand the disease pathogenesis.
7.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.
8.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
9.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 .
10.Protective effects of thioltransferase (TTase) on oxidative damaged human lens epithelial cells induced by ultraviolet radiation
Xiaoliang ZHENG ; Jie ZHANG ; Hong YAN
Recent Advances in Ophthalmology 2017;37(7):601-604
Objective To discuss the protective effects of thioltransferase (TTase) on oxidative damaged human lens epithelial cells (HLEC) induced by ultraviolet radiation.Methods HLEC were cultured in vitro and then randomly divided into 4 groups:Normal group:normal cultured HLEC;UV group:normal cultured HLEC + UV radiation (with 302 nm UV radiation irradiation intensity 55.56 μW · cm-2 for 15 minutes,totaling irradiation volume 500 J · m-2);TTase siRNA group:HLEC transfected with TTase siRNA;TTase siRNA + UV group:HLEC transfected with TTase siRNA + UV radiation(with 302 nm UV radiation irradiation intensity 55.56 μW · cm-2 for 15 minutes,totaling irradiation volume 500 J · m-2).TTase mRNA expression was measured by qRT-PCR,the cell proliferation was detected by LDH Assay Kit,and the TTase activity was measured.TTase expression was detected by Western blotting.The levels of TGSH,GSH and GSSG of HLEC were measured,and then GSSG/T-GSH ratio was calculated.Results Cell proliferation ability in UV group,TTase siRNA group and TTase siRNA + UV group were decreased by 21.0%,17.0% and 29.0% compared with normal group (all P < 0.05).TTase activity in UV group was 2.1 times of the normal group,TTlase siRNA group was 67.0% of the normal group,Tlase siRNA + UV group was 1.3 times of TTase siRNA group (all P < 0.05).TTase expression in UV group was 3.9 times of the normal group,TTase siRNA group was 35.0% of the normal group,TTase siRNA + UV group was 3.0 times of siRNA group (all P < 0.05).GSH content in UV group,TTase siRNA group and TTase siRNA + UV group were 68.4%,79.0%,61.7% of the normal group (all P < 0.05).GSSG content in UV group,TTase siRNA group and TTase siRNA + UV group were 2.3 times,1.4 times,3.7 times of the normal group (all P < 0.05).GSSG/T-GSH in UV group,TTase siRNA group and TTase siRNA + UV group were 3.1 times,1.7 times,5.2 times of the normal group (all P < 0.05).Conclusion TTase plays an important protective role in oxidative damaged HLEC induced by ultraviolet radiation.