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
4.Diversity-oriented synthesis and its application in drug discovery.
Lei ZHANG ; Mingyue ZHENG ; Hong LIU
Acta Pharmaceutica Sinica 2015;50(4):419-33
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.
5.Participation of Anticoagulant Professional Pharmacist in the Medication for a Pulmonary Embolism Pa-tient with Warfarin Resistance
Zheng DING ; Shanshan HONG ; Jinhua ZHANG
China Pharmacist 2016;19(2):322-324
Objective: To discuss the therapeutic regimen for warfarin resistant patients with the help of clinical pharmacists. Methods:The pharmacist analyzed the cause of warfarin resistance and provided the dose adjustment for a pulmonary embolism pa-tient. Results:The genotype of the patient was identified as VKORC1-1639AG by gene test. The patient was diagnosed as hereditary warfarin resistance excluding other causes. With the assistance of pharmacist, the problem of warfarin resistant was solved. Conclu-sion:For warfarin resistant patients, clinical pharmacists must definite the reason of warfarin resistant firstly and then carry out the therapeutic strategy. Gene detection may be used as an important guide for warfarin resistance.
6.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.
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.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 .
9.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
10.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.