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
;
Drug Discovery
;
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.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.
7.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.
8.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.
9.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.
10.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.