1.The role of structural protein Gag and related gene (protein) in late stages of the HIV-1 replication cycle and the inhibitors.
Acta Pharmaceutica Sinica 2010;45(2):205-14
The late stages of the HIV-1 replication cycle are important to the overall replication cycle. During the late stages, HIV-1 replication undergoes the processes of assembly, release, and maturation, resulting in the production of a mature virus particle capable of infecting a new target cell. The structural protein Gag and its related gene (protein) play a central role in these pathways. The different regions of Gag worked in concert to drive production of a mature infectious particle through protein-protein, protein-RNA and protein-lipid interactions. The designed drug aimed directly at these stages can efficiently block the maturation and infectivity of HIV-1. In this article, the role of structural protein Gag and related gene (protein) in late stages of the HIV-1 replication cycle and related inhibitors is reviewed.
2.Research progress of dual inhibitors targeting HIV-1 reverse transcriptase and integrase.
Hong LIU ; Peng ZHAN ; Xinyong LIU
Acta Pharmaceutica Sinica 2013;48(4):466-76
Both reverse transcriptase (RT) and integrase (IN) play crucial roles in the life cycle of HIV-1, which are also key targets in the area of anti-HIV drug research. Reverse transcriptase inhibitors are involved in the most employed drugs used to treat AIDS patients and HIV-infected people, while one of the integrase inhibitors has already been approved by US FDA to appear on the market. Great achievement has been made in the research on both, separately. Recently, much more attention of medicinal chemistry researchers has been attracted to the strategies of multi-target drugs. Compounds with excellent potency against both HIV RT and IN, evidently defined as dual inhibitors targeting both enzymes, have been obtained through considerable significant exploration, which can be classified into two categories according to different strategies. Combinatorial chemistry approach together with high throughput screening methods and multi-target-based virtual screening strategy have been useful tools for identifying selective anti-HIV compounds for long times; Rational drug design based on pharmacophore combination has also led to remarkable results. In this paper, latest progress of both categories in the discovery and structural modification will be covered, with a view to contribute to the career of anti-HIV research.
3.The application of structural optimization strategies in drug design of HIV NNRTIs.
Liu WANG ; Peng ZHAN ; Xinyong LIU
Acta Pharmaceutica Sinica 2012;47(11):1409-22
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) play an important roles in the prevention and treatment of AIDS. NNRTIs can specifically target at HIV reverse transcriptase (RT) and have the advantages of high potency and low toxicity, which make them a research focus for a long time. In the guidance of structural optimization strategies (bioisosterism, molecular hybridization and scaffold hopping) in medicinal chemistry, structural modification to lead compounds can be carried out to design new compounds with different levels, which will improve the efficiency of drug discovery and decrease the cost of drug development. It is an effective way to find new NNRTIs. In this review, we will expatiate on the application of different levels of structural optimization strategies in the NNRTIs structural modification with concrete examples.
4.Progress in the study of HIV-1 Vif and related inhibitors
Zhenyu LI ; Peng ZHAN ; Xinyong LIU
Acta Pharmaceutica Sinica 2010;45(6):684-93
Human immunodeficiency virus type 1 (HIV-1) viral infectivity factor (Vif), one of the accessory proteins, which is a small basic phosphoprotein, is essential for viral replication and pathogenesis. The best well-characterized function of Vif is its ability to neutralize the host cell antiviral factor, apolipoprotein B mRNA editing enzyme catalytic polypeptide like 3G (APOBEC3G), which makes the viral particles more infective. In addition, Vif can regulate the reverse transcription and the advanced stage of replication of the virus particle, as well as induce the termination of cell cycle at G2 stage and so on. The designed drug aimed directly at Vif can efficiently block the maturation and infectivity of HIV-1. In this review, the structure, function and especially the related inhibitors of Vif are reviewed.
5.Determination of Sinapine in Semen Raphani
Lifang LIU ; Yuxin WANG ; Xinyong ZHANG ; Xuefang LIU ;
Chinese Traditional Patent Medicine 1992;0(01):-
Objective: To determine the sinapine in Semen Raphani(Laifuzi) from different places by measns of RP HPLC. Method: The column empolyed was Alltima Phenyl Collumn(250?4.6mm,5?m). The mobile phase was acetonitrile 0.08 mol/LKH 2PO 4(15∶85). The flow rate was 1.0mL/min and detection was effected at 326nm results. Conclusion: The results show the method is accurate, rapid and reproducible. We found it has marked discrepancy in the content of Semen Raphani(Lai Fuzi) from different places.
6.Research and development of anti-interference portable transfusion-drop counter
Xingxi ZHU ; Xinyong HU ; Shitao QI ; Yun LIU ; Lin LI
Chinese Medical Equipment Journal 2003;0(11):-
Objective To resolve the difficulty in controlling the transfusion speed by medical personnel.Methods By using liquid drop sampling module,pulsing signals of liquid drop were obtained,and then they were enlarged,shaped and the wrong signals from the top and bottom surface of every drop were excluded before the standard triggered signals were sent out to SCM processing circuit,from which the real-time liquid drop speed and the average drop speed in every minute were obtained.Results Anti-interference and portable transfusion-drop counter could show the real-time liquid drop value and the average liquid drop value in every minute.Conclusion Anti-interference and portable transfusion-drop counter is convenient with simple structure and has been used in clinic.
7.In vitro antibacterial activity of tigecycline against carbapenems-resistant Acinetobacter calcoacetcus-Acinetobacter baumannii complex
Daohong ZHOU ; Yun PENG ; Xinyong CAI ; Yipeng LIU ; Min LI ; Yi WANG ; Weiping LU
International Journal of Laboratory Medicine 2014;(20):2771-2772
Objective To measure the in vitro antibacterial activity of tigecycline against carbapenems-resistant Acinetobacter calcoacetcus-Acinetobacter baumannii complex.Methods The isolated strains of carbapenems-resistant Acinetobacter calcoacetcus-Acinetobacter baumannii complex were collected in our hospital from December 2013 to February 2014.The MIC test strip was a-dopted to measure the MIC value of tigecycline.The break point adopted the judgment criteria published by FDA.Results All 61 strains of carbapenems-resistant Acinetobacter calcoacetcus-Acinetobacter baumannii complex had extremely high drug resistant rate to the commonly used antimicrobial agents.The sensitive rate of tigecycline was 80.3%,intermediation was 19.7% and no re-sistant strain was found in this study.MIC50 and MIC90 were 2 μg/mL and 3 μg/mL respectively.Conclusion Tigecycline has bet-ter in vitro antibacterial activity to the carbapenems-resistant Acinetobacter calcoacetcus-Acinetobacter baumannii complex isolated in our hospital.
8.Experimental Study on Synergistic and Attenuated Effect of Ginseng Polysaccharide Injection among Animals Treated with Cytoxan
Xinyong LYU ; Jun ZHOU ; Xiaoping SUN ; Lina LIU ; Zhenzhong WANG ; Wei XIAO
World Science and Technology-Modernization of Traditional Chinese Medicine 2014;(6):1372-1376
This article was aimed to study the inhibitory effect of ginseng polysaccharide injection on tumor growth a-mong ICR mice after inoculation of S180 cells, and its immune mechanism as well as its synergic effect in reducing toxicity of cytoxan (CTX). The experiment was carried out in ICR mice after inoculation of S180 cells. The mice were randomly divided into the model group, the control group, the CTX group, and the drug combination group. After 10 days of medication, the inhibition of tumor growth, WBC, thymus index and spleen index were measured in mice dur-ing the experiment. The immunodepressed mice model was induced by CTX. Effects of ginseng polysaccharide injec-tion on serum hemolysin and monomuclear macrophage phagocytosis were evaluated. The results showed that the com-bination of ginseng polysaccharide injection and CTX can significantly increase the tumor inhibiting rate. It can also reduce the side effect and toxicity of CTX, which may improve the immunosuppression induced by CTX. It was con-cluded that ginseng polysaccharide injection can increase the therapeutic effects and reduce the toxicity of CTX.
9.Study on chronic disease management ability and theory teaching model of undergraduates majoring in preventive medicine
Zan WANG ; Rui CHANG ; Junan LIU ; Xinyong GUO ; Qin AO ; Qi WANG ; Zuxun LU
Chinese Journal of Medical Education Research 2017;16(8):799-803
Objective Exploring theoretical teaching model of chronic diseases management of preventive medicine undergraduates,to provide feasible suggestions to improve the theoretical teaching of the chronic disease management ability of preventive medicine specialty in China so that graduates can better adapt to chronic diseases management work.Methods On the basis of reading a large number of relevant literature both at home and abroad,the research team designed questionnaires,and conducted a questionnaire survey on 190 respondents who engaged in chronic diseases management or teaching in central China.The content includes the understanding of the importance of training chronic disease management ability in undergraduate education of preventive medicine and the constitution and training mode of undergraduates' chronic disease management ability.EpiData 3.1 software was used to input survey data,SPSS 23.0 software was used for statistical description analysis,and the usage ratio and component ratio were used for statistical description analysis.Results The survey found that more than 50% of the respondents believed that training students with chronic disease management should focus on prevention,intervention services and health promotion ability,and chronic disease modules need to be added to undergraduate courses in preventive medicine.Conclusions preventive medicine undergraduates need to be improved,and medical colleges should change teaching model to increase undergraduates' ability of chronic diseases management.
10.Basic principles of selecting the site of blood reserve bank for preparedness against war
Yuxiu LIU ; Jun ZHENG ; Xiaoli XU ; Jianfeng LUAN ; Baolin YANG ; Yurong WANG ; Xinyong HU ; Xueming YI
Journal of Medical Postgraduates 2003;0(10):-
The blood reserve bank for preparedness against war,as a store of blood products and a base of blood supply,bears the responsibility of wartime emergency blood supply.Site selection is the basis of the construction of the blood reserve bank and directly related with its capacity of blood supply in both peace and wartime.The decision-making process concerning site selection is complicated and multi-aimed with various factors mutually related and conditioned.This paper proposes some basic principles of selecting the site of the blood reserve bank for preparedness against war,which are hoped to be beneficial for the demonstration of its site selection.