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.Design of Handhold Emergency Suction Apparatus
Liming TANG ; Tiebing LIU ; Xinyong HU ; Qingying TONG ; Guangming WU ; Jianqiang MAO
Chinese Medical Equipment Journal 1989;0(01):-
Objective To design a handhold emergency suction apparatus, in order to meet the needs of clinical therapy, field and on-site emergency treatment. Methods The apparatus was divided into such components as handle, grab handle, L tie, piston, waste liquid tank and its cap, and the junction between the parts, and then the optimum design of the components were performed. Results Through the optimum design, the apparatus was improved from the aspects of portability, easy-to-use and reliability. Conclusion It is proved by practice that the apparatus also can reduce the labor intensity of healthcare staff, and definitely satisfy the clinical rescue and the treatment needs.
8.Measurement of microvessel density in laryngeal carcinoma and its clinical significance
Liqiang ZHANG ; Xinyong LUAN ; Xinliang PAN ; Xiaodong TIAN ; Fenglei XU ; Dayu LIU ; Dapeng LEI
Journal of Clinical Otorhinolaryngology Head and Neck Surgery 2001;(3):115-117
Objective:To determine the microvessel density (MVD) in laryngeal carcinoma and its clinical significance.Method:Thirty-eight tumor specimens were selected from laryngeal cancer patients from January,1994 to March,1996.Histological sections of the tumors were stained immunohistochemically for factor Ⅷ.Using light microscopy,we counted microvessels per 400×field in the most active areas of tumor angiogenesis.Result:①The tumor blood vessels,composed of only one layer of endothelium were mainly distrbuted heterogenously in the interstitial tissue of laryngeal carcinoma with irregular lumen,poorly developed structure.②The MVD in the cancer tissues were statistically higher than that in peritumoral tissues (P<0.01).③The MVD in the cancer tissues in group of patients with metastasis to cervical lymphonodes were statistically higher than in group without metastasis (P<0.01),the MVD in the cancer tissues in group of advanced cases (Ⅲ,Ⅳ stages) were statistically higher than that in group of early cases (Ⅰ,Ⅱ stages,P<0.01).④There was no statistically difference in MVD in the cancer tissue between supraglottic and glottic laryngeal carcinoma patients (P>0.05).⑤There was no statistically difference in MVD in the cancer tissue among the G1,G2 and G3 group (P>0.05).Conclusion:The laryngeal cancer blood vessels have some characteristics that don′t appear in normal vessels.It is suggested that tumor angiogenesis can promote tumor growth and metastasis and MVD may be a new prognostic indicator of laryngeal carcinoma.
9.Clinical studies on sternocleidomastoid myoperiosteal flap for cervical tracheal reconstruction
Dapeng LEI ; Xinliang PAN ; Fenglei XU ; Liqiang ZHANG ; Dayu LIU ; Xinyong LUAN
Journal of Clinical Otorhinolaryngology Head and Neck Surgery 2001;(4):169-170
Objective:To introduce the experience of repairing the defect of cervical trachea wall by using the sternocleidomastoid myoperiosteal flap after the anterior or posterior wall of cervical trachea was invaded by cervical neoplasm. Method:Between 1989 to 1998 the sternocleidomastoid myoperiosteal flap was applied in 12 patients with different diseases, among which 3 cases were thyroid carcinoma, 5 cases were laryngeal carcinoma, 4 cases were cervical esophageal carcinoma. Result:The operation was successful. 12 patients were decannuated and had normal exercise tolerance. The time from reconstruction to decannulation was ranging from 20 days to 6 months. Conclusion: The sternocleidomastoid myoperiosteal flap is an ideal transplant for cervical tracheal reconstruction.
10.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.