1.Advancement in developing a new class of anti-AIDS drugs: HIV entry inhibitors
Chinese Pharmacological Bulletin 2003;0(09):-
Process of HIV fusion with target cells, mediated by the HIV envelope glycoprotein surface subunit gp120 and the transmembrane subunit gp41, is an important step for drug intervention. The membrane fusion events leading to HIV entry into the target cell are initiated by the binding of gp120 to CD4 and subsequently to a co-receptor, CXCR4 or CCR5. Consequently, gp41 undergoes conformational changes, resulting in the fusion between the viral and cellular membranes or between the infected and uninfected cells. Therefore, gp120 and gp41 on the virions and CD4 and coreceptors on the target cells may serve as targets for development of a new class of anti-HIV drugs, HIV entry inhibitors, with a mechanism of action different from those mediated by reverse transcriptase inhibitors (RTIs) and protease inhibitors (PIs), the two classes of antiretroviral drugs approved by FDA for clinical application. The successful development of a peptidic anti-HIV drug T-20, which is targeted to the HIV gp41, implies that HIV entry inhibitors are milestone in the current anti-HIV therapy. Application of the HIV entry inhibitors alone or in combination with the RTIs and PIs will increase the efficacy and reduce the toxicity of these anti-HIV drugs and will save lives of AIDS patients who fail to response to the current antiretroviral drugs. The advancement in the study and development of the HIV entry inhibitors was reviewed here in detail
2.Effects of nicardipine,urapidil,and esmolol on baroreflex sensitivity during induction in patients with essential hypertension
The Journal of Clinical Anesthesiology 2009;25(12):1028-1030
Objective To investigate the effects of nicardipine,urapidil,and esmolol on baroreflex sensitivity(BRS) in patients with essential hypertension(EH) during induction of general anesthesia.Methods EH patients were divided into four groups,who were given nicardipine 0.5μg/kg(group N,15 cases),urapidil 0.5 mg/kg(group U,16 cases),esmolol 0.25 mg/kg(group E,16 cases)or normal saline (group C,15 cases)at 2 min before induction.The induction of general anesthesia was performed with the same drugs.Sodium nitroprusside 50-100 μg was administered tomake systolic pressure(SBP)decreased by 15-25 mm Hg at different time points of before induction,before incubation,at 5,10,15,20 and 30 rain after intubation.The RR intervel on ECG was recor(ded and BRS was calculated during hypotensive period.Results BRS was reduced in groups of N,U and C after intubation compared with that before(P<0.05 or P<0.01),which was lower in grouP N than that in group C,but was higher in group E than that in group C at all time points(P<0.05).Conclusion The induction of general anesthesia may reduce BRS in EH patients.which is aggravatedby preinjection of nicardipine.Urapidil has no effect on BRS,but esmolol may increase BRS during induction of general anesthesia.
3.Comparative proteome research of epithelial cells and stroma from invasive ductal carcionma patients
Chinese Pharmacological Bulletin 2015;(5):697-703
Aim To study the difference of proteins expression of epithelial cells and stroma of breast canc-er patients.Methods Formalin-fixed paraffin-embed-ded tissue samples from invasive ductal carcionma pa-tients were stained by improved HE staining methods. And the neoplastic epithelium and stroma were micro-dissected using laser capture microdissection and ana-lysed by mass spectrometry.Results Total 43 1 differ-ent proteins were detected by mass spectrometry and there were respectively 384 and 298 different kinds of proteins identified in epithelial cells and stroma.A-mong them,25 1 proteins were commonly expressed in two samples,while the contents of 69 and 60 proteins in stroma were respectively higher or lower than the ones in epithelial cells.The expression level and local-ization of proteins identified in epithelial cells and stro-ma were associated with their roles in development and progression of tumor cells.Conclusions The differen-tial expression proteins between epithelial cells and stroma of invasive ductal carcionma patients may func-tion as biomarkers for breast cancer screenning,diag-nosis and prognosis.
4.Peptidic HIV fusion inhibitors targeting envelope glycoprotein transmembrane subunit gp41
Shuwen LIU ; Shuguang WU ; Shib JIANG
Chinese Pharmacological Bulletin 2003;0(11):-
HIV envelope glycoprotein transmembrane subunit gp41 plays a major role in the fusion of viral and target cell membranes. The extracellular region of gp41 consists of N-terminal fusion peptide and downstream N- and C-heptad repeat (NHR and CHR) regions. The peptidesderived from the NHR and CHR regions, designated N- and C-peptides, respectively, have potent inhibitory activity on the HIV mediated cell fusion. C-peptide T-20 has just got the approval of U.S. FDA, which became the first success of one new class anti-HIV agents, named HIV-fusion inhibitors. However, a relatively long peptide such as T-20 suffers from several limitations including proteolytic sensitivity, large dosage, therefore it is unable to produced by gene engineering. Alternately, shorter peptidic fusion inhibitors and active peptides suitable for gene engineering are pursued. In the recent years, this kind of peptide modifications are hot spots in HIV research field and contribute a lot to the inhibitory mechanism of N- and C-peptide.
5.Research on treatment of 120 cases of pulmonary Interstitial fibrosis with prednisone anti Shuxuening Injection
Ming WEI ; Li LIU ; Shuwen CHE
International Journal of Traditional Chinese Medicine 2010;32(2):152-153
Objective To study the clinical effect ofprednisone combined with Shuxuening injection on pulmonary interstitial fibrosis. Methods 120 cases were randomly recruited into a treatment group and a control group. The control group was treated with prednisone, and the treatment group was additionally given Shuxuening injection on the basis of the control group. The changes of vital capacity (VC), PO_2, PCO_2 and imaging were observed. Results The total effective rate was 81.67% and 66.67% in the treatment group and the control group Respectively, showing significant difference (P<0.05). VC and PO_2 were raised in both groups after the treatment (P<0.05), while the treatment group showed better results than the control group (P<0.05). PCO2 were also raised in both groups after the treatment (P<0.05), while there was no significant diference between the two groups (P > 0.05). There were 27 cases (45.00%) and 19 cases (31.67%) showed improvement in imaging in the treatment group and the control group respectively, manifesting a significant difference (P<0.05) . Conclusion Treatment of prednisone with Shuxuening injection is better than prednisone on pulmonary interstitial fibrosis. This method is worthy of clinic promotion.
6.Spiral CT Scanning Method and Technique Applied to Chest Examine:1000 Cases Analysis
Shiming TONG ; Hui LIU ; Shuwen YUAN
Journal of Chinese Physician 2001;0(07):-
Objective To evaluate the diagosis value of different spiral computed tomography(CT) chest scanning methods in the differentiation of various pulmonary diseases,in order to avoid x-ray irradiation damage and reduce patients economic burden,but the diagnosis criterion should be guaranteed still.Methods 1000 cases of chest scan by spiral CT were randomly analyzed.In 927 conventional scan cases,including 155 cases of simple plainscan,474 cases of direct contrast scan,25 cases of plain plus contrast scans,73 cases of CT angiography.In addition,high resolution CT(HRCT) for 105 cases,thin layer scan for 86 cases,dynamic scan for 6 cases,and 40 cases bronchgraphy diagnosis were also carried out in the conventional scanning cases.Results The different CT scanning methods were adapted for diffenent pulmonary diseases.An adaptive scanning method and technique can decrease X-ray irradiation dosage and rise accuracy of diagnosis.Conclusions Aptimal scanning method and technique should be alternative according the clinical need and the patients status.
7.Research progress on the structure of HIV envelope glycoprotein and related HIV entry inhibitors
Chenglai XIA ; Shibo JIANG ; Shuwen LIU
Chinese Pharmacological Bulletin 2003;0(08):-
HIV-1 envelope glycoprotein gp120 and gp41 are considered as two important parts in viral entry.In the process of virus entry,CD4 first binds to gp120 and causes the conformation of gp120 to change.Furthermore the conformation of gp41 has also been changed.Many peptides,macromolecular compounds and small molecule compounds which bind to gp120 or gp41 can deter the progress of virus entry.These compounds can play an important role in halting the spread of HIV-1 in this way.The structure and interaction of gp120 and gp41 are reviewed here,as well as the anti-HIV agents blocking the HIV entry by targeting the HIV-1 envelope glycoprotein.
9.Serum cystatin C and serum creatinine in evaluation of renal function in kidney diseases.
Hang LIU ; Xiangmei CHEN ; Shuwen LIU ; Al ET ;
Chinese Journal of Practical Internal Medicine 2006;0(S1):-
Objective To evaluate serum eystatin C as a marker of glomerular filtration rate(GFR)in kidney diseases and as screening test to detect reducing of GFR.Methods Serum cystatin C,serum creatinine and urine creatinine were measure in 81 patients with various nephropathies in our hospital.Additionally,serum eystatin C of 100 blood do- nors were measured as normol controls.Results The relationship rate between cystatin C and 24 hours creatinine clean- rance(R=-0.657)is better than between serum creatinine and 24 hours creatinine(R=-0.573).To creatinine cleanrance estimated by Cockcroft-Gault formular(Cockcroft),we also obtain the same results(r=-0.674 vs r=- 0.596).Cystatin C showed a high sensitivity and negative predictive value for detecting impaired glomerular function in patients,but the specificity and positive predictive valuewas slight low.There were no significantly differ between cysta- tin C and creatinine in receive-operating characteristic plot(ROC).Conclusion Cystatin C is a better marker than creatinine to detect reduced GFR as measured by 24 hours creatinine eleanrance and Cockcroft-Gault formular.The ef- ficacy of Cystatin C as a screening test need more confidents.
10.Application of hemodilution combined with tranexamic acid in neurosurgical operation
Xibao LUO ; Zhigui LIU ; Meng LIANG ; Gaoxiang LIN ; Shuwen ZHAI
Chinese Journal of Postgraduates of Medicine 2011;34(27):28-31
ObjectiveTo study the safety and effectiveness of acute hypervolemic hemodilution (AHH) combined with tranexamic acid(TA) in neurosurgical operation. Methods Forty patients underwent selective neurosurgical operation were divided into two groups by radom digits table with 20 cases each, both groups were infused HES(130/0.4) 20 ml/kg for AHH after anesthesia, TA intravenous injection of loading 10 mg/kg, 1 mg/(kg·h) continuous infusion until the end of surgery in experimental group,only for AHH in control group. The mean arterial blood pressure(MAP), central venous pressure(CVP), heart rate (HR), pulse oxygen saturation (SpO2) were measured before AHH (T0), A HH immediately (T1), 1 h after AHH (T2), at the end of operation (T3), and in the corresponding time hemoglobin (Hb), hematocrit (Hct),prothrombin time (PT), activated partial thromboplastin time (APTT), platelet ( Plt ), fibrinogen ( FIB ) were measured; the intraoperative bleeding, blood transfusion and transfusion rate were counted in both groups.ResultsThere was no significant difference in HR and MAP at different time between two groups (P >0.05),compaued with T0,CVP at T1,T2 was increased (P<0.05),Hb and Hct at T1,T2,T3 were decreased (P< 0.05 ). PT and APTT at T2,T3 were longer than that at T0 in control group (P< 0.05 ) ;Plt at T1 ,T2,T3 was lower in control group than that at T0 in two groups (P < 0.05 ), Plt at T2, T3 was obviously increased in control group compared with experimental group (P < 0.01 ) ; FIB at T2, T3 was lower than that at T0 in control group (P <0.05). The intraoperative bleeding, blood transfusion and transfusion rate in experimental group [(650 ±560) nl, (150 ± 50)ml,30%(6/20)]were lower than those in control group [(820 ±410) ml,(380 ±290) ml,60% (12/20)],there were significant differences between two groups(P <0.05).ConclusionAHH combined with TA has obvious effect of saving blood and hemodynamic stability with less influence on coagulation in neurosurgical operation.