3.Progress in the study of tubulin inhibitors.
Hai SHANG ; Li PAN ; Shu YANG ; Hong CHEN ; Maosheng CHENG
Acta Pharmaceutica Sinica 2010;45(9):1078-88
Microtubule is one of the key components of the cytoskeleton and plays an important role in the maintenance of cell shape and the process of signal transduction and mitosis. Due to the extreme importance of microtubule in the process of mitosis, tubulin becomes one of the most important targets for development of new anticancer drugs and tubulin inhibitors are used for the treatment of cancer nowadays. These inhibitors have antitumor activity by inhibiting or promoting the assembly of tubulin to microtubules and interfering the process of cell mitosis. This review summarized the research progress of the tubulin inhibitors, especially the introduction of the tubulin inhibitors of pharmacological activities and the progress of clinical research. Also, the development trend of these inhibitors is discussed.
5.Effects of mechanical stretch on expression of pentraxin-3 mRNA and protein in A549 cells
Huaqing SHU ; Qingping WU ; Lei YANG ; Hong ZHANG ; Shanglong YAO
Chinese Journal of Anesthesiology 2008;28(11):1023-1025
Objective To evaluate the effects of mechanical stretch on pentraxin-3(PTX-3)mRNA and protein expression in human alveolar epithelial cells (A549 cells).Methods The human lung epithelial adenocarcinoma cells A549(A549 cells)were purchased from cell biology laboratory,Tongji Medical College,Huazhong University of Science and Technology.The cultured A549 cells were inoculated on collagen Ⅰ BioFlex plates and divided into 5 groups(n=3 wells each):group Ⅰ normal control;groupⅡsham mechanical stretch;group Ⅲ mechanical stretch;groupⅣsiRNA and groupⅤ siRNA+mechanical stretch.In group Ⅲ the cells underwent square cyclic mechanical stretch for 4 h using the Flexercell Systcm.In group Ⅳ the cells were transfected with chemosynthetic PTX-3 specific siRNA by RNAi technique.In group Ⅴ at 24 h after being transfected with PTX-3 siRNA the cells underwent mechanical stretch for 4 h.In groupⅡ mechanical stretch of the cells were prevented by Flexstep.The expression of PTX-3 mRNA in the cells was detected by real-time PCR and the expression of PTX-3 protein in the culture media was determined by Western blotting.Apoptosis of the cells was measured bv flow cytometry(Beeten-Dickinson,USA).Results PTX-3 mRNA and protein expression was signlficantly up-regulated by mechanical stretch in groupⅢand decreased by transfection with siRNA in group Ⅳand Ⅴ as compared with group Ⅰ andⅡ(P<0.05 or 0.01).The apoptosis ratio was significantly higher in group Ⅲ and Ⅴ than in groupⅡ and was significantly lower in group Ⅴ thanin group Ⅲ(P<0.01).Conclusion Mechanical stretch can up-regulate PTX-3 mRNA expression in A549 cells.
6.Study on stability of N-terminal site-specific PEGylated uncase
Jian YANG ; Shu ZHU ; Lei CAI ; Hong TIAN ; Wenbing YAO
Chinese Journal of Biochemical Pharmaceutics 2010;31(1):29-31
Purpose The research was conducted to evaluate the stability of N-terminal site-specific PEGylated uricase. Methods The enzyme activity is used as an index to evaluate the thermal stability (at 4-80 ℃) , the pH stability, the ability of avoiding the trypsin digestion and half-life in vivo of PEG-uricase, then it is compared with uricase. Results PEGylated uricase is thermally more stable than uricase between 4 ℃ and 60 ℃, but at 70 ℃, the enzyme activity of both PEG-uricase and uricase decreases sharply. In the test of pH stability, the curve of uricase shows an obvious decrease of enzyme activity at 5 .2-6.0 and 9.2-10.0. The behavior of PEG-uricase indicates that the destabilizing was prevented effectively by PEGylation. The test of anti-trypsin digestion suggests that PEG-uricase retains 70% of its enzyme activity,but uricase only 20% ,200 minutes after being reserved in trypsin solution. Stability in vivo indicates that the half-life of PEG-uricase is 1 530 min and uricase, only 45 min. Conclusion PEGylated uricase has improved thermal stability, the pH stability, ability of protecting from trypsin digestion and stability in vivo.
7.Literature Analysis of 132 Cases of Adverse Drug Reaction Induced by Monoclonal Antibody
Shu YANG ; Haiwen SHI ; Xiuqing GAO ; Ge HONG ; Shan GAO
China Pharmacy 2015;(23):3223-3225
OBJECTIVE:To investigate rules and characteristics of the adverse drug reactions(ADR)induced by monoclonal antibodies,and provide reference for rational drug use. METHODS:The literatures of ADR induced by monoclonal antibodies from Jan. 1979 to Dec. 2014 were retrieved and analyzed. RESULTS:Among the 132 ADRs induced by monoclonal antibodies,57 were male(43.18%),75 were female(56.82%),the ratio of male to female was 1∶1.3,the youngest was 2 years old,and oldest was 111 years old;Adalimumab dominated monoclonal antibody drugs(70 cases,53.03%);there were a maximum of ADR(44) within 1 d,accounting for 33.33%;ADR induced by monoclonal antibodies mainly were skin lesions (20.72%),systemic reac-tions(18.42%)and cardiovascular system damage(16.78%),with the specific performance of rash,itching,chills,fever,palpi-tation,rapid heartbeat and so on. CONCLUSIONS:ADR induced by monoclonal antibodies is more common in the clinic. The clin-ic should timely promote and strengthen the patients' care to ensure safe drug use and improve level of clinical treatment.
8.Clinical Efficacy of Entecavir for Chronic Serious Hepatitis B
Hong WANG ; Shu YANG ; Xiuzhong ZENG ; Qiangsheng XU ; Zhemei HUANG
China Pharmacy 2007;0(26):-
OBJECTIVE: To discuss the significance of Entecavir(ETV) in the treatment of chronic serious hepatitis B(HBV).METHODS: 54 patients with chronic serious hepatitis B were assigned to receive combined therapy in which antiviral drugs such as interferon and(or) nucleoside(acid) analogues antiviral drugs were excluded(control group,n=26) or combined therapy in combination with entecavir(0.5 mg?d-1) qd(treatment group,n=28).The course of treatment in both groups were 6 weeks.The hepatic function,HBV markers and HBV-DNA quantitation were deteted every two weeks.The improvement rate of patients after the completion of treatment were recorded.RESULTS: In the follow-up of six weeks,serum HBV-DNA and total bilirubin levels decreased markedly,and significant difference was noted between compared with the control group;ALT,AST,ALB and PT decreased in both groups,but the differnces between the two groups were not significant;there was no signficnant differnce in improvement rate between the treatment group and the control group(89.3% versus 84.6%).CONCLUSION: Entecavir can rapidly lower serum HBV-DNA level,downregulate bilirubin level,improve liver function,improve patients prognosis in patients with hepatitis B,thus it can be used to treat serious hepatitis B.However,used in short term,the survival rate of patients with severe hepatitis B can hardly be improved.
9.Critical Antigenic Structure in Inducing Immune Damage of Peripheral Nerve Following Campylobacter Jejuni Infection
xiao-hong, WANG ; xiao-mei, SHU ; bing-zhu, YANG
Journal of Applied Clinical Pediatrics 2004;0(12):-
0.05).3.Thirty-three point three percent of animals from parental strain group were found fibrillations potentials and the po-sitive sharp waves in gastrocnemius electromyogram,no obvious abnormal waves were found in animals from both waaF mutant and control group.Conclusions The ganglioside-like epitope in LOS of CJ is critical antigen in inducing GM1-IgG antibody and in inducing conduction block of peripheral nerve,therefore,provide a support for the molecular mimicry theory as a pathogenesis in the axonal GBS following CJ infection.
10.Analysis of clinical features of hepatitis B virus/hepatitis C virus coinfected patients with different virological profiles
Ka ZHANG ; Hong CAO ; Xiaoan YANG ; Lubiao CHEN ; Xiaolü HONG ; Xin SHU ; Gang LI ; Qihuan XU
Chinese Journal of Infectious Diseases 2011;29(7):429-432
Objective To understand the clinical features of hepatitis B virus(HBV)/hepatitis C virus(HCV)coinfected patients with different virological profiles.Methods The clinical data of 186 patients with HBV/HCV coinfection from May 1999 to May 2010 in the Third Affiliated Hospital of Sun Yat-Sen University were analyzed retrospectively.The demographic data,epidemiological data,laboratory results and pathological index were analyzed.The statistical analysis was done using t test and chi square test.Results A total of 186 patients were divided into 4 groups:66(35.5%)in HBV DNA(-)/HCV RNA(-)group,8(4.3%)in HBV DNA(+)/HCV RNA(+)group,68(36.6%)in HBV DNA(+)/HCV RNA(-)group and 44(23.7%)in HBV DNA(-)/HCV RNA(+) group.The gender composition,complication incidence,transmission among drug users,alanine aminotransferase(ALT)level,total bilirubin(TBil)level,prothrombin activity(PTA)and hapatitis B e antigen(HBeAg)negative rate were all significantly different among four groups(F or x2=11.578,8.451,11.738,2.669,5.102,4.254 and 18.413,respectively;all P<0.05).In groups of HCV RNA(-)and HCV RNA(+),the proportions of patients infected through drug abuse were 49.3%and 23.1%,respectively(x2=9.987,P:0.002)and blood transfusion transmission were 29.9%and 46.2%,respectively(x2=4.412,P=0.036).When HBV DNA was negative,the median ALT levels in HCV RNA(-)and HCV RNA(+)patients were 177 U/L and 62 U/L,respectively(t=2.200,P<0.05),median TBil levels were 133 μmol/L and 20μmol/L,respectively (t=3.608,P<0.05)and PTA were 70.6%±27.7%and 83.3%±27.8%,respectively(t=-1.982,P<0.05).The HBeAg negative rate was not affected by HCV RNA levels(t=0.707,P>0.05).The HBeAg negative rate in HBV DNA(-)patients was 85.5%,which was higher than that in HBV DNA(+)patients(59.2%)(x2=16.393,P<0.05).Conclusions HBV DNA(+/-)/HCV RNA(-)profile were major components in HBV/HCV confection.HBV DNA level is related to disease progression and prognosis,but not relate to disease severity.Liver function damage and disease severity are aggravated with HCV RNA level decreases.HBV DNA level is related to HBeAg negative rate,while HCV RNA level is not related to HBeAg seroconversion rate.