3.In vitro Antiviral activity of a berberine derivant HB-13 against herpes simplex virus
Jian-Bing WU ; Xin-Yu LI ; Lin LIN ; Pan-Gen CUI ; Jia-Run ZHENG ;
Chinese Journal of Dermatology 2003;0(11):-
Objective To evaluate the in vitro antiviral activity of HB-13,a compound derivant from berberine and its prodrug berberine,against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2). Methods Vero cells were cultured in vitro and infected with HSV.Then,various concentrations of HB-13, berberine,and aciclovir were used to treat these infected cells.The cytopathic effect was observed to deter- mine the antiviral effects and cytotoxicity of HB-13 and berberine.Results For HB-13,berberine and acy- clovir,the half toxicity concentration (TC_(50)) to Vero cells was 31.99,380 and more than 800?g/mL, respectively;the average half inhibitory concentration (IC_(50)) against HSV-1 was 1.328,more than 100,and 0.443?g/mL,respectively,the treatment index (TI) against HSV-1 was 24.09,less than 3.80,and more than 1805.87,respectively;the IC_(50) against HSV-2 was 1.344,more than 100,and 0.679?g/mL,respectively,the TI against HSV-2 was 23.80,less than 3.80 and more than 1178.20,respectively.Conclusion HB-13 possesses marked antiviral activity against HSV-1 and HSV-2 in vitro,while berberine does not.
4.Antitumor activity of erythromycin on human neuroblastoma cell line (SH-SY5Y).
Yongsheng, JIA ; Xiaoyun, MA ; Xiaoli, WEI ; Xin, LI ; Haitao, YAN ; Xiaoyan, LIU ; Jianquan, ZHENG
Journal of Huazhong University of Science and Technology (Medical Sciences) 2011;31(1):33-8
Antitumor effects of erythromycin and the related mechanism were investigated in the present study. Neuroblastoma cells (SH-SY5Y) were exposed to erythromycin at different concentrations for different durations. Cell proliferation was measured by cell counting, and cell viability was examined by MTT assay. Cell cycle phase distribution and the cytosolic calcium level were detected by flow cytometry. Mitochondrial membrane potential was measured by the JC-1 probe staining and fluorescent microscopy. The expression of an oncogene (c-Myc) and a tumor suppressor [p21 (WAF1/Cip1)] proteins was analyzed by using Western blotting. Erythromycin could inhibit the proliferation of SH-SY5Y cells in a concentration- and time-dependent manner. The cell cycle was arrested at S phase. Mitochondrial membrane potential collapsed and the cytosolic calcium was overloaded in SH-SY5Y cells when treated with erythromycin. The expression of c-Myc protein was down-regulated, while that of p21 (WAF1/Cip1) protein was up-regulated. It was concluded that erythromycin could restrain the proliferation of SH-SY5Y cells. The antitumor mechanism of erythromycin might involve regulating the expression of c-Myc and p21 (WAF1/Cip1) proteins.
5.Antitumor efficacy of irinotecan-loaded galactosyl modified lipid bilayer-coated mesoporous silica nanoparticles against hepatocellular carcinoma cells.
Xi CHEN ; Xin-Xin ZHANG ; Fei-Fei LI ; Ya-Nan ZHAO ; Zheng JIA ; Yong GAN ; Juan LI
Acta Pharmaceutica Sinica 2014;49(5):718-725
The purpose of this study is to prepare galactosyl modified lipid bilayer-coated mesoporous silica nanoparticles (GPEM) to enhance the antitumor efficacy against hepatocellular carcinoma cells. The irinotecan (CPT-11) loaded mesoporous silica nanoparticles (MSNs) was coated with the Gal-P123 modified functional lipid bilayer by thin-film dispersion method. Nanoparticles were characterized with particle size, zeta potential, morphology and drug release in vitro. Afterwards, the cell uptake, intracellular concentration of CPT-11, cell apoptosis rate and cytotoxicity were evaluated on human hepatocellular carcinoma cell line Huh-7. The results showed that MSNs were coated with intact lipid bilayers and the nanoparticles had clear core-shell structure. GPEM is stable with the mean particle size of (78.01 +/- 2.04) nm. The low leakage rate in normal physiological conditions in vitro is contributed to the protection of stable lipid bilayer, and the fast drug release in acid environment due to the destruction of the lipid bilayer. On the cell level, the vector could improve the intracellular CPT-11 concentration by 4 times because of the functional lipid bilayer. The high CPT-11 concentration led to the increasement of apoptosis rate by 48.6%, and the reduction of half maximal inhibitory concentration (IC50) values of CPT-11 by 2 times, indicating stronger cell cytotoxicity.
Antineoplastic Agents
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chemistry
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pharmacokinetics
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Apoptosis
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Camptothecin
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analogs & derivatives
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chemistry
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pharmacokinetics
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Carcinoma, Hepatocellular
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drug therapy
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pathology
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Drug Carriers
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chemistry
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Drug Delivery Systems
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methods
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Humans
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Lipid Bilayers
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chemistry
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Liver Neoplasms
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drug therapy
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pathology
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Nanoparticles
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chemistry
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Particle Size
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Silicon Dioxide
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chemistry
7.The heterogeneity of anti-GBM autoantibodies in sera from patients with anti-GBM disease and its clinical correlation
Chang LIU ; Zhen QU ; Rui YANG ; Juan ZHAO ; Xiaoyu JIA ; Xin ZHENG ; Zhangsuo LIU ; Zhao CUI ; Minghui ZHAO
Journal of Peking University(Health Sciences) 2009;41(6):625-629
Objective:To investigate the heterogeneity of epitopes recognized by anti-GBM autoantibodies in sera from a large cohort of Chinese patients with anti-GBM disease and its clinical significance.Methods: The present study included 108 patients with anti-GBM disease who were diagnosed in our hospital, between Jan 1991 and May 2009, with complete clinical and renal pathological data. Sera or plasma exchange of the patients were used to incubate with cryostat section of normal human renal tissue for indirect immunofluorescence (IIF) assay. The cryostat sections of normal renal tissue were pre-treated by 6 mol/L urea to unmask cryptic epitopes, and untreated cryostat sections were used to detect natural exposed epitopes. The sera were diluted from 1:2 to 1:512 to determine titers of anti-GBM autoantibodies Patients with anti-GBM autoantibodies against cryptic or exposed epitopes were further stratified;their clinical and pathological associations were analyzed. Results: Sera from all the 108 patients could recognize cryptic epitopes on normal renal tissue ( urea treated section). IIF showed IgG linear staining along GBM. However, sera from 56/108 patients (group A) could also recognize exposed epitopes on normal renal tissue (untreated section) ; sera from the rest 52/108 patients (group B) could not recognize exposed epitopes. In urea treated condition, the average titer of anti-GBM autoantibodies from sera of patients in group A was significantly higher than that in group B (P<0.01) , ANCA-positive patients in group A were significant less than that in group B (P<0.01) . There was no significant difference between the two groups in regard to other clinical data (including serum creatinine) and renal histopathologic data. Conclusion: Anti-GBM autoantibodies from some patients with anti-GBM disease could recognize natural exposed epitopes, however, their anti-GBM titer for cryptic epitopes was higher than that of those recognizing cryptic epitopes only and the prevalence of serum ANCA was significantly less.
8.Identification and early diagnosis for traditional Chinese medicine-induced liver injury based on translational toxicology.
Jia-Bo WANG ; Xiao-He XIAO ; Xiao-Xi DU ; Zheng-Sheng ZOU ; Hai-Bo SONG ; Xiao-Xin GUO
China Journal of Chinese Materia Medica 2014;39(1):5-9
Recently traditional Chinese medicine (TCM)-induced liver injury has been an unresolved critical issue which impacts TCM clinical safety. The premise and key step to reduce or avoid drug-induced liver injury (DILI) is to identify the drug source of liver injury in early stage. Then the timely withdrawal of drug and treatment can be done. However, the current diagnosis of DILI is primarily governed by exclusive method relying on administering history supplied by patients and experience judgment from doctors, which lacks objective and reliable diagnostic indices. It is obvious that diagnosis of TCM-induced liver injury is especially difficult due to the complicated composition of TCM medication, as well the frequent combination of Chinese and Western drugs in clinic. In this paper, we proposed construction of research pattern and method for objective identification of TCM-related DILI based on translational toxicology, which utilizes clinical specimen to find specific biomarkers and characteristic blood-entering constituents, as well the clinical biochemistry and liver biopsy. With integration of diagnosis marker database, bibliographic database, medical record database and clinical specimen database, an integrative diagnosis database for TCM-related DILI can be established, which would make a transformation of clinical identification pattern for TCM-induced liver injury from subjective and exclusive to objective and index-supporting mode. This would be helpful to improve rational uses of TCM and promote sustainable development of TCM industry.
Animals
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Biomarkers, Pharmacological
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metabolism
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Biopsy
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methods
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Chemical and Drug Induced Liver Injury
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diagnosis
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metabolism
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pathology
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Early Diagnosis
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Humans
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Liver
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drug effects
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pathology
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Medicine, Chinese Traditional
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adverse effects
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Rats
9.Survey of defluoridation water improvement project in Shanxi province from 2005 to 2009
San-xiang, WANG ; Jun, LI ; Zheng-hui, WANG ; Qing-zhen, JIA ; Xiang-dong, ZHANG ; Xiao-tian, CHENG ; Xin-ping, WEN
Chinese Journal of Endemiology 2011;30(1):56-59
Objective To learn the present status of defluoridation water improvement project in Shanxi province in order to provide scientific basis for speeding up the prevention and control of endemic fluorosis.Methods According to "The National Technical Scheme for Endemic Disease Control" from 2005 to 2009, the investigation points were selected in the counties that implemented the measures of water improvement and defluoridation,the status of drinking water defluoridation Project was investigated, and the water fluoride levels were determined by fluoride selective ion electrode. Results The primary status was surveyed in 1658 water improvement and defluoridation projects in 51 counties. The resource of drinking water for water improvement and defluoridation projects was mostly ground water[accounting for 93.12% (1544/1658)]. Among 1658 water improvement and defluoridation projects 1405 projects worked well(accounting for 84.74%) and 190 projects intermittently worked (accounting for 11.46%). Sixty three projects abandoned (accounting for 3.80%), in Datong basin the abandoned projects accounted for 36.36% (12/33). Water fluoride content of 1595 water improvement and defluoridation projects had been determined, among them water fluoride content of 874 projects were above 1.0 mg/L (accounting for 54.80%). The situations of exceeded national standard in the five basins was different(H = 33.22,P < 0.01). The rate of over national standard of fluoride levels in drinking water was 88.37%(38/43) in Datong basin. Therefore, in Datong basin water improvement should be strengthened. Conclusions In Shanxi province the water improvement and defluoridation projects are basically running normally. However, the qualified rate is lower for the water improvement and defluoridation projects. The water improvement status varies dramatically among areas.The situation is still grim in Shanxi province. Water improvement and defluoridation needs to be strengthened to improve the effect of prevention and control of the disease.
10.Effect of ethyl acetate extract of sappan wood on expression of myocardial GrB mRNA in rat model of allogeneic ectopic cardiac transplantation.
Jia-Xin ZHENG ; Ya-Bin ZHOU ; Ying-Zhe LIU
Chinese Journal of Integrated Traditional and Western Medicine 2008;28(6):537-540
OBJECTIVETo explore the action mechanism of the immune active components of sappon wood (SWE) for antagonizing reject reaction by observing the influence of its ethyl acetate extract on mRNA expression of myocardial GrB in rat model of allogenic ectopic cardiac transplantation.
METHODSAnimal model of abdominal cardiac ectopic transplantation was established taking Wistar rat as the donor and SD rat as the receptor. The successfully modeled rats were randomly divided into the model group, the SWE group and the CsA group. GrB mRNA expression was detected by RT-PCR method and myocardial pathomorphologic picture was observed in routine.
RESULTSThe pathologic changes in the SWE group (23 scores) and the CsA group (14 scores) were milder than in the model group (31 scores), the former two could markedly alleviate the myocardial pathologic injury (P<0.05, P<0.01). The GrB mRNA expression in the model group was 1.3000 +/- 0.1207, the SWE group 0. 7070 +/- 0.1215, and the CsA group 0.6700 +/- 0.0997, respectively; compared with the model group, the latter two could obviously down-regulate the expression of GrB mRNA (P<0.01) and no significant difference was found between the latter two groups (P>0.05).
CONCLUSIONSWE could alleviate the pathologic change, down-regulate the mRNA expression of myocardial GrB in allogenic ectopic transplanted myocardium of rats, it is possibly one of the factors for its antagonizing effect against reject reaction.
Acetates ; chemistry ; Animals ; Caesalpinia ; chemistry ; Gene Expression Regulation, Enzymologic ; drug effects ; Graft Rejection ; drug therapy ; Granzymes ; genetics ; Heart ; drug effects ; Heart Transplantation ; immunology ; Male ; Models, Animal ; Myocardium ; metabolism ; pathology ; Plant Extracts ; pharmacology ; therapeutic use ; RNA, Messenger ; genetics ; metabolism ; Rats ; Transplantation, Homologous