2.Cytotoxicity of epigallocatechin-3-gallate to LNCaP cells in the presence of Cu2+.
Hai-ning YU ; Sheng-rong SHEN ; Yao-kang XIONG
Journal of Zhejiang University. Science. B 2005;6(2):125-131
Epigallocatechin-3-gallate (EGCG) has shown remarkably anti-cancer activity, with its bioactivity being related to reactive conditions, such as pH and metal ions. The present study investigated the degradation of EGCG and its effect on prostate cancer cell in the presence of Cu2+. EGCG was incubated with prostate cancer cells, LNCaP, pretreated with or without Cu2+. EGCG in F-12 medium was quantified using HPLC and the viability of cells was assessed by gel electrophoresis, flow cytometry, and electron microscope. The results of HPLC showed that EGCG degraded completely within 12 h in F-12 medium with or without Cu2+. Gel electrophoresis and flow cytometry did not detect apoptosis of LNCaP cells when they were incubated with EGCG. Electron microscopy examination revealed that EGCG-Cu2+ complex led to damage of cytoplasm membrane in LNCaP cells. It was speculated that not EGCG, but its oxide and complex with Cu2+, are the bioactive components responsible for its cytotoxicity to LNCaP prostate cancer cells.
Anticarcinogenic Agents
;
administration & dosage
;
Apoptosis
;
drug effects
;
Catechin
;
administration & dosage
;
analogs & derivatives
;
Cell Line, Tumor
;
Cell Proliferation
;
drug effects
;
Cell Survival
;
drug effects
;
Copper
;
administration & dosage
;
metabolism
;
Dose-Response Relationship, Drug
;
Drug Combinations
;
Humans
;
Male
;
Prostatic Neoplasms
;
drug therapy
;
pathology
;
physiopathology
3.Non-nucleoside reverse transcriptase inhibitors (Part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines.
Yuan-Zhen XIONG ; Hai-Rong HU ; Fen-Er CHEN ; Jan BALZARINI ; Christophe PANNECOUQUE ; Erik de CLERCQ
Acta Pharmaceutica Sinica 2009;44(2):145-149
Eight new diaryltriazine derivatives containing 4-allylamino and 4-azido substitutes guided by molecular docking have been designed and synthesized based on our previous work. The evaluation of HIV inhibitory activity demonstrated that all compounds were potent against HIV-1 replication. The most active compound 7c exhibited activity against HIV-1 (IC50 = 0.034 micromol x L(-1), SI = 6,475) and the double mutant strain (IC50 = 9.39 micromol x L(-1)) in the micromolar range, which was more potent than nevirapine.
Anti-HIV Agents
;
chemical synthesis
;
chemistry
;
pharmacology
;
Catalytic Domain
;
HIV-1
;
drug effects
;
Inhibitory Concentration 50
;
Molecular Structure
;
Reverse Transcriptase Inhibitors
;
chemical synthesis
;
chemistry
;
pharmacology
;
Triazines
;
chemical synthesis
;
chemistry
;
pharmacology
4.A case-control study on risk factors for nosocomial infection by extended-spectrum beta-lactamases-producing bacteria.
Rong JIN ; Xiang-yang LI ; Hai-shen KONG ; Guo-xiong LI ; Wei WANG
Chinese Journal of Preventive Medicine 2003;37(1):41-44
OBJECTIVETo explore the risk factors for nosocomial infection caused by extended-spectrum beta-lactamases (ESBLs)-producing bacteria in hospitals of Zhejiang province.
METHODSOne hundred and eighty-five cases with nosocomial infection (108 men and 77 women, with an average age of 55 +/- 17 years) caused by positive-ESBLs bacteria, including 59 cases of respiratory infection, 71 with urinary infection, ten with blood infection, 30 with wound infection and 59 with other infection, and 77 controls with nosocomial infection (54 men and 23 women, with an average age of 54 +/- 20 years) caused by negative-ESBLs bacteria, including 38 cases of respiratory infection, 20 with urinary infection, six with blood infection, eight with wound infection and five with other infection, from six hospitals in Zhejiang Province were studied during May 1999 to May 2000. Data were analyzed with unconditional logistic regression and principal component analysis (PCA).
RESULTSMultivariate unconditional logistic regression analysis showed that the independent risk factors for nosocomial infection were use of the third generation cephalosporins for more than three days (odds ratio, OR 4.52, 95% confidence interval of OR 2.30 - 8.89), combined use of antibiotics (OR 2.86, 95% CI 1.51 - 5.43), use of quinolones for more than three days (OR 2.44, 95% CI 1.18 - 5.04), use of adrenal cortical hormone (OR 2.16, 95% CI 1.08 - 4.31) and oxygen inhalation (OR 2.56, 95% CI 1.14 - 5.72). Five principal components were extracted from the 14 risk factors for nosocomial infection with ESBLs-producing bacteria by principal component analysis, with a contribution of cumulative variance of 60.2%, and arranged in an order as follows, use of ventilator, tracheal intubation or tracheotomy, oxygen inhalation, retaining needle in vein, indwelling urethral catheter, use of the third generation cephalosporins over three days, hospitalization over ten days, use of quinolones over three days, combined use of antibiotics, use of aminoglycosides antibiotic over a week, use of adrenal cortical hormone, catheterized examination and prophylactic use of antibiotics.
CONCLUSIONSNosocomial infection with ESBLs-producing bacteria could attribute to multiple factors, mainly to invasive manipulation and use of antibiotics.
Case-Control Studies ; Cephalosporins ; pharmacology ; China ; epidemiology ; Cross Infection ; epidemiology ; microbiology ; Drug Resistance, Bacterial ; physiology ; Drug Therapy, Combination ; pharmacology ; Drug Utilization ; Female ; Humans ; Length of Stay ; Male ; Microbial Sensitivity Tests ; Middle Aged ; Multivariate Analysis ; Risk Factors ; beta-Lactamases ; metabolism
5.Vascular dysfunction in the offspring of AT1 receptor antibody-positive pregnant rats during high-salt diet.
Xi ZHANG ; Su-Li ZHANG ; Hai-Yan XIONG ; Yun-Hui DU ; Lin QUAN ; Jie YANG ; Xiu-Rui MA ; Hui-Rong LIU
Acta Physiologica Sinica 2011;63(2):149-154
Antibody against the angiotensin AT1 receptor (AT1-Ab) could disturb placental development. The placenta is the key organ between mother and fetus. Placental damage will seriously impair fetal growth and development in utero, leading to intrauterine growth restriction (IUGR). Based on the fetal origins of adult disease (FOAD) hypothesis, IUGR could increase a propensity to develop adult onset cardiovascular disease (CVD). The present study was designed to determine whether vascular function has changed in the adult offspring of AT1-Ab positive pregnant rats. Twenty four female rats (8-week-old, AT1-Ab negative) were randomly divided into two groups, immunized and vehicle groups. Immunized group received active immunization to establish AT1-Ab-positive model, while vehicle group was subjected to Freund's adjuvant without antigen. After 8 weeks of immunization, the antibody titers in sera from the female rats were detected by enzyme-linked immunosorbent assay (ELISA). Then all the female rats were mated with normal Wistar male rats and became pregnant. Immunized/vehicle group offspring rats (I offspring/V offspring) were raised to 40-week-old under standard chow feeding. Then the two groups' offspring rats were given a high-salt diet for 12 weeks (4% NaCl in chow feeding). Systolic blood pressure (SBP) was measured dynamically by noninvasive blood pressure system. The vascular ring experiment was performed to detect vascular function and reactivity. As detected by ELISA, the titers of antibody peaked at the 8th week (OD values: 2.75 ± 0.08 vs 0.33 ± 0.01, P < 0.01 vs vehicle group at the same time point). There was no significant difference of SBP between the two groups' offspring rats during the high-salt diet (P > 0.05). Isolated thoracic aortic rings of I offspring had significantly decreased constriction under norepinephrine treatment (P < 0.01 vs V offspring) and significantly decreased dilation under acetylcholine treatment (P < 0.05 vs V offspring). These results suggest that the offspring of AT1-Ab-positive pregnant rats are more susceptible to vascular functional abnormality while being fed high-salt diet.
Animals
;
Antibodies
;
blood
;
Cardiovascular Diseases
;
etiology
;
physiopathology
;
Disease Susceptibility
;
Female
;
Fetal Growth Retardation
;
physiopathology
;
Immunization
;
Pregnancy
;
Prenatal Exposure Delayed Effects
;
Rats
;
Rats, Wistar
;
Receptor, Angiotensin, Type 1
;
immunology
;
Sodium Chloride, Dietary
;
administration & dosage
;
adverse effects
6.hPARP1 genetic polymorphism in southern Chinese Han and Miao populations.
Huan-wen TANG ; Hai-rong LIANG ; Zhi-xiong ZHUANG ; Da-lin HU
Chinese Journal of Medical Genetics 2006;23(5):578-580
OBJECTIVETo study hPARP1 genetic polymorphism in southern Chinese Han and Miao populations.
METHODSBlood samples from 187 and 210 southern healthy Han and Miao populations were collected. The mutations of exons 12,13,16 and 17 of hPARP1 gene were investigated by PCR-single-strand conformation polymorphism(SSCP).
RESULTSFragments of 253 bp,313 bp,175 bp,362 bp within exons 12,13,16 and 17 respectively of hPARP1 gene were amplified by multiple PCR. An SSCP variant in exons 12,13,16 and 17 of PARP1 gene in 187 healthy Han and 210 healthy Miao individuals was identified. Seven single-base substitutions compared with the sequence of PARP1 gene were identified: a T to C transition in exon 12 (Phe548Ser), a G to T transition in exon 13 (Ala683Ser), a G to T transition in exon 16 (Asp798Tyr), and a A to G transition in exon 17 (His808Arg).
CONCLUSIONThere were polymorphism sites in exons 12,13,16,17 of hPARP1 gene in southern Chinese Han and Miao populations; these results may be useful for the establishment of PARP1 genotyping, and these newly described PARP1 alleles would be advantageous indicators for population studies.
Adult ; Alleles ; China ; Exons ; genetics ; Female ; Gene Frequency ; Genotype ; Humans ; Male ; Poly (ADP-Ribose) Polymerase-1 ; Poly(ADP-ribose) Polymerases ; genetics ; Polymerase Chain Reaction ; Polymorphism, Single Nucleotide ; genetics ; Polymorphism, Single-Stranded Conformational
7.Low concentration of hydroquinone-induced adaptive response in hPARP-1 protein normal and deficient cells.
Huan-wen TANG ; Hai-rong LIANG ; Zhi-xiong ZHUANG ; Yun HE
Chinese Journal of Industrial Hygiene and Occupational Diseases 2005;23(4):274-277
OBJECTIVETo investigate whether or not adaptive response of hPARP-1 protein normal and deficient cells is induced by low dose of hydroquinone (HQ), and to analyze the relationship between the adaptive response and micronuclei formation, and cell cycle alteration in human embryo lung fibroblasts (HLF), so as to elucidate the mechanism of adaptive response.
METHODSHLF, HLFC and HLFP cells pretreated with low concentration were retreated by high concentration of HQ. Cellular viability, the rate of micronuclei and abnormal nuclei, cell cycle and DNA strand break were determined.
RESULTSThe tolerance to 80.0 micromol/L concentration of HQ was enhanced when HLF, HLFC and HLFP cells were pretreated with HQ from 0.001 - 0.050 micromol/L. There were varying degrees of micronuclei and abnormal nuclei in three cells pretreated with low concentration of HQ and then retreated with high concentration of HQ; the cell numbers of G1, G2, S phase in cell cycle were obviously different. When compared with only high attack dose, the micronuclei rate and abnormal nuclei rate of HLF, HLFC and HLFP decreased by pretreatment with HQ at high concentration (P < 0.05), meanwhile increased by pretreatment with HQ at low concentration (P < 0.05). HLF, HLFC and HLFP showed blockage in G2 phase when pretreated with HQ at 0 approximately 0.05 micromol/L, but HLFP showed blockage in G1 phase, and in S phase at 1.0 and 2.0 micromol/L.
CONCLUSIONThe level of adaptive response of hPARP-1 protein deficient cells was lower than normal cell, suggesting that hPARP-1 protein may play an important role in the adaptive response of cells, which may be related with the regulation of cell cycle.
Cell Cycle ; Cell Nucleus ; Cell Survival ; Cells, Cultured ; Dose-Response Relationship, Drug ; Fibroblasts ; cytology ; drug effects ; metabolism ; Humans ; Hydroquinones ; toxicity ; Lung ; cytology ; Poly (ADP-Ribose) Polymerase-1 ; Poly(ADP-ribose) Polymerases ; metabolism
8.Epidemiologicai analysis of plague in Qinghai province from 2001 to 2010
Bai-qing, WEI ; Zu-yun, WANG ; Rong-jie, WEI ; Rui-xia, DAI ; Hai-hong, ZHAO ; Xiao-yan, YANG ; Hao-ming, XIONG ; You-quan, XIN ; Jun, LI
Chinese Journal of Endemiology 2011;30(5):521-523
Objective To explore the plague epidemical trend of nearly a 10 years data in Qinghai province to provide basis for making the prevention and control measures. Method The regional distribution and time distribution of animal and human plague, monitoring and plague foci of survey data in Qinghai from 2001 to 2010 were analyzed with Excel software 2003. Results In Qinghai province, a total of 167 strains of Yersinia pestis were isolated from infected animals and insects in 10 years. Yersinia pestis was mainly distributed in Wulan,Delinha, Geermu, and Tianjun, along the Qinghai-Xizang railway. Human plague was occurred every year from 2001 to 2010 except 2002, 2007, 2008, and 2010. In the 10 years, there were 37 plague cases and 16 of these cases died, the mortality was 43.24%. The plague cases were mainly distributed in Nangqian, Qumalai, Chenduo,Zhiduo, Xinghai, Tongde, Tianjun, Wulan and Qilian. And these cases were found mostly in the period from May to October, especially in the period from August to October. Major clinical type of the plague cases was lung-type (62.16%,23/37). Conclusions The plague epidemic situation in Qinghai province is still severe, animal plague occurred year after year, and human plague outbreaks occasionally. Monitoring and early warning in the key areas should be strengthened, and the comprehensive measures of plague prevention and control should be carried out to reduce the incidence and prevalence of plague.
9.Study on the transmission of Hantaan virus and Orientia tsutsugamushi by naturally dual infected Leptotrombidium scutellare through stinging.
Juan YU ; Xiao-zhao DENG ; Zhan-qiu YANG ; Ping-ping YAO ; Han-ping ZHU ; Hai-rong XIONG ; Chun-lei LI ; Yun ZHANG
Chinese Journal of Preventive Medicine 2010;44(4):324-328
OBJECTIVETo investigate whether Leptotrombidium scutellare could be naturally infected by both Hantaan virus (HV) and Orientia tsutsugamushi (OT) and transmission status by stinging.
METHODS3459 Leptotrombidium scutellares from mice bodies and 3265 which were free were collected in the epidemic area of hemorrhagic fever with renal syndrome (HFRS) and tsutsugamushi disease.15 days later, the suspensions of lung and spleen of mice with 6 in a group stung by 1, 5 or 10 infected mites were injected intra-cerebrally into other mice for the detection of HV and OT in the next 6 generations of the mice, with immunofluorescent antibody technique (IFAT) and Giemsa staining technique. The passages of Vero-E6 cells inoculated on the aseptic filtrations from different number of infected mites were used to detect HV and OT pathogens. HV-RNA and OT-DNA were detected by PCR.
RESULTSAfter passage, HV positive mouse body mite group out of both 5 and 10 mites in the sixth generation, OT positive mouse body mite group out of the 10 mites in the sixth generation, both HV and OT positive mouse body mite group out of 1 mite in the fifth and sixth generation, both HV and OT positive mouse body mite group out of 5 and 10 mites in the sixth generation, and free mites group out of 1, 5 and 10 mites in the sixth generation, were found one mouse infected by both HV and OT, respectively. Out of the fourth generation of Vero-E6 cells, one sample was found both HV and OT positive out of 5 and 10 HV and OT mouse body mite group, respectively. In the sixth generation, both HV and OT positive cells were detected in one mouse mite group and the 1, 5, 10 free mite groups, respectively. HV-RNA and OT-DNA were all detected by PCR.
CONCLUSIONBoth HV and OT could be coexisted in wild Leptotrombidium scutellare and transmitted by stinging.
Animals ; Hantaan virus ; Hemorrhagic Fever with Renal Syndrome ; transmission ; Insect Bites and Stings ; Mice ; Mice, Inbred Strains ; Mites ; parasitology ; virology ; Murinae ; Orientia tsutsugamushi ; Scrub Typhus ; transmission ; Trombiculidae
10.Half-dose Zenapax for acute rejection prevention after renal transplantation.
Yun-song ZHU ; An-ping XU ; Huei-xu HE ; Li-pei FAN ; Hai-bo NIE ; Juen NV ; Wei-nie HU ; Qing-rong LI ; Zhi-xiong DENG
Journal of Southern Medical University 2006;26(12):1818-1820
OBJECTIVETo investigate the efficacy and safety of half-dose Zenapax for prevention of acute rejection after renal transplantation.
METHODSAccording to the immunosuppressive regimen and renal function after transplantation, patients were divided into 4 groups, namely groups A, B, C, and D of 90, 73, 11 and 13 patients, respectively. Blood creatinine measured 1 week after operation was <176.6 micromol/L in groups A and B, and was >353 micromol/L in groups C and D. Patients in groups A and C were given 25 mg Zenapax (0.5 mg/kg) and MMF 0.75 g before operation, and those in groups B and D had only MMF of 0.75 g. All patients were given Pred, CsA and MMF after operation, and the rejection episodes, the time of acute rejection onset, the rate of rejection reversal and complications were analyzed in the time period of 6 months after operation.
RESULTSAfter the operation, 13 patients (14.4%) developed acute rejection in group A, 18 (24.6%) in group B, 6 (54.5%) in group C and 7 (53.8%) in group D (P<0.01). The incidence of acute rejection in group B was significantly lower than that in groups C and D groups (P<0.01), and the latter two groups had similar incidence. The time of acute rejection onset ranged from 3 to 9 days postoperatively (mean 6.2-/+3.2 days) in group A, significantly delayed as compared with that in group B (range 2-8 days, mean 4.7-/+3.1 days), group C (range 2-7 days, mean 4.3-/+4.2 days) and group D group (range 2-9 days, mean 3.9-/+3.5 days), but the time was similar between groups B, C, and D (P>0.05). All acute rejection cases in group A was reversed, and the rate of reversal was 88.9% (16/18) in group B, 83.3% in group C, and 71.4% in group D. No significant differences were noted in such complications as infection, vascular injuries or gastrointestinal reactions between the 4 groups (P>0.05).
CONCLUSIONZenapax at the dose of 25 mg can safely decrease the risk of acute rejection in patients with good postoperative renal function recovery, but dose not seem effective in patients with delayed graft function recovery.
Acute Disease ; Adolescent ; Adult ; Antibodies, Monoclonal ; administration & dosage ; Antibodies, Monoclonal, Humanized ; Creatinine ; blood ; Female ; Follow-Up Studies ; Graft Rejection ; etiology ; prevention & control ; Humans ; Immunoglobulin G ; administration & dosage ; Immunosuppressive Agents ; administration & dosage ; Kidney Transplantation ; adverse effects ; methods ; Male ; Middle Aged ; Postoperative Complications ; etiology ; prevention & control ; Treatment Outcome