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A series of [1,3]dioxolo[4,5-f]isoindolone derivatives were designed, synthesized and evaluated as inhibitors of acetylcholinesterases (AChE). Furthermore, their effects on memory impairment of mice induced by scopolamine were investigated with step-through test. The results suggested that most of the target compounds exhibited potential inhibition on AChE with IC50 values at micromolar range. Compounds I1 (IC50 value of 0.086 μmol · L(-1)) and I2 (IC50 value of 0.080 μmol · L(-1)) showed the strongest AChE inhibitory activity, which are equipotent to donepezil (IC50 value of 0.094 μmol · L(-1)). Moreover, compounds I1-I4 could improve the memory impairment induced by scopolamine in mice.
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A series of novel 4-substituted-3-nitrobenzamide derivatives were designed and synthesized. The structures of the target compounds were confirmed with 1H NMR, 13C NMR, MS and element analysis. Anti-tumor activities against HCT-116, MDA-MB435 and HL-60 cell lines in vitro were evaluated by SRB assay. The results indicated most of the target compounds exhibited potent anti-tumor activity. Compound 4a showed the most potent inhibitory activities against three cancer cell lines with the GI50 values of 1.904-2.111 micromol x L(-1). Compounds 4g, 41-4n exhibited more potent inhibitory activities against MDA-MB435 and HL-60 cell lines with the GI50 values of 1.008-3.586 micromol x L(-1) and 1.993-3.778 micromol x L(-1), respectively. The structure-activity relationship of these compounds is discussed preliminarily.
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OBJECTIVE To study the lower respiratory tract Acinetobacter baumannii infection in cardiac ICU and its risk factors,in order to take effective control measures. METHODS The risk factors of 5 cases respiratory A. baumannii infection in cardiac ICU of our hospital were investigated. RESULTS Patients with A. baumannii infections were concentrated,accounting for 21.7% at the same period in external cardiac ICU. According to the exposure time among children,the regional distribution and the same kinds of pathogens,the nospital acquired infection was determined as a local outbreak epidemia. The pathogenic microorganism monitoring carried out on ventilator-pipes,hands of health care workers and cardiopulmonary bypass machines etc. A. baumannii was found in tube of warming devices. CONCLUSIONS The in-door distribution and pracedures in cardiac ICU do not meet hygiene requirements,the poor sterile concept among medical staff and bad compliance of hand-washing,and the longterm use of mechanical ventilation,broad-spectrum antibiotics and immunosuppressive agents. All these factors contribute the outbreak of hospital acquired infection.
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OBJECTIVE To study the effect of different antibiotic and nursing care in the treatment of patients with malignant tumor complicating with infection,analyze the high-risk factors and provide the dependable basis for controlling infection in hospital.METHODS In the retrospective investigation of our department,there were 82 times of 68 patients complicating with infection from Jan 2006 to Jun 2007.We analyzed the constituent proportion of infection and risk factors.The patients were divided into 4 groups,group A treated with broad-spectrum antibiotic,group B treated with narrow-spectrum antibiotic,group C treated with de-escalation therapy and group D treated with escalation therapy.We observed the course of therapy and the clinical effect.RESULTS The respiratory tract infection was 68.29%(56/82)and it was the highest one.The difference between groups C and D was significantly in susceptible factors(P
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OBJECTIVE To find out the epidemiology of Salmonella aberdeen outbreaks in NICU and the ways to preventing and treating this nosocomial infection. METHODS The 22 cases who developed S.aberdeen in NICU from Mar 26 to Apr 20 2007 were studied prospectively to find out the reasons of the epidemic and treatment s based on the fecal sample culture results. RESULTS These 22 inpatients fecal samples cultures were tested positive for S.aberdeen,but 14 of 22 inpatients were developed infectious diarrhea. CONCLUSIONS S.aberdeen is confirmed as the cause to this infectious diarrhea outbreak,which is mainly transmitted by close contacts.The occurrence of infection outbreak can be reduced or controlled by emphasizing the hands hygiene and aseptic operation of medical workers,attaching importance to surface disinfection of environment and equipments,and establishing the early warning mechanism.
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OBJECTIVE To investigate the trends of susceptibility of Enterobacter cloacae isolates to antimicrobial agents from Shandong provincial nosocomial infection surveillance system. METHODS The data from Shandong provincial nosocomial infection surveillance system from Aug 2001 to Jul 2004 were summarized and analyzed.(RESULTS) In the period of study from Aug 2002 to Jul 2004,231 strains of E.cloacae were collected.The (sputum),(urine) and wounds were major specimens,and accounted for 55.41%, 10.82% and 9.96% from total(specimens),respectively.The resistant rates of E.cloacae isolates to antimicrobials,except imipenem,increased to some extend.CONCLUSIONS Antimicrobial resistance of clinical isolates of E.cloacae threatens the success of(infectious) disease treatment.It is very important to promote the rational use of antimicrobial agents for control of resistance and to take effective measures for the prevention of infections.
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BACKGROUND: Alzheimer disease is a senile degenerative disease of nervous system. Neuron apoptosis is regarded as one of possible reasons,and neuron culture in vitro is a common method to research the mechanism of apoptosis.OBJECTIVE: To observe the influences of nitric oxide-donor, sodium nitroprusside (SNP), on the expression of gene cpp32 in the cultured hippocarnpal neurons in vitro.DESIGN: A randomized controlled animal experiment. SETTING: Institute of Biochemistry and Molecular Biology in Guangdong Medical College.MATERIALS: The experiment was carried out in the Institute of Biochemistry and Molecular Biology, Guangdong Medical College, and newborn (＜ 24 hours) Sprague-Dawley rats were used.METHODS: The hippocampl neurons of rats were primarily cultured, and then treated with SNP of different terminal concentrations (0, 25, 50, 100,200, 400 μmol/L) for 24 hours, and the expressions of mRNA and protein were analyzed with RT-PCR and Western blot respectively. The hippocampl neurons of rats were treated with SNP of different terminal concentrations (0, 25, 50, 100, 200, 400 μmol/L) for 12 hours, and the activity of CPP32 enzyme was detected with CPP32 activity detected kit.MAIN OUTCOME MEASURES: The expressions cpp32 mRNA and CPP32 protein and activity of CPP32 were detected.RESULTS: The cpp32 mRNA expression was unchanged as the increasing dose of SNP, but the pro-CPP32 was activated and the activity of CPP32 was increased significantly at 50 μmol/L SNP which was 3.02 times of that in the control group, and reached to the maximal value at 100 μmol/L which was 3.47 times of that in the control group.CONCLUSION: SNP cannot increase the cpp32 mRNA expression, but can increase degradation of pro-CPP32 and activate CPP32.
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Objective To study the effects of A?25-35 on the expression of gene P21,CDK4,E2F1 and BAX in cultured PC12 cells.MethodsPC12 cells were treated with 25 ?mol/L A?25-35,the relation between cell cycle redistribution and apoptosis was analyzed by flow cytometry(FCM).Protein and mRNA expression of P21,CDK4,E2F1 and BAX were detected by RT-PCR and Western-blot respectively.Results About 90% PC12 cells were found arrest on G0/G1 by FCM being deprived serum.Treated with 25 ?mol/L A?25-35 for 8,16,24 h,the percent of S phase cells was raised remarkably(P
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OBJECTIVE To investigate the trends of susceptibility of Staphylococcus isolates to antimicrobial agents analyzed by the Shandong provincial nosocomial infection surveillance system.METHODS The data from Jan 2002 to Dec 2005 were summarized and analyzed by the Shandong provincial nosocomial infection surveillance system.RESULTS During this period,1644 strains of first isolate from each patient were collected.Major specimens were sputum,wounds,skin soft tissue and urine,which were 39.72%,22.08%,9.43% and 7.54% in total specimens,respectively.The drug-resistant rates of Staphylococcus isolates to antimicrobials were high,except to vancomycin.CONCLUSIONS Antimicrobial resistance of clinical isolates threatens the success of infectious disease treatment.It is very important to promote the rational use of antimicrobial agents for control of resistance and to take effective measures for the prevention of infections.
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OBJECTIVE To investigate the relationship of nosocomial infection with use of antimicrobial agents.METHODS A retrospective study of 171 cases admitted from Nov 2004 to Apr 2005 in a general hospital.RESULTS Sixteen thrush cases all were found to have prior use of antimicrobial agents with average time about(12.5?8.10) days.Twenty six out of 57 surgical cases had wound infection,all used antimicrobial agents preoperatively.Inadequate use of antimicrobial agents manifested as prolonged use or over frequent drug change or improper combined use of drugs etc.CONCLUSIONS Protracted use of antimicrobial agents may be related with development of thrush.Rational use of antimicrobial agents is to be emphysized.
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OBJECTIVE To investigate the distribution and bacterial resistance of nosocomial infection.METHODS The data of 45 hospitals from Shandong Provincial Nosocomial Surveillance System from Jan 2003 to Dec 2005 were analyzed.RESULTS Of total 5 626 isolates strains from the nosocomial infection cases,G-bacilli,G+ cocci and fungi accounted for 58.27%,25.84% and 15.89%,respectively.The ampicillin-resistant rate of commonly encountered G-bacilli was above 89%.There were 72.98% of E.coli resistant to ciprofloxacin.The rates of resistance of S.aureus and coagulase negative Staphylococcus to penicillin,ampicillin and erythromycin were all above 80%;the lincomycin-resistant rate of S.aureus increased gradually to 86.64%.CONCLUSIONS Drug resistance of the nosocomial infective bacteria is a serous problem.Surveillance of bacterial resistance should be strengthened.
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OBJECTIVE To find out epidemiological features of fulminant Acinetobacter baumannii nosocomial infection in cardiac SICU and the ways to prevent and treat this nosocomial infection. METHODS The case histories from 5 inpatients who developed A.baumannii nosocomial infection in cardiac SICU from July 8 to 26,2004 were studied retrospectively to find out the reasons of the epidemia and treatments based on the sputum culture results. RESULTS These 5 inpatients developed lower respiratory tract infection on top of their original severe disease.Within 15 days,their sputum cultures were positive for A.baumannii,4 of them recovered but one died. CONCLUSIONS The inpatients got the same nosocomial infection within the same period because of lowered resistance owing to unreasonable layout of cardiac SICU,their original weakness is due to various invasive operation like long duration mechanical ventilation,lack of isolation and sterilization,etc.
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OBJECTIVE: To study the mechanisms of the antitumor and immunoregulation functions of polyporus polysaccharide (PPS). METHODS: The production of nitric oxide (NO), the activity and mRNA expression of inducible nitric oxide synthase (iNOS) in peritoneal macrophages of mice administered with different dose of PPS were observed by Griess reaction, fluorimetry assay and RT-PCR, respectively. RESULTS: PPS could elevate the iNOS activity with dose-dependence and stimulate the iNOS mRNA expression of peritoneal macrophages in mice. CONCLUSION: The regulation of PPS on the production of NO in peritoneal macrophages of mice may occur at transcriptional level of iNOS. This indicates that the mechanism of PPS's antitumor and immunoregulation functions may be related to increasing NO output of macrophages through stimulating iNOS's denovo synthesis.
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Medical biochemistry is a frontal science, esp. molecular biology. The bilingual teaching in medical biochemistry has not only advantages but also disadvantages. By making use of its advantages and correcting its shortcomings, we should try our best to be close to international level in the teaching of medical biochemistry.
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Purpose:Study the changes of mitochondria membrane potential of HL 60 cell induced by horseshoe crab hemocyte peptides. Methods:HL 60 cells were treated with horseshoe crab hemocyte peptides 0,12.5,25,50,100 ?g/ml for 2,4,6,8,10,12,14h. HL 60 cells were stained with Rhodamine123 before mitochondria membrane potential was detected. Change of mitochondria membrane potential of HL 60 cell was analyzed by flow cytometry. Results:Mitochondria membrane potential of HL 60 cells was stable from 0 to 14h in control groups,however mitochondria membrane potential was decreased when HL 60 cells were treated with horseshoe crab hemocyte peptides 12.5～100 ?g/ml for 0 to 14h.Conclusions:Decrease of mitochondria membrane potential was dependant on concentrations of peptides and time of peptides treatment, it was relative between horseshoe crab hemocyte peptides inducing HL 60 cells apoptosis and decrease of mitochondria membrane potential.
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Objective To analyze the incidence of hospital-acquired infection and the distribution of pathogens through data from the hospital infection surveillance networks in Shandong. Methods A meta-analysis was made of the data submitted by the hospitals involved in the provincial surveillance networks from August 2001 to July 2004. Results The surveillance data involved 1 776 030 hospitalized patients, of whom 43 355 had a hospital-acquired infection, the incidence of hospital-acquired infection being 2.44‰. Respiratory-tract infections were most frequent, followed by gastroenteric-tract infections, urinary-tract infections and surgical-site infections. A total of 6 251 strains of pathogens were isolated, the most commonly identified pathogens being Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Klebsiella pneumoniae, Candida albicans and Staphylococcus epidermidis. Conclusion It is imperative to reinforce the sterilization of air and medical instruments, strictly abide by aseptic manipulation, and promote the rational use of antimicrobials. Hospital infection surveillance ought to be conducted by the combined method of prevalence surveys and the targeted surveillance of key sectors.
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Objective To study the effect of procyanidins (PC) on mRNA and protein expression of par-4 and bcl-2 genes in PC12 cells induced by A?_ 25-35 . Methods Cell survival rate was evaluated by MTT assay and apoptosis was analyzed by Hoechst 33258-PI fluorescence staining. The expressions of mRNA and protein for par-4 and bcl-2 were tested by RT-PCR and Western blotting. Results Pretreatment with different concentrations of PC (5、10、20, and 30 mg/L) for 1 h increased the survival rate of PC12 cell in a dose-dependent manner. PC prevented the PC12 cells nuclei from shrinkage, condensation, and cleavage induced by A?_ 25-35 . PC decreased the expression of par-4 mRNA and protein, and increased the expression of bcl-2 mRNA and protein. Conclusion PC can protect PC12 cells from apoptosis induced by A?_ 25-35 in a dose dependent manner. The mechanism of protection is likely related to decreasing the par-4 gene expression and increasing the bcl-2 gene expression.
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OBJECTIVE To investigate the incidence of nosocomial infection in ICU patients and its risk factors to take measures to prevent from infection. METHODS The nosocomial infection of ICU patients in 12 hospitals from Oct to Dec 2007 using the method of target monitoring was investigated. The nosocomial infection rate was regalated by the method of ASA. The invasive procedure and the associated infection rate were analyzed. RESULTS Among 2087 inpatients in ICU,236 suffered from nosocomial infection,The nosocomial infection incidence was 11.31%,and the nosocomial infection rate per day was 2.38% after regulated by the method of ASA. The patient incidence of nosocomial infection was 3.57%,and the nosocomial infection rate per day was 0.67%. CONCLUSIONS The patients in ICU are susceptible population of nosocomial infection,target monitoring in ICU is an effective surveillance method to reduce the prevalence of nosocomial infection.
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Object To investigate the mechanisms of action of lentinan (LTN) activated mouse peritoneal macrophages to produce nitric oxide (NO). Methods The effects of LTN on NO output and intracellular glutathione (GSH) in mouse peritoneal macrophages and the correlation of them were studied. Results (1) LTN can significantly increase production of NO in mouse peritoneal macrophages, decrease level of intracellular GSH followed increase of NO production. (2) The above effect can be blocked efficiently by the NO production inhibitors. (3) NO production can be inhibited by GSH lowering drugs. Conclusion LTN increase NO production with depletion of intracellular GSH in the activated mouse peritoneal macrophages. It suggested that intracellular GSH plays an important role in regulation of NO production and protection of host cells from cytotoxic attack induced by NO.
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Aim To study the effective mechanism of curcumin on abnormal cell cycle and apoptosis of serum-deprived PC12 cells induced by ?-amyloid peptide 25-35(A?25-35).Methods Synchronized PC12 cells were pretreated with 5 ?mol?L-1 Cur for 1 h,and then 25 ?mol?L-1 A?25-35 for 24 h.Protein and mRNA expression of p21,CDK4,E2F1 and bax were detected by RT-PCR and Western blot respectively.Results After synchronized PC12 cells being pretreated with 5 ?mol?L-1 Cur for 1 h,the mRNA and protein expression of p21 gene were increased gradually,while CDK4,E2F1 and bax gene were decreased.Conclusion Cur maybe effects the redistribution of cell cycle and apoptosis of serum-deprived PC12 cells induced by A?25-35,through increasing the mRNA and protein expression of p21,and decreasing the mRNA and protein expression of CDK4,E2F1 and bax gene.