Aged ; Humans ; Male ; Middle Aged ; Receptors, Interleukin-2 ; blood ; Silicosis ; blood ; classification ; T-Lymphocyte Subsets ; metabolism

OBJECTIVE To investigate the drug resistance of ESBLs-producing Escherichia coli and Klebsiella pneumoniae in local nosocomial infection,for guiding the clinical drug resistance. METHODS ATB analysis system was used for identification of bacteria,extra-susceptibility tests were detected by K-B method. RESULTS The isolation rate of ESBLs-producing E. coli and the K. pneumoniae was 29.9% and 30.8%,respectively. The drug susceptibility was indicated the resistance rate of ESBLs producing strains to antibacterial agents except imipenem was higher than that of non-ESBLs producing strains. CONCLUSIONS Detecting drug resistance of ESBLs producing strains is of important significance for guiding the clinical rational use of antibacterials and controling the epidemics.

The target compounds were prepared from 5-aminobenzimidazolone by two steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The AChE inhibitory activity of compound 4d is the best of them, and its IC50 value is equal to 7.2 μmol·L(-1), which is better than that of rivastigmine; moreover the 4d had no inhibitory activities to BuChE. Therefore, the inhibitory activities of 5-aminobenzimidazolone derivatives to acetylcholinesterase are worth further researching.
Acetylcholinesterase ; metabolism ; Benzimidazoles ; chemical synthesis ; chemistry ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; Drug Design ; Phenylcarbamates ; chemistry ; Rivastigmine ; Structure-Activity Relationship

In this paper, fourteen new L-proline derivatives were designed and synthesized, and their acetlcholinesterase (AChE) inhibitory activities were also investigated in vitro. New L-proline derivatives were prepared from substituted 2-bromo-1-acetophenones through four-step reaction; and their bioactivities as AChE inhibitors were measured by Ellman spectrophotometry. The results showed that the target compounds had a certain AChE inhibitory activity to in vitro. The bioactivity of compound 8b was the best of them, and its IC50 value was 5.45 µmol.L-1, which was better than that of rivastigmine. So the acetylcholinesterase inhibitory activities of new L-proline derivatives were worth to be further studied.
Acetylcholinesterase ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; Drug Design ; Proline ; analogs & derivatives ; Rivastigmine ; chemistry ; Structure-Activity Relationship

Abstract: Our previous work revealed berberine can significantly enhance the susceptibility of fluconazole against fluconazole-resistant Candida albicans, which suggested that berberine has synergistic antifungal activity with fluconazole. Preliminary SAR of berberine needs to be studied for the possibility of investigating its target and SAR, improving its drug-likeness, and exploring new scaffold. In this work, 13-substitutited benzyl berberine derivatives and N-benzyl isoquinoline analogues were synthesized and characterized by 1H NMR and MS. Their synergetic activity with fluconazole against fluconazole-resistant Candida albicans was evaluated in vitro. The 13-substitutited benzyl berberine derivatives 1a-1e exhibited comparable activity to berberine, which suggested that the introduction of functional groups to C-13 can maintain its activity. The N-benzyl isoquinolines, which were designed as analogues of berberine with its D ring opened, exhibited lower activity than berberine. However, compound 2b, 2c, and 4b showed moderate activity, which indicated that berberine may be deconstructed to new scaffold with synergistic antifungal activity with fluconazole. The results of our research may be helpful to the SAR studies on its other biological activities.

Objective:To investigate any change in the effective connectivity between the bilateral anterior central gyruses after transcranial magnetic stimulation (TMS).Methods:Twenty-one healthy subjects were examined using resting state functional magnetic resonance imaging (rs-fMRI) before and after receiving continuous theta burst stimulation (cTBS). The brain atlas of the Institute of Automation of the Chinese Academy of Sciences was used for fine partitioning of the bilateral anterior central gyruses. Granger causality analysis was used to compare any changes in the effective connectivity between them.Results:After the cTBS inhibited the right M1 area, significant changes in effective connectivity among the sub-regions of the bilateral M1 area were observed. The effective connectivity of the right upper limb to the left upper limb and the left head to face were weakened, while that of the left upper limb to the right head, as well as of the face to the right upper limb was enhanced.Conclusion:For people whose right M1 area has been inhibited by cTBS, the effective connectivity changes in both upper limb functional areas of the M1 region reflect inter-hemispheric inhibition. Opposite changes were found in the trunk and upper limbs.

Background: Glutamine and glutamate are known to play important roles in cancer biology. However, no detailed information is available in terms of their levels of involvement in various biological processes across different cancer types, whereas such knowledge could be critical for understanding the distinct characteristics of different cancer types. Our computational study aimed to examine the functional roles of glutamine and glutamate across different cancer types. Methods: We conducted a comparative analysis of gene expression data of cancer tissues versus normal control tis-sues of 11 cancer types to understand glutamine and glutamate metabolisms in cancer. Specifically, we developed a linear regression model to assess differential contributions by glutamine and/or glutamate to each of seven biological processes in cancer versus control tissues. Results: While our computational predictions were consistent with some of the previous observations, multiple novel predictions were made: (1) glutamine is generally not involved in purine synthesis in cancer except for breast cancer, and is similarly not involved in pyridine synthesis except for kidney cancer; (2) glutamine is generally not involved in ATP production in cancer; (3) glutamine's contribution to nucleotide synthesis is minimal if any in cancer;(4) glutamine is not involved in asparagine synthesis in cancer except for bladder and lung cancers; and (5) glutamate does not contribute to serine synthesis except for bladder cancer. Conclusions: We comprehensively predicted the roles of glutamine and glutamate metabolisms in selected meta-bolic pathways in cancer tissues versus control tissues, which may lead to novel approaches to therapeutic devel-opment targeted at glutamine and/or glutamate metabolism. However, our predictions need further functional validation.

As medicine and food plants, the market demand of Zamthoxyli Pericarpium is extensive, and the sanshool in Zamthoxyli Pericarpium is getting attention gradually. However, because of the low content and not establishing rating evaluation method for sanshool and lack of standards, the research on substance basis and physiological activity is necessary. This article reviewed the extraction, separation, purification and biological activities of sanshoolin Zamthoxyli Pericarpium in recent years to provide development and utilization of Zamthoxyli Pericarpium.

Objective To study on intervene function of Sinisan with the ultra structure of hippo-campus in rats with sleep disorder induced by post traumatic stress disorder.Methods Fifty SD rats were divided equally into five groups:blank control group,model group,negative control group,positive control group and experimental group.The control blank group did not copy the model,do not receive drugs,the normal feeding.Model group,repetitive post-traumatic stress disorder model was induced by current stimulation,but not receive drugs.Negative control group,equal volume of 0.9％ NaCl.Positive control group (paroxetine hydrochloride 0.42 mg ·mL-1) and experimental group (Sinisan,containing crude drug 0.24 g · mL-1).It given to drugs 1 h before the model establishment.The rats were administered with 10 mL · kg-1,once a day,for a total of 7 d.The changes of ultra structure of CA1 and CA3 area in hippo-campus with rats were observed by transmission electronmicroscope.Results In the blank control group,the hippocampal neurons were clearly defined,and the synaptic space was obvious in the CA1 and CA3 area.Compared with the blank control group,in the model group,the synaptic structure of hippocampal neurons was significantly changed,the synaptic vesicles were reduced and the synaptic structure was not clear in the CA1 and CA3 area.Compared with the model group,the negative control group was same too,which indicated that there was no significant stress effect on the rats after intragastric administration of saline.Compared with the negative control group,positive control group and experimental group hippocampal neurons synapse structure was restored,and the two groups were similar in the CA1 and CA3 area.Conclusion Transmission electronmicroscope was used to study the ultra structure of CA1 and CA3 in rats hippo-campus with characteristic difference.

Objective To study the effects of sleep latency to the intervention of Sinisan in rats with post-traumatic stress and sleep disorder (PTSD).Methods Fifty SD rats were divided equally into 5 groups:sham operation group,model group,negative control group group,positive control group and experimental group.PTSD model was made by claustrophobia,but not in sham operation group.The model group was not given the drug,the negative control group was given equal volume 0.9％ NaC1,and the positive control group was given paroxetine hydrochloride 0.42 mg · mL-1.The experimental group was perfused with the decoction of Sinisan (containing 0.24 g · mL-1) 10 mL · kg-1.The drug was administered 1 h before the stress model was administered once a day for a total of 7 d.After intervention on the 7th day,nonrapid eye movements sleep (NREMS) and eye movements sleep (REMS) were detected.Results The REMS and NREMS of sham operation group and model group were respectively (8.66 ± 3.04),(23.27 t 10.15) min;(65.90 ± 25.08),(109.36 ± 43.43) min,the differences between groups were statistically significant(all P ＜ 0.01);the result suggest that difficulty in falling asleep appears in rats after modeling.The REMS and NREMS of the positive control group and the experimental group were respectively (8.17 ±2.29),(6.83 ±2.84) min;(162.29 ±46.19),(195.24 ±67.96) min.Comparison between the drugs groups and model group,the difference was statistically significant (P ＜0.05,P ＜0.01).These Results suggested that both paroxetine hydrochloride and Sinisan can significantly promote the sleep of rats.Conclusion Traditional Chinese medicine compound Sinisan can obviously promote the rats with sleep disorder caused by PTSD.