Chemical constituents from Paris rugosa rhizomes and their antimicrobial activities / 中国中药杂志

Paris rugosa(Melanthiaceae) only grows in Yunnan province of China at present, and its chemical constituents have not been systematically studied. In this study, nine compounds, including one new compound pariposide G(1) and eight known compounds of cerin(2), stigmast-4-en-3-one(3), β-ecdysone(4), ophiopogonin C'(5), methyl protogracillin(6), gracillin(7), parissaponin H(8), and parisyunnanoside G(9), were isolated and identified from the ethanol extract of P. rugosa rhizomes by column chromatography methods and semi-preparative high-performance liquid chromatography(HPLC). Compounds 1-9 were isolated from this plant for the first time. The antibacterial and antifungal activities of all the compounds were evaluated. The results showed that ophiopogonin C' had strong inhibitory effects on Candida albicans [MIC_(90)=(4.68±0.01) μmol·L~(-1)] and the fluconazole-resistant strain of C. albicans [MIC_(90)=(4.66±0.02) μmol·L~(-1)].

Resistance of C57BL/6 Mice to Different Artemisinin-sensitive Strains of PbK173 / 中国实验方剂学杂志

ObjectiveThe tolerance of C57BL/6 mice to artemisinin-sensitive and -resistant strains of Plasmodium berghei （Pb） K173 and the differences in blood parameters， spleen coefficient and spleen structure during infection were compared to explore whether the artemisinin resistance of Pb would aggravate malaria infection. MethodPbK173 artemisinin-sensitive and -resistant strains were tested in parallel. C57BL/6 mice were randomly divided into 1 control group， 4 artemisinin-sensitive strain groups and 4 artemisinin-resistant strain groups by body weight. Each infection group was simultaneously inoculated （ip） with 1×107 infected red blood cells （iRBCs） of sensitive/resistant strain. For the mice in the survival test group， the body weight was recorded every day post infection， and the tail vein blood smear was collected to calculate the Pb infection rate. In the other infection groups， peripheral blood and spleen were collected on 2， 5 and 9 d after infection. Peripheral blood parameters， spleen coefficient， pathological section of spleen and spleen cells were detected in each group. ResultOn 1-3 d after infection， the infection rate of the resistant strain （0.4±0.0， 0.8±0.1， 1.9±0.4）% was always higher than that of the sensitive strain （0.2±0.1， 0.4±0.1， 1.1±0.3）% （P<0.01）. From the 4th d of infection， the infection rate of the two groups gradually approached. The survival period of the sensitive strain group （20.5±1.2） d was shorter than that of the resistant strain group （23.3±1.4） d （P<0.01）. On the 9th d， the white blood cell count of the sensitive strain group （16.2±1.1）×109 cells/L was higher than that of the resistant strain group （10.6±1.8）×109 cells/L （P<0.01）. Flow cytometry analysis of spleen cells showed that the sensitive strain group （3.6±0.4） demonstrated a higher CD4+/CD8+ value than the resistant strain group （2.3±0.2） on the 9th d （P<0.01）. The spleen of C57BL/6 infected mice was gradually enlarged during infection， and on the 9th d， the resistant strain group （3.1±0.1）% showed a higher spleen coefficient than the sensitive strain group （2.7±0.2）% （P<0.01）. In the early stage of C57BL/6 infected mice， the red pulp of spleen was hyperemic and swollen. On the 9th d， the marginal area of the spleen disappeared and the structure of the red and white pulp was destroyed. ConclusionWithout drug treatment， the protective immune responses of peripheral blood and spleen of C57BL/6 mice were more sensitive to PbK173 artemisinin-sensitive strain. The artemisinin-resistant strain of PbK173 bred with mouse-to-mouse blood transmission and increased artemisinin dose exhibited shortened growth period and reduced toxicity.

Effect of compound houttuynia mixture on influenza virus in vitro / 药学学报

Compound houttuynia mixture belongs to OTC class A medicine, which is made from Houttuynia cordata, Scutellaria baicalensis, Radix Isatidis, Forsythia, and Lonicera. As a kind of compound preparation of traditional Chinese medicine, houttuynia cordata mixture has extensive pharmacological effects, for example, clearing away heat and detoxifying, thus it is used for the sore throat, acute pharyngitis, and tonsillitis with wind-heat syndrome. In this study, the antiviral activity against influenza viruses and the primary mechanism of compound houttuynia mixture was evaluated. The antiviral effect of compound houttuynia mixture was determined by cytopathic effects (CPE), Western blot, quantitive reverse transcription PCR (qRT-PCR), and virus titer assays. The effect of houttuynia mixture on the replication cycle of influenza virus was evaluated by time-of-addition assay. In conclusion, the results showed that the compound houttuynia mixture had a broad-spectrum effect against influenza virus, including the international common influenza virus strains, the drug-resistant strains and the highly pathogenic avian influenza viruses H5N1 and H7N9. It mainly impairs the early stage of the viral replication.

The anti-HIV-1 activities of benzophenones non-nucleoside reverse transcriptase inhibitors in vitro / 药学学报

To evaluate the anti-HIV-1 activities of 5 benzophenones non-nucleoside reverse transcriptase inhibitors (NNRTIs) such as DY1203, DY1204, DY1119, DY1208 and DY1209 in vitro, the cytotoxicity of 5 compounds were tested on C8166, MT-4, H9 and PBMC with the MTT assay. The anti-HIV-1 activities of compounds were evaluated on laboratory-adapted strain, drug-resistant strains and primary isolated strains by p24 antigen expression ELISA. The inhibition of HIV-1 recombinant reverse transcriptase activity was assessed by ELISA assay. Among 5 compounds, DY1203 and DY1204 showed low cytotoxicities with CC50 greater than 200 μg·mL-1. DY1119, DY1208 and DY1209 showed strong anti-HIV-1 activities against HIV-1IIIB, HIV-174V, HIV-1RF/V82F/184V, HIV-1NL4-3 gp41(36G) N42S, HIV-1KM018, HIV-1TC-1 and HIV-1Wan. However, NNRTIs drug-resistant strain HIV-1A17 showed different resistance to these compounds. The 5 compounds proved active against HIV-1 recombinant reverse transcriptase. DY1208 is expected to become a new lead compound for its high therapeutic index. The results can provide new information for HIV-1 drug research and promote the development of new HIV-1 drugs.

The genotyping of ofloxacin-resistant mycobacterium tuberculosis with MIRU-VNTR in Hangzhou city / 预防医学

Objective To evaluate the application of MIRU - VNTR analysis in genotyping of the ofloxacin - resistant mycobacterium tuberculosis in Hangzhou. Methods From April 2010 to June 2012,the clinical isolates of mycobacterium tuberculosis were collected from designated TB hospitals in Hangzhou for drug sensitivity test. The ofloxacin -resistant mycobacterium tuberculosis strains were typed with RD105 deletion test and MIRU-VNTR typing method respectively,and the results from both methods were compared. Results A total of 52 ofloxacin -resistant mycobacterium tuberculosis strains were collected. Using RD105 deletion test,43 strains(82. 69%)belonged to mycobacterium tuberculosis Beijing family. Using a 12-locus MIRU-VNTR typing,52 distinct MIRU-VNTR patterns were detected in the 52 ofloxacin-resistant strains. The Hunter-Gaston discriminatory index(HGI)was 0. 999. Except MIRU40 and ETR-F,the other 10 MIRU-VNTR loci showed moderate or high discriminatory power for both Beijing genotype isolates and non -Beijing genotype isolates. Conclusion The selected 10 MIRU-VNTR loci has a higher discriminatory power and are appropriate for the ofloxacin-resistant mycobacterium tuberculosis genotyping.

Pathogenic Bacteria Resistance to Disinfectants in Hospital Infection / 环境与健康杂志

Hospital infection has become a global public health problem. The strain of anti-disinfectant, same as the antibiotic-resistant strain, will lead to the failure of the disinfection of the hospital, which will cause hospital infection. The bacterial resistance to disinfectants and resistance mechanism is not clear. Most of the studies focused on the cell research, the molecular research, non-physiological mechanism of resistance, in recent years, the selection pressure, outflow pump were studied. Currently, disinfectants abuse, improper handling and inadequate amount of disinfectant were considered as the main cause of the resistance development.

Identification and Drug Sensitive Test for Foot Fungi / 中华医院感染学杂志

OBJECTIVE To explore the changes in foot fungus mobility and its drug resistance for further etiology investigation and clinical treatment. METHODS Sabourand′s agar culture medium was used to culture fungi, ID identification strip was employed to identify the fungi and drug sensitive test was performed by disk diffusion test. RESULTS The incidence of Trichophyton rubrum infection was the highest (79.1%). The isolated fungi were relatively sensitive to amphotericin B (AMB, 98.9%) and itraconazole (ITC, 98.0%), and resistant to 5-fluorocytosine (5-FC, 22.1%). CONCLUSIONS Detection technique of fungal infection should be improved and anti-fungal medicine should be used reasonably according to the results of drug sensitive test so that the fungal infection, especially fungi-resistant infection could be reduced.

Effect of propolis on cariogenesis of main cariogenic streptococci and their fluoride-resistant strains / 第三军医大学学报

Objective To evaluate the effects of propolis on the growth of S.mutans ATCC 25175(S.m),S.sobrinus 6715(S.s) and their fluoride-resistant strains(S.m-FR,S.s-FR),and the change of their glucosyltransferase(GTF).Methods S.m and S.s were induced with sodium fluoride by minimum inhibitory concentration(MIC) to induce fluoride-resistant strains(S.m-FR and S.s-FR).Fluid dilution method was used to observe the effects of different levels of propolis on growth of S.m,S.m-FR,S.s and S.s-FR.Chemistry enzyme analysis was used to detect the influence of propolis on the enzyme activity of GTF.Results MIC of propolis for S.m,S.m-FR,S.s and S.s-FR were respectively 0.39,0.78,0.20 and 0.39 g/L.MBC of propolis for them were respectively 0.78,1.56,1.56,and 1.56 g/L.GTF of S.m,S.m-FR,S.s,and S.s-FR was decreased gradually with the increase of concentration of propolis.There were significant differences among total sample groups,and each experimental group and positive control group as well(P

Comparison of formation and morphologic features of digestive vacuoles and haemozoin between chloro-quine-sensitive and chloroquine-resistant strains of Plasmodium berghei / 第二军医大学学报

Objective: To understand the morphologic foundation for differences in drug-resistance, virulence and immunity between chloroquine-sensitive (N) and chloroquine-resistant (RC) strains of Plasmodium berghei. Methods: The RC strain and the N strain were compared concerning the formation and morphologic features of digestive vacuoles and haemozoin with transmission electron microscope. Results: There was a single large digestive vacuole and multiple micro-single-mem-braned vacuole-like structures in the trophozoites of the N strain, and haemozoins centralized and fused during their schizo-gony were situated under the plasma membrane. Whereas there were few digestive vacuoles in the trophozoites of the RC strain, but with multiple micro-single-membraned vacuole-like structures instead. The RC strain formed obviously less hemo-zoins than that of the N strain and the hemozoins were not centralized and fused during the schizogony. Conclusion: The RC strain forms multiple single-membraned food vacuole-like structures in the trophozoites, and has different mechanism for detoxifying free heme with N strain and the features may be the foundation for the difference in drug-resistance, virulence, immunity between RC strain and N strain of Plasmodium berghei.

Cobalt transport in a cobalt-resistant strain of Neurospora crassa.

Uptake of Co2+ by cobalt-resistant strain is dependent on Co2+ concentration in the medium and is linear with time. The uptake is unaffected by metabolic inhibitors and decreased at low pH values. The uptake is independent of temperature in the range 0–40° C. The transport system is a passive diffusion process, unlike in the parent wild type strain where it is energy-dependent. It is possible that Mg2+ transport system is not involved in Co2+ transport in this strain, since the Co2+ uptake is not suppressed by Mg2+ as in the parent strain.