ABSTRACT
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.
ABSTRACT
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.