RESUMEN
Aim To explore the anti-cancer effects of ZL-n-91, a novel and highly selective phosphodiesterase 4 inhibitor, on the osteosarcoma U2OS cells.Methods CCK-8 assay was used to detect the inhibitory effect of ZL-n-91 with different concentrations(0, 20, 40, 80, 160, 240, 320, 400, 480 μmol·L-1)and different intervention time(0, 24, 48, 72, 96 h)on the proliferation of U2OS cells.Tablet clone forming experiment was used to detect the effect of ZL-n-91 on the clonality of U2OS cells.Flow cytometry was used to detect the cell apoptosis and cell cycle distribution.Western blot was employed to detect the expression of Bcl-2, CDK2, CDK4, CyclinD1, CyclinE1 protein.Results The inhibitory rate of ZL-n-91 on U2OS cells was concentration- and time-dependent(P<0.05), and its half inhibition rate IC50 was 174.1 μmol·L-1.ZL-n-91 significantly inhibited the clonality of U2OS cells(P<0.01).ZL-n-91 significantly induced cell apoptosis, and caused cell cycle arrest at G0/G1 phase in U2OS cells(P<0.01).The results of Western blot showed that ZL-n-91 significantly down-regulated the expression of Bcl-2, CDK2, CDK4, CyclinD1, CyclinE1 proteins in U2OS cells(P<0.05).Conclusions The novel selective phosphodiesterase 4 inhibitor, ZL-n-91, can significantly inhibit the proliferation of osteosarcoma U2OS cells with induction of cell cycle arrest and cell apoptosis, and may become a potential anti-cancer agent.
RESUMEN
Aim: To investigate the effect of ZL-n-91, a novel phosphodiesterase 4 (PDE4) inhibitor, on proliferation, cell cycle and apoptosis of human glioma U87 cells. Methods In vitro the different concentrations of ZL-n-91 were set up to evaluate the proliferation of U87 cells by CCK-8 assay. The cell apoptosis and cell cycle distribution were examined by flow cytometry. The expression of CDK2, CDK4, cyclin Dl and apoptosis-related protein Bax and Bcl-2 proteins were detected by Western blot. A subcutaneous transplanted tumor model of U87 in nude mice was established for the in vivo experiment using a dosage of 5 mg · kg
RESUMEN
Background: HAART (Highly active antiretroviral therapy) is the cornerstone of management of patients with HIV infection. Antiretroviral therapy was started in the year 1986 with the first drug Zidovudine (ZDV). Later on, other antiretroviral drugs (NRTIs, NNRTIs and Pls) were introduced. Dual and mono therapies were used initially but the problem of resistance emerged. Currently, 3 or more ARV drugs are recommended globally for the treatment of people with HIV infection.Methods: A cross-sectional descriptive study conducted at a tertiary care Hospital over 200 patients, two commonly used medications are ZLN (Zidovudine+Lamivudine+Nevirapine) and TLE (Tenofovir+Lamivudine+Efavirenz ). The factors considered to affect the clinical and immunologic outcomes in both groups were assessed using baseline CD4 count, WHO clinical staging, presence of chronic diarrhea, anemia, and baseline weight, occurrence of TB, and switching of ART regimen.Results: A total of 200 patients were included in the study. ART documents of 100 patients are on Zidovudine+Lamivudine+Nevirapine) and 100 patients are on TLE (Tenofovir+Lamivudine+Efavirenz) regimen. Out of 200 patients, 97 were males and 103 were females. Maximum number of subjects were in the age of 15-45 years (82.5%) followed by 45 and above (17.5%). Mean age was 34.5±2.5 (years) with range 15 to 65 years. The baseline CD4 count of the patients, 94 were <350 and 6 were ≥350 on ZLN, in case of TLE 82 were <350 and 18 were ≥350. CD4 count after 6 months in 200 patients as follows, 60 were <350 and 40 were ≥350 in case of TLE 53 were <350 and 47 were ≥350.Conclusions: This research finding concluded that there is no critical difference between the two medications in regards to serious adverse events but did find that TDF is superior to AZT in terms of immunologic response and adherence and more frequent emergence of resistance.
RESUMEN
Background: While treating patients with HIV infection it is important to achieve more than 95% compliance to ART (Antiretroviral Therapy) in order to suppress viral replication.Methods: This was a retrospective, observational, record based study of HIV positive patients undergoing treatment with ZLN (zidovudine 300 mg, lamivudine 150 mg, nevirapine 200 mg) and TLE ( tenofovir 300 mg, lamivudine 150 mg, efavirenz 600 mg) regimens. The treatment charts of the patients fulfilling inclusion and exclusion criteria were reviewed.Results: Analysis of adherence showed that there were 12 patients out of 150 on ZLN regimen and 31 patients out of 150 on TLE regimen were nonadherent to the respective treatments.Conclusions: In this observational study patients on ZLN regimen were showing greater compliance than TLE regimen.