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Objective To screen α-glucosidase inhibitors from root extract of Cichorium glundulosum (CGR) by UF-LC-MS and molecular docking. Methods The inhibitory activity of CGR extract was evaluated by establishing enzyme inhibitor model, Meanwhile, four active compounds from CGR extract were screened by UF-LC-MS and identified as α-glucosidase inhibitors, which were verified by using Autodock Software. Results The results showed that two compounds that combined with α-glucosidase well were screened out, including baicalin and lactupicrin, which showed significant α-glucosidase inhibitory activity in the concentration range of 0.1-2 mg/mL in a dose-dependent manner. Conclusion Our work provide theoretical basis for screening natural and high affinity enzyme inhibitors from CGR by using UF-LC-MS and molecular docking and further study of the hypoglycemic effect of C. glundulosum.
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OBJECTIVE@#To investigate the effect of baicalin derivative 02-036 on proliferation and apoptosis human Burkitt lymphoma cell line CA46 and its related mechanisms.@*METHODS@#The MTT assay and cell colony formation assay were used to measure the growth inhibition of CA46 cells after 02-036 treatment. The flow cytometry with AnnexinV-FITC/PI double staining was employed to detect the apoptosis induction effect of 02-036 on CA46 cells. Cell cycle distribution of CA46 cells was estimeted by using DNA ploid analysis. Western blot was used to determine the changes of apoptosis-related proteins, including C-MYC, BCL-2, Procaspase-9, Procaspase-3, PARP and Cleaved-PARP.@*RESULTS@#Baicalin derivative 02-036 obviously inhibited the proliferation of CA46 cells, with dose- and time-dependent manner (r=0.963, r=0.992). The averaged IC value of CA46 cells was (6.04±0.11) μmol/L after 48-hour treatment. Low concentration of 02-036 could significantly inhibit the colony formation of CA46 cells. Flow cytometry analysis confirmed that 02-036 could effectively induce CA46 cell apoptosis. The apoptosis rate correlated with drug concentrations (r=0.959). Also, DNA ploid analysis showed that the cell cycle of CA46 was arrested in the S phase. The expression levels of BCL-2, Pro-caspase-9, Pro-caspase-3, PARP and C-MYC proteins decreased with a 02-036-dose dependent manner (r values were -0.990, -0.939, -0.971 and -0.967, respectively). In contrast, the expression level of cleaved-PARP increased with the same manner (r=0.920).@*CONCLUSION@#Baicalin derivative 02-036 can effectively inhibit the proliferation and induce apoptosis of CA46 cells, and its related mechanisms may be correlated with the down-regulation of apoptosis-related molecule expression levels, such as BCL-2, Pro-caspase-9, Pro-caspase-3, PARP and C-MYC.
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Humans , Apoptosis , Burkitt Lymphoma , Cell Line, Tumor , Cell Proliferation , FlavonoidsABSTRACT
Objective Mifepristone (MIF) can inhibit triple-negative breast cancer cell (TNBC) survival at high concentra-tions. The purpose of the present study is to study the effect of mifepristone derivatives on triple-negative breast cancer cell (TNBC) survival at low concentrations. Methods SUM149PT and HCC1937 triple negative breast cancer cells were used in the study; the experiment was set in four groups: DMSO group,MIF group(10 μmol/L MIF),5 μmol/L FZU-00,033 group and 10 μmol/L FZU-00,033 group. They were treated with 24,48,72 h,and cell viability was measured by SRB. KLF5 overexpression HCC1937 cell line was used in the study; the experiment was set in four groups: PCDH-DMSO group(PCDH vector,DMSO),PCDH-FZU-00,033 group (PCDH vector,10 μmol/L FZU-00,033),KLF5-DMSO group(overexpress KLF5,DMSO),KLF5-FZU-00,033 group(overexpress KLF5,10 μmol/L FZU-00,033). Cell apoptosis was investigated by detecting PARP cleavage using Western blot. In order to investi-gate how FZU-00,033 reduced cell viability,we detected KLF5 protein expression after drug treatment. On the basic of the original PC-DH-DMSO group,PCDH-FZU-00,033 group,KLF5-DMSO group and KLF5-FZU-00,033 group,5 μmol/L PCDH-FZU-00,033 group (PCDH vector,5 μmol/L FZU-00,033),5 μmol/L KLF5-FZU-00,033 group(overexpress KLF5,5 μmol/L FZU-00,033). Western blot was used to detect the effect of FZU-00,033 in KLF5 overexpression cell line. Results Compared with DMSO group,5 μmol/L FZU-00,033 group,10 μmol/L FZU-00,033 group and MIF group decreasd TNBC cell viability more efficiently at 24,48,72h (P<0.01); the cell survival rate of DMSO group,5 μmol/L FZU-00,033 group,10 μmol/L FZU-00,033 group and MIF group was [(100±4)%,(17±2)%,(5±1)%,(58±1)%] respectively in SUM149PT cell line and was [(100±7)%,(39±1)%,(30±1)%,(62±1)%] respectively in HCC1937 cell line. Compared with MIF group,5 μmol/L FZU-00,033 group and 10 μmol/L FZU-00,033 group decreasd TNBC cell viability more efficiently at 24,48,72 h (P<0.01). Compared with DMSO group,5 μmol/L FZU-00,033 group,10 μmol/L FZU-00,033 group and MIF group suppressed KLF5 expression more potently and increased cell apoptosis. Com-pared with 10 μmol/L MIF group,5 μmol/L FZU-00,033 group and 10 μmol/L FZU-00,033 group significantly increased apoptosis. Compared with PCDH-DMSO group,10 μmol/L PCDH-FZU-00,033 group decreasd TNBC cell viability more efficiently at 48,72 h and cell survial rate was [(100±6)% vs (39±2)%,P<0.05] and [(100±3)% vs (21±1)%,P<0.05] respectively. Compared with KLF5-DMSO group,10 μmol/L KLF5-FZU-00,033 group decreasd TNBC cell viability more efficiently at 48,72h and cell survial rate was [(100±1)% vs (47±1)%,P<0.05] and [(100±1)% vs (27±1)%,P<0.05] respectively; Meanwhile,Compared with 10 μmol/L PCDH-FZU-00,033 group,10 μmol/L KLF5-FZU-00,033 group increased TNBC cell viability more efficiently at 48,72 h (P<0.05). Compared with PCDH-DMSO group,5 μmol/L PCDH-FZU-00,033 group and 10 μmol/L PCDH-FZU-00,033 group in-creased cell apoptosis; Compared with KLF5-DMSO group,5 μmol/L KLF5-FZU-00,033 group and 10 μmol/L KLF5-FZU-00,033 group increased cell apoptosis. Conclusion Novel mifepristone derivative FZU-00,033 suppressed TNBC cell viability partially through suppressing KLF5 expression.
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Objective To investigate the epidemic characteristics of mycoplasmal pneumonia outbreak in a middle school, and to provide suggestions for outbreak prevention and control.Methods Principle and method of field epidemiology was used and,speciously,questionnaire investigation was carried out for the outbreak of mycoplasmal pneumonia.Outbreak characteristics and corresponding emergency intervention were discussed.Results There was an outbreak of mycoplasmal pneumonia in 2 classes of the middle school,and the attack rate was 42.50%.The attack rate of other classes was 6.75%.Timely identification and diagnosis of the disease,and comprehensive control to prevent the spread of the epidemic,brought the disease under control.Conclusion The outbreak of mycoplasmal pneumoniae infection is associated with the close contact in daily activities.Emergency intervention can prevent the further spread of the disease.