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Aim To synthesize 8-bromo-ethoxy Rhein and investigate its mechanisms and inhibition effect on hepatitis B surface antigen ( HBsAg ) and e antigen ( HBeAg) in HepG2.2.15 cells.Methods 8-bromo-ethoxy Rhein was synthesized based on the chemical structure of Rhein , and its structure was identified by IR,1 H-NMR and 13 C-NMR spectra.MTT assay was used to test the inhibitory effect of 8-bromo-ethoxy Rhein on HepG2.2.15 cells.After the cells treatment by 8-bromo-ethoxy Rhein , the HBsAg and HBeAg in cell supernatant were detected by ELISA .The expres-sion of hepatitis B virus X gene ( HBx) was detected by Western blot .The cell cycles were examined with flow cytometry.The intracellular free calcium concentration was detected by laser scanning confocal microscopy . Results The structure of 8-bromo-ethoxy Rhein was confirmed by IR,1 H-NMR and 13 C-NMR.MTT results showed that synthetic product and Rhein could inhibit the cell proliferation in HepG2.2.15 cells.After trea-ted with 8-bromo-ethoxy Rhein and Rhein for 72 h,the half inhibitory concentration 50%( IC50 ) was 14.29 mg? L-1 and 11.59 mg? L-1 , respectively .Using non-cytotoxic dose of 8-bromo-ethoxy Rhein , the inhibitory effect on HBsAg and HBeAg was gradually enhanced with increasing 8-bromo-ethoxy Rhein concentration . The inhibitory effect of synthetic product on hepatitis B virus was better than that of Rhein .8-bromo-ethoxy Rhein could down-regulate the expression of HBx , in-tracellular calcium ion concentration and block the hepatitis B virus ( HBV ) replication.Flow cytometry results showed 8-bromo-ethoxy Rhein didn′t affect the cell cycle .Conclusions Compare with Rhein , the synthesis of 8-bromo-ethoxy Rhein shows stronger inhi-bition on hepatitis B virus in HepG2.2.15, and its mechanisms may involve down-regulating the expres-sion of HBx and reducing calcium ion concentration .
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Aim To investigate the effects of emodin isolated from Guangxi P.multiflorum Thunb on the expression of KU70/KU80 in hypoxic nasopharyngeal cancer CNE-1 cells and reveal the relationship between radiosensitization of emodin monomer and DNA repair genes.Methods The expression of hypoxia inducible factor-1?(HIF-1?)and DNA double-strand break repair genes(KU70/KU80)between the experimental groups and the control group under hypoxic condition was detected by the real-time fluorescence quantitative RT-PCR.Results Expression of HIF-1? was significantly increased under hypoxia condition.HIF-1? had no change after treatment with emodin alone.The expression level of KU70/KU80 was induced by radiation.Compared with radiation alone group,radiation combined hypoxia group obviously enhanced the expression of KU70/KU80.KU70/KU80 mRNA expression significantly reduced after radiation combined with emodin under hypoxic condition.Conclusion In the hypoxic environment,emodin combined with radiotherapy can effectively inhibit the expression of HIF-1 ? and DNA double-strand break repair genes(KU70/KU80),which may be its mechanism of radiosensitization.
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AIM To observe the effects of Oxymatrine on induction of apoptosis in human ovarian cancer SKOV3 cells. METHODS Apoptosis induced by Oxymatrine in human ovarian cancer SKOV3 cells was tested by MTT assay, fluorescent microscope, and DNA gel eletrophoresis. RESULTS SKOV3 cell viability dropped down depending on the Oxymatrine concentration and treatment time. When incubated with Oxymatrine (0 189 mmol?L -1 and 0 378 mmol?L -1 ) for 48 h, SKOV3 cells showed morphological changes associated with the characters of apoptosis under fluorescent microscope. Typical DNA ladder was found during gel eletrophoresis. CONCLUSION Oxymatrine can induce apoptosis in SKOV3 cell lines.