A series of novel N-methylbisindolylmaleimides and natural amino acid conjugates were synthesized and evaluated for their inhibitory activity against six tumor cell lines.Most of the compounds exhibited moderate in vi...A series of novel N-methylbisindolylmaleimides and natural amino acid conjugates were synthesized and evaluated for their inhibitory activity against six tumor cell lines.Most of the compounds exhibited moderate in vitro cytotoxic activities in the range of 10-100μmol/L.展开更多
Conjugated polymers with bisindolylmaleimide （BIM） backbone are obtained by the condensation polymerization of methyl and octanyl N-substituted BIMs with 4,4＇-difluoro-diphenylsulfone and 4,4＇-difluoro-diphenylket...Conjugated polymers with bisindolylmaleimide （BIM） backbone are obtained by the condensation polymerization of methyl and octanyl N-substituted BIMs with 4,4＇-difluoro-diphenylsulfone and 4,4＇-difluoro-diphenylketone. The structures of polymers are confirmed by F!rlR and NMR spectroscopy. The polymers exhibit both high glass transition temperatures （Tg 〉 175℃） and high decomposition temperatures （T5 〉 395 ℃）. Meanwhile, The uV-vis absorption and fluorescence spectra of the polymers are similar to the corresponding substituted BIMs. The quantum chemistry calculations indicate that the first excited states of polymers are mostly contributed by BIM structures.展开更多
Introduction: The existence of receptor-mediated endocytosis (RME) means that selectivity and selectivity occurs in capturing macromolecules. Protein kinase C (PKC) which can be expressed by almost all cells are prote...Introduction: The existence of receptor-mediated endocytosis (RME) means that selectivity and selectivity occurs in capturing macromolecules. Protein kinase C (PKC) which can be expressed by almost all cells are proteins important in signal transduction groove that plays a role in a number of cell activity, e.g. phagocytosis. Aims: The purpose of this study is to determine the expression of RME after modulating the PKC which is characterized by the number of Candida albicans cells attached to the surface of macrophages. Methods: Peritoneal macrophages cultured BALB/c mice are treated with PMA and/or bisindolylmaleimides of providing levels of 5 ng/ml to 100 ng/ml for 10 minutes. Then immediately insert Candida albicans and observe every 30 minutes for 120 minutes. The research design used the same subject. Data collected in the form of number of Candida albicans cells attached to the surface of macrophages are analyzed with ANOVA statistical test (one way) to show the differences between treatments. Results: The test shows statistically significant difference in the number of Candida albicans cells attached to the surface of macrophages after administration of various levels of PMA (p 0.001). The higher level of PMA is given, the more active the PKC is, the more RME are formed, the more Candida albicans cells attached to the surface of macrophages. Another result shows statistically significant difference in the number of Candida albicans cells attached to the surface of macrophages after administration of various levels of bisindolylmaleimides (p 0.001). The higher level of bisindolylmaleimide is given, the less active PKC is, and the less RME are formed, the less Candida albicans cells attached to the surface of macrophages. Conclusion: Research shows that activator PKC (PMA) can increase the expression of RME on macrophages. Another research shows that inhibitor PKC (bisindolylmaleimides) can decrease the expression of RME on macrophages.展开更多
文摘A series of novel N-methylbisindolylmaleimides and natural amino acid conjugates were synthesized and evaluated for their inhibitory activity against six tumor cell lines.Most of the compounds exhibited moderate in vitro cytotoxic activities in the range of 10-100μmol/L.
基金financially supported by the Research Fund for the Doctoral Program of Southwest University of Science and Technology(No. 15zx7137)the Research Fund for Joint Laboratoryfor Extreme Conditions Matter Properties(Nos. 13zxjk04, 14tdjk03)
文摘Conjugated polymers with bisindolylmaleimide （BIM） backbone are obtained by the condensation polymerization of methyl and octanyl N-substituted BIMs with 4,4＇-difluoro-diphenylsulfone and 4,4＇-difluoro-diphenylketone. The structures of polymers are confirmed by F!rlR and NMR spectroscopy. The polymers exhibit both high glass transition temperatures （Tg 〉 175℃） and high decomposition temperatures （T5 〉 395 ℃）. Meanwhile, The uV-vis absorption and fluorescence spectra of the polymers are similar to the corresponding substituted BIMs. The quantum chemistry calculations indicate that the first excited states of polymers are mostly contributed by BIM structures.
文摘Introduction: The existence of receptor-mediated endocytosis (RME) means that selectivity and selectivity occurs in capturing macromolecules. Protein kinase C (PKC) which can be expressed by almost all cells are proteins important in signal transduction groove that plays a role in a number of cell activity, e.g. phagocytosis. Aims: The purpose of this study is to determine the expression of RME after modulating the PKC which is characterized by the number of Candida albicans cells attached to the surface of macrophages. Methods: Peritoneal macrophages cultured BALB/c mice are treated with PMA and/or bisindolylmaleimides of providing levels of 5 ng/ml to 100 ng/ml for 10 minutes. Then immediately insert Candida albicans and observe every 30 minutes for 120 minutes. The research design used the same subject. Data collected in the form of number of Candida albicans cells attached to the surface of macrophages are analyzed with ANOVA statistical test (one way) to show the differences between treatments. Results: The test shows statistically significant difference in the number of Candida albicans cells attached to the surface of macrophages after administration of various levels of PMA (p 0.001). The higher level of PMA is given, the more active the PKC is, the more RME are formed, the more Candida albicans cells attached to the surface of macrophages. Another result shows statistically significant difference in the number of Candida albicans cells attached to the surface of macrophages after administration of various levels of bisindolylmaleimides (p 0.001). The higher level of bisindolylmaleimide is given, the less active PKC is, and the less RME are formed, the less Candida albicans cells attached to the surface of macrophages. Conclusion: Research shows that activator PKC (PMA) can increase the expression of RME on macrophages. Another research shows that inhibitor PKC (bisindolylmaleimides) can decrease the expression of RME on macrophages.
