Bacterial infections have become a global issue that requires urgent attention,particularly regarding to emergence of multidrug resistant bacteria.We developed quaternary amine-containing antimicrobial poly(bile acid)...Bacterial infections have become a global issue that requires urgent attention,particularly regarding to emergence of multidrug resistant bacteria.We developed quaternary amine-containing antimicrobial poly(bile acid)s that contain a hydrophobic core of lithocholic acid in the main-chain.Interestingly,by choosing appropriate monomers,these cationic polymers can form core-shell micelles.These polymers exhibited biocidal activity against both Gram-positive and Gram-negative bacterial species.It is demonstrated that the micelles can deliver hydrophobic antibiotics that functionally have dual antimicrobial activities.Cytotoxicity assays against HeLa cells showed dosage-dependent toxicity for polymers with longer linkers.展开更多
近年来,聚合胆汁酸螯合剂(polymeric bile acid sequestrant,PBAS)用于治疗高胆固醇血症受到越来越多的关注。这些聚合物通常是带正电荷的非吸收性树脂,能选择性地结合并从胃肠道除去胆汁酸,降低血浆胆固醇水平。不同类型的聚合物的胆...近年来,聚合胆汁酸螯合剂(polymeric bile acid sequestrant,PBAS)用于治疗高胆固醇血症受到越来越多的关注。这些聚合物通常是带正电荷的非吸收性树脂,能选择性地结合并从胃肠道除去胆汁酸,降低血浆胆固醇水平。不同类型的聚合物的胆汁酸螯合机制不同,本文综述并讨论了含有季铵基团的两亲性聚合物、环糊精及聚β-环糊精和分子印迹聚合物3类不同PBAS的合成路径、体外胆汁酸结合活性以及体内降脂活性及其影响因素,旨在为PBAS的后续研究提供帮助。展开更多
基金The authors would like to thank National Science Foundation(DMR-1608151).
文摘Bacterial infections have become a global issue that requires urgent attention,particularly regarding to emergence of multidrug resistant bacteria.We developed quaternary amine-containing antimicrobial poly(bile acid)s that contain a hydrophobic core of lithocholic acid in the main-chain.Interestingly,by choosing appropriate monomers,these cationic polymers can form core-shell micelles.These polymers exhibited biocidal activity against both Gram-positive and Gram-negative bacterial species.It is demonstrated that the micelles can deliver hydrophobic antibiotics that functionally have dual antimicrobial activities.Cytotoxicity assays against HeLa cells showed dosage-dependent toxicity for polymers with longer linkers.
文摘近年来,聚合胆汁酸螯合剂(polymeric bile acid sequestrant,PBAS)用于治疗高胆固醇血症受到越来越多的关注。这些聚合物通常是带正电荷的非吸收性树脂,能选择性地结合并从胃肠道除去胆汁酸,降低血浆胆固醇水平。不同类型的聚合物的胆汁酸螯合机制不同,本文综述并讨论了含有季铵基团的两亲性聚合物、环糊精及聚β-环糊精和分子印迹聚合物3类不同PBAS的合成路径、体外胆汁酸结合活性以及体内降脂活性及其影响因素,旨在为PBAS的后续研究提供帮助。