Evolution of 8-esterified cycloberberines as a novel class of antibacterial agents against MDR gram-positive strains by targeting DNA polymerase IIIC

• Published in: Bioorganic chemistry Vol. 163; p. 108640
• Main Authors: Fan, Tianyun, Zhao, Liping, Ma, Xican, Tang, Jia, Duan, Qionglu, Zhu, Xi, Liu, Yonghua, Jiang, Jiandong, Li, Yinghong, Song, Danqing
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.08.2025
• Subjects: Animals; Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; Antibacterial activity; Berberine - analogs & derivatives; Berberine - chemical synthesis; Berberine - chemistry; Berberine - pharmacology; Cycloberberine ester; DNA polymerase IIIC; Dose-Response Relationship, Drug; Drug Resistance, Multiple, Bacterial - drug effects; Gram-Positive Bacteria - drug effects; Humans; Interleukins - chemistry; Methicillin-Resistant Staphylococcus aureus - drug effects; Mice; Microbial Sensitivity Tests; Molecular Structure; MRSA; Structure-Activity Relationship; Antibacterial activity; Cycloberberine ester; DNA polymerase IIIC; Structure-activity relationship; MRSA

The constant evolution of Methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant S. aureus (VRSA) constitutes a major threat to human health with limited treatment options. In our previous studies, we invented an innovative cycloberberine (CBBR) scaffold to battle MRSA and other...