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1.
Article in English | WPRIM | ID: wpr-773562

ABSTRACT

A series of berberine derivatives were synthesized by introducing substituted benzyl groups at C-9. All these synthesized compounds (4a-4m) were screened for their in vitro antibacterial activity against four Gram-positive bacteria and four Gram-negative bacteria and evaluated for their antifungal activity against three pathogenic fungal strains. All these compounds displayed good antibacterial and antifungal activities, compared to reference drugs including Ciprofloxacin and Fluconazole; Compounds 4f, 4g, and 4l showed the highest antibacterial and antifungal activities. Moreover, all the synthesized compounds were docked into topoisomerase II-DNA complex, which is a crucial drug target for the treatment of microbial infections. Docking results showed that H-bond, π-π stacked, π-cationic, and π-anionic interactions were responsible for the strong binding of the compounds with the target protein-DNA complex.


Subject(s)
Anti-Bacterial Agents , Chemistry , Pharmacology , Antifungal Agents , Chemistry , Pharmacology , Bacteria , Berberine , Chemistry , Pharmacology , Drug Design , Fungi , Molecular Docking Simulation , Structure-Activity Relationship
2.
Article in English | WPRIM | ID: wpr-812351

ABSTRACT

A series of berberine derivatives were synthesized by introducing substituted benzyl groups at C-9. All these synthesized compounds (4a-4m) were screened for their in vitro antibacterial activity against four Gram-positive bacteria and four Gram-negative bacteria and evaluated for their antifungal activity against three pathogenic fungal strains. All these compounds displayed good antibacterial and antifungal activities, compared to reference drugs including Ciprofloxacin and Fluconazole; Compounds 4f, 4g, and 4l showed the highest antibacterial and antifungal activities. Moreover, all the synthesized compounds were docked into topoisomerase II-DNA complex, which is a crucial drug target for the treatment of microbial infections. Docking results showed that H-bond, π-π stacked, π-cationic, and π-anionic interactions were responsible for the strong binding of the compounds with the target protein-DNA complex.


Subject(s)
Anti-Bacterial Agents , Chemistry , Pharmacology , Antifungal Agents , Chemistry , Pharmacology , Bacteria , Berberine , Chemistry , Pharmacology , Drug Design , Fungi , Molecular Docking Simulation , Structure-Activity Relationship
3.
Chinese Pharmaceutical Journal ; (24): 429-433, 2017.
Article in Chinese | WPRIM | ID: wpr-858767

ABSTRACT

Berberine belongs to the quaternary ammonium type isoquinoline alkaloid known as berberinum. In traditional Chinese medicine, it has long been used to treat infections of the gastrointestinal tract disease caused by bacteria. Recent studies found that berberine has a good anti-tumor effect,but it is difficult pass through the cell membrane due to its poor fat-soluble, which limit its clinical application. By modifing chemical structure, some researchers have investigated the relationship between activity effects and structures of berberine and its derivatives, and have found a series of anti-tumor activity enhanced berberine derivatives. In this review, the recent research progress of the anti-tumor effects and their mechanisms of berberine and its derivatives are focused, which may provide reference for the design and development of anticancer drugs based on the structure of berberine

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