The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives

Jing Wang; Teng Yang; Huang Chen; Yun Nan Xu; Li Fang Yu; Ting Liu; Jie Tang; Zhengfang Yi; Cai Guang Yang; Wei Xue; Fan Yang

doi:10.1016/j.ejmech.2017.01.012

The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives

Jing Wang
, Teng Yang
, Huang Chen
, Yun Nan Xu
, Li Fang Yu
, Ting Liu
, Jie Tang
, Zhengfang Yi
, Cai Guang Yang
, Wei Xue^*
, Fan Yang

^*Corresponding author for this work

East China Normal University
Guizhou University
CAS - Shanghai Institute of Materia Medica

Research output: Contribution to journal › Article › peer-review

58 Scopus citations

Abstract

A series of novel 9, 13-disubstituted berberine derivatives have been synthesized and evaluated for the antibacterial activities against Staphylococcus aureus, including Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). Compound 20 shows the most potent activity against the growth of Newman strain, with a MIC value of 0.78 μg/mL, which is comparable with the positive control vancomycin. In addition, compound 20, 21, and 33 are highly antistaphylococcal active against five strains of multidrug-resistant S. aureus, with MIC values of 0.78–1.56 μg/mL. Of note, theses antibacterial active compounds have no obvious toxicity to the viability of human fibroblast (HAF) cells at the MIC concentration.

Original language	English
Pages (from-to)	424-433
Number of pages	10
Journal	European Journal of Medicinal Chemistry
Volume	127
DOIs	https://doi.org/10.1016/j.ejmech.2017.01.012
State	Published - 2017

Keywords

Antistaphylococcal activity
Berberine derivatives
Cytotoxicity
Multidrug-resistant

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10.1016/j.ejmech.2017.01.012

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@article{7ad1b8faf4824fa989db1258708115e5,

title = "The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives",

abstract = "A series of novel 9, 13-disubstituted berberine derivatives have been synthesized and evaluated for the antibacterial activities against Staphylococcus aureus, including Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). Compound 20 shows the most potent activity against the growth of Newman strain, with a MIC value of 0.78 μg/mL, which is comparable with the positive control vancomycin. In addition, compound 20, 21, and 33 are highly antistaphylococcal active against five strains of multidrug-resistant S. aureus, with MIC values of 0.78{\textendash}1.56 μg/mL. Of note, theses antibacterial active compounds have no obvious toxicity to the viability of human fibroblast (HAF) cells at the MIC concentration.",

keywords = "Antistaphylococcal activity, Berberine derivatives, Cytotoxicity, Multidrug-resistant",

author = "Jing Wang and Teng Yang and Huang Chen and Xu, \{Yun Nan\} and Yu, \{Li Fang\} and Ting Liu and Jie Tang and Zhengfang Yi and Yang, \{Cai Guang\} and Wei Xue and Fan Yang",

note = "Publisher Copyright: {\textcopyright} 2017 Elsevier Masson SAS",

year = "2017",

doi = "10.1016/j.ejmech.2017.01.012",

language = "英语",

volume = "127",

pages = "424--433",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

}

TY - JOUR

T1 - The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives

AU - Wang, Jing

AU - Yang, Teng

AU - Chen, Huang

AU - Xu, Yun Nan

AU - Yu, Li Fang

AU - Liu, Ting

AU - Tang, Jie

AU - Yi, Zhengfang

AU - Yang, Cai Guang

AU - Xue, Wei

AU - Yang, Fan

PY - 2017

Y1 - 2017

N2 - A series of novel 9, 13-disubstituted berberine derivatives have been synthesized and evaluated for the antibacterial activities against Staphylococcus aureus, including Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). Compound 20 shows the most potent activity against the growth of Newman strain, with a MIC value of 0.78 μg/mL, which is comparable with the positive control vancomycin. In addition, compound 20, 21, and 33 are highly antistaphylococcal active against five strains of multidrug-resistant S. aureus, with MIC values of 0.78–1.56 μg/mL. Of note, theses antibacterial active compounds have no obvious toxicity to the viability of human fibroblast (HAF) cells at the MIC concentration.

AB - A series of novel 9, 13-disubstituted berberine derivatives have been synthesized and evaluated for the antibacterial activities against Staphylococcus aureus, including Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). Compound 20 shows the most potent activity against the growth of Newman strain, with a MIC value of 0.78 μg/mL, which is comparable with the positive control vancomycin. In addition, compound 20, 21, and 33 are highly antistaphylococcal active against five strains of multidrug-resistant S. aureus, with MIC values of 0.78–1.56 μg/mL. Of note, theses antibacterial active compounds have no obvious toxicity to the viability of human fibroblast (HAF) cells at the MIC concentration.

KW - Antistaphylococcal activity

KW - Berberine derivatives

KW - Cytotoxicity

KW - Multidrug-resistant

UR - https://www.scopus.com/pages/publications/85009200813

U2 - 10.1016/j.ejmech.2017.01.012

DO - 10.1016/j.ejmech.2017.01.012

M3 - 文章

C2 - 28092858

AN - SCOPUS:85009200813

SN - 0223-5234

VL - 127

SP - 424

EP - 433

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives

Abstract

Keywords

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