Novel 3-substituted ocotillol-type triterpenoid derivatives as antibacterial candidates

Yi Bi; Cong Ma; Hengyuan Zhang; Zhiwen Zhou; Jian Yang; Zhenlei Zhang; Qingguo Meng; Peter J. Lewis; Jinyi Xu

doi:10.1111/cbdd.12337

Novel 3-substituted ocotillol-type triterpenoid derivatives as antibacterial candidates

Yi Bi, Cong Ma, Hengyuan Zhang, Zhiwen Zhou, Jian Yang, Zhenlei Zhang, Qingguo Meng, Peter J. Lewis, Jinyi Xu

Research output: Journal article publication › Journal article › Academic research › peer-review

18 Citations (Scopus)

Abstract

Plant-derived triterpenoid saponins are involved in the plant defense system by targeting bacterial membranes. A series of ocotillol-type triterpenoid derivatives were synthesized starting from PPD, one of the main components of Panax ginseng and their antibacterial activity against several representative bacteria were evaluated. Compounds 5 and 11 exhibited excellent antibacterial activity with MIC values of 1 μg/mL against Staphylococcus aureus and 8 μg/mL and 4 μg/mL against Bacillus subtilis, respectively. Furthermore, when compounds 5 and 11 were combined with two commercial antibiotics kanamycin and chloramphenicol, they showed strong synergistic activity at sub-MIC levels against S. aureus USA300 and B. subtilis 168. Moreover, chloramphenicol turned from a bacteriostatic to a bactericidal agent when combined with compound 11 against B. subtilis 168.

Original language	English
Pages (from-to)	489-496
Number of pages	8
Journal	Chemical Biology and Drug Design
Volume	84
Issue number	4
DOIs	https://doi.org/10.1111/cbdd.12337
Publication status	Published - 1 Oct 2014
Externally published	Yes

Keywords

antibacterial activity
ocotillol-type
synergistic effect
triterpenoid saponin

ASJC Scopus subject areas

Biochemistry
Molecular Medicine

More information

10.1111/cbdd.12337

Cite this

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title = "Novel 3-substituted ocotillol-type triterpenoid derivatives as antibacterial candidates",

abstract = "Plant-derived triterpenoid saponins are involved in the plant defense system by targeting bacterial membranes. A series of ocotillol-type triterpenoid derivatives were synthesized starting from PPD, one of the main components of Panax ginseng and their antibacterial activity against several representative bacteria were evaluated. Compounds 5 and 11 exhibited excellent antibacterial activity with MIC values of 1 μg/mL against Staphylococcus aureus and 8 μg/mL and 4 μg/mL against Bacillus subtilis, respectively. Furthermore, when compounds 5 and 11 were combined with two commercial antibiotics kanamycin and chloramphenicol, they showed strong synergistic activity at sub-MIC levels against S. aureus USA300 and B. subtilis 168. Moreover, chloramphenicol turned from a bacteriostatic to a bactericidal agent when combined with compound 11 against B. subtilis 168.",

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AU - Bi, Yi

AU - Ma, Cong

AU - Zhang, Hengyuan

AU - Zhou, Zhiwen

AU - Yang, Jian

AU - Zhang, Zhenlei

AU - Meng, Qingguo

AU - Lewis, Peter J.

AU - Xu, Jinyi

PY - 2014/10/1

Y1 - 2014/10/1

N2 - Plant-derived triterpenoid saponins are involved in the plant defense system by targeting bacterial membranes. A series of ocotillol-type triterpenoid derivatives were synthesized starting from PPD, one of the main components of Panax ginseng and their antibacterial activity against several representative bacteria were evaluated. Compounds 5 and 11 exhibited excellent antibacterial activity with MIC values of 1 μg/mL against Staphylococcus aureus and 8 μg/mL and 4 μg/mL against Bacillus subtilis, respectively. Furthermore, when compounds 5 and 11 were combined with two commercial antibiotics kanamycin and chloramphenicol, they showed strong synergistic activity at sub-MIC levels against S. aureus USA300 and B. subtilis 168. Moreover, chloramphenicol turned from a bacteriostatic to a bactericidal agent when combined with compound 11 against B. subtilis 168.

AB - Plant-derived triterpenoid saponins are involved in the plant defense system by targeting bacterial membranes. A series of ocotillol-type triterpenoid derivatives were synthesized starting from PPD, one of the main components of Panax ginseng and their antibacterial activity against several representative bacteria were evaluated. Compounds 5 and 11 exhibited excellent antibacterial activity with MIC values of 1 μg/mL against Staphylococcus aureus and 8 μg/mL and 4 μg/mL against Bacillus subtilis, respectively. Furthermore, when compounds 5 and 11 were combined with two commercial antibiotics kanamycin and chloramphenicol, they showed strong synergistic activity at sub-MIC levels against S. aureus USA300 and B. subtilis 168. Moreover, chloramphenicol turned from a bacteriostatic to a bactericidal agent when combined with compound 11 against B. subtilis 168.

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KW - ocotillol-type

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JO - Chemical Biology and Drug Design

JF - Chemical Biology and Drug Design

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Novel 3-substituted ocotillol-type triterpenoid derivatives as antibacterial candidates

Abstract

Keywords

ASJC Scopus subject areas

More information

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