A clerodane diterpene from Polyalthia longifolia as a modifying agent of the resistance of methicillin resistant

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A Customizable Approach for the Enzymatic Production and Purification of Diterpenoid Natural Products
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Vivek Kumar Gupta1, Nimisha Tiwari1, Priyanka Gupta1

  • 1Molecular Bioprospection Department, CSIR-Central Institute of Medicinal and Aromatic Plants, P.O. CIMAP, Lucknow-226015, India.

Phytomedicine : International Journal of Phytotherapy and Phytopharmacology
|May 11, 2016
PubMed
Abstract

Insights

Clerodane diterpene (CD) enhances antibiotic effectiveness against drug-resistant Staphylococcus aureus by inhibiting efflux pumps. This natural compound shows promise in combating rising antimicrobial resistance, offering new hope for treating staphylococcal infections.

Area of Science:

  • Pharmacology
  • Microbiology
  • Natural Products Chemistry

Background:

  • Staphylococcus aureus infections pose a global health threat.
  • Multidrug resistance (MDR) compromises conventional antibiotic efficacy.
  • Novel resistance-modifying agents (RMAs) are crucial for effective treatment.

Purpose of the Study:

  • To evaluate the resistance-modifying activity of Clerodane diterpene (CD) from Polyalthia longifolia against MRSA.
  • To assess the impact of CD on the innate immune response in vitro and in vivo.
  • To elucidate the mechanism of action, including efflux pump inhibition.

Main Methods:

  • In vitro susceptibility testing using microdilution assays and time-kill curves.
  • In vivo efficacy studies in a Staphylococcus aureus-infected Swiss albino mice model.
  • Flow cytometry for efflux pump activity and qRT-PCR for gene expression analysis.

Main Results:

  • CD significantly reduced fluoroquinolone minimum inhibitory concentrations (MICs) up to 16-fold.
  • Combination therapy with CD and norfloxacin lowered bacterial burden in multiple organs in vivo.
  • CD inhibited ethidium bromide efflux and modulated norA efflux pump gene expression.

Conclusions:

  • CD demonstrates significant drug resistance-modifying potential by inhibiting MDR efflux pumps.
  • This study is the first to report the efflux pump inhibitory activity of CD.
  • CD represents a promising natural compound for enhancing current antimicrobial therapies.
Keywords:
Clerodane diterpeneEfflux pump inhibitorFluoroquinolonesMRSAResistance- modifying agents

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