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<p>The issue of antimicrobial resistance, along with the reduced efficacy of available antibiotics, constitutes a significant concern for public health. <i>Picralima nitida</i> is a Ghanaian plant used for the treatment of infections and may yield new antibiotics with reduced susceptibility to the efflux mechanism. Our research aimed to isolate and characterize antimicrobial and resistance-modifying compounds from <i>P. nitida</i>. Using chromatographic and spectroscopic techniques, akuammidine and akuammine were isolated from the chloroform fraction. Using in vitro tests, the effects of the extracts and isolated compounds were investigated using microdilution, biofilm, and efflux pump inhibitory assays against resistant microbial strains. In silico studies were performed to investigate the modes of intermolecular binding interactions between the two compounds and AcrB, MexB, LasR, and FtsZ. Akuammidine and akuammine showed significant inhibition of biofilm formation in <i>P. aeruginosa</i>, <i>S. aureus</i>, and <i>B. subtilis</i>, with akuammidine achieving inhibition rates of 60%, 67%, and 53%, respectively, and akuammine showing inhibition rates of 61%, 27%, and 61%, respectively. Both compounds exhibited efflux pump inhibition activity on the organisms used. Molecular docking showed that both compounds established important interactions with key amino acid residues in the proteins. Higher binding energies were obtained for AcrB and MexB. Akuammidine showed binding affinities of − 7.2&#xa0;kcal/mol and − 8.7&#xa0;kcal/mol for AcrB and MexB, respectively. Akuammine showed binding affinities of − 7.2&#xa0;kcal/mol and − 7.7&#xa0;kcal/mol for AcrB and MexB, respectively. These findings suggest the potential application of these compounds in the design of antibiotics, which are less susceptible to resistance mechanisms.</p>

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In vitro and in silico evaluation of Picralima nitida monoterpene indole alkaloids as antimicrobial resistance modifiers

  • 期刊论文

  • 发表日期：

    2026年7月30日

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  • Makafui Adzo Gbemu,
  • Susana Dufie Boatey,
  • Prince Dagadu Okyere,
  • Yaw Duah Boakye,
  • John Nii Addotey,
  • Rita Akosua Dickson,
  • Edmund Ekuadzi

摘要

The issue of antimicrobial resistance, along with the reduced efficacy of available antibiotics, constitutes a significant concern for public health. Picralima nitida is a Ghanaian plant used for the treatment of infections and may yield new antibiotics with reduced susceptibility to the efflux mechanism. Our research aimed to isolate and characterize antimicrobial and resistance-modifying compounds from P. nitida. Using chromatographic and spectroscopic techniques, akuammidine and akuammine were isolated from the chloroform fraction. Using in vitro tests, the effects of the extracts and isolated compounds were investigated using microdilution, biofilm, and efflux pump inhibitory assays against resistant microbial strains. In silico studies were performed to investigate the modes of intermolecular binding interactions between the two compounds and AcrB, MexB, LasR, and FtsZ. Akuammidine and akuammine showed significant inhibition of biofilm formation in P. aeruginosa, S. aureus, and B. subtilis, with akuammidine achieving inhibition rates of 60%, 67%, and 53%, respectively, and akuammine showing inhibition rates of 61%, 27%, and 61%, respectively. Both compounds exhibited efflux pump inhibition activity on the organisms used. Molecular docking showed that both compounds established important interactions with key amino acid residues in the proteins. Higher binding energies were obtained for AcrB and MexB. Akuammidine showed binding affinities of − 7.2 kcal/mol and − 8.7 kcal/mol for AcrB and MexB, respectively. Akuammine showed binding affinities of − 7.2 kcal/mol and − 7.7 kcal/mol for AcrB and MexB, respectively. These findings suggest the potential application of these compounds in the design of antibiotics, which are less susceptible to resistance mechanisms.