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Antimicrobial Evalu...
Antimicrobial Evaluation of Two Polycyclic Polyprenylated Acylphloroglucinol Compounds: PPAP23 and PPAP53.
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Ammanath, Aparna Viswanathan (author)
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Matsuo, Miki (author)
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Wang, Huanhuan (author)
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Kraus, Frank (author)
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Bleisch, Anton (author)
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Peslalz, Philipp (author)
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Mohammad, Majd (author)
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- Deshmukh, Megshree (author)
- Gothenburg University,Göteborgs universitet,Institutionen för medicin, avdelningen för reumatologi och inflammationsforskning,Institute of Medicine, Department of Rheumatology and Inflammation Research
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Grießhammer, Anne (author)
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Purkayastha, Moushumi (author)
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Vorbach, Andreas (author)
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Macek, Boris (author)
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Brötz-Oesterhelt, Heike (author)
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Maier, Lisa (author)
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Kretschmer, Dorothee (author)
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Peschel, Andreas (author)
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- Jin, Tao, 1973 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för medicin, avdelningen för reumatologi och inflammationsforskning,Institute of Medicine, Department of Rheumatology and Inflammation Research
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Plietker, Bernd (author)
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Götz, Friedrich (author)
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(creator_code:org_t)
- 2024
- 2024
- English.
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In: International Journal of Molecular Sciences. - 1422-0067. ; 25:15
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https://doi.org/10.3...
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Abstract
Subject headings
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- Polycyclic polyprenylated acylphloroglucinols (PPAPs) comprise a large group of compounds of mostly plant origin. The best-known compound is hyperforin from St. John's wort with its antidepressant, antitumor and antimicrobial properties. The chemical synthesis of PPAP variants allows the generation of compounds with improved activity and compatibility. Here, we studied the antimicrobial activity of two synthetic PPAP-derivatives, the water-insoluble PPAP23 and the water-soluble sodium salt PPAP53. In vitro, both compounds exhibited good activity against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium. Both compounds had no adverse effects on Galleria mellonella wax moth larvae. However, they were unable to protect the larvae from infection with S. aureus because components of the larval coelom neutralized the antimicrobial activity; a similar effect was also seen with serum albumin. In silico docking studies with PPAP53 revealed that it binds to the F1 pocket of human serum albumin with a binding energy of -7.5 kcal/mol. In an infection model of septic arthritis, PPAP23 decreased the formation of abscesses and S. aureus load in kidneys; in a mouse skin abscess model, topical treatment with PPAP53 reduced S. aureus counts. Both PPAPs were active against anaerobic Gram-positive gut bacteria such as neurotransmitter-producing Clostridium, Enterococcus or Ruminococcus species. Based on these results, we foresee possible applications in the decolonization of pathogens.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine (hsv//eng)
Keyword
- Animals
- Phloroglucinol
- pharmacology
- chemistry
- analogs & derivatives
- Mice
- Methicillin-Resistant Staphylococcus aureus
- drug effects
- Molecular Docking Simulation
- Anti-Bacterial Agents
- pharmacology
- chemistry
- Humans
- Microbial Sensitivity Tests
- Larva
- drug effects
- Staphylococcal Infections
- drug therapy
- Enterococcus faecium
- drug effects
- Moths
- drug effects
- Ketones
- Spiro Compounds
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Ammanath, Aparna ...
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Matsuo, Miki
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Wang, Huanhuan
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Kraus, Frank
-
Bleisch, Anton
-
Peslalz, Philipp
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show more...
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Mohammad, Majd
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Deshmukh, Megshr ...
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Grießhammer, Ann ...
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Purkayastha, Mou ...
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Vorbach, Andreas
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Macek, Boris
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Brötz-Oesterhelt ...
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Maier, Lisa
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Kretschmer, Doro ...
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Peschel, Andreas
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Jin, Tao, 1973
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Plietker, Bernd
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Götz, Friedrich
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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Clinical Medicin ...
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International Jo ...
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University of Gothenburg