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Two Flavonols from Artemisa annua which Potentiate the Activity of Berberine and Norfloxacin Against a Resistant Strain of Staphylococcus aureus
Abstract
Bioassay-guided fractionation of an extract of Artemisia annua L. (Asteraceae) was conducted in order to assess the possible presence in the plant material of inhibitors of bacterial multidrug resistance pumps. Fractions were tested for Staphylococcus aureus growth inhibition in the presence of a subinhibitory dose of the weak antibacterial alkaloid berberine. Active fractions yielded the flavones chrysosplenol-D and chrysoplenetin, which themselves had very weak growth inhibitory action, but which made a potent combination with berberine. In comparison with work on other flavonols, it is likely that potentiation is due to the inhibition of an S. aureus multidrug resistance (MDR) pump. These same two flavonols were earlier reported to potentiate the activity of artemisinin against Plasmodium falciparum.
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“These flavones include: casticin (227), artemetin (228) [91], chrysosplenol D (225) and chrysoplenetin (226) [92]”
From The Biosynthesis of Artemisinin (Qinghaosu) and the Phytochemistry of Artemisia annua L. (Qinghao) (2010) · cites this paper as [92]
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Shahid, M., Dar, F. K., Ismaeel, A. Y., Al-Mahmeed, A. E., Sindi, K. A., Malik, A., & Khan, H. M. (2013) · Springer eBooks · doi:10.1007/978-94-007-6603-7_5 · Cited by 4
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Dreier, J. (2014) · ASM Press eBooks · doi:10.1128/9781555815615.ch15 · Cited by 4
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Importance of efflux pumps in subjugating antibiotic resistance
Singh, T., Dar, S. A., Das, S., & Haque, S. (2020) · Elsevier eBooks · doi:10.1016/b978-0-12-818480-6.00010-2 · Cited by 6
Tummaruk, P., Tantilertcharoen, R., & Prapasarakul, N. (2009) · Cited by 3
Detection of efflux pump activity among clinical isolates of Staphylococcus and Micrococcus species
Adeluola, A. O., Oyedeji, K. S., Mendie, U. E., et al. (2018) · Tropical Journal of Pharmaceutical Research · doi:10.4314/tjpr.v16i11.18 · Cited by 2
Zgurskaya, H. I., Lomovskaya, O., Lewis, K., & Bostian, K. A. (2007) · CRC Press eBooks · doi:10.1201/9781420008753.ch4 · Cited by 2
Self-citationPharmacophore development and validation for inhibitors of the bacterial NorA efflux pump
Dupree, T. (2005) · Research Online (University of Wollongong) · Cited by 2
Natural Product as Efflux Pump Inhibitors Against MRSA Efflux Pumps: An Update
Ahirrao, P., Kalia, R., & Jachak, S. M. (2022) · Springer eBooks · doi:10.1007/978-981-16-3120-7_19 · Cited by 1
Studies on bacterial Efflux pump inhibitors in land plants
Brown, A. R. (2015) · NC Digital Online Collection of Knowledge and Scholarship (The University of North Carolina at Greensboro)
Mohan, A., Nisha, A. R., & Keerthika, V. (2020) · International Journal of Scientific Research in Science and Technology · doi:10.32628/ijsrst20754
Research progress on berberine and its derivatives
Sun, J., Wang, J., Xie, X., Wang, J., Zhou, Y., & Liu, H. (2025) · Scientia Sinica Chimica · doi:10.1360/ssc-2025-0104
Mini review on antidiabetic botanicals: molecular insights and future prospects
Selvi, G. S. A., Rani, T. P. K. P., Döss, A., Aranganayaki, J., Kabir, N. A., Pole, R. P. P., & Satheesh, S. (2026) · Oriental Pharmacy and Experimental Medicine · doi:10.1007/s13596-026-00893-7
Metadata
- Authors
- Stermitz, F. R., Scriven, L. N., Tegos, G., & Lewis, K.
- Affiliations
- Colorado State University (US)
- Northeastern University (US)
- Venue
- Planta Medica
- Publisher
- Georg Thieme Verlag KG
- Published
- 2002-12
- Volume
- 68
- Issue
- 12
- Pages
- 1140-1141
- ISSN
- 0032-0943 (ISSN-L)
- 1439-0221
- OpenAlex
- W2039587632
- Cited by
- 114
- References
- 0
- Citations by year
- 2026: 1 · 2025: 4 · 2023: 4 · 2022: 6 · 2021: 6 · 2020: 10 · 2019: 6 · 2018: 3 · 2017: 2 · 2016: 3 · 2015: 5 · 2014: 6 · 2013: 5 · 2012: 9
- FWCI
- 0.93
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Planta Medica (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Colorado State University
- National Institutes of Health (5r01gm059903-03)
- National Institute of General Medical Sciences (R01 GM 59903)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › Bioactive natural compounds
- Life Sciences › Agricultural and Biological Sciences › Food Science › Essential Oils and Antimicrobial Activity
- Physical Sciences › Chemistry › Organic Chemistry › Sesquiterpenes and Asteraceae Studies
- Keywords
- Artemisia annua, flavonols, berberine, norfloxacin, Staphylococcus aureus, multidrug resistance, efflux pump inhibitors, bioassay-guided fractionation
- MeSH terms
- Anti-Infective Agents, Berberine, Drug Synergism, Flavonoids, Norfloxacin, Plant Extracts, Staphylococcus aureus, Molecular Structure, Drug Resistance, Bacterial, Artemisia annua
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