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The Spectrum of Berberine Antibacterial and Antifungal Activities

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Promising Antimicrobials from Natural Products

Abstract

Isoquinoline alkaloid berberine is a typical multitarget or multicomponent molecule of botanical origin. It is extensively used for hundreds of years in the treatment of various infectious diseases and in traditional medicine. Numerous studies from academic institutions and pharma industry reported several pharmacological effects and efficacy of berberine in the treatment of inflammation, cancer, and diabetes. The plethora of beneficial activities rely on the existence of multiple mechanisms of its action, mainly related to cell cycle arrest and apoptosis. Considering its antifungal and antibacterial activities, berberine targets bacterial cell walls and cell membranes, as well as DNA and RNA. It disturbs membrane potential and rigidity by forming reactive oxygen species (ROS). The influence on protein expression is evident in affecting efflux pumps. Berberine also potentiates activity of several antibiotics and antifungal drugs, demonstrating synergistic antibacterial activity, and has detrimental effect on biofilm matrix of several pathogens, including multidrug-resistant (MDR) bacteria and yeasts. In this chapter, we focus on the antimicrobial effects of berberine and plausible mechanisms of actions involved, and give future perspective on the potential of berberine-based therapy.

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Abbreviations

ALP:

Alkaline phosphatase

ATCC:

American Type Culture Collection

cAMP-PKA:

Cyclic adenosine monophosphate–dependent protein kinase

CYP51:

Fungal sterol 14α-demethylase

DNA:

Deoxyribonucleic acid

ERG:

ETS (erythroblast transformation-specific)-related gene

ESKAPE pathogens:

Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species

GPx:

Glutathione peroxidase

GR:

Glutathione reductase

GSH/GSSH:

Reduced glutathione/oxidized glutathione ratio

HSF1:

Heat shock factor 1

LC-MS/MS:

Liquid chromatography–tandem mass spectrometry

MAPK:

Mitogen-activated protein kinase

MDR:

Multidrug resistant

MIC:

Minimal inhibitory concentration

MRSA:

Methicillin-resistant Staphylococcus aureus

MSSA:

Methicillin-sensitive Staphylococcus aureus

NAcDG:

N-acetyl-D-glucosamine

ROS:

Reactive oxygen species

SEM:

Scanning electron microscopy

SOD:

Superoxide dismutase

TEM:

Transmission electron microscopy

YPD:

Yeast extract–peptone–dextrose

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Kosalec, I., Jembrek, M.J., Vlainić, J. (2022). The Spectrum of Berberine Antibacterial and Antifungal Activities. In: Rai, M., Kosalec, I. (eds) Promising Antimicrobials from Natural Products. Springer, Cham. https://doi.org/10.1007/978-3-030-83504-0_7

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