Berberine reverses multidrug resistance in Candida albicans by hijacking the drug efflux pump Mdr1p

Tong, Yaojun; Zhang, Jingyu; Sun, Nuo; Wang, Xiang Ming; Qi, Wei; Huang, Ren; Pu, Yonglin; Dai, Huanqin; Ren, Biao; Pei, Gang; Song, Fuhang; Zhu, Guoliang; Xia, Xuekui; Chen, Xiangyin; Jiang, Lan; Wang, Shenlin; Ouyang, Liming; Xie, Ning; Zhang, Buchang; Jiang, Yuanying; Liu, Xueting; Calderone, Richard; Bai, Fan; Zhang, Lixin; Alterovitz, Gil

doi:10.1016/j.scib.2020.12.035

Cited by 26 publications

(15 citation statements)

References 37 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This compound can also hijack the overexpressed Mdr1p and though reduce antifungal resistance in C. albicans . Additionally, it was elucidated that application of berberine was efficient also in vivo, since it can lengthen the survival time of mice with blood-borne dissemination of Mdr1p overexpressed multidrug-resistant candidiasis [ 63 ].…”

Section: Recent Update On Antifungal Targets and Strategiesmentioning

confidence: 99%

Emerging Antifungal Targets and Strategies

Ivanov

Ćirić

Stojković

2022

IJMS

View full text Add to dashboard Cite

Despite abundant research in the field of antifungal drug discovery, fungal infections remain a significant healthcare burden. There is an emerging need for the development of novel antifungals since those currently available are limited and do not completely provide safe and secure protection. Since the current knowledge regarding the physiology of fungal cells and the infection mechanisms is greater than ever, we have the opportunity to use this for the development of novel generations of antifungals. In this review, we selected and summarized recent studies describing agents employing different antifungal mechanisms. These mechanisms include interference with fungal resistance, including impact on the efflux pumps and heat shock protein 90. Additionally, interference with virulence factors, such as biofilms and hyphae; the impact on fungal enzymes, metabolism, mitochondria, and cell wall; and antifungal vaccines are explored. The agents investigated belong to different classes of natural or synthetic molecules with significant attention given also to plant extracts. The efficacy of these antifungals has been studied mainly in vitro with some in vivo, and clinical studies are needed. Nevertheless, there is a large quantity of products employing novel antifungal mechanisms that can be further explored for the development of new generation of antifungals.

show abstract

Section: Recent Update On Antifungal Targets and Strategiesmentioning

confidence: 99%

Emerging Antifungal Targets and Strategies

Ivanov

Ćirić

Stojković

2022

IJMS

View full text Add to dashboard Cite

show abstract

“…Berberine is an isoquinoline alkaloid isolated from the traditional Chinese herbal Coptis chinensis Franch., which has been reported to have various pharmacological activities, such as anti-inflammatory, 12,13 antimicrobial, [14][15][16] anti-Parkinson's, 17,18 antitumor, 19,20 and antiviral, 21,22 among others. 23,24 A report has shown that berberine exhibited antifungal activity against various pathogenic fungi with minimum inhibitory concentration (MIC) values ranging from 10 to 160 μg ml −1 , such as Candida albicans, Candida krusei, Candida glabrata and Candida dubliniensis.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, and biological evaluation of novel berberine derivatives against phytopathogenic fungi

Zhou

Yang

Luo

et al. 2022

Pest Management Science

View full text Add to dashboard Cite

BACKGROUND: The abuse of chemical fungicides not only leads to toxic residues and resistance in plant pathogenic fungi, but also causes environmental pollution and side effects on in humans and animals. Based on the antifungal activities of berberine, seven different types of berberine derivatives (A1-G1) were synthesized, and their antifungal activities against six plant pathogenic fungi were evaluated (Rhizoctonia solani, Botrytis cinerea, Fusarium graminearum, Phytophthora capsici, Sclerotinia sclerotiorum, and Magnaporthe oryzae). RESULTS:The results for antifungal activities in vitro showed that berberine derivative E1 displayed good antifungal activity against R. solani with a median effective concentration (EC 50 ) of 1.77 ∼g ml −1 , and berberine derivatives F1 and G1 demonstrated broad-spectrum antifungal activities with EC 50 values ranging from 4.43 to 42.23 ∼g ml −1 against six plant pathogenic fungi. Berberine derivatives (E2-E29, F2-F18, and G2-G9) were further synthesized to investigate the structure-activity relationship (SAR), and compound E20 displayed significant antifungal activity against R. solani with an EC 50 value of 0.065 ∼g ml −1 . Preliminary mechanism studies showed that E20 could cause mycelial shrinkage, cell membrane damage, mitochondrial abnormalities and the accumulation of harmful reactive oxygen species, resulting in cell death in R. solani. Moreover, in vivo experimental results showed that the protective effect of E20 was 97.31% at 5 ∼g ml −1 , which was better than that of the positive control thifluzamide (50.13% at 5 ∼g ml −1 ).CONCLUSION: Berberine derivative E20 merits further development as a new drug candidate with selective and excellent antifungal activity against R. solani.

show abstract

“…It has been used in Traditional Chinese Medical systems in China and Ayurvedic system in India for a very long time ( Gaba et al, 2021 ; Xu et al, 2021 ). Modern pharmacological studies have proved that BBR has abundant biological activities including anti-inflammatory ( Bai et al, 2020 ; Ma et al, 2020 ; Fu et al, 2021 ), anti-oxidant ( Eissa et al, 2018 ; Seth et al, 2021 ), anti-bacterial ( Wang et al, 2009 ; Avci et al, 2018 ; Tong et al, 2021 ), viricide ( Hayashi et al, 2007 ; Cecil et al, 2011 ; Hung et al, 2019 ), cardiovascular protection ( Salehi and Filtz, 2011 ; Li et al, 2014 ; Wang L. et al, 2020 ), hypolipidemic ( Hu et al, 2012 ; Zhou et al, 2014 ), anti-diabetic ( Lee et al, 2006 ; Ye et al, 2016 ; Di et al, 2021 ), anti-tumor ( Liu et al, 2017 ; Zhang et al, 2020 ; Ren et al, 2021 ), anti-ulcer ( Li et al, 2020 ; Xiong et al, 2021 ), anti-neurodegeneration ( Liang et al, 2017 ; Hussien et al, 2018 ; Živančević et al, 2022 ), and anti-rheumatoid arthritis ( Huang et al, 2021 ; Li et al, 2022 ) ( Figure 1 ).…”

Section: Introductionmentioning

confidence: 99%

Structural modifications of berberine and their binding effects towards polymorphic deoxyribonucleic acid structures: A review

Mou

Deng

et al. 2022

Front. Pharmacol.

View full text Add to dashboard Cite

Berberine (BBR) is a plant derived quaternary benzylisoquinoline alkaloid, which has been widely used in traditional medicines for a long term. It possesses broad pharmacological effects and is widely applied in clinical. In recent years, the anti-tumor effects of BBR have attracted more and more attention of the researchers. The canonical right-handed double-stranded helical deoxyribonucleic acid (B-DNA) and its polymorphs occur under various environmental conditions and are involved in a plethora of genetic instability-related diseases especially tumor. BBR showed differential binding effects towards various polymorphic DNA structures. But its poor lipophilicity and fast metabolism limited its clinical utility. Structural modification of BBR is an effective approach to improve its DNA binding activity and bioavailability in vivo. A large number of studies dedicated to improving the binding affinities of BBR towards different DNA structures have been carried out and achieved tremendous advancements. In this article, the main achievements of BBR derivatives in polymorphic DNA structures binding researches in recent 20 years were reviewed. The structural modification strategy of BBR, the DNA binding effects of its derivatives, and the structure activity relationship (SAR) analysis have also been discussed.

show abstract

Berberine reverses multidrug resistance in Candida albicans by hijacking the drug efflux pump Mdr1p

Cited by 26 publications

References 37 publications

Emerging Antifungal Targets and Strategies

Emerging Antifungal Targets and Strategies

Design, synthesis, and biological evaluation of novel berberine derivatives against phytopathogenic fungi

Structural modifications of berberine and their binding effects towards polymorphic deoxyribonucleic acid structures: A review

Contact Info

Product

Resources

About