Screening of compounds of Evernia prunastri (L.) for their antiproliferative activity in glioblastoma cells

Shcherbakova, A; Nyugen, L; Koptina, A; Backlund, Anders; Shurgin, A.; Romanov, E. M.

doi:10.1055/s-0036-1596552

Cited by 3 publications

(3 citation statements)

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“…In the T98G cell line, the cytotoxic effects of evernic acid were observed only for the highest tested concentration (100 µM). Shcherbakova et al found that the U-87 GBM cell line was sensitive to evernic acid, but also to E. prunastri extract [43]. In our study, the treatment with E. prunastri extract dose-dependently reduced the number of living cells.…”

Section: Discussionsupporting

confidence: 62%

Lichen-Derived Compounds and Extracts as Biologically Active Substances with Anticancer and Neuroprotective Properties

et al. 2021

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Lichens are a source of chemical compounds with valuable biological properties, structurally predisposed to penetration into the central nervous system (CNS). Hence, our research aimed to examine the biological potential of lipophilic extracts of Parmelia sulcata, Evernia prunastri, Cladonia uncialis, and their major secondary metabolites, in the context of searching for new therapies for CNS diseases, mainly glioblastoma multiforme (GBM). The extracts selected for the study were standardized for their content of salazinic acid, evernic acid, and (−)-usnic acid, respectively. The extracts and lichen metabolites were evaluated in terms of their anti-tumor activity, i.e., cytotoxicity against A-172 and T98G cell lines and anti-IDO1, IDO2, TDO activity, their anti-inflammatory properties exerted by anti-COX-2 and anti-hyaluronidase activity, antioxidant activity, and anti-acetylcholinesterase and anti-butyrylcholinesterase activity. The results of this study indicate that lichen-derived compounds and extracts exert significant cytotoxicity against GBM cells, inhibit the kynurenine pathway enzymes, and have anti-inflammatory properties and weak antioxidant and anti-cholinesterase properties. Moreover, evernic acid and (−)-usnic acid were shown to be able to cross the blood-brain barrier. These results demonstrate that lichen-derived extracts and compounds, especially (−)-usnic acid, can be regarded as prototypes of pharmacologically active compounds within the CNS, especially suitable for the treatment of GBM.

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Section: Discussionsupporting

confidence: 62%

Lichen-Derived Compounds and Extracts as Biologically Active Substances with Anticancer and Neuroprotective Properties

et al. 2021

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“…The extracts with the highest activity against both growing biofilms and 24 h old biofilms, E. prunastri and R. fastigiata , were dominated by the presence of the previously-mentioned evernic acid [ 29 , 30 ]. E. prunastri and evernic acid have already been studied for their antiproliferative and antimicrobial activities [ 31 , 32 ]. In a recent publication, the effect of evernic acid on bacterial biofilm has been evaluated and this depside has demonstrated a capacity to inhibit Pseudomonas aeruginosa quorum sensing systems [ 33 ].…”

Section: Resultsmentioning

confidence: 99%

Antifungal and Anti-Biofilm Activities of Acetone Lichen Extracts against Candida albicans

et al. 2017

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Candida albicans is a commensal coloniser of the human gastrointestinal tract and an opportunistic pathogen, especially thanks to its capacity to form biofilms. This lifestyle is frequently involved in infections and increases the yeast resistance to antimicrobials and immune defenses. In this context, 38 lichen acetone extracts have been prepared and evaluated for their activity against C. albicans planktonic and sessile cells. Minimum inhibitory concentrations of extracts (MICs) were determined using the broth microdilution method. Anti-biofilm activity was evaluated using tetrazolium salt (XTT) assay as the ability to inhibit the maturation phase (anti-maturation) or to eradicate a preformed 24 h old biofilm (anti-biofilm). While none of the extracts were active against planktonic cells, biofilm maturation was limited by 11 of the tested extracts. Seven extracts displayed both anti-maturation and anti-biofilm activities (half maximal inhibitory concentrations IC50_mat and IC50_biof ≤ 100 µg/mL); Evernia prunastri and Ramalina fastigiata were the most promising lichens (IC50_mat < 4 µg/mL and IC50_biof < 10 µg/mL). Chemical profiles of the active extracts performed by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC) have been analyzed. Depsides, which were present in large amounts in the most active extracts, could be involved in anti-biofilm activities. This work confirmed that lichens represent a reservoir of compounds with anti-biofilm potential.

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“…Another study showed that EA extracted from Ramalina fastigiata has antioxidant capacity and an antimicrobial effect on E. coli [ 16 ]. Others reported EA inhibits the proliferations of U-87 human glioblastoma cells and HeLa cells (a cervical cancer cell line) [ 17 , 18 ]. However, only one study has reported that it has a protective effect on U373-MG glioblastoma and SH-SY5Y neuroblastoma cells [ 13 ], and to date, no report has been issued on its neuroprotective effects in the presence of the neurodegenerative disease.…”

Section: Introductionmentioning

confidence: 99%

Neuroprotective and Anti-Inflammatory Effects of Evernic Acid in an MPTP-Induced Parkinson’s Disease Model

Lee

Suh

Yang

et al. 2021

IJMS

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Oxidative stress, mitochondrial dysfunction, and neuroinflammation are strongly associated with the pathogenesis of Parkinson’s disease (PD), which suggests that anti-oxidative and anti-inflammatory compounds might provide an alternative treatment for PD. Here, we evaluated the neuroprotective effects of evernic aid (EA), which was screened from a lichen library provided by the Korean Lichen Research Institute at Sunchon National University. EA is a secondary metabolite generated by lichens, including Ramalina, Evernia, and Hypogymnia, and several studies have described its anticancer, antifungal, and antimicrobial effects. However, the neuroprotective effects of EA have not been studied. We found that EA protected primary cultured neurons against 1-methyl-4-phenylpyridium (MPP+)-induced cell death, mitochondrial dysfunction, and oxidative stress, and effectively reduced MPP+-induced astroglial activation by inhibiting the NF-κB pathway. In vivo, EA ameliorated MPTP-induced motor dysfunction, dopaminergic neuronal loss, and neuroinflammation in the nigrostriatal pathway in C57BL/6 mice. Taken together, our findings demonstrate that EA has neuroprotective and anti-inflammatory effects in PD models and suggest that EA is a potential therapeutic candidate for PD.

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Screening of compounds of Evernia prunastri (L.) for their antiproliferative activity in glioblastoma cells

Cited by 3 publications

References 0 publications

Lichen-Derived Compounds and Extracts as Biologically Active Substances with Anticancer and Neuroprotective Properties

Lichen-Derived Compounds and Extracts as Biologically Active Substances with Anticancer and Neuroprotective Properties

Antifungal and Anti-Biofilm Activities of Acetone Lichen Extracts against Candida albicans

Neuroprotective and Anti-Inflammatory Effects of Evernic Acid in an MPTP-Induced Parkinson’s Disease Model

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