Effects of quercetin and artemetin prenylation on bioavailability and bioactivity

Salamone, Stefano; Nieddu, Mariella; Khalili, Adil; Sansaro, Andrea; Bombardelli, Ezio; Rosa, Antonella; Pollastro, Federica

doi:10.1016/j.chemphyslip.2021.105137

Cited by 7 publications

(27 citation statements)

References 22 publications

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“…As reported by Salamone et al (2021) , ART and 8-p-ART were able to affect HeLa cell viability at concentrations higher than 25 µM after 72 h of incubation. Our preliminary results reported in Supplementary Figure S1 are fully in line with those reported in Salamone et al (2021 ). Moreover, both compounds changed the cell lipid composition, thus affecting the lipid metabolism which is recognized as a novel anti-cancer target.…”

Section: Introductionsupporting

confidence: 71%

“…This was the first potential target disclosed for ART even though it was found by indirect evidence such as the modulation of microtubule depolymerization. Thus, encouraged by the results obtained on HeLa cells considering ART and 8-p-ART as promising anti-cancer compounds ( Salamone et al, 2021 ; Rosa et al, 2022 ), we moved to identify filamins as more reliable targets using an unbiased approach.…”

Section: Discussionmentioning

confidence: 99%

“…Moreover, both compounds changed the cell lipid composition, thus affecting the lipid metabolism which is recognized as a novel anti-cancer target. Moreover, phase-contrast images of HeLa cells after 72-h treatment with both molecules showed some changes in the cell morphology compared to control cells, mainly in terms of cell elongation ( Salamone et al, 2021 ). Thus, since it was demonstrated that the prenylation hardly enlarged the cytotoxic effect in cancer HeLa cells, and also increasing the alteration of cell phospholipid and fatty acid composition, the 8-p-ART isomer has also been tested here in comparison with ART in cell assays.…”

Section: Introductionmentioning

confidence: 99%

“…However, ART targets in cancer cells have not been truly recognized, and thus we moved to investigate its complete interactome in HeLa cell lysates. It has been recently reported Frontiers in Molecular Biosciences frontiersin.org that eupatilin, a chemical analog of ART, showed a cytotoxic effect on cancer HeLa cells (Rosa et al, 2020) and the effect of ART and 8-prenylated-artemetin (8-p-ART, Figure 1B) has been investigated on this cell line (Salamone et al, 2021). As reported by Salamone et al (2021), ART and 8-p-ART were able to affect HeLa cell viability at concentrations higher than 25 µM after 72 h of incubation.…”

Section: Introductionmentioning

confidence: 99%

“…It has been recently reported Frontiers in Molecular Biosciences frontiersin.org that eupatilin, a chemical analog of ART, showed a cytotoxic effect on cancer HeLa cells (Rosa et al, 2020) and the effect of ART and 8-prenylated-artemetin (8-p-ART, Figure 1B) has been investigated on this cell line (Salamone et al, 2021). As reported by Salamone et al (2021), ART and 8-p-ART were able to affect HeLa cell viability at concentrations higher than 25 µM after 72 h of incubation. Our preliminary results reported in Supplementary Figure S1 are fully in line with those reported in Salamone et al (2021).…”

Section: Introductionmentioning

confidence: 99%

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Drug affinity-responsive target stability unveils filamins as biological targets for artemetin, an anti-cancer flavonoid

Ferraro

Belvedere

Petrella

et al. 2022

Front. Mol. Biosci.

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Artemetin is a valuable 5-hydroxy-3,6,7,3′,4′-pentamethoxyflavone present in many different medicinal plants with very good oral bioavailability and drug-likeness values, owing to numerous bioactivities, such as anti-inflammatory and anti-cancer ones. Here, a multi-disciplinary plan has been settled and applied for identifying the artemetin target(s) to inspect its mechanism of action, based on drug affinity-responsive target stability and targeted limited proteolysis. Both approaches point to the disclosure of filamins A and B as direct artemetin targets in HeLa cell lysates, also giving detailed insights into the ligand/protein-binding sites. Interestingly, also 8-prenyl-artemetin, which is an artemetin more permeable semisynthetic analog, directly interacts with filamins A and B. Both compounds alter filamin conformation in living HeLa cells with an effect on cytoskeleton disassembly and on the disorganization of the F-actin filaments. Both the natural compound and its derivative are able to block cell migration, expectantly acting on tumor metastasis occurrence and development.

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Section: Introductionsupporting

confidence: 71%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Drug affinity-responsive target stability unveils filamins as biological targets for artemetin, an anti-cancer flavonoid

Ferraro

Belvedere

Petrella

et al. 2022

Front. Mol. Biosci.

Self Cite

View full text Add to dashboard Cite

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Fatty Acid Ratios as Parameters to Discriminate Between Normal and Tumoral Cells and Compare Drug Treatments in Cancer Cells

Rosa

Nieddu

Pollastro

et al. 2023

Euro J Lipid Sci & Tech

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The fatty acid (FA) composition of cell membranes represents a metabolic biomarker. However, the FA profile reproducibility in cell cultures remains a significant challenge. In this study, cell FA ratios are validated as metabolic markers alternative to cell FA. To this goal, cell samples belonging to cancer HeLa cells and normal 3T3 fibroblasts, from various experimental sets, are analyzed by a high‐performance liquid chromatography system coupled with a photodiode array detector and evaporative light scattering detector (HPLC‐DAD/ELSD), and the ratios among the main FA are calculated. Principal component analysis (PCA) separately performed on FA and FA ratio data indicates similar clustering of cell samples concerning the cell type. Moreover, similar scores values t[1] and t[2] and graphical distances are calculated in the PCA plots separately performed on FA and FA ratios measured in cancer HeLa cells subjected to various antitumoral compounds. Last, PCA applied to selected FA ratios measured in various cell lines, obtained in similar experimental conditions, allows to discriminate between normal and tumoral cells. The results substantiate FA ratios as a cell‐specific fingerprint, characterized by reproducibility across intra‐laboratory conditions, useful for cell characterization, discrimination between normal and tumoral cells, and the comparison of different drug treatments. Practical Applications: The reproducibility of the fatty acid (FA) profile in cell cultures remains a significant challenge. Results obtained from this study improve knowledge about the role of the FA ratio profile as a cell‐specific fingerprint characterized by reproducibility across intra‐laboratory conditions. The characterization of the specific FA ratio profile of a cell culture, under standardized experimental conditions, can facilitate the comparative evaluation of cell data sets for nutritional, metabolic, and pharmacological studies, overcoming differences in cell culture conditions and FA extraction/analytical procedures.

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Kaempferol, a potential neuroprotective agent in neurodegenerative diseases: From chemistry to medicine

Jin

Zhang

Wang

2023

Biomedicine & Pharmacotherapy

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Effects of quercetin and artemetin prenylation on bioavailability and bioactivity

Cited by 7 publications

References 22 publications

Drug affinity-responsive target stability unveils filamins as biological targets for artemetin, an anti-cancer flavonoid

Drug affinity-responsive target stability unveils filamins as biological targets for artemetin, an anti-cancer flavonoid

Fatty Acid Ratios as Parameters to Discriminate Between Normal and Tumoral Cells and Compare Drug Treatments in Cancer Cells

Kaempferol, a potential neuroprotective agent in neurodegenerative diseases: From chemistry to medicine

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