Cytotoxic and proliferation-inhibitory activity of natural and synthetic fungal tropolone sesquiterpenoids in various cell lines
Year: 2024
Type: article
Abstract: Fungal specialized metabolites are known for their potent biological activities, among which tropolone sesquiterpenoids (TS) stand out for their diverse bioactivities. Here, we report cytotoxic and proliferation inhibitory effects of the recently discovered TS compounds 4-hydroxyxenovulene B and 4-dihydroxy norpycnidione, and the structurally related 4-hydroxy norxenovulene B and xenovulene B. Inhibition of metabolic activity after TS treatment was observed in Jurkat, PC-3 and FAIK3-5 cells, whereas MDA-MB-231 cells were unresponsive to treatment. Structurally similar epolones were shown to induce erythropoietin (EPO). Therefore, FAIK3-5 cells, which can naturally produce EPO, were applied to test the compounds in this regard. While no effect on EPO production in FAIK3-5 cells could be demonstrated, effects on their proliferation, viability, and morphology were observed depending on the presence of tropolone moieties in the molecules. Our study underlines the importance of relevant cell models for bioactivity testing of compounds with unknown mechanisms of action.
Source: Heliyon
Institution: Leibniz University Hannover
Language: English
Subfield: Pharmacology
Field: Medicine
Domain: Health Sciences
Open Access status: gold
Estimated APC paid: $2,100
Funders: Niedersächsische Ministerium für Wissenschaft und Kultur, European Commission, Ministerium für Wissenschaft, Forschung und Kunst Baden-Württemberg, Gottfried Wilhelm Leibniz Universität Hannover, Technische Universität Braunschweig, Horizon 2020 Framework Programme, European Research Council, Leibniz-Gemeinschaft, Horizon 2020, H2020 European Research Council
OpenAlex ID: W4402512495