Details
| Original language | English |
|---|---|
| Article number | e37713 |
| Journal | Heliyon |
| Volume | 10 |
| Issue number | 22 |
| Early online date | 13 Sept 2024 |
| Publication status | Published - 30 Nov 2024 |
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.
Keywords
- Bioactivity, Cytotoxicity, Erythropoietin, Proliferation, Synthetic biology, Tropolone sesquiterpenoids
ASJC Scopus subject areas
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In: Heliyon, Vol. 10, No. 22, e37713, 30.11.2024.
Research output: Contribution to journal › Article › Research › peer review
}
TY - JOUR
T1 - Cytotoxic and proliferation-inhibitory activity of natural and synthetic fungal tropolone sesquiterpenoids in various cell lines
AU - Bergmann, Timna C.
AU - Menssen, Max
AU - Schotte, Carsten
AU - Cox, Russell J.
AU - Lee-Thedieck, Cornelia
N1 - Publisher Copyright: © 2024 The Authors
PY - 2024/11/30
Y1 - 2024/11/30
N2 - 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.
AB - 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.
KW - Bioactivity
KW - Cytotoxicity
KW - Erythropoietin
KW - Proliferation
KW - Synthetic biology
KW - Tropolone sesquiterpenoids
UR - http://www.scopus.com/inward/record.url?scp=85208460020&partnerID=8YFLogxK
U2 - 10.1016/j.heliyon.2024.e37713
DO - 10.1016/j.heliyon.2024.e37713
M3 - Article
AN - SCOPUS:85208460020
VL - 10
JO - Heliyon
JF - Heliyon
SN - 2405-8440
IS - 22
M1 - e37713
ER -