Pharmacological activities of sesquiterpene lactone trilobolide and its conjugates as promising compounds for anticancer and immunomodulatory therapies

0534702 - ÚOCHB 2021 JP eng A - Abstract
Kmoníčková, Eva - Rimpelová, S. - Jurášek, M. - Džubák, P. - Sedlák, D. - Zídek, Zdeněk - Harmatha, Juraj - Drašar, P.
Pharmacological activities of sesquiterpene lactone trilobolide and its conjugates as promising compounds for anticancer and immunomodulatory therapies.
Proceedings for Annual Meeting of The Japanese Pharmacological Society WCP2018. Tokyo: Japanese Pharmacological Society, 2018. „OR34-3“.
[World Congress of Basic and Clinical Pharmacology /18./. 01.07.2018-06.07.2018, Kyoto]
Institutional support: RVO:61388963
Keywords : SERCA inhibitor * cancer * cytokines
OECD category: Medicinal chemistry
https://doi.org/10.1254/jpssuppl.WCP2018.0_OR34-3

Trilobolide and its conjugates exhibited sufficient intracellular accumulation and specific localization. Cytotoxic effects were observed in submicromolar concentrations in some drug-resistant cancer cell lines. Trilobolide is less toxic for fibroblasts and macrophages. Specific immunostimulatory effect (NO production, IFN-gamma, IL-2 secretion) of trilobolides is dose- and structure-dependent. Trilobolide-porphyrin conjugates with low toxicity, represent an interesting tool for photodynamic therapy. In summary, trilobolide and its conjugates could be a useful tool in anti-cancer, anti-infectious and immunomodulatory therapies.
Permanent Link: http://hdl.handle.net/11104/0313470