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BODIPY-based fluorescent liposomes with sesquiterpene lactone trilobolide
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SYSNO ASEP 0476521 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title BODIPY-based fluorescent liposomes with sesquiterpene lactone trilobolide Author(s) Škorpilová, Ludmila (UEB-Q)
Rimpelová, S. (CZ)
Jurášek, M. (CZ)
Buděšínský, Miloš (UOCHB-X) RID, ORCID
Lokajová, Jana (UOCHB-X)
Effenberg, R. (CZ)
Slepička, P. (CZ)
Ruml, T. (CZ)
Kmoníčková, Eva (UEM-P) RID
Drašar, P. B. (CZ)
Wimmer, Zdeněk (UEB-Q) RID, ORCIDNumber of authors 11 Source Title Beilstein Journal of Organic Chemistry. - : Beilstein - Institut zur Foerderung der Chemischen Wissenschaften - ISSN 1860-5397
Roč. 13, JUL 4 (2017), s. 1316-1324Number of pages 9 s. Language eng - English Country DE - Germany Keywords BODIPY conjugates ; Cancer targeting ; Drug delivery ; Liposomes ; Natural compounds ; Sesquiterpene lactone trilobolide Subject RIV CC - Organic Chemistry OECD category Organic chemistry Subject RIV - cooperation Institute of Experimental Medicine - Pharmacology ; Medidal Chemistry R&D Projects LD15012 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) LO1304 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Institutional support UEB-Q - RVO:61389030 ; UOCHB-X - RVO:61388963 ; UEM-P - RVO:68378041 UT WOS 000405427300001 EID SCOPUS 85023616975 DOI 10.3762/bjoc.13.128 Annotation Like thapsigargin, which is undergoing clinical trials, trilobolide is a natural product with promising anticancer and anti-inflammatory properties. Similar to thapsigargin, it has limited aqueous solubility that strongly reduces its potential medicinal applications. The targeted delivery of hydrophobic drugs can be achieved using liposome-based carriers. Therefore, we designed a traceable liposomal drug delivery system for trilobolide. The fluorescent green-emitting dye BODIPY, cholesterol and trilobolide were used to create construct 6. The liposomes were composed of dipalmitoyl-3-trimethylammoniumpropane and phosphatidylethanolamine. The whole system was characterized by atomic force microscopy, the average size of the liposomes was 150 nm in width and 30 nm in height. We evaluated the biological activity of construct 6 and its liposomal formulation, both of which showed immunomodulatory properties in primary rat macrophages. The uptake and intracellular distribution of construct 6 and its liposomal formulation was monitored by means of live-cell fluorescence microscopy in two cancer cell lines. The encapsulation of construct 6 into the liposomes improved the drug distribution in cancer cells and was followed by cell death. This new liposomal trilobolide derivative not only retains the biological properties of pure trilobolide, but also enhances the bioavailability, and thus has potential for the use in theranostic applications. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2018
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