BODIPY-based fluorescent liposomes with sesquiterpene lactone trilobolide

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F17%3A00476521" target="_blank" >RIV/61388963:_____/17:00476521 - isvavai.cz</a>

Alternative codes found

RIV/61389030:_____/17:00476521 RIV/68378041:_____/17:00476521 RIV/00216208:11140/17:10366002 RIV/60461373:22330/17:43913135 RIV/60461373:22310/17:43913135

Result on the web

<a href="http://dx.doi.org/10.3762/bjoc.13.128" target="_blank" >http://dx.doi.org/10.3762/bjoc.13.128</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3762/bjoc.13.128" target="_blank" >10.3762/bjoc.13.128</a>

Result language

angličtina

Original language name

BODIPY-based fluorescent liposomes with sesquiterpene lactone trilobolide

Original language description

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.

Czech name

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Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

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OECD FORD branch

10401 - Organic chemistry

Project

Result was created during the realization of more than one project. More information in the Projects tab.

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2017

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Beilstein Journal of Organic Chemistry

ISSN

1860-5397

e-ISSN

—

Volume of the periodical

13

Issue of the periodical within the volume

JUL 4

Country of publishing house

DE - GERMANY

Number of pages

9

Pages from-to

1316-1324

UT code for WoS article

000405427300001

EID of the result in the Scopus database

2-s2.0-85023616975