PPARγ Agonistic Activity of Mimulone and Diplacone Encapsulated in Liposomes and Cyclodextrin Complexes
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00027162%3A_____%2F25%3AN0000146" target="_blank" >RIV/00027162:_____/25:N0000146 - isvavai.cz</a>
Alternative codes found
RIV/00216224:14160/25:00143932
Result on the web
<a href="https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/open.202500209" target="_blank" >https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/open.202500209</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1002/open.202500209" target="_blank" >10.1002/open.202500209</a>
Alternative languages
Result language
angličtina
Original language name
PPARγ Agonistic Activity of Mimulone and Diplacone Encapsulated in Liposomes and Cyclodextrin Complexes
Original language description
The therapeutic application of flavonoids is limited by their low solubility, bioavailability, and metabolic stability. This study evaluates the peroxisome proliferator-activated receptor gamma (PPARγ) agonistic activity of two geranylated flavonoids from Paulownia tomentosa, mimulone and diplacone, and compares the efficacy of different nanoparticle delivery systems, including liposomes and cyclodextrins, in preserving their biological activity. Using the PPARγ CALUX reporter gene assay, it is shown that mimulone dissolved in DMSO and incubated with cell culture activates the PPARγ pathway, resulting in 2.97-fold and 3.9-fold increases in luciferase activity at concentrations of 5 and 2.5 μM, respectively. Diplacone, however, shows significant cytotoxicity, with an average cell viability of about 10% at 10 μM. Encapsulation in anionic, cationic, and neutral liposomes results in a significant reduction of biological activity of both flavonoids, with the best formulation (anionic liposomes) preserving only 54% of mimulone's activity. In contrast, hydroxypropyl-β-cyclodextrins (HP-β-CDs) retain up to 91.5% of mimulone's biological activity and significantly improve the viability profile of diplacone, maintaining cell viability at ≈100%. The performance of the HP-β-CDs can be attributed to their ability to form stable inclusion complexes with hydrophobic molecules. These results suggest that cyclodextrin-based delivery systems might effectively address solubility and stability challenges associated with flavonoid therapy.
Czech name
—
Czech description
—
Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
—
OECD FORD branch
30104 - Pharmacology and pharmacy
Result continuities
Project
<a href="/en/project/GA22-03187S" target="_blank" >GA22-03187S: Rational Design of Polysaccharide‐based Particulate Systems for the Delivery of Mucosal Therapeutics with Broad Spectrum of Biological Activities</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2025
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
ChemistryOpen
ISSN
2191-1363
e-ISSN
2191-1363
Volume of the periodical
14
Issue of the periodical within the volume
12
Country of publishing house
DE - GERMANY
Number of pages
12
Pages from-to
"e202500209"
UT code for WoS article
001542920500001
EID of the result in the Scopus database
2-s2.0-105012191749