PPARγ Agonistic Activity of Mimulone and Diplacone Encapsulated in Liposomes and Cyclodextrin Complexes

Kód výsledku v 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>

Nalezeny alternativní kódy

RIV/00216224:14160/25:00143932

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

PPARγ Agonistic Activity of Mimulone and Diplacone Encapsulated in Liposomes and Cyclodextrin Complexes

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

PPARγ Agonistic Activity of Mimulone and Diplacone Encapsulated in Liposomes and Cyclodextrin Complexes

Popis výsledku anglicky

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.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

30104 - Pharmacology and pharmacy

Projekt

<a href="/cs/project/GA22-03187S" target="_blank" >GA22-03187S: Racionální design částicových polysacharidových systémů pro přívod léčiv s širokým spekterem biologické aktivity k terapii sliznic</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2025

Kód důvěrnosti údajů

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

Název periodika

ChemistryOpen

ISSN

2191-1363

e-ISSN

2191-1363

Svazek periodika

14

Číslo periodika v rámci svazku

12

Stát vydavatele periodika

DE - Spolková republika Německo

Počet stran výsledku

12

Strana od-do

"e202500209"

Kód UT WoS článku

001542920500001

EID výsledku v databázi Scopus

2-s2.0-105012191749