Leoligin, the Major Lignan from Edelweiss (Leontopodium nivale subsp. alpinum), Promotes Cholesterol Efflux from THP-1 Macrophages
Jazyk angličtina Země Spojené státy americké Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
27220065
PubMed Central
PMC4924082
DOI
10.1021/acs.jnatprod.6b00227
Knihovny.cz E-zdroje
- MeSH
- ABC transportéry metabolismus MeSH
- Asteraceae chemie MeSH
- ateroskleróza MeSH
- biologický transport MeSH
- daktinomycin farmakologie MeSH
- lidé MeSH
- lignany chemie izolace a purifikace farmakologie MeSH
- makrofágy metabolismus MeSH
- messenger RNA metabolismus MeSH
- molekulární struktura MeSH
- oxaziny metabolismus MeSH
- polymerázová řetězová reakce MeSH
- sirotčí receptory metabolismus MeSH
- western blotting MeSH
- xantheny metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- ABC transportéry MeSH
- daktinomycin MeSH
- leoligin MeSH Prohlížeč
- lignany MeSH
- messenger RNA MeSH
- oxaziny MeSH
- resazurin MeSH Prohlížeč
- sirotčí receptory MeSH
- xantheny MeSH
Leoligin is a natural lignan found in Edelweiss (Leontopodium nivale ssp. alpinum). The aim of this study was to examine its influence on cholesterol efflux and to address the underlying mechanism of action. Leoligin increases apo A1- as well as 1% human plasma-mediated cholesterol efflux in THP-1 macrophages without affecting cell viability as determined by resazurin conversion. Western blot analysis revealed that the protein levels of the cholesterol efflux transporters ABCA1 and ABCG1 were upregulated, whereas the SR-B1 protein level remained unchanged upon treatment with leoligin (10 μM, 24 h). Quantitative reverse transcription PCR further uncovered that leoligin also increased ABCA1 and ABCG1 mRNA levels without affecting the half-life of the two mRNAs in the presence of actinomycin D, a transcription inhibitor. Proteome analysis revealed the modulation of protein expression fingerprint in the presence of leoligin. Taken together, these results suggest that leoligin induces cholesterol efflux in THP-1-derived macrophages by upregulating ABCA1 and ABCG1 expression. This novel activity suggests leoligin as a promising candidate for further studies addressing a possible preventive or therapeutic application in the context of atherosclerosis.
Department of Pharmacognosy University of Vienna Vienna Austria
Institute of Applied Synthetic Chemistry Vienna University of Technology Vienna Austria
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The Forty-Sixth Euro Congress on Drug Synthesis and Analysis: Snapshot †
