ArticleAtherosclerosis2011
Leoligin, the major lignan from Edelweiss, activates cholesteryl ester transfer protein.
Article in Atherosclerosis, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
15 citing papers in PubMed, 42 citations in OpenAlex.
- Identification of a novel oral potential multiple agonist for obesity treatment: multi-target in silico study.Journal of computer-aided molecular design · 2026Article
- Hairy Roots as Producers of Coumarins, Lignans, and Xanthones.Molecules (Basel, Switzerland) · 2025Review
- Nanodelivery of Bioactive Natural Products: A Targeted Therapeutic Breakthrough for Atherosclerosis.Pharmaceutics · 2025Review
- Identification and Characterization of a Leoligin-Inspired Synthetic Lignan as a TGR5 Agonist.Journal of natural products · 2025Article
- Cholesterol-Lowering Phytochemicals: Targeting the Mevalonate Pathway for Anticancer Interventions.Frontiers in genetics · 2022Review
- Bioactivity of Dietary Polyphenols: The Role in LDL-C Lowering.Foods (Basel, Switzerland) · 2021Review
- Leoligin-inspired synthetic lignans with selectivity for cell-type and bioactivity relevant for cardiovascular disease.Chemical science · 2019Article
- Leoligin, the Major Lignan from Edelweiss (Leontopodium nivale subsp. alpinum), Promotes Cholesterol Efflux from THP-1 Macrophages.Journal of natural products · 2016Article
- Pharmacophore Models and Pharmacophore-Based Virtual Screening: Concepts and Applications Exemplified on Hydroxysteroid Dehydrogenases.Molecules (Basel, Switzerland) · 2015Review
- Discovery and resupply of pharmacologically active plant-derived natural products: A review.Biotechnology advances · 2015Review
- Accessing biological actions of Ganoderma secondary metabolites by in silico profiling.Phytochemistry · 2015Review
- Article
- Virtual screening as a strategy for the identification of xenobiotics disrupting corticosteroid action.PloS one · 2012Article
- Clinical and Radiographic Evaluation of Locally Delivered Plant Stem Cells for Treatment of Periodontitis: Randomized Clinical Trial.Contemporary clinical dentistryArticle
- Drugs from nature targeting inflammation (DNTI): a successful Austrian interdisciplinary network project.Monatshefte fur chemieReview
Corrections and comments
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Authors and funding
14 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
objectiveCholesteryl ester transfer protein (CETP) plays a central role in the metabolism of high-density lipoprotein particles. Therefore, we searched for new drugs that bind to CETP and modulate its activity.
methodsA preliminary pharmacophore-based parallel screening approach indicated that leoligin, a major lignan of Edelweiss (Leontopodium alpinum Cass.), might bind to CETP. Therefore we incubated leoligin ex vivo at different concentrations with human (n=20) and rabbit plasma (n=3), and quantified the CETP activity by fluorimeter. Probucol served as positive control. Furthermore, we dosed CETP transgenic mice with leoligin and vehicle control by oral gavage for 7 days and measured subsequently the in vivo modulation of CETP activity (n=5 for each treatment group).
resultsIn vitro, leoligin significantly activated CETP in human plasma at 100 pM (p=0.023) and 1 nM (p=0.042), respectively, whereas leoligin concentrations of 1 mM inhibited CETP activity (p=0.012). The observed CETP activation was not species specific, as it was similar in magnitude for rabbit CETP. In vivo, there was also a higher CETP activity after oral dosage of CETP transgenic mice with leoligin (p=0.015). There was no short-term toxicity apparent in mice treated with leoligin.
conclusionCETP agonism by leoligin appears to be safe and effective, and may prove to be a useful modality to alter high-density lipoprotein metabolism.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.