Please use this identifier to cite or link to this item: doi:10.22028/D291-27503
Title: Triterpene Acids from Frankincense and Semi-Synthetic Derivatives That Inhibit 5-Lipoxygenase and Cathepsin G
Author(s): Koeberle, Andreas
Henkel, Arne
Verhoff, Moritz
Tausch, Lars
König, Stefanie
Fischer, Dagmar
Kather, Nicole
Seitz, Stefanie
Paul, Michael
Jauch, Johann
Werz, Oliver
Language: English
Title: Molecules
Volume: 23
Issue: 2
Publisher/Platform: MDPI
Year of Publication: 2018
DDC notations: 540 Chemistry
Publikation type: Journal Article
Abstract: Age-related diseases, such as osteoarthritis, Alzheimer’s disease, diabetes, and cardiovascular disease, are often associated with chronic unresolved inflammation. Neutrophils play central roles in this process by releasing tissue-degenerative proteases, such as cathepsin G, as well as pro-inflammatory leukotrienes produced by the 5-lipoxygenase (5-LO) pathway. Boswellic acids (BAs) are pentacyclic triterpene acids contained in the gum resin of the anti-inflammatory remedy frankincense that target cathepsin G and 5-LO in neutrophils, and might thus represent suitable leads for intervention with age-associated diseases that have a chronic inflammatory component. Here, we investigated whether, in addition to BAs, other triterpene acids from frankincense interfere with 5-LO and cathepsin G. We provide a comprehensive analysis of 17 natural tetra- or pentacyclic triterpene acids for suppression of 5-LO product synthesis in human neutrophils. These triterpene acids were also investigated for their direct interference with 5-LO and cathepsin G in cell-free assays. Furthermore, our studies were expanded to 10 semi-synthetic BA derivatives. Our data reveal that besides BAs, several tetra- and pentacyclic triterpene acids are effective or even superior inhibitors of 5-LO product formation in human neutrophils, and in parallel, inhibit cathepsin G. Their beneficial target profile may qualify triterpene acids as anti-inflammatory natural products and pharmacological leads for intervention with diseases related to aging.
DOI of the first publication: 10.3390/molecules23020506
Link to this record: urn:nbn:de:bsz:291--ds-275038
ISSN: 1420-3049
Date of registration: 30-Jan-2020
Faculty: NT - Naturwissenschaftlich- Technische Fakultät
Department: NT - Chemie
Professorship: NT - Prof. Dr. Johann Jauch
Collections:SciDok - Der Wissenschaftsserver der Universität des Saarlandes

Files for this record:
File Description SizeFormat 
molecules-23-00506.pdf2,26 MBAdobe PDFView/Open

This item is licensed under a Creative Commons License Creative Commons