Planta Med 2019; 85(18): 1411
DOI: 10.1055/s-0039-3399692
Abstracts of Short Lectures
Short Lectures Monday, September 02, 2019
Short Lectures C: Biological and Pharmacological Activities of Natural Products
© Georg Thieme Verlag KG Stuttgart · New York

Sesquiterpene lactones from Siegesbeckia orientalis inhibit pro-inflammatory functions of human neutrophils

NS Engels
1   University of Innsbruck,, Institute of Pharmacy/ Pharmacognosy and Center for Molecular Biosciences Innsbruck (CMBI), Innrain 80-82, 6020 Innsbruck, Austria
,
B Waltenberger
1   University of Innsbruck,, Institute of Pharmacy/ Pharmacognosy and Center for Molecular Biosciences Innsbruck (CMBI), Innrain 80-82, 6020 Innsbruck, Austria
,
B Michalak
2   Medical University of Warsaw,, Department of Pharmacognosy and Molecular Basis of Phytotherapy, Faculty of Pharmacy, Banacha 1, 02-097 Warsaw, Poland
,
F-R Chang
3   Kaohsiung Medical University,, Department of Pharmacognosy, Faculty of Pharmacy, 80708 Kaohsiung, Taiwan
,
AK Kiss
2   Medical University of Warsaw,, Department of Pharmacognosy and Molecular Basis of Phytotherapy, Faculty of Pharmacy, Banacha 1, 02-097 Warsaw, Poland
,
H Stuppner
1   University of Innsbruck,, Institute of Pharmacy/ Pharmacognosy and Center for Molecular Biosciences Innsbruck (CMBI), Innrain 80-82, 6020 Innsbruck, Austria
› Author Affiliations
Further Information

Publication History

Publication Date:
20 December 2019 (online)

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Siegesbeckia orientalis (Asteraceae), more commonly referred to as hy thiêm in traditional Vietnamese medicine (TVM), is used in Vietnam to treat arthritis, rheumatism, and gout [1]. In an initial screening of extracts from plants used in traditional Vietnamese medicine, the dichloromethane (DCM) extract from the aerial parts of Siegesbeckia orientalis showed distinct inhibitory effects on the release of interleukin (IL)-8 in human neutrophils.

The phytochemical investigation of the bioactive Siegesbeckia orientalis DCM extract led to the isolation of nine compounds. One diterpene, 17(13→14)-abeo-ent-3S*,13S*,16-trihydroxystrob-8(15)-ene, was identified as a new natural product.

The isolated compounds were tested in vitro to evaluate their effects on the pro-inflammatory functions of stimulated human neutrophils: IL-8, IL-1β, tumor necrosis factor (TNF-α), and monocyte chemoattractant protein 1 (MCP-1) release, reactive oxygen species (ROS) generation, and expression of adhesion molecules (CD11a, CD11b, and CD62L).

Four sesquiterpene lactones inhibited IL-8 production with IC50 values between 0.7 and 6.3 µM, and TNF-α production with IC50 values between 18.2 and 31.9 µM, respectively. Furthermore, they significantly inhibited IL-1β, ROS, and MCP-1 production and decreased the expression of the adhesion molecules CD11a, CD11b, and CD62L.

In conclusion, the bioactivity of the DCM extract could be traced back to the presence of sesquiterpene lactones, which seem to interact with several potential therapeutic pathways including the NF-κB pathway, a key regulator of inflammation in rheumatoid arthritis [2]. Therefore, these findings support the traditional use of Siegesbeckia orientalis in the treatment of joint pain and rheumatism.

 

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