Next Article in Journal
Evaluating Antitumor and Antioxidant Activities of Yellow Monascus Pigments from Monascus ruber Fermentation
Next Article in Special Issue
Development of an LC–Tandem Mass Spectrometry Method for the Quantitative Analysis of Hercynine in Human Whole Blood
Previous Article in Journal
Supercritical CO2 Extraction of Eruca sativa Using Cosolvents: Phytochemical Composition by LC-MS Analysis
Previous Article in Special Issue
Ethanolic Extract of Origanum vulgare Suppresses Propionibacterium acnes-Induced Inflammatory Responses in Human Monocyte and Mouse Ear Edema Models
Article Menu

Export Article

Open AccessArticle
Molecules 2018, 23(12), 3241;

Structural Moieties Required for Cinnamaldehyde-Related Compounds to Inhibit Canonical IL-1β Secretion

Department of Food Science, Yuanpei University of Medical Technology, No. 306, Yuanpei Street, Hsinchu 300, Taiwan
Author to whom correspondence should be addressed.
Academic Editor: Arduino A. Mangoni
Received: 7 November 2018 / Revised: 2 December 2018 / Accepted: 6 December 2018 / Published: 7 December 2018
(This article belongs to the Special Issue Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry-II)
Full-Text   |   PDF [3967 KB, uploaded 7 December 2018]   |  
  |   Review Reports


Suppressing canonical NOD-like receptor protein 3 (NLRP3) inflammasome-mediated interleukin (IL)-1β secretion is a reliable strategy for the development of nutraceutical to prevent chronic inflammatory diseases. This study aimed to find out the functional group responsible for the inhibitory effects of cinnamaldehyde-related compounds on the canonical IL-1β secretion. To address this, the suppressing capacities of six cinnamaldehyde-related compounds were evaluated and compared by using the lipopolysaccharide (LPS)-primed and adenosine 5′-triphosphate (ATP)-activated macrophages. At concentrations of 25~100 μM, cinnamaldehyde and 2-methoxy cinnamaldehyde dose-dependently inhibited IL-1β secretion. In contrast, cinnamic acid, cinnamyl acetate, cinnamyl alcohol and α-methyl cinnamaldehyde did not exert any inhibition. Furthermore, cinnamaldehyde and 2-methoxy cinnamaldehyde diminished expressions of NLRP3 and pro-IL-1β. Meanwhile, cinnamaldehyde and 2-methoxy cinnamaldehyde prevented the ATP-induced reduction of cytosolic pro-caspase-1 and increase of secreted caspase-1. In conclusion, for cinnamaldehyde-related compounds to suppress NLRP3 inflammasome-mediated IL-1β secretion, the propenal group of the side chain was essential, while the substituted group of the aromatic ring played a modifying role. Cinnamaldehyde and 2-methoxy cinnamaldehyde exerted dual abilities to inhibit canonical IL-1β secretion at both stages of priming and activation. Therefore, there might be potential to serve as complementary supplements for the prevention of chronic inflammatory diseases. View Full-Text
Keywords: cinnamaldehyde; 2-methoxy cinnamaldehyde; NLRP3 inflammasome; IL-1β; sterile inflammation cinnamaldehyde; 2-methoxy cinnamaldehyde; NLRP3 inflammasome; IL-1β; sterile inflammation

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Share & Cite This Article

MDPI and ACS Style

Ho, S.-C.; Chang, Y.-H.; Chang, K.-S. Structural Moieties Required for Cinnamaldehyde-Related Compounds to Inhibit Canonical IL-1β Secretion. Molecules 2018, 23, 3241.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top