Nrf2 and VCAM-1 regulation may play a role in the anti-inflammatory mechanism of xylopic acid

Background: Xylopic acid (XA) is a kaurene diterpene which naturally exists in African plants such as Xylopia aethiopica [1]. It has been documented to exhibit acute and chronic anti-inflammatory activities [2].

Aim: The current work sets out to identify the potential molecular inflammation target(s) of xylopic acid.

Methods: Selection of targets was based on the proven bioactivity of XA as potential anti-inflammatory agent using in silico prediction tool named SPiDER [3]. Nuclear factor erythroid 2-related factor 2 (Nrf2) signaling and protein expression of Nrf2 target gene, heme oxygenase-1 (HO-1), were investigated using luciferase reporter gene assay and human umbilical vein endothelial cells (HUVEC) respectively, while effect on vascular cell adhesion molecule-1 (VCAM-1) expression was studied using HUVEC-tert cell line.

Results: XA showed enhanced activation of Nrf2 in a concentration dependent manner and slightly increased HO-1 protein expression levels. Expression of VCAM-1 was reduced to 70% in XA-treated cells.

Conclusion: XA exhibits its anti-inflammatory action via regulation of VCAM-1 and Nrf2 expression.

Fig. 1 Effect of xylopic acid on HO-1 protein expression levels in HUVEC cells. Values are mean ± SEM, n = 3. *** p < 0.001 compared to the control.

• References

• 1 Osafo N, Obiri DD, Antwi AO. et al. The acute anti-inflammatory action of xylopic acid isolated from Xylopia aethiopica. J Basic Clin Physiol Pharmacol 2018; 20180019
• 2 Osafo N, Obiri DD, Danquah KO. et al. Potential effects of xylopic acid on acetic acid-induced ulcerative colitis in rats. Turk J Gastroenterol 2019; 30 (08) 732-744
• 3 Reutlinger M, Koch CP, Reker D. et al. Chemically advanced template search (CATS) for scaffold-hopping and prospective target prediction for “orphan” molecules. Mol Inf 2013; 32: 133-138

Publication History

Article published online:
12 December 2022