Pharmacological insight into the anti-inflammatory activity of sesquiterpene lactones from Neurolaena lobata (L.) R.Br. ex Cass

R. McKinnon, M. Binder, I. Zupkó, T. Afonyushkin, I. Lajter, A. Vasas, R. De Martin, C. Unger, H. Dolznig, R. Diaz, R. Frisch, C. M. Passreiter, G. Krupitza, J. Hohmann, B. Kopp, V. N. Bochkov

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16 Citations (Scopus)

Abstract

Purpose: Neurolaena lobata is a Caribbean medicinal plant used for the treatment of several conditions including inflammation. Recent data regarding potent anti-inflammatory activity of the plant and isolated sesquiterpene lactones raised our interest in further pharmacological studies. The present work aimed at providing a mechanistic insight into the anti-inflammatory activity of N. lobata and eight isolated sesquiterpene lactones, as well as a structure-activity relationship and in vivo anti-inflammatory data.

Methods: The effect of the extract and its compounds on the generation of pro-inflammatory proteins was assessed in vitro in endothelial and monocytic cells by enzyme-linked immunosorbent assay. Their potential to modulate the expression of inflammatory genes was further studied at the mRNA level. In vivo anti-inflammatory activity of the chemically characterized extract was evaluated using carrageenan-induced paw edema model in rats.

Results: The compounds and extract inhibited LPS- and TNF-α-induced upregulation of the pro-inflammatory molecules E-selectin and interleukin-8 in HUVECtert and THP-1 cells. LPS-induced elevation of mRNA encoding for E-selectin and interleukin-8 was also suppressed. Furthermore, the extract inhibited the development of acute inflammation in rats.

Conclusions: Sesquiterpene lactones from N. lobata interfered with the induction of inflammatory cell adhesion molecules and chemokines in cells stimulated with bacterial products and cytokines. Structure-activity analysis revealed the importance of the double bond at C-4-C-5 and C-2-C-3 and the acetyl group at C-9 for the anti-inflammatory activity. The effect was confirmed in vivo, which raises further interest in the therapeutic potential of the compounds for the treatment of inflammatory diseases.

Original languageEnglish
Pages (from-to)1695-1701
Number of pages7
JournalPhytomedicine
Volume21
Issue number12
DOIs
Publication statusPublished - Oct 15 2014

Keywords

  • Anti-inflammatory
  • Chemokines
  • Natural products
  • Neurolaena lobata
  • Sesquiterpene lactones

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine

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  • Cite this

    McKinnon, R., Binder, M., Zupkó, I., Afonyushkin, T., Lajter, I., Vasas, A., De Martin, R., Unger, C., Dolznig, H., Diaz, R., Frisch, R., Passreiter, C. M., Krupitza, G., Hohmann, J., Kopp, B., & Bochkov, V. N. (2014). Pharmacological insight into the anti-inflammatory activity of sesquiterpene lactones from Neurolaena lobata (L.) R.Br. ex Cass. Phytomedicine, 21(12), 1695-1701. https://doi.org/10.1016/j.phymed.2014.07.019