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

Research output: Contribution to journalArticle

13 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

Fingerprint

Sesquiterpenes
Lactones
Anti-Inflammatory Agents
Pharmacology
E-Selectin
Interleukin-8
Inflammation
Messenger RNA
Carrageenan
Cell Adhesion Molecules
Structure-Activity Relationship
Medicinal Plants
Chemokines
Edema
Up-Regulation
Therapeutics
Endothelial Cells
Enzyme-Linked Immunosorbent Assay
Cytokines
Gene Expression

Keywords

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

ASJC Scopus subject areas

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

Cite this

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

In: Phytomedicine, Vol. 21, No. 12, 15.10.2014, p. 1695-1701.

Research output: Contribution to journalArticle

McKinnon, R, Binder, M, Zupkó, I, Afonyushkin, T, Lajter, I, Vasas, A, De Martin, R, Unger, C, Dolznig, H, Diaz, R, Frisch, R, Passreiter, CM, Krupitza, G, Hohmann, J, Kopp, B & Bochkov, VN 2014, 'Pharmacological insight into the anti-inflammatory activity of sesquiterpene lactones from Neurolaena lobata (L.) R.Br. ex Cass', Phytomedicine, vol. 21, no. 12, pp. 1695-1701. https://doi.org/10.1016/j.phymed.2014.07.019
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. / Pharmacological insight into the anti-inflammatory activity of sesquiterpene lactones from Neurolaena lobata (L.) R.Br. ex Cass. In: Phytomedicine. 2014 ; Vol. 21, No. 12. pp. 1695-1701.
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AU - McKinnon, R.

AU - Binder, M.

AU - Zupkó, I.

AU - Afonyushkin, T.

AU - Lajter, I.

AU - Vasas, A.

AU - De Martin, R.

AU - Unger, C.

AU - Dolznig, H.

AU - Diaz, R.

AU - Frisch, R.

AU - Passreiter, C. M.

AU - Krupitza, G.

AU - Hohmann, J.

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N2 - 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.

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