Inhibition of NF-kB and metalloproteinase-9 expression and secretion by parthenolide derivatives

doi:10.1016/j.bmcl.2009.02.080

Bioorganic & Medicinal Chemistry Letters

Volume 19, Issue 7, 1 April 2009, Pages 1858-1860

https://doi.org/10.1016/j.bmcl.2009.02.080 Get rights and content

Abstract

Semisynthetic derivatives of parthenolide (1) were tested on NF-kB driven transcription and metalloproteinase-9 (MMP-9) expression and secretion. The four membered ring compounds 5 and 6, obtained by acidic treatment of 1, exhibited a higher activity with respect to 1 in all the biological assays. Then an increased ability of the 5 and 6 to inhibit NF-kB driven transcription may lead to a down-regulation of MMP-9 expression and secretion. This work provides new details about the structural requisites for NF-kB inhibition.

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Acknowledgements

This work was supported by private grants to Centro Studi e Ricerche sulla Caratterizzazione e Sicurezza d’Uso di Sostanze Naturali-Giovanni Galli. We are grateful to Dr. Carla Vender and the CRA (Consiglio per la Ricerca e la Sperimentazione in Agricoltura, Villazzano—Trento) for providing the aerial part of Tanacetum parthenium L.

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Inhibition of NF-kB and metalloproteinase-9 expression and secretion by parthenolide derivatives

Abstract

Graphical abstract

Section snippets

Acknowledgements

J. Biol. Chem.

J. Biol. Chem.

Life Sci.

Gastroenterology

Phytochemistry

Phytochemistry

Phytochemistry

Phytochemistry

Bioorg. Med. Chem.

Bioorg. Med. Chem.

J. Immunol. Methods

Phytochemistry

Nat. Prod. Rep.