Cynaropicrin and inhibition of NF-κB activation: A structure activity relationship study. Issue 12 (15th June 2019)

• Record Type: Journal Article
• Authors: Li, Jing; Yoshida, Yusuke; Kurita, Manami; Usuki, Toyonobu
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 12(2019)
• Page Start: 1518
• Page End: 1521
• Publication Date: 2019-06-15
• Subjects: Cynaropicrin -- NF-κB -- SAR -- Derivatization; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.04.004
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Cynaropicrin is a guaianolide sesquiterpene lactone with a 5-7-5 tricyclic skeleton, four exo-olefins, and two hydroxyl groups. This natural product has various biological activities including anti-inflammatory properties and antitrypanosomal activity. It was also found to suppress photoaging of the skin by inhibiting the transcription activity of nuclear factor-kappa B (NF-κB). In this paper, nine chemical derivatives of cynaropicrin were prepared, and the structure activity relationship (SAR) study for NF-κB inhibition by measuring relative light units (RLU) was conducted.