Issue 5, 2016

Synthesis and mode of action of oligomeric sesquiterpene lactones

Abstract

Covering: up to 2015

In this highlight we describe two case studies from our laboratory, involving the biomimetic syntheses and the biological mechanism elucidation of the bioactive oligomeric sesquiterpenoids, (+)-ainsliadimer A (4) and (−)-ainsliatrimer A (5). Ainsliadimer A possesses potent anti-inflammatory activity by inhibition of the NF-κB signalling pathway via binding at a previously untargeted allosteric site. (−)-Ainsliatrimer A induces apoptosis in cancer cells by activation of PPARγ. Furthermore, we highlight a new bioorthogonal ligation (TQ-ligation) developed in our laboratory which facilitates the target identification of complex natural products via pre-target fluorescence imaging and affinity chromatography. Generally, this paper will discuss the complete process from total synthesis to biological studies of complex natural products, and from the establishment of new bio-orthogonal chemistry to successful target identification. Our approach provides a systematic and efficient methodology for addressing the challenge of natural product target identification.

Graphical abstract: Synthesis and mode of action of oligomeric sesquiterpene lactones

Article information

Article type
Highlight
Submitted
06 अगस्त 2015
First published
29 अक्तूबर 2015

Nat. Prod. Rep., 2016,33, 602-611

Author version available

Synthesis and mode of action of oligomeric sesquiterpene lactones

C. Li, A. X. Jones and X. Lei, Nat. Prod. Rep., 2016, 33, 602 DOI: 10.1039/C5NP00089K

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements