Synthesis and structure anti-inflammatory activity relationships studies of andrographolide derivatives

Abstract

Andrographolide is a main bioactive diterpene lactone in A. paniculata with anti-inflammatory activity. In this study, a series of andrographolide derivatives were synthesized and evaluated for their structure-anti-inflammatory activity relationships in vivo. Among all compounds, isoandrographolide and 14-deoxyandrographolide showed stronger anti-inflammatory activity than andrographolide. The results indicated that the introduction of tetrahydrofuran ring and cyclic olefinic bond plays an important role in enhancing the anti-inflammatory activity of andrographolide derivatives. Isoandrographolide and 14-deoxyandrographolide are potent inhibitor of inflammation.

Keywords:

• Andrographolide derivatives
• anti-inflammatory activity
• egg white-induced rat paw edema model

Acknowledgments

We wish to thank Analysis and Test Center of School of Chemical Institute of Chemical Industry for providing us with the ¹HNMR and MS analysis and test work.

Disclosure statement

No conflict of interest was reported by the authors.

Additional information

Funding

This study was partly supported by the National Natural Science Foundation of China [grant number 81373974]. Dr Han also thanks for the support of the Henan Programs for Science and Technology Development [grant number 142300410370]. Dr Liu thanks for the support of the Henan Science and Technology Development Plan Project [grant number 162102210176]. Also thanks for the support of the Key Scientific and Technological Research Projects of Henan Education Department [grant number 15B350001].