Synthesis and structure anti-inflammatory activity relationships studies of andrographolide derivatives
Ling Liu1,2, Yan Yan2, Lihua Zheng2
1Institute of Pharmacy of Henan University, Henan University, Kaifeng 475001, P R China.
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.[Formula: see text].
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