Evaluation of the Anti-inflammatory Potential of Chinese Botanicals

Abstract

Traditional Chinese medicine (TCM) has been using about 1300 plants for anti-inflammatory purposes. Activity guided isolation in a medium throughput approach has resulted in the discovery of a number of new drug leads. From the fruits of Evodia rutaecarpa (Juss.) Benth. (Rutaceae), several quinolinone alkaloids, like 1-methyl-2-nonyl-4(1H)-quinolinone, 1-methyl-2-(6Z)-6-undecenyl-4(1H)-quinolinone, 1-methyl-2-(4Z,7Z)-4,7-tridecadienyl-4(1H)-quinolinone, evo-carpine and 1-methyl-2-(6Z,9Z)-6,9-pentadecadienyl-4(1H)-quinolinone, have been isolated which showed strong inhibitory activity on leukotriene biosynthesis in human polymorphonuclear granulocytes [1]. They showed no cytotoxic activity and might bind to the lipid binding site of 5-LOX [2]. Moreover they were very effective against mycobacteria [3]. From Centipeda minima (L.) A. Braun & Asch. (Asteraceae) a series of sesquiterpene lactones, like 6-O-methylacrylplenolin, 6-O-angeloylplenolin and 6-O-tigloyl-plenolin, have been isolated, which exhibited strong inhibitory properties on inducible nitric oxide synthase (iNOS) in RAW 264.7 macrophages [4]. Extracts from Chinese herbs have shown inhibitory properties on expression of NF-kB1 in THP-1 cells [5]. Overexpression of this transcription factor is associated with inflammatory diseases, like rheumatoid arthritis, atherosclerosis, asthma and inflammatory bowel disease. Sesquiterpenes, like parthenolide and helenalin have been demonstrated to be responsible for that effect [6]. Acknowledgements: Part of the work has been supported by Zukunftsfonds Styria (“TCM Research Center Graz”).