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eCAM Advance Access published online on December 3, 2007
eCAM, doi:10.1093/ecam/nem129
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© 2007 The Author(s).
This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/2.0/uk/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.

Inhibitory Potencies of Several Iridoids on Cyclooxygenase-1, Cyclooxygnase-2 Enzymes Activities, Tumor Necrosis factor-{alpha} and Nitric Oxide Production In Vitro

Kyoung Sik Park, Bong Hyun Kim and Il-Moo Chang

Natural Products Research Institute, College of Pharmacy, Seoul National University, 28-Yungun-dong, Jongro-ku, Seoul 110-460, Korea

To verify the anti-inflammatory potency of iridoids, seven iridoid glucosides (aucubin, catalpol, gentiopicroside, swertiamarin, geniposide, geniposidic acid and loganin) and an iridoid aglycone (genipin) were investigated with in vitro testing model systems based on inhibition of cyclooxygenase (COX)-1/-2 enzymes, the tumor necrosis factor-{alpha} (TNF-{alpha}) formation and nitric oxide (NO) production. The hydrolyzed-iridoid products (H-iridoid) with β-gludosidase treatment only showed inhibitory activities, and revealed different potencies, depending on their chemical structures. Without the β-gludosidase treatment, no single iridoid glycoside exhibited any activities. The aglycone form (genipin) also did not show inhibitory activities. To compare anti-inflammatory potency, the inhibitory concentrations (IC50) in each testing system were measured. The hydrolyzed-aucubin product (H-aucubin) with β-gludosidase treatment showed a moderate inhibition on COX-2 with IC50 of 8.83 µM, but much less inhibition (IC50, 68.9 µM) on COX-1 was noted. Of the other H-iridoid products, the H-loganin and the H-geniposide exhibited higher inhibitory effects on COX-1, revealing IC50 values of 3.55 and 5.37 µM, respectively. In the case of TNF-{alpha} assay, four H-iridoid products: H-aucubin, H-catalpol, H-geniposide and H-loganin suppressed the TNF-{alpha} formation with IC50 values of 11.2, 33.3, 58.2 and 154.6 µM, respectively. But other H-iridoid products manifested no significant activity. Additional experiments on NO production were conducted. We observed that only the H-aucubin exhibited a significant suppression with IC50 value of 14.1 µM. Genipin, an agycone form, showed no inhibitory effects on all testing models, implying the hydrolysis of the glycosidic bond of iridoid glycoside is a pre-requisite step to produce various biological activities.

Keywords: anti-inflammation – cyclooxygenase – iridoids –nitric oxide – tumor necrosis factor-{alpha}

For reprints and all correspondence: Il-Moo Chang, Natural Products Research Institute, College of Pharmacy, Seoul National University, 28-Yungun-dong, Jongro-ku, Seoul 110-460, Korea. Tel: +82-2-740-8921; Fax: +82-2-745-1015; E-mail: changim{at}snu.ac.kr

Received November 19, 2006; accepted July 27, 2007


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