Anti-oxidative and anti-inflammatory activities of caffeoyl derivatives from the barks of Ilex rotunda

The barks of Ilex rotunda Thunb. (IR) have been used for the treatment of common cold, tonsillitis and intestinal ulcer. As part of our continuous search for new anti-oxidative and anti-inflammatory agents from natural sources, we tried to isolate caffeoyl derivatives from the bark of IR. Activity guided isolations of the 80% MeOH extract yielded two new caffeoyl hemiterpenes (1 and 2), tentatively named rotundarpene and rotundarpenoside B, together with 6 caffeoyl derivatives which were methyl caffeic acid (3), 5-caffeoylquinic acid (4), 3,5-dicaffeoylquinic acid (5), 1,4-dicaffeoylquinic acid (6), 3,4.5-tricaffeoylquinic acid (7) and 3,5-dicaffeoyl shikimic acid (8), respectively.

In order to evaluate anti-oxidative and anti-inflammatory activities of 1-8, DPPH radical scavenging activity and inhibitory activity on nitric oxide production in LPS-stimulated RAW 246.7 cells were measured in vitro. All caffeoyl derivatives (1-8) showed potent anti-oxidative and anti-inflammatory activities, and these results suggested that caffeoyl derivatives from IR might be developed as anti-oxidative and anti-inflammatory agents.

Acknowledgement: This study was supported by a grant of the Korea Healthcare technology R&D Project, Ministry for Health, Welfare & Family Affairs, Republic of Korea (A091121)

References: 1. Damtoft S, Jensen SR (1995) Phytochemistry 39: 923–924.

2. Jiang JH et al. (2005)J Nat Prod 68: 397–399.