Anti-Inflammatory Activity Comparison among Scropoliosides—Catalpol Derivatives with 6-O-Substituted Cinnamyl Moieties

Abstract

We have previously shown that scropolioside B has higher anti-inflammatory activity than catalpol does after the inhibition of nuclear factor (NF)-κB activity and IL-1β expression, maturation, and secretion. Various scropoliosides were extracted, isolated, and purified from Scrophularia dentata Royle ex Benth. We then compared their anti-inflammatory activities against LPS-induced NF-κB activity, cytokines mRNA expression, IL-1β secretion, and cyclooxygenase-2 activity. The inhibitory effects of the scropoliosides varied depending on whether the 6-O-substituted cinnamyl moiety was linked to C′′ 2-OH, C′′3-OH, or C′′4-OH, and on the number of moieties linked, which is closely related to the enhancement of antiinflammatory activity. Among these compounds, scropolioside B had the strongest antiinflammatory effects.

Keywords

• scropoliosides
• 6-O-substituted cinnamyl moiety
• antiinflammatory effect
• NF-κB
• cytokines