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Molecules 2015, 20(11), 19823-19836; doi:10.3390/molecules201119659

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

1
Murad Research Institute for Modernized Chinese Medicine, Shanghai University of Traditional Chinese Medicine
2
School of Pharmacy, Shanghai University of Traditional Chinese Medicine
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 11 September 2015 / Revised: 30 September 2015 / Accepted: 7 October 2015 / Published: 3 November 2015
(This article belongs to the Section Medicinal Chemistry)
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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. View Full-Text
Keywords: scropoliosides; 6-O-substituted cinnamyl moiety; antiinflammatory effect; NF-κB; cytokines scropoliosides; 6-O-substituted cinnamyl moiety; antiinflammatory effect; NF-κB; cytokines
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Zhu, T.; Zhang, L.; Ling, S.; Qian, F.; Li, Y.; Xu, J.-W. Anti-Inflammatory Activity Comparison among Scropoliosides—Catalpol Derivatives with 6-O-Substituted Cinnamyl Moieties. Molecules 2015, 20, 19823-19836.

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