Morroniside cinnamic acid conjugate as an anti-inflammatory agent

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• 作者：Yoshinori Takeda ; Naomi Tanigawa ; Fortunatus Sunghwa ; Masayuki Ninomiya ; Makoto Hagiwara ; Kenji Matsushita ; Mamoru Koketsu
• 关键词：Morroniside ; 7-O-Cinnamoylmorroniside ; Anti-inflammatory activity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：15 August 2010
• 年：2010
• 卷：20
• 期：16
• 页码：4855-4857
• 全文大小：295 K

文摘

A morroniside cinnamic acid conjugate was prepared and evaluated on E-selectin mediated cell–cell adhesion as an important role in inflammatory processes. 7-O-Cinnamoylmorroniside exhibited excellent anti-inflammatory activity (IC₅₀ = 49.3 μM) by inhibiting the expression of E-selectin; further, it was more active than another cinnamic-acid-conjugated iridoid glycoside (harpagoside; IC₅₀ = 88.2 μM), 7-O-methylmorroniside, and morroniside itself. As a result, 7-O-cinnamoylmorroniside was observed to be a potent inhibitor of TNF-α-induced E-selectin expression.