Eucryphin analog's total synthesis, anti-inflammatory activity for DNFB-induced contact hypersensitivity and structure-activity relationship
JOURNAL OF MOLECULAR STRUCTURE(2023)
摘要
Eucryphin, a natural product widely found in plants, has a variety of biological activities. In this work, a series of eucryphin analogs were designed, synthesized, characterized and the anti-inflammatory activity in vivo was evaluated comparing with eucryphin and its 7-O-glycosyl derivatives to study the structure-activity relationship. Eucryphin exhibited remarkable anti-inflammatory activity and minor side effects in 2,4-dinitrofluorobenzene (DNFB) induced mice auricle edema model. Glycosyl substitution at the position of C-3 was essential for the anti-inflammatory activity. Methyl substitution at C-2 and glycosylation at C-7 of eucryphin reduce anti-inflammatory activity.
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关键词
Chromone derivatives,Synthesis,Anti-inflammatory,Structure-activity relationship
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