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含有倍半萜内酯的植物Eupatorium formosa-num在台湾省是民间抗炎退热草药。本文研究了29个倍半萜内酯及其类似物的抗炎活性和构-效关系。一般抗炎筛选中发现,凡具有α-次甲基-γ-内酯结构的化合物都显示一定的抗炎活性(2.5mg/kg,2次/天)。分子中若增加一个环成烯酮基,如堆心菊内酯,活性最强(抑制率72%);当其α-次甲基被饱和后,活性基本消失;与胺类化合物形成的加成物后,活性显著降低(26%)。环戊烯酮的双键被饱和后,活性稍有降低,6-羟基被酯化或掩蔽后活性亦降低。倍半萜母核的结构类型亦与活性有关,如伪愈创内酯类的活性(49%)大
Eupatorium formosa-num, a sesquiterpene lactone-containing plant in Taiwan, is a folk anti-inflammatory antipyretic herbal medicine. In this paper, the anti-inflammatory activity and the structure-activity relationship of 29 sesquiterpene lactones and their analogues were studied. It has been found in general anti-inflammatory screening that all the compounds with α-methyne-γ-lactone structure show some anti-inflammatory activity (2.5 mg / kg, twice daily). If the molecule is added a ring of ketene, such as bilobalide lactamase, the most active (inhibition rate of 72%); when its α-methyl is saturated, the activity disappeared; with the formation of amine compounds plus After formation, the activity was significantly reduced (26%). After the double bond of cyclopentenone is saturated, the activity is slightly decreased, and the activity of 6-hydroxy is also esterified or masked. The structure type of sesquiterpenoid nucleus is also related to activity, such as the activity of pseudorastole (49%).