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Six new tigliane diterpenoids with anti-inflammatory activity from Euphorbia kansuensis
Institution:1. State Key Laboratory of Functions and Applications of Medicinal Plants & School of Pharmacy, Guizhou Medical University, Guian New District 550025, Guizhou, China;2. School of Basic Medical Sciences, Guizhou Medical University, Guian New District 550025, Guizhou, China;3. School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, Guangdong, China
Abstract:Six new tigliane diterpenoids, euphkanoids A ? F (16), along with 12 known diterpenoids (718) were isolated from the roots of Euphorbia kansuensis, a traditional Chinese medicinal plant. Their structures were elucidated by spectroscopic analysis, ECD calculation and chemical methods. Compounds 13 represent the unusual examples of tigliane diterpenoids with a conjugated olefinic aldehyde moiety. 118 and two hydrolyzed analogues (1c and 4a) were screened for the inhibitory effects on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW264.7 cells. The results showed that 13 and 6 markedly inhibited NO production with IC50 values in the range of 4.8–11.3 μM, which were more active than the positive control quercetin (IC50 = 12.3 μM).
Keywords:Anti-inflammatory  NO inhibitory activity  Tigliane diterpenoid
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