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Kaempferol and Kaempferol Rhamnosides with Depigmenting and Anti-Inflammatory Properties 收藏

Kaempferol和Kaempferol rhamnosides,具有甲状腺和抗炎性质
摘要
The objective of this study was to examine the biological activity of kaempferol and its rhamnosides. We isolated kaempferol (1), a-rhamnoisorobin (2), afzelin (3), and kaempferitrin (4) as pure compounds by far-infrared (FIR) irradiation of kenaf (Hibiscus cannabinus L.) leaves. The depigmenting and anti-inflammatory activity of the compounds was evaluated by analyzing their structure-activity relationships. The order of the inhibitory activity with regard to depigmentation and nitric oxide (NO) production was kaempferol (1) > a-rhamnoisorobin (2) > afzelin (3) > kaempferitrin (4). However, a-rhamnoisorobin (2) was more potent than kaempferol (1) in NF-kB-mediated luciferase assays. From these results, we conclude that the 3-hydroxyl group of kaempferol is an important pharmacophore and that additional rhamnose moieties affect the biological activity negatively.
摘要译文
本研究的目的是检查Kaempferol及其犀牛的生物活性。我们孤立的Kaempferol,A-rhamoisorobin(2),Afzelin(3)和Kaempferitrin(4)作为乳面(芙蓉Cancabinus L.)叶的远红外(FIR)照射。通过分析它们的结构 - 活性关系来评估化合物的脱粒和抗炎活性。关于脱敏和一氧化氮(NO)产生的抑制活性的顺序是kaempferol,A-rhamnoisorobin(2)> afzelin(3)> kaempferitrin(4)。然而,在NF-KB介导的荧光素酶测定中,A-rhamoisorobin(2)比kaempferol(1)更有效。从这些结果来看,我们得出结论,Kaempferol的3-羟基是一个重要的药镜,并且额外的鼠李糖部分产生负面影响。
Ho Sik Rho[ 1;[*]; Amal Kumar Ghimeray[ 2]; Dae Sung Yoo[ 2]; Soo Mi Ahn[ 3]; Sun Sang Kwon[ 4]; Keun Ha Lee[ 4]; Dong Ha Cho[ 2];Jae Youl Cho[ 5;[*]. Kaempferol and Kaempferol Rhamnosides with Depigmenting and Anti-Inflammatory Properties[J]. Molecules Online, 2011,16(4): 3338