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Two new lathyrane-type diterpenoid glycosides with IL-6 production inhibitory activity from the roots of Euphorbia kansui
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-02-27 , DOI: 10.1016/j.bmcl.2018.02.050
Young-Mi Kim , Jongmin Ahn , Hee-Sung Chae , Young Hee Choi , Jinwoong Kim , Young-Won Chin

As part of our ongoing search for anti-inflammatory compounds from higher plants, we isolated and elucidated two new diterpenoid glycosides, kansuingol A (1) and kansuingol B (2), from the roots of Euphorbia kansui. These structures were elucidated by extensive spectroscopic methods such as NMR and MS. Compounds were assessed for their IL-6 production inhibitory activity in PMA + A23187-stimulated HMC-1 cells. As a result, compounds 1 and 2 exerted inhibitory activities in the production of IL-6 with IC50 values of 2.96, and 1.94 μM, respectively. Further, kansuingol A (1) decreased mRNA expressions of TNF-α and IL-6.



中文翻译:

甘蓝大戟根中两种具有IL-6产生抑制活性的新型Lathyrane型二萜糖苷

作为我们从高等植物中寻找抗炎化合物的不断努力的一部分,我们从大戟一品的根中分离并阐明了两种新的二萜类糖苷,甘肃醇A(1)和甘肃醇B(2)。通过广泛的光谱学方法(例如NMR和MS)阐明了这些结构。评估化合物在PMA + A23187刺激的HMC-1细胞中IL-6产生的抑制活性。结果,化合物12在IL-6的产生中发挥抑制活性,其IC 50值分别为2.96和1.94μM。此外,甘蔗丁醇A(1)降低了TNF-α和IL-6的mRNA表达。

更新日期:2018-02-27
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