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Hydroxylated Ethacrylic and Tiglic Acid Derivatives from the Stems and Branches of Enkianthus chinensis and Their Potential Anti-inflammatory Activities
Journal of Natural Products ( IF 5.1 ) Pub Date : 2020-10-14 , DOI: 10.1021/acs.jnatprod.0c00286
Hai-Qiang Wang 1 , Shuang-Gang Ma 1 , Ming-Bao Lin 1 , Qi Hou 1 , Min Ma 1 , Shi-Shan Yu 1
Affiliation  

Two new hydroxylated ethacrylic acid derivatives (compounds 1 and 2) and 11 new hydroxylated tiglic acid derivatives (compounds 313), together with one known compound (compound 14), were isolated from the stems and branches of Enkianthus chinensis. Their structures were established by extensive spectroscopic analyses, while their absolute configurations were determined by X-ray crystallographic methods (compounds 1 and 2), Mo2(OAc)4-induced electronic circular dichroism experiments (compounds 3 and 4), and chemical methods (compounds 511). This study is the first investigation on the secondary metabolites of this species. The anti-inflammatory activities of all isolated compounds were evaluated in an LPS-induced mouse peritoneal macrophage model. Notably, compounds 3 and 12 both exerted potent inhibitory effects on NO production with IC50 values of 2.9 and 1.2 μM, respectively.

中文翻译:

来自花环草茎和枝的羟基化乙基丙烯酸和替格酸衍生物及其潜在的抗炎活性

两个新的羟基化的乙基丙烯酸衍生物(化合物12)和11个新的羟基化的惕各酸衍生物(化合物3 - 13),与一种已知化合物(化合物一起14),分离从茎和树枝吊钟红豆杉。它们的结构是通过广泛的光谱分析确定的,而它们的绝对构型是通过 X 射线晶体学方法(化合物12)、Mo 2 (OAc) 4诱导的电子圆二色性实验(化合物34) 和化学方法(化合物511)。本研究是对该物种次生代谢物的首次调查。在 LPS 诱导的小鼠腹腔巨噬细胞模型中评估了所有分离化合物的抗炎活性。值得注意的是,化合物312都对 NO 产生发挥了有效的抑制作用,IC 50值分别为 2.9 和 1.2 μM。
更新日期:2020-10-26
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