4.7 Article

Hydroxylated Ethacrylic and Tiglic Acid Derivatives from the Stems and Branches of Enkianthus chinensis and Their Potential Anti-inflammatory Activities

Journal

JOURNAL OF NATURAL PRODUCTS
Volume 83, Issue 10, Pages 2867-2876

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.0c00286

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Funding

  1. National Natural Science Foundation of China [21732008]
  2. CAMS Innovation Fund for Medical Sciences (CIFMS) [2016I2M-3-010]
  3. National Mega-project for Innovative Drugs [2018ZX09711001-008]

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Two new hydroxylated ethacrylic acid derivatives (compounds 1 and 2) and 11 new hydroxylated tiglic acid derivatives (compounds 3-13), 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), Mo-2(OAc)(4)-induced electronic circular dichroism experiments (compounds 3 and 4), and chemical methods (compounds 5-11). 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 mu M, respectively.

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