4.7 Article

Twelve novel sesquiterpenes with anti-inflammatory and cholesterol-lowering activities from burdock leaves

期刊

BIOORGANIC CHEMISTRY
卷 127, 期 -, 页码 -

出版社

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2022.105940

关键词

Burdock Leaf; Sesquiterpenes; Anti-inflammatory; Cholesterol lowering; Atherosclerosis

资金

  1. National Key Research and Devel-opment Program of China [2017YFC1701904]
  2. Traditional Chinese Medicine Scientific Research Project of Henan Province [20-21ZY1027]

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This study isolated specific sesquiterpenoids from burdock leaves and demonstrated their anti-inflammatory and cholesterol-lowering activities. Compound 4 showed the strongest cholesterol-lowering effect and reduced the release of pro-inflammatory mediators by inhibiting specific signaling pathways. These findings provide chemical basis and scientific evidence for further research on burdock leaves as anti-atherosclerosis agents.
Nine new cadinane-type sesquiterpenoids (1-9) and three new eucalyptane-type sesquiterpenes (10-12) were isolated from the ethyl acetate extract of Burdock leaves, which were commonly used for preventing or treating atherosclerosis in China. Their structures were confirmed by extensive spectroscopic analysis, single-crystal X-ray diffraction analysis and ECD calculations. Compound 1 possessed the rare large conjugated skeleton. All the isolates were evaluated for anti-inflammatory and cholesterol-lowering activities by the LPS-and oxidized-low density-lipoprotein-stimulated RAW 264.7 cells, respectively. As the results, all isolates could decrease the productions of NO, and down-regulate the accumulation of cholesterol. Among them, 4 showed the most potent cholesterol-lowering effect. For the high content of 4 in the herb, mechanistic study of 4 was performed and the results showed that 4 markedly reduced the release of pro-inflammatory mediators which was probably associated with inhibition of the PI3K/Akt and 5-LOX signaling pathways. The findings of this study demonstrated the anti-inflammatory/cholesterol-lowering effects of the new sesquiterpenes from burdock leaves, which provides chemical basis and scientific evidence for the herb used as anti-atherosclerosis agents for the further study. The sesquiterpene lactones of burdock leaves are expected to become new small molecule inhibitors for the treatment of AS.

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