期刊
JOURNAL OF NATURAL PRODUCTS
卷 83, 期 9, 页码 2545-2558出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.9b00597
关键词
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资金
- Natural Science Foundation of China [81903541, 81860615, 21762048, 81422046]
- Yunnan Applicative and Basic Research Program [2018FY001, 2018FA048]
- Foundation of Yunnan Educational Committee [2018JS002]
- Natural Science Foundation of Yunnan University [2017YDQN03]
- Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education [2017KF02]
- Program for Changjiang Scholars and Innovative Research Team in University [IRT_17R94]
- Project of Innovative Research Team of Yunnan Province
- Yun Ling Scholar Project
A phytochemical study on the aerial parts of Leonurus japonicus led to the isolation and identification of 38 labdane diterpenoids, including 18 new (1, 2, 11, 12, 16-21, 24, 30-34, 37, 38) and 20 known (3-10, 13-15, 22, 23, 25-29, 35, 36) analogues. Their structures were elucidated based on physical data analysis, including 1D and 2D NMR, HRMS, UV, IR, and X-ray diffraction. The structure of the known compound 4 was confirmed by single-crystal X-ray diffraction data. These compounds can be divided into furanolabdane (1-10), tetrahydrofuranolabdane (11-15), lactonelabdane (16-23), labdane (24-29), and seco-labdane (30-38) type diterpenoids. All compounds were screened by lipopolysaccharide (LPS)-induced nitric acid (NO) production in RAW264.7 cells to evaluate anti-inflammatory effects. Compounds 1, 5, 10-13, 16-19, 31-33, and 38 inhibited NO production with IC50 values lower than 50 mu M, with compound 30 being the most active, with an IC50 value of 3.9 +/- 1.7 mu M. Further studies show that compound 30 inhibits pro-inflammatory cytokine production and IKK alpha/beta phosphorylation and restores the I kappa B expression levels in the NF-kappa B signaling pathway.
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