Bioactive A-ring rearranged limonoids from the root barks of .
10.1016/j.apsb.2019.02.009
- Author:
Faliang AN
1
;
Xiaobing WANG
1
;
Minghua YANG
1
;
Jun LUO
1
;
Lingyi KONG
1
Author Information
1. Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
- Publication Type:Journal Article
- Keywords:
Anti-inflammatory activity;
ECD spectrum calculation;
Neotecleanin-type;
Propionibacterium acnes;
Single-crystal X-ray diffraction;
THP-1 human monocytic cell;
Walsura robusta;
limonoid
- From:
Acta Pharmaceutica Sinica B
2019;9(3):545-556
- CountryChina
- Language:English
-
Abstract:
Screening active natural products, rapid identification, and accurate isolation are of great important for modern natural lead compounds discovery. We hereby reported the isolation of seven new neotecleanin-type limonoids (-), seven new limonoids with 5-oxatricyclo[5.4.0.11., 4.]hendecane ring system (-), and two new precursors (-) together with four known limonoids (-) from the root barks of . Their structures, including their absolute configurations, were elucidated based on analyses of HR-ESI-MS, 1D/2D NMR, ECD spectrum calculations and single-crystal X-ray diffraction techniques. Compounds , , , , , , showed significant anti-inflammatory activities in LPS-induced RAW 264.7 cell line, BV2 microglial cells, and -stimulated THP-1 human monocytic cells. Walrobsin M () exhibited anti-inflammatory activity with IC value of 7.96±0.36 μmol/L, and down-regulated phosphorylation levels of ERK and p38 in a dose-dependent manner.