中国天然药物, 2016, Vol.14 (5), p.363-369
2016
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Details
- Autor(en) / Beteiligte
- Titel
- Antagonistic effects of extracts from Artemisia rupetris L. and Leontopodium leontopodioides to CC chemokine receptor 2b （CCR2b）
- Ist Teil von
- 中国天然药物, 2016, Vol.14 (5), p.363-369
- Erscheinungsjahr
- 2016
- Quelle
- Alma/SFX Local Collection
- Beschreibungen/Notizen
- The present study was designed to establish a suitable assay to explore CCR2b receptor antagonists from the natural products ofArtemisia rupetris and Leontopodium leontopodioides. An aequorin assay was developed as a cell-based assay suitable for 384-well microplate and used for screening CCR2b receptor antagonists from natural products. Through establishing suitable conditions, the assay was shown to be suitable for screening of CCR2b receptor antagonists. Seven compounds were identified in preliminary screening. Five of them showed evident dose-response relationship in secondary screening. The structure--activity relationship study suggested that 7-position hydroxyl group of flavonoids was necessary, a polar group should be introduced on the 3-position, and the substituents on 2-position benzene ring of flavonoids have little influence on the potentency of the inhibition activity on CCR2b receptor. The ortho-position dihydroxyl structure in quinic acid compounds may be important. In conclusion, Compounds HR