Antagonistic effects of extracts from Artemisia rupetris L. and Leontopodium leontopodioides to CC chemokine receptor 2b (CCR2b).
10.3724/SP.J.1009.2016.00363
- Author:
Qin-Wei YU
1
;
Jie HU
1
;
Hao WANG
2
;
Xin CHEN
1
;
Fang ZHAO
1
;
Peng GAO
1
;
Qiu-Bin YANG
3
;
Dan-Dan SUN
4
;
Lu-Yong ZHANG
5
,
6
;
Ming YAN
7
Author Information
1. Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009, China.
2. Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
3. School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, China.
4. School of Traditional Chinese Medicine, China Pharmaceutical University, Nanjing 210009, China.
5. Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009, China
6. Key Laboratory of Drug Quality Control and Pharmacovigilance (China Pharmaceutical University), Ministry of Education, Nanjing 210009, China. Electronic address: lyzhang@cpu.edu.cn.
7. Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009, China. Electronic address: brookming@cpu.edu.cn.
- Publication Type:Journal Article
- Keywords:
Aequorin assay;
Artemisia rupetris;
CCR2b antagonist;
Inflammation;
Leontopodium leontopodioides
- MeSH:
Artemisia;
chemistry;
Asteraceae;
chemistry;
Drug Evaluation, Preclinical;
Humans;
Kinetics;
Plant Extracts;
chemistry;
pharmacology;
Receptors, CCR2;
antagonists & inhibitors;
genetics;
metabolism;
Structure-Activity Relationship
- From:
Chinese Journal of Natural Medicines (English Ed.)
2016;14(5):363-369
- CountryChina
- Language:English
-
Abstract:
The present study was designed to establish a suitable assay to explore CCR2b receptor antagonists from the natural products of Artemisia 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-1, 5, 7, and AR-20, 35 showed activity as antagonist of CCR2b receptor, which shed lights on the development of novel drugs as CCR2b receptor antagonists for preventing inflammation related diseases.
