Synthesis and biological evaluation of novel chalcone aromatic oxygen alkyl acids compounds
10.16438/j.0513-4870.2015-0958
- VernacularTitle:新型查尔酮芳氧烷酸类化合物的合成及其生物活性研究
- Author:
Wei-jun HUANG
1
;
Di XIE
1
;
Jia-ming LI
1
;
Yan-chun ZHANG
1
;
Jian ZUO
1
;
Hui-cai LIU
1
Author Information
1. College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230038, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
removing blood stasis;
ligustrazine;
chalcone aromatic oxygen alkyl acids compound;
synthesis;
anti-platelet aggregation;
hypolipidemic
- From:
Acta Pharmaceutica Sinica
2016;51(4):600-
- CountryChina
- Language:Chinese
-
Abstract:
Six novel ligustrazine chalcone aromatic oxygen alkyl acids compounds and two pyridine chalcone aromatic oxygen alkyl acids ester compounds were synthesized according to the traditional Chinese medicine theory removing blood stasis. The structures of target compounds were identified by IR, NMR and ESI-MS. The inhibitory activities of platelet aggregation induced by adenosine diphosphate (ADP) and arachidonic acid (AA) were measured by the liver microsomal incubation method in vitro. Hypolipidemic activities of compounds were tested in vivo for better inhibitory activities of platelet aggregation. Preliminary pharmacological results showed that compounds 7c, 8a and 11a had potent inhibitory activity against platelet aggregation induced by AA, compounds 7c, 7d, 8a and 11b showed significant inhibitory activity against platelet aggregation induced by ADP. Compounds 7c and 8a exhibited good hypolipidemic activities in high-fat-diet (HFD) induced hyperlipidemia C57/BL6 mice and worthy for further investigation.
