Inhibitory activities of 3-O-β-chacotriosyl pentacyclic triterpenoids against the entry of H5 N1 influenza viruses in vitro
10.3969/j.issn.1001-1978.2015.05.012
- VernacularTitle:马铃薯三糖五环三萜类化合物体外抗H5N1流感病毒的活性评价
- Author:
Gaopeng SONG
;
Xintian SHEN
;
Sumei LI
;
Yibin LI
;
Jihong FAN
;
Qianqian LIANG
;
Shuwen LIU
- Publication Type:Journal Article
- Keywords:
H5N1 avian influenza virus;
influenze vi-rus entry inhibitor;
synthesis;
hemagglutinin;
struc-ture-activity relationships;
pentacyclic triterpenoids
- From:
Chinese Pharmacological Bulletin
2015;(5):647-654
- CountryChina
- Language:Chinese
-
Abstract:
Aim To study the inhibitory activities of potential new anti-influenza virus agents,3-O-β-chaco-triosyl pentacyclic triterpenoids against the entry of H5N1influenza viruses.Methods Three target com-pounds were designed and synthesized structurally re-lated to the lead compound 3-O-β-chacotriosyl dioscin derivative (1 )with inhibitory activities against H5N1 influenza viruses.The inhibitory activities of these tar-get compounds were tested at a cellular level pseudo vi-rus system targeting H5N1 influenza viruse entry.Re-sults All the compounds 1 a,1 b and 1 c showed po-tent inhibitory activities against the entry of A/Thai-land/Kan353/2004 pseudo virus into the target cells, of which compound 1 b showed the best inhibitory activ-ity with an IC50 value of (1.25 ±0.22)μmol·L-1. Conclusion The SARs analysis of these compounds indicated that replacement of the aglycone moiety of compound 1 with pentacyclic triterpenoids could in-crease antiviral activity.Different types of pentacyclic triterpen as aglycone residue had the significant influ-ence on the inhibitory activity (1 b >1 c >1 a),sug-gesting ursane type of triterpenes was superior to the two other kinds of triterpenes as aglycone residue.
