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Nan Fang Yi Ke Da Xue Xue Bao. 2015 Jun 20;35(6):789-94.
[3-O-β-chacotriosyl benzyl ursolate inhibits entry of H5N1 influenza virus into target cells].
[Article in Chinese]
Song GP1, Shen XT, Li YB, Zheng YS, Xiong P, Liu SW.
Author information
Abstract
OBJECTIVE:
To study the inhibitory activities of 3-O-β-chacotriosyl benzyl ursolate and its derivatives as potential new anti-influenza virus agents against the entry of H5N1 influenza viruses into the target cells.
METHODS:
Four target compounds were designed and synthesized, which were structurally related to the lead compound 3-O-β-chacotriosyl methyl ursolate (1). The inhibitory activities of these compounds were tested at a cellular level psuedovirus system targeting H5N1 influenza viruse entry.
RESULTS AND CONCLUSION:
The compounds 1b, 1c and 1d showed potent inhibitory activities against the entry of A/Thailand/Kan353/2004 pseudovirus into the target cells, and among them compound 1d showed the strongest inhibitory activity with an IC50 value of 0.96∓0.10 ?mol/L. The structure-activity relationship analysis of these compounds indicated that when 17-COOH of ursolic acid was esterified, introduction of Me groups rather than aryl groups more strongly enhanced the inhibitory activity. Changing 17-COOH of ursolic acid into amide could increase the antiviral activity and decrease the cytotoxicity of the compounds in MDCK cells.
PMID: 26111672 [PubMed - in process] Free full text
[3-O-β-chacotriosyl benzyl ursolate inhibits entry of H5N1 influenza virus into target cells].
[Article in Chinese]
Song GP1, Shen XT, Li YB, Zheng YS, Xiong P, Liu SW.
Author information
Abstract
OBJECTIVE:
To study the inhibitory activities of 3-O-β-chacotriosyl benzyl ursolate and its derivatives as potential new anti-influenza virus agents against the entry of H5N1 influenza viruses into the target cells.
METHODS:
Four target compounds were designed and synthesized, which were structurally related to the lead compound 3-O-β-chacotriosyl methyl ursolate (1). The inhibitory activities of these compounds were tested at a cellular level psuedovirus system targeting H5N1 influenza viruse entry.
RESULTS AND CONCLUSION:
The compounds 1b, 1c and 1d showed potent inhibitory activities against the entry of A/Thailand/Kan353/2004 pseudovirus into the target cells, and among them compound 1d showed the strongest inhibitory activity with an IC50 value of 0.96∓0.10 ?mol/L. The structure-activity relationship analysis of these compounds indicated that when 17-COOH of ursolic acid was esterified, introduction of Me groups rather than aryl groups more strongly enhanced the inhibitory activity. Changing 17-COOH of ursolic acid into amide could increase the antiviral activity and decrease the cytotoxicity of the compounds in MDCK cells.
PMID: 26111672 [PubMed - in process] Free full text