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Structure-aided optimization of 3-O-beta-chacotriosyl ursolic acid as novel H5N1 entry inhibitors with high selective index

文献类型： 外文期刊

作者： Liao, Yixian 1 ; Chen, Lizhu 3 ; Li, Sumei 4 ; Cui, Zi-ning 2 ; Lei, Zhiwei 5 ; Li, Hui 1 ; Liu, Shuwen 3 ; Song, Gaopeng 1 ;

作者机构： 1.South China Agr Univ, Coll Mat & Energy, Guangzhou 510642, Guangdong, Peoples R China

2.South China Agr Univ, Guangdong Prov Key Lab Microbial Signals & Dis Co, Integrat Microbiol Res Ctr, State Key Lab Conservat & Utilizat Subtrop Agrobi, Guangzhou 510642, Guangdong, Peoples R China

3.Southern Med Univ, Sch Pharmaceut Sci, Guangzhou 510515, Guangdong, Peoples R China

4.Jinan Univ, Sch Med, Dept Human Anat, Guangzhou 510632, Guangdong, Peoples R China

5.Guizhou Acad Agr Sci, Guizhou Tea Reasearch Inst, Guiyang 550006, Guizhou, Peoples R China

关键词： 3-O-beta chacotriosyl pentacyclic triterpenoids; H5N1 entry inhibitors; Structure-activity relationships

期刊名称：BIOORGANIC & MEDICINAL CHEMISTRY （ 影响因子：3.641； 五年影响因子：3.319 ）

ISSN： 0968-0896

年卷期： 2019 年 27 卷 18 期

页码：

收录情况： SCI

摘要： Currently, entry inhibitors contribute immensely in developing a new generation of anti-influenza virus drugs. Our earlier studies have identified that 3-O-beta-chacotriosyl ursolic acid (1) could inhibit H5N1 pseudovirus by targeting hemagglutinin (HA). In the present study, a series of C-28 modified pentacyclic triterpene saponins via conjugation with a series of amide derivatives were synthesized and their antiviral activities against influenza A/Duck/Guangdong/99 virus (H5N1) in MDCK cells were evaluated. The SARs analysis of these compounds revealed that introduction of certain amide structures at the 17-COOH of ursolic acid could significantly enhance both their antiviral activity and selective index. This study indicated that the attachment of the methoxy group or Cl atom to the phenyl ring at the ortho- or para-position was crucial to improve inhibitory activity. Mechanism studies demonstrated that these title triterpenoids could bind tightly to the viral envelope HA to block the attachment of viruses to host cells, which was consistent with docking studies.

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