Inhibition of Enterovirus 71 replication by 7-hydroxyflavone and diisopropyl-flavon7-yl Phosphate.
Enterovirus 71 (EV71) is the major causative agent of hand, foot, and mouth disease, which has been continuously prevalent in Asia in recent years. In children, severe cases can lead to death, and no prophylactic or therapeutic measures against EV71 infection are available. The 3C proteases of EV71...
| Main Authors: | , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Public Library of Science (PLoS)
2014-01-01
|
| Series: | PLoS ONE |
| Online Access: | http://europepmc.org/articles/PMC3963929?pdf=render |
| _version_ | 1819266075754233856 |
|---|---|
| author | Jianmin Wang Haoxiang Su Ting Zhang Jiang Du Sheng Cui Fan Yang Qi Jin |
| author_facet | Jianmin Wang Haoxiang Su Ting Zhang Jiang Du Sheng Cui Fan Yang Qi Jin |
| author_sort | Jianmin Wang |
| collection | DOAJ |
| description | Enterovirus 71 (EV71) is the major causative agent of hand, foot, and mouth disease, which has been continuously prevalent in Asia in recent years. In children, severe cases can lead to death, and no prophylactic or therapeutic measures against EV71 infection are available. The 3C proteases of EV71 play an important role in viral replication and are an ideal drug target. In previous work, we resolved the crystal structure for EV71 3Cpro. In this report, we took advantage of the automated docking program AutoDock 4.0 to simulate EV71 3Cpro-ligand conformation. 7-hydroxyflavone (HF) and its phosphate ester(FIP) were predicted to bind with EV71 3Cpro.In an in vitro protease inhibition assay, FIP inhibited EV71 3Cpro protease activity. Both flavones were highly active against EV71, protecting cells from EV71 infection. Replication of viral RNA and formation of EV71 plaque were all strongly inhibited in cells. These results indicated that HF and FIP may serve as potential protective agents in the treatment of patients with chronic EV71 infection. |
| first_indexed | 2024-12-23T20:55:31Z |
| format | Article |
| id | doaj.art-f96b025efc5f417ea092c0f96190342d |
| institution | Directory Open Access Journal |
| issn | 1932-6203 |
| language | English |
| last_indexed | 2024-12-23T20:55:31Z |
| publishDate | 2014-01-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS ONE |
| spelling | doaj.art-f96b025efc5f417ea092c0f96190342d2022-12-21T17:31:33ZengPublic Library of Science (PLoS)PLoS ONE1932-62032014-01-0193e9256510.1371/journal.pone.0092565Inhibition of Enterovirus 71 replication by 7-hydroxyflavone and diisopropyl-flavon7-yl Phosphate.Jianmin WangHaoxiang SuTing ZhangJiang DuSheng CuiFan YangQi JinEnterovirus 71 (EV71) is the major causative agent of hand, foot, and mouth disease, which has been continuously prevalent in Asia in recent years. In children, severe cases can lead to death, and no prophylactic or therapeutic measures against EV71 infection are available. The 3C proteases of EV71 play an important role in viral replication and are an ideal drug target. In previous work, we resolved the crystal structure for EV71 3Cpro. In this report, we took advantage of the automated docking program AutoDock 4.0 to simulate EV71 3Cpro-ligand conformation. 7-hydroxyflavone (HF) and its phosphate ester(FIP) were predicted to bind with EV71 3Cpro.In an in vitro protease inhibition assay, FIP inhibited EV71 3Cpro protease activity. Both flavones were highly active against EV71, protecting cells from EV71 infection. Replication of viral RNA and formation of EV71 plaque were all strongly inhibited in cells. These results indicated that HF and FIP may serve as potential protective agents in the treatment of patients with chronic EV71 infection.http://europepmc.org/articles/PMC3963929?pdf=render |
| spellingShingle | Jianmin Wang Haoxiang Su Ting Zhang Jiang Du Sheng Cui Fan Yang Qi Jin Inhibition of Enterovirus 71 replication by 7-hydroxyflavone and diisopropyl-flavon7-yl Phosphate. PLoS ONE |
| title | Inhibition of Enterovirus 71 replication by 7-hydroxyflavone and diisopropyl-flavon7-yl Phosphate. |
| title_full | Inhibition of Enterovirus 71 replication by 7-hydroxyflavone and diisopropyl-flavon7-yl Phosphate. |
| title_fullStr | Inhibition of Enterovirus 71 replication by 7-hydroxyflavone and diisopropyl-flavon7-yl Phosphate. |
| title_full_unstemmed | Inhibition of Enterovirus 71 replication by 7-hydroxyflavone and diisopropyl-flavon7-yl Phosphate. |
| title_short | Inhibition of Enterovirus 71 replication by 7-hydroxyflavone and diisopropyl-flavon7-yl Phosphate. |
| title_sort | inhibition of enterovirus 71 replication by 7 hydroxyflavone and diisopropyl flavon7 yl phosphate |
| url | http://europepmc.org/articles/PMC3963929?pdf=render |
| work_keys_str_mv | AT jianminwang inhibitionofenterovirus71replicationby7hydroxyflavoneanddiisopropylflavon7ylphosphate AT haoxiangsu inhibitionofenterovirus71replicationby7hydroxyflavoneanddiisopropylflavon7ylphosphate AT tingzhang inhibitionofenterovirus71replicationby7hydroxyflavoneanddiisopropylflavon7ylphosphate AT jiangdu inhibitionofenterovirus71replicationby7hydroxyflavoneanddiisopropylflavon7ylphosphate AT shengcui inhibitionofenterovirus71replicationby7hydroxyflavoneanddiisopropylflavon7ylphosphate AT fanyang inhibitionofenterovirus71replicationby7hydroxyflavoneanddiisopropylflavon7ylphosphate AT qijin inhibitionofenterovirus71replicationby7hydroxyflavoneanddiisopropylflavon7ylphosphate |