Please use this identifier to cite or link to this item:
https://doi.org/10.1016/j.bcp.2021.114820
DC Field | Value | |
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dc.title | Discovery of 14S-(2’-chloro-4’-nitrophenoxy)-8R/S,17-epoxy andrographolide as EV-A71 infection inhibitor | |
dc.contributor.author | Dai, K | |
dc.contributor.author | Tan, JK | |
dc.contributor.author | Qian, W | |
dc.contributor.author | Lee, RCH | |
dc.contributor.author | Hann Chu, JJ | |
dc.contributor.author | Zhou, GC | |
dc.date.accessioned | 2022-12-08T09:55:31Z | |
dc.date.available | 2022-12-08T09:55:31Z | |
dc.date.issued | 2021-12-01 | |
dc.identifier.citation | Dai, K, Tan, JK, Qian, W, Lee, RCH, Hann Chu, JJ, Zhou, GC (2021-12-01). Discovery of 14S-(2’-chloro-4’-nitrophenoxy)-8R/S,17-epoxy andrographolide as EV-A71 infection inhibitor. Biochemical Pharmacology 194 : 114820-. ScholarBank@NUS Repository. https://doi.org/10.1016/j.bcp.2021.114820 | |
dc.identifier.issn | 0006-2952 | |
dc.identifier.issn | 1873-2968 | |
dc.identifier.uri | https://scholarbank.nus.edu.sg/handle/10635/235429 | |
dc.description.abstract | Human enterovirus A71 (EV-A71) is a major etiological agent of hand-foot-and-mouth disease (HFMD) and there is presently no internationally approved antiviral against EV-A71. In this study, it is disclosed that 14S-(2’-chloro-4’-nitrophenoxy)-8R/S,17-epoxy andrographolide (2) was discovered to be an effective inhibitor against EV-A71 infection showing significant reduction of viral titre. In addition to EV-A71, compound 2 exerts broad-spectrum antiviral effects against other enteroviruses. It is revealed that compound 2 inhibits the post-entry stages of EV-A71 viral replication cycle and significantly reduces viral protein expression of structural proteins such as VP0 and VP2 via inhibiting EV-A71 RNA replication. Moreover, the inhibitory property of compound 2 is specific to viral RNA replication. Furthermore, compound 2 is more likely to target a host factor in EV-A71 RNA replication. As a result, introduction of epoxide at positions 8 and 17 of andrographolide is effective for anti-EV-A71 infection and is a potential anti-EV-A71 strategy. Further work to discover more potent andrographolide derivatives and elucidate comprehensive SAR is under way. | |
dc.publisher | Elsevier BV | |
dc.source | Elements | |
dc.subject | Andrographolide | |
dc.subject | Broad-spectrum anti-enterovirus agent | |
dc.subject | Epoxide | |
dc.subject | Human enterovirus A71 | |
dc.subject | Targeting host factor | |
dc.subject | Viral RNA replication | |
dc.subject | Animals | |
dc.subject | Cell Survival | |
dc.subject | Chlorocebus aethiops | |
dc.subject | Diterpenes | |
dc.subject | Dose-Response Relationship, Drug | |
dc.subject | Drug Discovery | |
dc.subject | Enterovirus A, Human | |
dc.subject | Enterovirus Infections | |
dc.subject | Humans | |
dc.subject | Vero Cells | |
dc.subject | Virus Replication | |
dc.type | Article | |
dc.date.updated | 2022-12-08T05:51:28Z | |
dc.contributor.department | MEDICINE | |
dc.contributor.department | MICROBIOLOGY AND IMMUNOLOGY | |
dc.description.doi | 10.1016/j.bcp.2021.114820 | |
dc.description.sourcetitle | Biochemical Pharmacology | |
dc.description.volume | 194 | |
dc.description.page | 114820- | |
dc.published.state | Published | |
Appears in Collections: | Elements Staff Publications |
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1-s2.0-S0006295221004366-main.pdf | Published version | 3.61 MB | Adobe PDF | CLOSED | Published | |
R221208n13_Manuscript.pdf | 1.3 MB | Adobe PDF | OPEN | Pre-print | View/Download |
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