Baicalein and baicalin as Zika virus inhibitors

Oo, Adrian; Teoh, Boon‐Teong; Sam, Sing‐Sin; Bakar, Sazaly Abu; Zandi, Keivan

doi:10.1007/s00705-018-4083-4

Cited by 74 publications

(55 citation statements)

References 32 publications

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“…In silico analyzes, as molecular docking has been used to indicate the potential mechanism of action of flavonoids against Zika virus 24,39 . Once the experimental data indicated that NAR could act on the replication, maturation or assembly of viral particles, we employed molecular modeling to assess the hypothesis that NAR may act as a non-competitive inhibitor of the NS2B-NS3 viral protease.…”

Section: Resultsmentioning

confidence: 99%

The citrus flavonoid naringenin impairs the in vitro infection of human cells by Zika virus

Cataneo

Kuczera

Koishi

et al. 2019

Sci Rep

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The Zika virus (ZIKV) is an arthropod-borne virus that belongs to the Flaviviridae family. The ZIKV infection is usually asymptomatic or is associated with mild clinical manifestations; however, increased numbers of cases of microcephaly and birth defects have been recently reported. To date, neither a vaccine nor an antiviral treatment has become available to control ZIKV replication. Among the natural compounds recognized for their medical properties, flavonoids, which can be found in fruits and vegetables, have been found to possess biological activity against a variety of viruses. Here, we demonstrate that the citrus flavanone naringenin (NAR) prevented ZIKV infection in human A549 cells in a concentration-dependent and ZIKV-lineage independent manner. NAR antiviral activity was also observed when primary human monocyte-derived dendritic cells were infected by ZIKV. NAR displayed its antiviral activity when the cells were treated after infection, suggesting that NAR acts on the viral replication or assembly of viral particles. Moreover, a molecular docking analysis suggests a potential interaction between NAR and the protease domain of the NS2B-NS3 protein of ZIKV which could explain the anti-ZIKV activity of NAR. Finally, the results support the potential of NAR as a suitable candidate molecule for developing anti-ZIKV treatments.

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Section: Resultsmentioning

confidence: 99%

The citrus flavonoid naringenin impairs the in vitro infection of human cells by Zika virus

Cataneo

Kuczera

Koishi

et al. 2019

Sci Rep

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show abstract

“…In addition, silymarin was shown to exhibit antiviral activity against CHIKV as it was able to reduce both its replication efficiency and down-regulate the production of viral proteins involved in the replication [10]. Likewise, baicalein was able to inhibit Zika virus replication at postinfection stages [29].…”

Section: Discussionmentioning

confidence: 99%

Antiviral activity of silymarin in comparison with baicalein against EV-A71

Lalani

Anasir

Poh

2020

BMC Complement Med Ther

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Background: The hand, foot and mouth disease (HFMD) is a febrile and exanthematous childhood disease mainly caused by Enterovirus 71 (EV-A71). In severe HFMD, virulent EV-A71 strains can cause acute flaccid paralysis and cardiopulmonary edema leading to death. Currently, no FDA approved antiviral treatment or vaccine is available for EV-A71. Flavonoids such as silymarin and baicalein are known to possess in vitro antiviral properties against viruses. In this study, the cytotoxicity and antiviral activity of silymarin, baicalein and baicalin were investigated. Methods: The cytotoxic effects of three flavonoids towards rhabdomyosarcoma (RD) cells were first examined using cell proliferation MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium] assay. Compounds found to be non-cytotoxic in RD cells were evaluated for their in vitro antiviral properties against the EV-A71 subgenotype B4 strain 41 (5865/SIN/000009) using antiviral assays. Viral infectivity was determined by reduction of the formation of plaques in RD cells. For the measurement of RNA copy number, the real time quantitative reverse transcription PCR (qRT-PCR) was used. The most potent compound was further evaluated to determine the mode of action of inhibition by time course, virus attachment and entry assays in Vero cells. Results: Silymarin was shown to exert direct extracellular virucidal effects against EV-A71 at 50% inhibitory concentration (IC 50) of 15.2 ± 3.53 μg/mL with SI of 10.53. Similarly, baicalein exhibited direct extracellular virucidal effects against EV-A71 at a higher IC 50 value of 30.88 ± 5.50 μg/mL with SI of 13.64. Besides virucidal activity, silymarin was shown to block both viral attachment and entry of EV-A71 to inhibit infection in Vero cells. Conclusions: Silymarin has a stronger inhibition activity against EV-A71 in comparison to baicalein. It could serve as a promising antiviral drug to treat EV-A71 infections.

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“…Baicalin [Figure 3(3)], which has high affinity to the virus E protein and low toxicity to cells, can inhibit ZIKV from entering cells (Table 2; Oo et al, 2019). (-)-Epigallocatechin gallate (EGCG), a polyphenol from green tea, was shown to inhibit many viruses [Figure 3(4) and Table 2; Isaacs et al, 2008; Nance et al, 2009; Calland et al, 2012].…”

Section: Current Small-molecule Inhibitors Against Zikv Infection Andmentioning

confidence: 99%

“…Baicalein [Figure 3(42)], a flavonoid analog, could downregulate ZIKV replication up to 10 h post-infection, while prophylactic effects were evident in pretreated Vero cells with IC 50 ≈ 0.004 μM and selectivity index (SI) ≈ 105,000 (Table 3; Oo et al, 2019). It also has antiviral activity against DENV, chikungunya virus (CHIKV), and influenza virus (Zandi et al, 2012; Moghaddam et al, 2014; Jin et al, 2018; Oo et al, 2018).…”

Section: Current Small-molecule Inhibitors Against Zikv Infection Andmentioning

confidence: 99%

Development of Small-Molecule Inhibitors Against Zika Virus Infection

et al. 2019

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In recent years, the outbreak of infectious disease caused by Zika virus (ZIKV) has posed a major threat to global public health, calling for the development of therapeutics to treat ZIKV disease. Here, we have described the different stages of the ZIKV life cycle and summarized the latest progress in the development of small-molecule inhibitors against ZIKV infection. We have also discussed some general strategies for the discovery of small-molecule ZIKV inhibitors.

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Baicalein and baicalin as Zika virus inhibitors

Cited by 74 publications

References 32 publications

The citrus flavonoid naringenin impairs the in vitro infection of human cells by Zika virus

The citrus flavonoid naringenin impairs the in vitro infection of human cells by Zika virus

Antiviral activity of silymarin in comparison with baicalein against EV-A71

Development of Small-Molecule Inhibitors Against Zika Virus Infection

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