Antiviral activity of pinocembrin against Zika virus replication

Lee, Jia Le; Loe, Marcus Wing Choy; Lee, Regina Ching Hua; Chu, Justin Jang Hann

doi:10.1016/j.antiviral.2019.04.003

Cited by 72 publications

(40 citation statements)

References 35 publications

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“…The compounds did not inhibit DENV envelope-induced fusion under acidic pH ( Supplementary Figure S5 ). Therefore, it was likely that TH011 and TH002 would inhibit the DENV translation and replication similar to the previously characterized pinocembrin ( TH022 ) in ZIKV replicon [ 17 ].…”

Section: Resultsmentioning

confidence: 67%

“…Besides LLC/MK2 and Huh-7, TH011 displayed mild cytotoxicity to THP-1, HepG2, and HEK-293 cell lines ( Table 2 ). The original pinocembrin ( TH022 ) was previously reported as DENV2, and Zika viruses inhibitor with moderate efficacies [ 16 ] at the EC 50 s of 15.45, and 17.4 µM, respectively [ 11 , 17 ]. Therefore, we concluded that the dibromopinocembrin ( TH011 ) was more potent than its original compound for DENV2 inhibition.…”

Section: Resultsmentioning

confidence: 99%

“…Original pinocembrin ( TH022 ) was previously characterized as a ZIKV post-entry inhibitor in a cell-based system [ 17 ], and pinostrobin ( TH019 ) was a non-competitively inhibit DENV NS2B-3 protease (pro) activity in vitro [ 13 ]. Other flavanone derivatives were previously reported as inhibitors of the viral envelope (E) [ 11 ], NS2B-3 pro [ 14 ], NS5 polymerase (pol) [ 21 ], and cellular factors involving in viral replication [ 22 ].…”

Section: Resultsmentioning

confidence: 99%

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Dibromopinocembrin and Dibromopinostrobin Are Potential Anti-Dengue Leads with Mild Animal Toxicity

et al. 2020

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Dengue infection is one of the most deleterious public health concerns for two-billion world population being at risk. Plasma leakage, hemorrhage, and shock in severe cases were caused by immunological derangement from secondary heterotypic infection. Flavanone, commonly found in medicinal plants, previously showed potential as anti-dengue inhibitors for its direct antiviral effects and suppressing the pro-inflammatory cytokine from dengue immunopathogenesis. Here, we chemically modified flavanones, pinocembrin and pinostrobin, by halogenation and characterized them as potential dengue 2 inhibitors and performed toxicity tests in human-derived cells and in vivo animal model. Dibromopinocembrin and dibromopinostrobin inhibited dengue serotype 2 at the EC50s of 2.0640 ± 0.7537 and 5.8567 ± 0.5074 µM with at the CC50s of 67.2082 ± 0.9731 and >100 µM, respectively. Both of the compounds also showed minimal toxicity against adult C57BL/6 mice assessed by ALT and Cr levels in day one, three, and eight post-intravenous administration. Computational studies suggested the potential target be likely the NS5 methyltransferase at SAM-binding pocket. Taken together, these two brominated flavanones are potential leads for further drug discovery investigation.

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Section: Resultsmentioning

confidence: 67%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

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Dibromopinocembrin and Dibromopinostrobin Are Potential Anti-Dengue Leads with Mild Animal Toxicity

et al. 2020

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“…They analyzed cell viability and viral titers and finally identified pinocembrin (present in honey, tea, and red wine) as an anti-Zika compound. It was observed that the pinocembrin strongly inhibited the Zika virus infection in JEG-3infected cells, and also revealed that it inhibits the viral replication at post entry stages inside the cell (Lee et al 2019) . Likewise, LeCher et al (2019) have identified the potential phytochemical that is effective against herpes B virus.…”

Section: Flavonoids As Antiviral Agentsmentioning

confidence: 96%

Phytochemicals as Antiviral Agents: Recent Updates

Ghildiyal

Prakash

Chaudhary

et al. 2020

Plant-Derived Bioactives

131

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“…For example, ZIKV spread rapidly in 2015 in at least 33 regions and countries in Central and South America, such as Brazil, becoming an epidemic that affected between 0.5 and 1.5 million people [4e7]. ZIKV infection has been associated with several neurological complications, such as Guillain-Barr e syndrome in adults and microcephaly in infants [8,9].…”

Section: Introductionmentioning

confidence: 99%

Cephalotaxine inhibits Zika infection by impeding viral replication and stability

Lai

2020

Biochemical and Biophysical Research Communications

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a b s t r a c tThe Zika virus (ZIKV) is a mosquito-borne flavivirus that has reemerged as a serious public health problem around the world. Syndromes of infected people range from asymptomatic infections to severe neurological disorders, such as Guillain-Barr e syndrome and microcephaly. Screening anti-ZIKV drugs derived from Chinese medicinal herbs is one method of identifying antiviral agents. In this paper, we report that (1) Cephalotaxine (CET), an alkaloid isolated from Cephalotaxus drupacea, was effective in inhibiting ZIKV activity in vitro (i.e., in Vero and A549 cell lines) and (2) the mechanisms which underlie these effects involve virucidal activity and a decrease in viral replication. Specifically, CET was found to decrease ZIKV RNA and viral protein expression, inhibit ZIKV replication, and inhibit ZIKV mRNA/protein production. We also determined that CET is effective in inhibiting dengue virus 1e4 (DENV1-4). Taken together, our findings indicate that CET could be an effective lead compound in the treatment of ZIKV and also suggest that further investigation and development of CET-derived drugs may lead to a new class of anti-Flavivirus medications.

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Antiviral activity of pinocembrin against Zika virus replication

Cited by 72 publications

References 35 publications

Dibromopinocembrin and Dibromopinostrobin Are Potential Anti-Dengue Leads with Mild Animal Toxicity

Dibromopinocembrin and Dibromopinostrobin Are Potential Anti-Dengue Leads with Mild Animal Toxicity

Phytochemicals as Antiviral Agents: Recent Updates

Cephalotaxine inhibits Zika infection by impeding viral replication and stability

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