The comprehensive study on the therapeutic effects of baicalein for the treatment of COVID-19 in vivo and in vitro

Song, Junke; Xu, Yanfeng; Yang, Dezhi; Zhang, Li; Yang, Shumei; Zhang, Wen; Wang, Jinhua; Tian, Shuo; Yang, Shengqian; Yuan, Tianyi; Liu, Ailin; Lv, Qi; Li, Fengdi; Liu, Hongqi; Hou, Biyu; Peng, Xiaozhong; Lü, Yang; Du, Guanhua

doi:10.1016/j.bcp.2020.114302

Cited by 124 publications

(90 citation statements)

References 46 publications

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“…Previous studies have demonstrated that baicalein, both in naked, as well as nanoparticle-encapsulated forms were biocompatible to human gingival epithelial cells [ 19 ]. Furthermore, from the systemic context, baicalein has demonstrated hepatoprotective properties [ 20 ]. There is evidence to show the anti-quorum sensing activity and biofilm inhibitory potential of Baicalein against Staphylococcus aureus [ 21 ], Avian Pathogenic E. coli (APEC) [ 22 ] and Candida albicans [ 23 ].…”

Section: Introductionmentioning

confidence: 99%

Baicalein Inhibits Streptococcus mutans Biofilms and Dental Caries-Related Virulence Phenotypes

et al. 2021

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Dental caries, the most common oral disease, is a major public healthcare burden and affects more than three billion people worldwide. The contemporary understanding of the need for a healthy microbiome and the emergence of antimicrobial resistance has resulted in an urgent need to identify compounds that curb the virulence of pathobionts without microbial killing. Through this study, we have demonstrated for the first time that 5,6,7-trihydroxyflavone (Baicalein) significantly downregulates crucial caries-related virulence phenotypes in Streptococcus mutans. Baicalein significantly inhibited biofilm formation by Streptococcus mutans UA159 (MBIC50 = 200 μM), without significant growth inhibition. Notably, these concentrations of baicalein did not affect the commensal S. gordonii. Strikingly, baicalein significantly reduced cell surface hydrophobicity, autoaggregation and acid production by S. mutans. Mechanistic studies (qRT-PCR) showed downregulation of various genes regulating biofilm formation, surface attachment, quorum sensing, acid production and competence. Finally, we demonstrate the potential translational value of baicalein by reporting synergistic interaction with fluoride against S. mutans biofilms.

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Section: Introductionmentioning

confidence: 99%

Baicalein Inhibits Streptococcus mutans Biofilms and Dental Caries-Related Virulence Phenotypes

et al. 2021

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“…Additionally, this nutraceutical agent alleviated the lesions of lung tissue and suppressed replication of SARS-CoV-2 in mice. Furthermore, this compound improved respiratory function and reduced inflammation, corroborated by decreasing the level of IL-1β and TNF-α in lipopolysaccharide (LPS)-induced acute lung injury of mice [ 246 ]. Docking evidence revealed that flavonoids biochanin A and silymarin strongly interact with the active site of SARS-CoV-2 spike glycoprotein and ACE2, respectively [ 247 ].…”

Section: Importance Of Phytochemicals In Combating Covid-19mentioning

confidence: 99%

Targeting Multiple Signal Transduction Pathways of SARS-CoV-2: Approaches to COVID-19 Therapeutic Candidates

et al. 2021

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Due to the complicated pathogenic pathways of coronavirus disease 2019 (COVID-19), related medicinal therapies have remained a clinical challenge. COVID-19 highlights the urgent need to develop mechanistic pathogenic pathways and effective agents for preventing/treating future epidemics. As a result, the destructive pathways of COVID-19 are in the line with clinical symptoms induced by severe acute coronary syndrome (SARS), including lung failure and pneumonia. Accordingly, revealing the exact signaling pathways, including inflammation, oxidative stress, apoptosis, and autophagy, as well as relative representative mediators such as tumor necrosis factor-α (TNF-α), nuclear factor erythroid 2-related factor 2 (Nrf2), Bax/caspases, and Beclin/LC3, respectively, will pave the road for combating COVID-19. Prevailing host factors and multiple steps of SARS-CoV-2 attachment/entry, replication, and assembly/release would be hopeful strategies against COVID-19. This is a comprehensive review of the destructive signaling pathways and host–pathogen interaction of SARS-CoV-2, as well as related therapeutic targets and treatment strategies, including potential natural products-based candidates.

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“…Several studies have pointed out the anti-SARS-CoV-2 effects of S. baicalensis compounds, with an emphasis on baicalein and baicalin [36][37][38][39][40], wogonin [39], and oroxylin A [39].…”

Section: Ligand Preparationmentioning

confidence: 99%

“…Song et al [37] revealed that baicalein significantly inhibited replication of the virus and relieved the lesions of lung tissue in hACE2 transgenic mice infected with SARS-CoV-2. Moreover, Huang [41] noticed that baicalein and wogonin could be employed as the main active ingredients for the management of COVID-19 by targeting ACE2 and 3CLpro proteins.…”

Section: Ligand Preparationmentioning

confidence: 99%

Scutellaria baicalensis Flavones as Potent Drugs against Acute Respiratory Injury during SARS-CoV-2 Infection: Structural Biology Approaches

et al. 2020

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Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection can result in severe damage to the respiratory system. With no specific treatment to date, it is crucial to identify potent inhibitors of SARS-CoV-2 Chymotrypsin-like protease (3CLpro) that could also modulate the enzymes involved in the respiratory damage that accompanies SARS-CoV-2 infection. Here, flavones isolated from Scutellaria baicalensis (baicalein, baicalin, wogonin, norwogonin, and oroxylin A) were studied as possible compounds in the treatment of SARS-CoV-2 and SARS-CoV-2-induced acute lung injuries. We used structural bioinformatics and cheminformatics to (i) identify the critical molecular features of flavones for their binding activity at human and SARS-CoV-2 enzymes; (ii) predict their drug-likeness and lead-likeness features; (iii) calculate their pharmacokinetic profile, with an emphasis on toxicology; (iv) predict their pharmacodynamic profiles, with the identification of their human body targets involved in the respiratory system injuries; and (v) dock the ligands to SARS-CoV-2 3CLpro. All flavones presented appropriate drug-like and kinetics features, except for baicalin. Flavones could bind to SARS-CoV-2 3CLpro at a similar site, but interact slightly differently with the protease. Flavones’ pharmacodynamic profiles predict that (i) wogonin strongly binds at the cyclooxygenase2 and nitric oxide synthase; (ii) baicalein and norwogonin could modulate lysine-specific demethylase 4D-like and arachidonate 15-lipoxygenase; and (iii) baicalein, wogonin, norwogonin, and oroxylin A bind to SARS-CoV-2 3CLpro. Our results propose these flavones as possible potent drugs against respiratory damage that occurs during SARS-CoV-2 infections, with a strong recommendation for baicalein.

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The comprehensive study on the therapeutic effects of baicalein for the treatment of COVID-19 in vivo and in vitro

Abstract: Graphical abstract

Cited by 124 publications

References 46 publications

Baicalein Inhibits Streptococcus mutans Biofilms and Dental Caries-Related Virulence Phenotypes

Baicalein Inhibits Streptococcus mutans Biofilms and Dental Caries-Related Virulence Phenotypes

Targeting Multiple Signal Transduction Pathways of SARS-CoV-2: Approaches to COVID-19 Therapeutic Candidates

Scutellaria baicalensis Flavones as Potent Drugs against Acute Respiratory Injury during SARS-CoV-2 Infection: Structural Biology Approaches

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