Active Ingredients of Reduning Injection Maintain High Potency against SARS-CoV-2 Variants

Zhang, Xiao; Xu, Huan; Qu, Ze-yang; Ma, Xiaoxin; Huang, Boxuan; Sun, Meng-si; Wang, Buqing; Wang, Guanyu

doi:10.1007/s11655-022-3686-5

Cited by 6 publications

(6 citation statements)

References 36 publications

(36 reference statements)

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“…Moreover, luteolin has been found to directly inhibit SARS‐CoV‐2 infection. In October 2022, Xiao et al (2022) demonstrated that luteolin, the main active component of redundancy injections, binds to the S‐protein of SARS‐CoV‐2 and inhibits its replication in BHK21‐hACE2 cells. In addition, luteolin inhibits the activities of the main protease (Chaves et al, 2022) and RNA‐dependent RNA polymerase (Munafò et al, 2022) of SARS‐CoV‐2, leading to the inhibition of viral replication in vivo.…”

Section: Introductionmentioning

confidence: 99%

Luteolin inhibits spike protein of severe acute respiratory syndrome coronavirus‐2 (SARS‐CoV‐2) binding to angiotensin‐converting enzyme 2

Zhu,

Yan,

Shi

et al. 2023

Phytotherapy Research

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Severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) causes coronavirus disease 2019 (COVID‐19), a respiratory illness that poses a serious threat to global public health. In an essential step during infection, SARS‐CoV‐2 uses the receptor‐binding domain (RBD) of the spike (S) protein to engage with angiotensin‐converting enzyme 2 (ACE2) in host cells. Chinese herbal medicines and their active components exhibit antiviral activity, with luteolin being a flavonoid that can significantly inhibit SARS‐CoV infection. However, whether it can block the interaction between the S‐protein RBD of SARS‐CoV‐2 and ACE2 has not yet been elucidated. Here, we investigated the effects of luteolin on the binding of the S‐protein RBD to ACE2. By employing a competitive binding assay in vitro, we found that luteolin significantly blocked the binding of S‐protein RBD to ACE2 with IC50 values of 0.61 mM, which was confirmed by the neutralized infection with SARS‐CoV‐2 pseudovirus in vivo. A surface plasmon resonance‐based competition assay revealed that luteolin significantly affects the binding of the S‐protein RBD to the ACE2 receptor. Molecular docking was performed to predict the binding sites of luteolin to the S‐protein RBD‐ACE2 complex. The active binding sites were defined based on published literature, and we found that luteolin might interfere with the mixture at residues including LYS353, ASP30, and TYR83 in the cellular ACE2 receptor and GLY496, GLN498, TYR505, LEU455, GLN493, and GLU484 in the S‐protein RBD. These residues may together form attractive charges and destroy the stable interaction of S‐protein RBD‐ACE2. Luteolin also inhibits SARS‐CoV‐2 spike protein‐induced platelet spreading, thereby inhibiting the binding of the spike protein to ACE2. Our results are the first to provide evidence that luteolin is an anti‐SARS‐CoV‐2 agent associated with interference between viral S‐protein RBD‐ACE2 interactions.

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Section: Introductionmentioning

confidence: 99%

Luteolin inhibits spike protein of severe acute respiratory syndrome coronavirus‐2 (SARS‐CoV‐2) binding to angiotensin‐converting enzyme 2

Zhu,

Yan,

Shi

et al. 2023

Phytotherapy Research

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“…Pseudovirusbased assays have facilitated the screening of natural compounds for their ability to inhibit SARS-CoV-2 entry into host cells. Furthermore, pseudovirus technology has been crucial in studying the mechanisms of action of potential antiviral compounds against SARS-CoV-2 and its variants [60][61][62][63][64][65][66][67][68][69][72][73][74][75][76][77][78][79][80][82][83][84][85]. Luteolin-7-O-glucuronide (L7OG) and folic acid (FA) showed promising entry inhibitory activity against SARS-CoV-2 pseudotypes harboring alpha and omicron spike proteins [60].…”

Section: Discussionmentioning

confidence: 99%

“…Recently, a similar study was reported by Xiao, Z regarding SARS-CoV-2. A pseudovirus system tested the efficacy of quercetin and luteolin to inhibit SARS CoV-2 pseudovirus and genetic variants of SARS-CoV-2, including alpha variant B.1.1.7, beta variant B.1.351, delta variant B.1.617, and omicron [83].…”

Section: Natural Therapeutic Compounds Against Coronavirusesmentioning

confidence: 99%

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Pseudovirus-Based Systems for Screening Natural Antiviral Agents: A Comprehensive Review

Trischitta,

Tamburello,

Venuti

et al. 2024

IJMS

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Since the outbreak of COVID-19, researchers have been working tirelessly to discover effective ways to combat coronavirus infection. The use of computational drug repurposing methods and molecular docking has been instrumental in identifying compounds that have the potential to disrupt the binding between the spike glycoprotein of SARS-CoV-2 and human ACE2 (hACE2). Moreover, the pseudovirus approach has emerged as a robust technique for investigating the mechanism of virus attachment to cellular receptors and for screening targeted small molecule drugs. Pseudoviruses are viral particles containing envelope proteins, which mediate the virus’s entry with the same efficiency as that of live viruses but lacking pathogenic genes. Therefore, they represent a safe alternative to screen potential drugs inhibiting viral entry, especially for highly pathogenic enveloped viruses. In this review, we have compiled a list of antiviral plant extracts and natural products that have been extensively studied against enveloped emerging and re-emerging viruses by pseudovirus technology. The review is organized into three parts: (1) construction of pseudoviruses based on different packaging systems and applications; (2) knowledge of emerging and re-emerging viruses; (3) natural products active against pseudovirus-mediated entry. One of the most crucial stages in the life cycle of a virus is its penetration into host cells. Therefore, the discovery of viral entry inhibitors represents a promising therapeutic option in fighting against emerging viruses.

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“…Additionally, luteolin also inhibits RdRp activity [ 25 ]. Xiao et al, in a SARS-CoV-2 pseudovirus experiment, discovered that luteolin is able to bind to the S protein and significantly inhibits the entry of SARS-CoV-2 into cells with an EC50 less than 7 μmol/L [ 118 ]. COVID-19 can cause a loss of smell or taste.…”

Section: Anti-sars-cov-2 Activity Of Flavonoidsmentioning

confidence: 99%

A Comprehensive Review of Natural Flavonoids with Anti-SARS-CoV-2 Activity

Yang

Liu

et al. 2023

Molecules

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The COVID-19 pandemic caused by SARS-CoV-2 has majorly impacted public health and economies worldwide. Although several effective vaccines and drugs are now used to prevent and treat COVID-19, natural products, especially flavonoids, showed great therapeutic potential early in the pandemic and thus attracted particular attention. Quercetin, baicalein, baicalin, EGCG (epigallocatechin gallate), and luteolin are among the most studied flavonoids in this field. Flavonoids can directly or indirectly exert antiviral activities, such as the inhibition of virus invasion and the replication and inhibition of viral proteases. In addition, flavonoids can modulate the levels of interferon and proinflammatory factors. We have reviewed the previously reported relevant literature researching the pharmacological anti-SARS-CoV-2 activity of flavonoids where structures, classifications, synthetic pathways, and pharmacological effects are summarized. There is no doubt that flavonoids have great potential in the treatment of COVID-19. However, most of the current research is still in the theoretical stage. More studies are recommended to evaluate the efficacy and safety of flavonoids against SARS-CoV-2.

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Active Ingredients of Reduning Injection Maintain High Potency against SARS-CoV-2 Variants

Cited by 6 publications

References 36 publications

Luteolin inhibits spike protein of severe acute respiratory syndrome coronavirus‐2 (SARS‐CoV‐2) binding to angiotensin‐converting enzyme 2

Luteolin inhibits spike protein of severe acute respiratory syndrome coronavirus‐2 (SARS‐CoV‐2) binding to angiotensin‐converting enzyme 2

Pseudovirus-Based Systems for Screening Natural Antiviral Agents: A Comprehensive Review

A Comprehensive Review of Natural Flavonoids with Anti-SARS-CoV-2 Activity

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