Role of tannic acid against SARS-cov-2 cell entry by targeting the interface region between S-protein-RBD and human ACE2

Chen, Xi; Wang, Ziyuan; Wang, Jing; Yao, Yifan; Wang, Qian; Huang, Jiahao; Xiang, Xianping; Zhou, Yifan; Xue, Yan; Li, Yan; Gao, Xiang; Wang, Lijun; Chu, Ming; Wang, Yuedan

doi:10.3389/fphar.2022.940628

“…In addition, tannic acid has shown potent inhibition of main protease (Mpro)/3CLpro and TMPRSS2, which are essential proteins for the propagation of SARS-CoV-2 [69,70]. In particular, it was confirmed that tannic acid prevented pseudotyped SARS-CoV-2 entrance by preventing S-RBD from attaching to ACE2 [71,72]. Notably, orally administered tannic acid isomers have exhibited effectiveness against SARS-CoV-2 variants such as Delta and Omicron [73].…”

Section: Antiviral Activities Of Compounds Against the Pseudotyped Vi...mentioning

confidence: 96%

Antiviral Effects of Secondary Metabolites from Jatropha podagrica Leaves against the Pseudotyped Virus of SARS-CoV-2 Omicron

Jang,

Lee,

Ju

et al. 2023

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Jatropha podagrica holds a longstanding place in traditional herbal medicine, primarily utilized for addressing skin infections, acting as antipyretics, diuretics, and purgatives. In this study, our primary objective was to investigate the secondary metabolites present in J. podagrica leaves, with the aim of pinpointing natural compounds exhibiting potential antiviral activities. Five secondary metabolites (1–5), including an auronol glycoside (1), two coumarins (2 and 3), a chromane (4) and a gallotannin (5), were isolated from J. podagrica leaves. Compound 1 presented as an amalgamation of unseparated mixtures, yet its intricate composition was adroitly unraveled through the strategic deployment of a chiral HPLC column. This tactic yielded the isolation of epimers (+)-1 and (−)-1, ascertained as unreported auronol glycosides. The structures of these novel compounds, (+)-1 and (−)-1, were elucidated to be (2S)-hovetrichoside C [(+)-1] and (2R)-hovetrichoside C [(−)-1] through NMR data and HR-ESIMS analyses, enzymatic hydrolysis, and comparison of optical rotation values. Cytotoxicity and antiviral effects were assessed for the isolated compounds ((+)-1, (−)-1 and 2–5), along with compound 1a (the aglycone of 1), in the A549 human alveolar basal epithelial cell line. Each compound demonstrated a cell viability of approximately 80% or higher, confirming their non-toxic nature. In the group of compounds, compounds 3–5 demonstrated antiviral effects based on RT-qPCR results, with individual enhancements ranging from approximately 28 to 38%. Remarkably, compound 4 exhibited the most substantial antiviral effect. Utilization of compound 4 to assess immune boosting and anti-inflammatory effects revealed increased levels of STING, RIG-I, NLRP3, and IL-10 along with a decrease in TNF-α and IL-6. Therefore, these findings underscore the potential of these active compounds 3–5 not only as therapeutic agents for SARS-CoV-2 but also as new contenders for upcoming pandemics.

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Chemical Recording of Pump‐Specific Drug Efflux in Living Cells

Sun,

Chen,

Yang

et al. 2024

Angewandte Chemie

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Drug efflux — a process primarily facilitated by efflux pumps such as multidrug resistance proteins (MRPs) — plays a pivotal role in cellular resistance to chemotherapy resistance. Conventional approaches to assess drug efflux are predominantly conducted in vitro and often lack pump specificity. Here we report the bioorthogonal reporter inhibiting efflux (BRIEF) strategy, which enables the recording of pump‐specific drug efflux in living cells. In BRIEF, a specific substrate is engineered as a bioorthogonal efflux probe (BEP) for specific pumps. The cellular concentration and protein labeling level of the probe can be augmented when the test drug is transported by the same pumps. Serendipitously, we discovered that per‐O‐acetylated unnatural monosaccharides, initially designed for metabolic glycan labeling, are exported by some MRPs. Using Ac4GlcNAl as a BEP, we studied the structure‐efflux relationship of flavonoids and identified small molecules, including tannic acid, cholesterol and gallic acid, as novel MRP substrates in high‐throughput screening. Tannic acid, known for anti‐tumor and anti‐SARS‐CoV‐2 properties, showed increased efficacy upon MRP inhibition. Additionally, BRIEF was adapted to assess p‐glycoprotein‐mediated efflux using Rhodamine 123 as a BEP, leveraging its light‐activatable proximity labeling ability. BRIEF provides a versatile approach to investigate drug efflux and enhance chemotherapy strategies.

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Chemical Recording of Pump‐Specific Drug Efflux in Living Cells

Sun,

Chen,

Yang

et al. 2024

Angew Chem Int Ed

0

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Drug efflux — a process primarily facilitated by efflux pumps such as multidrug resistance proteins (MRPs) — plays a pivotal role in cellular resistance to chemotherapy resistance. Conventional approaches to assess drug efflux are predominantly conducted in vitro and often lack pump specificity. Here we report the bioorthogonal reporter inhibiting efflux (BRIEF) strategy, which enables the recording of pump‐specific drug efflux in living cells. In BRIEF, a specific substrate is engineered as a bioorthogonal efflux probe (BEP) for specific pumps. The cellular concentration and protein labeling level of the probe can be augmented when the test drug is transported by the same pumps. Serendipitously, we discovered that per‐O‐acetylated unnatural monosaccharides, initially designed for metabolic glycan labeling, are exported by some MRPs. Using Ac4GlcNAl as a BEP, we studied the structure‐efflux relationship of flavonoids and identified small molecules, including tannic acid, cholesterol and gallic acid, as novel MRP substrates in high‐throughput screening. Tannic acid, known for anti‐tumor and anti‐SARS‐CoV‐2 properties, showed increased efficacy upon MRP inhibition. Additionally, BRIEF was adapted to assess p‐glycoprotein‐mediated efflux using Rhodamine 123 as a BEP, leveraging its light‐activatable proximity labeling ability. BRIEF provides a versatile approach to investigate drug efflux and enhance chemotherapy strategies.

show abstract

Role of tannic acid against SARS-cov-2 cell entry by targeting the interface region between S-protein-RBD and human ACE2

Cited by 3 publications

References 49 publications

Antiviral Effects of Secondary Metabolites from Jatropha podagrica Leaves against the Pseudotyped Virus of SARS-CoV-2 Omicron

Antiviral Effects of Secondary Metabolites from Jatropha podagrica Leaves against the Pseudotyped Virus of SARS-CoV-2 Omicron

Chemical Recording of Pump‐Specific Drug Efflux in Living Cells

Chemical Recording of Pump‐Specific Drug Efflux in Living Cells

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