Baicalin and Baicalein Inhibit Src Tyrosine Kinase and Production of IL-6

Jelić, Dubravko; Lower-Nedza, Agnieszka D.; Brantner, Adelheid; Blažeković, Biljana; Bian, Baolin; Yang, Jian; Brajša, Karmen; Vladimir‐Knežević, Sanda

doi:10.1155/2016/2510621

Cited by 16 publications

(9 citation statements)

References 23 publications

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“…It has been demonstrated that DENinduced inflammation triggers ROS production, which activates NF-κB followed by release of pro-inflammatory cytokine (IL-6), chemokines and iNOS-all these events leads to hepatocarcinogenesis (44) . Our results are consistent with the research results of Jelic et al, (45) confirming the anti-inflammatory potential effect of resveratrol decreasing IL-6 levels.…”

Section: (30)supporting

confidence: 94%

Therapeutic Effects of Resveratrol and Baicalein on Hepatocellular Carcinoma Induced In Rats

Fekry¹,

Keshta²,

Nawara³

2016

Biochemistry Letters

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Background: Hepatocellular carcinoma (HCC), one of the most common cancers in the world, is a leading cause of cancer-related mortality. Resveratrol (RSV) and Baicalein (BE) are naturally derived polyphenolic compounds showed promising chemo-preventive effects against cancer. Aim: The present study aims to investigate the antioxidant activity of RSV and/or BE against induced HCC in rats. Methods: 48 Swiss male adult albino rats were divided into 6 groups: Group I served as a negative control injected intraperitoneally (I.P) with sterile saline; Group II were injected I.P with (0.25%) Dimethylsulphoxide (DMSO); Group III were injected I.P with Diethylnitrosamine (DEN) (200 mg/kg.bw) once; Group IV injected by DEN then treated with BE (20 mg/kg.bw) I.P for 10 consecutive days; Group V injected by DEN then treated with RSV (2.5 mg/kg.bw) orally for consecutive 10 days; Group VI injected by DEN then treated with BE and RSV. Plasma was collected for some biochemical studies and different antioxidant assays. Results: DEN-induced HCC that manifested by a significant drop in antioxidants levels, alterations in liver functions, and induced-inflammation. While, treatment with RSV and/or BE ameliorated liver injury by decreasing (alanine transferase (ALT), aspartate transferase (AST) activities, and Galectin-3 (Gal-3) levels. Also, they reversed the oxidative stress by the reduction of malondialdehyde (MDA) and nitric oxide (NO) levels and restoration of superoxide dismutase (SOD), glutathione-S-transferase (GST) activities, and reduced glutathione (GSH) levels. They decreased interlukin-6 (IL-6) levels. These data suggested that RSV or BE exhibited a significant role against HCC, which might be related to their antioxidant and antiinflammatory activities. Conclusions:Although combined treatment with RSV and BE significantly exerting a potential therapeutic effects, individual administration was more effective in HCC treatment. These novel findings suggested that RSV and BE have an antagonistic effect suggesting concerted efforts are needed to identify the most optimal combinatorial strategies.

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Section: (30)supporting

confidence: 94%

Therapeutic Effects of Resveratrol and Baicalein on Hepatocellular Carcinoma Induced In Rats

Fekry¹,

Keshta²,

Nawara³

2016

Biochemistry Letters

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“…The results of Tsai [ 36 ] revealed that baicalein can protect against the acute lung injury induced by lipopolysaccharide in rats. The results of Jeli [ 37 ] revealed that baicalein exhibit good inhibitory activities of both production of cytokine IL-6 and tyrosine kinase.…”

Section: Discussionmentioning

confidence: 99%

The antityrosinase and antioxidant activities of flavonoids dominated by the number and location of phenolic hydroxyl groups

Ai-ren

Dong

et al. 2018

Chin Med

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BackgroundCompounds with the ability to scavenge reactive oxygen species (ROS) and inhibit tyrosinase may be useful for the treatment and prevention from ROS-related diseases. The number and location of phenolic hydroxyl of the flavonoids will significantly influence the inhibition of tyrosinase activity. Phenolic hydroxyl is indispensable to the antioxidant activity of flavonoids. Isoeugenol, shikonin, baicalein, rosmarinic acid, and dihydromyricetin have respectively one, two, three, four, or five phenolic hydroxyls. The different molecular structures with the similar structure to l-3,4-dihydroxyphenylalanine (l-DOPA) were expected to the different antityrosinase and antioxidant activities.MethodsThis investigation tested the antityrosinase activity, the inhibition constant, and inhibition type of isoeugenol, shikonin, baicalein, rosmarinic acid, and dihydromyricetin. Molecular docking was examined by the Discovery Studio 2.5 (CDOCKER Dock, Dassault Systemes BIOVIA, USA). This experiment also examined the antioxidant effects of the five compounds on supercoiled pBR322 plasmid DNA, lipid peroxidation in rat liver mitochondria in vitro, and DPPH, ABTS, hydroxyl, or superoxide free radical scavenging activity in vitro.ResultsThe compounds exhibited good antityrosinase activities. Molecular docking results implied that the compounds could interact with the amino acid residues in the active site center of antityrosinase. These compounds also exhibited antioxidant effects on DPPH, ABTS, hydroxyl, or superoxide free radical scavenging activity in vitro, lipid peroxidation in rat liver mitochondria induced by Fe2+/vitamin C system in vitro, and supercoiled pBR322 plasmid DNA. The activity order is isoeugenol < shikonin < baicalein < rosmarinic acid < dihydromyricetin. The results showed the compounds with more phenolic hydroxyls have more antioxidant and antityrosinase activities.ConclusionThis was the first study of molecular docking for modeling the antityrosinase activity of compounds. This was also the first study of the protective effects of compounds on supercoiled pBR322 plasmid DNA, the lipid peroxidation inhibition activity in liver mitochondria. These results suggest that the compounds exhibited antityrosinase and antioxidant activities may be useful in skin pigmentation and food additives.Electronic supplementary materialThe online version of this article (10.1186/s13020-018-0206-9) contains supplementary material, which is available to authorized users.

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“…Natural flavone, baicalein is a bioactive compound which was first isolated from the roots of Scutellaria baicalensis Georgi (Baikal/Chinese skullcap) and Scutellaria lateriflora L. (American skullcap), flowering plants in the family Lamiaceae. However, it is also present in leaves of Thymus vulgaris L. (common thyme) as well as in Oroxylum indicum (L.) Kurz (Indian trumpet flower) (11).…”

Section: Sources Of Baicalein and Related Compoundsmentioning

confidence: 99%

Can Baicalein Become a New Drug for Covid-19?

Patočka¹,

Navrátilová²,

Kuča³

et al. 2021

Mil. Med. Sci. Lett.

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The ongoing coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become a global health crisis. Flavon baicalein, a major bioactive molecule of Scutellaria baicalensis, inhibits the replication of SARS-CoV-2 which causes severe acute respiratory syndrome in humans. Animal experiments show that baicalein has the character of a broad-spectrum coronavirus drug. It is non-toxic and can inhibit SARS-CoV-2-induced damage. Baicalein may therefore be a promising therapeutic drug for the treatment of COVID-19.

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Baicalin and Baicalein Inhibit Src Tyrosine Kinase and Production of IL-6

Cited by 16 publications

References 23 publications

Therapeutic Effects of Resveratrol and Baicalein on Hepatocellular Carcinoma Induced In Rats

Therapeutic Effects of Resveratrol and Baicalein on Hepatocellular Carcinoma Induced In Rats

The antityrosinase and antioxidant activities of flavonoids dominated by the number and location of phenolic hydroxyl groups

Can Baicalein Become a New Drug for Covid-19?

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