Myricetin inhibits panel of kinases implicated in tumorigenesis

Stoll, Stefani Natali; Bitencourt, Shanna; Laufer, Stefan; Goettert, Márcia Inês

doi:10.1111/bcpt.13201

Cited by 16 publications

(7 citation statements)

References 37 publications

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“…36,37,40 Myricetin has also been reported as an inhibitor against multiple kinases implicated in tumorigenesis. 41 Furthermore, hyperoside was identified as an effective inhibitor of human cytochrome P450 2D6 (CYP2D6) with an IC 50 of 1.2 μM. 42 Our cocrystal structure showed that myricetin allosterically inhibited RNase L activity by binding to the ATP pocket, which is similar to sunitinib as characterized in our previous study.…”

Section: ■ Discussion and Conclusionmentioning

confidence: 64%

“…Hyperoside is often isolated from various medicinal plants, for example Hypericum perforatum and Crataegus davisii . Many pharmacological studies reported that myricetin, vitexin, and hyperoside can be used in anti-inflammatory responses and cardioprotective, antiviral, and antitumor treatments. ,, Myricetin has also been reported as an inhibitor against multiple kinases implicated in tumorigenesis . Furthermore, hyperoside was identified as an effective inhibitor of human cytochrome P450 2D6 (CYP2D6) with an IC 50 of 1.2 μM …”

Section: Discussionmentioning

confidence: 99%

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Identification of Small Molecule Inhibitors of RNase L by Fragment-Based Drug Discovery

et al. 2021

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The pseudokinase-endoribonuclease RNase L plays important roles in antiviral innate immunity and is also implicated in many other cellular activities. The inhibition of RNase L showed therapeutic potential for Aicardi-Goutières syndrome (AGS). Thus, RNase L is a promising drug target. In this study, using an enzyme assay and NMR screening, we discovered 13 inhibitory fragments against RNase L. Cocrystal structures of RNase L separately complexed with two different fragments were determined in which both fragments bound to the ATP-binding pocket of the pseudokinase domain. Myricetin, vitexin, and hyperoside, three natural products sharing similar scaffolds with the fragment AC40357, demonstrated a potent inhibitory activity in vitro. In addition, myricetin has a promising cellular inhibitory activity. A cocrystal structure of RNase L with myricetin provided a structural basis for inhibitor design by allosterically modulating the ribonuclease activity. Our findings demonstrate that fragment screening can lead to the discovery of natural product inhibitors of RNase L.

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Section: ■ Discussion and Conclusionmentioning

confidence: 64%

Section: Discussionmentioning

confidence: 99%

Identification of Small Molecule Inhibitors of RNase L by Fragment-Based Drug Discovery

et al. 2021

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“…Myricetin is found in a variety of fruits and vegetables, nutrient‐enriched foods, especially grapes, and berries used in winemaking (Wang et al, 2019). Some studies reported that myricetin has antihypertensive and antitumor effects (Godse et al, 2010; Jiang et al, 2019; Stoll et al, 2019). Cetin‐Karaca & Newman (2015) found that myricetin showed significant antimicrobial activity against Escherichia coli , Salmonella paratyphi , Salmonella enterica , and Salmonella enteritidis .…”

Section: Resultsmentioning

confidence: 99%

“…Myricetin is found in a variety of fruits and vegetables, nutrient-enriched foods, especially grapes, and berries used in winemaking (Wang et al, 2019). Some studies reported that myricetin has antihypertensive and antitumor effects (Godse et al, 2010;Jiang et al, 2019;Stoll et al, 2019).…”

Section: The Major Phenolic Components Of Kefir Samples Containingmentioning

confidence: 99%

Phenolic compounds, amino acid profiles, and antibacterial properties of kefir prepared using freeze‐dried Arbutus unedo L. and Tamarindus indica L. fruits and sweetened with stevia, monk fruit sweetener, and aspartame

Günaydı

Ayar

2022

Food Processing Preservation

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| INTRODUC TI ON"Added sugar" means sugar (beet sugar or cane sugar) added to foods during production, preparation, and consumption to improve flavor and textural properties and increase the energy value of foods (McCain et al., 2018). Since excessive sugar consumption causes health problems such as obesity, hypertension, and diabetes, in recent years, product development studies have focused on using natural or artificial low-calorie sweeteners instead of sugar (Beltrami et al., 2018). The sweeteners permitted for use in food by the US Food and Drug Administration (FDA) are acesulfame-potassium, aspartame, advantame, neotame, saccharin, sucralose, steviol glycosides purified from the leaves of Stevia rebaudiana (Bertoni) Bertoni (≥95% pure) and Siraitia grosvenorii (monk fruit) extracts (containing 25%, 45%, or 55% Mogroside V). Compared to table sugar (sucrose), the sweetness degree of these sweeteners varies between 100× and 20,000× (FDA, 2018;Sylvetsky & Rother, 2016).Fermented dairy products are widely consumed worldwide and become more attractive to consumers as their health effects are understood more clearly (García-Burgos et al., 2020). The health effects of these products are mostly due to the probiotics they contain, and they have gained an important place among functional

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“…56 Its protective effects in chronic diseases may be achieved by inhibiting inflammation-triggering and related protein kinases with the potential to treat COPD. 57 In emphysema models, ellagic acid, as a natural antioxidant, has a protective effect against pulmonary hypertension and the development of lung and heart damage induced by elastase. 58 Luteolin, a natural flavonoid, can treat COPD by altering the M1/M2 polarization of macrophages, thereby exerting anti-inflammatory effects through downregulation of p-STAT3 and upregulation of p-STAT6, 59 as well as through ERK-mediated inflammation, apoptosis, and autophagy inhibition.…”

Section: Discussionmentioning

confidence: 99%

Unraveling the Molecular Mechanism of Xuebijing Injection in the Treatment of Chronic Obstructive Pulmonary Disease by Combining Network Pharmacology and Affymetrix Array

Lin

Zhang

et al. 2022

Natural Product Communications

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Xuebijing injection (XBJ), one of the classical prescriptions for treating inflammation-related diseases, has been used to chronic obstructive pulmonary disease (COPD) in clinical practice. However, its molecular mechanism is still unclear. Network pharmacology combined with Affymetrix arrays and molecular docking techniques were applied to explore the molecular mechanism of XBJ for COPD. Predictive analysis of 728 active compounds in XBJ and 6 sets of Affymetrix arrays expression data resulted in 106 potential therapeutic targets. Next, based on the active compound-co-target network topology analysis, most of these targets were found to be modulated by quercetin, myricetin, and ellagic acid. Furthermore, protein–protein interaction (PPI) analysis revealed that the key targets may be EGFR, STAT3, AKT1, CCND1, MMP9, AR, ESR1, and PTGS2. Then, by constructing a component-target-pathway network, we found that XBJ was a multi-pathway, multi-target, multi-compound synergistic therapy for COPD, and four key targets were involved in the FoxO signaling pathway. Luteolin and salvianolic acid b had the optimal binding ability to several key proteins. Therefore, we hypothesize that quercetin, myricetin, ellagic acid, luteolin, and salvianolic acid b mainly contribute to the therapeutic effect of XBJ on COPD by modulating the FoxO signaling pathway by regulating EGFR, STAT3, AKT1, and CCND1. XBJ exerts anti-inflammatory and antioxidative stress effects through the PI3K/Akt/FoxO axis combined with MMP9, AR, ESR1, and PTGS2 to regulate other signaling pathways.

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Myricetin inhibits panel of kinases implicated in tumorigenesis

Cited by 16 publications

References 37 publications

Identification of Small Molecule Inhibitors of RNase L by Fragment-Based Drug Discovery

Identification of Small Molecule Inhibitors of RNase L by Fragment-Based Drug Discovery

Phenolic compounds, amino acid profiles, and antibacterial properties of kefir prepared using freeze‐dried Arbutus unedo L. and Tamarindus indica L. fruits and sweetened with stevia, monk fruit sweetener, and aspartame

Unraveling the Molecular Mechanism of Xuebijing Injection in the Treatment of Chronic Obstructive Pulmonary Disease by Combining Network Pharmacology and Affymetrix Array

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