Ivy leaves dry extract EA 575® mediates biased β2-adrenergic receptor signaling

Meurer, Fabio; Schulte-Michels, Janka; Häberlein, Hanns; Franken, Sebastian

doi:10.1016/j.phymed.2021.153645

Cited by 4 publications

(6 citation statements)

References 29 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Этот сдвиг в сторону передачи сиг налов G-белка/цАМФ обеспечивает молекулярную осно ву для клинически доказанной эффективности препара тов плюща при лечении заболеваний нижних дыхатель ных путей. В этом свете препараты на основе плюща потенциально могут уменьшить p-аррестин-опосредованные побочные эффекты в новых комбинированных терапевтических подходах [22]. Кроме того, были выяв лены противовоспалительные эффекты сухого экстракта листьев плюща через влияние на транскрипционную активность NFkB.…”

Section: Infections In Otorhinolaryngologyunclassified

The place of phytotherapy in the treatment of acute upper respiratory tract infections

Орлова

2022

Medicinskij sovet

View full text Add to dashboard Cite

Phytotherapy is based on the use of herbal medicines. Treatment with phytopreparations is characterized by efficiency, low risk of adverse events and the ability to enhance the effect of complex therapy. Herbal preparations are subject to standard requirements for quality control, safety and effectiveness. Inflammatory diseases of the respiratory tract are characterized by numerous symptoms that significantly reduce the quality of life of the patient. Along with pathogenetic therapy, symptomatic treatment is used. For the treatment of respiratory diseases, phytopreparations with antipyretic, immunomodulatory, anti-inflammatory, antitussive, mucolytic, bronchodilator and other clinically proven effects are used. The most common symptom of inflammatory diseases of the respiratory tract is cough. Many medicinal plants have antitussive effects. Ivy leaf extract has pronounced antitussive and mucolytic properties. The therapeutic effects of ivy are primarily due to the presence of saponins in its composition. Numerous randomized controlled trials have proven the efficacy and safety of H. Helix-based drugs in the treatment of cough in adults. A meta-analysis conducted by Barnes LA et al revealed that monopreparations and combined phytopreparations, including H. Helix, reduce the frequency and intensity of cough caused by viral respiratory infection. In a study involving 5,162 children, efficacy in the treatment of productive cough in children was proven. Currently, there are several medicines based on ivy leaves in liquid and solid forms on the pharmaceutical market of Russia. It leading position in sales of mucolytic agents of plant origin in Russia, due to its high efficiency and low frequency of adverse events.

show abstract

Section: Infections In Otorhinolaryngologyunclassified

The place of phytotherapy in the treatment of acute upper respiratory tract infections

Орлова

2022

Medicinskij sovet

View full text Add to dashboard Cite

show abstract

“…This biased signalling by EA 575 ® provides an explanation for the bronchospasmolytic and secretolytic effects and a reduction in βarrestin-mediated negative adverse effects [6]. The anti-inflammatory effects of EA 575 ® are substantiated by the β-arrestin-independent inhibition of NFκB, presumably by the inhibition of IκBα phosphorylation, leading to decreased IL-6 release [6,10,11].…”

Section: Introductionmentioning

confidence: 99%

“…Until now, the main mechanism of action has been explained by influencing the β 2 -adrenergic receptor (β 2 -AR). It has been shown that α-hederin identified in EA 575 ® indirectly inhibits the GRK2-mediated phosphorylation of β 2 -AR [5], which is the reason for the decrease in the recruitment of β-arrestin 2 by EA 575 ® [6]. This leads to the inhibition of β 2 -AR internalisation [7][8][9], which, in turn, results in increased β 2 -adrenergic responsiveness, as evidenced by a corresponding increase in receptor binding and cAMP formation [6,8].…”

Section: Introductionmentioning

confidence: 99%

“…It has been shown that α-hederin identified in EA 575 ® indirectly inhibits the GRK2-mediated phosphorylation of β 2 -AR [5], which is the reason for the decrease in the recruitment of β-arrestin 2 by EA 575 ® [6]. This leads to the inhibition of β 2 -AR internalisation [7][8][9], which, in turn, results in increased β 2 -adrenergic responsiveness, as evidenced by a corresponding increase in receptor binding and cAMP formation [6,8]. This biased signalling by EA 575 ® provides an explanation for the bronchospasmolytic and secretolytic effects and a reduction in βarrestin-mediated negative adverse effects [6].…”

Section: Introductionmentioning

confidence: 99%

“…This leads to the inhibition of β 2 -AR internalisation [7][8][9], which, in turn, results in increased β 2 -adrenergic responsiveness, as evidenced by a corresponding increase in receptor binding and cAMP formation [6,8]. This biased signalling by EA 575 ® provides an explanation for the bronchospasmolytic and secretolytic effects and a reduction in βarrestin-mediated negative adverse effects [6]. The anti-inflammatory effects of EA 575 ® are substantiated by the β-arrestin-independent inhibition of NFκB, presumably by the inhibition of IκBα phosphorylation, leading to decreased IL-6 release [6,10,11].…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Ivy Leaf Dry Extract EA 575® Has an Inhibitory Effect on the Signalling Cascade of Adenosine Receptor A2B

Meurer

Häberlein

Franken

2023

IJMS

Self Cite

View full text Add to dashboard Cite

Ivy leaf dry extract EA 575® is used to improve complaints of chronic inflammatory bronchial diseases and acute inflammation of the respiratory tract accompanied by coughing. Its mechanism of action has so far been explained by influencing β2-adrenergic signal transduction. In the present study, we investigated a possible influence on adenosine receptor A2B (A2BAR) signalling, as it has been described to play a significant and detrimental role in chronic inflammatory airway diseases. The influence of EA 575® on A2BAR signalling was assessed with measurements of dynamic mass redistribution. Subsequently, the effects on A2BAR-mediated second messenger cAMP levels, β-arrestin 2 recruitment, and cAMP response element (CRE) activation were examined using luciferase-based HEK293 reporter cell lines. Lastly, the impact on A2BAR-mediated IL-6 release in Calu-3 epithelial lung cells was investigated via the Lumit™ Immunoassay. Additionally, the adenosine receptor subtype mediating these effects was specified, and A2BAR was found to be responsible. The present study demonstrates an inhibitory influence of EA 575® on A2BAR-mediated general cellular response, cAMP levels, β-arrestin 2 recruitment, CRE activation, and IL-6 release. Since these EA 575®-mediated effects occur within a time frame of several hours of incubation, its mode of action can be described as indirect. The present data are the first to describe an inhibitory effect of EA 575® on A2BAR signalling. This may offer an explanation for the beneficial clinical effects of the extract in adjuvant asthma therapy.

show abstract

Future directions for the discovery of natural product-derived immunomodulating drugs: an IUPHAR positional review

Wainwright

Teixeira

Adelson

et al. 2022

Pharmacological Research

View full text Add to dashboard Cite

Ivy leaves dry extract EA 575® mediates biased β2-adrenergic receptor signaling

Cited by 4 publications

References 29 publications

The place of phytotherapy in the treatment of acute upper respiratory tract infections

The place of phytotherapy in the treatment of acute upper respiratory tract infections

Ivy Leaf Dry Extract EA 575® Has an Inhibitory Effect on the Signalling Cascade of Adenosine Receptor A2B

Future directions for the discovery of natural product-derived immunomodulating drugs: an IUPHAR positional review

Contact Info

Product

Resources

About