Grifolin derivatives from <i>Albatrellus ovinus</i> as <scp>TRPV</scp>1 receptor blockers for cosmetic applications

Hettwer, Stefan; Bänziger, Stefan; Suter, Brigit; Obermayer, Barbara

doi:10.1111/ics.12385

Cited by 7 publications

(3 citation statements)

References 23 publications

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“…In vitro, the IC 50 values of TRPV1 receptor inhibition were law expressed in µM range with Hill coefficients between 1.5 and 2.4. In addition, grifolin was able to demonstrate in vivo effects by reducing skin reddening and microcirculation, as well as stinging and burning sensations [ 25 ].…”

Section: Resultsmentioning

confidence: 99%

Pharmacological Effects of Grifolin: Focusing on Anticancer Mechanisms

Bouyahya

Allam

Zeouk³

et al. 2022

Molecules

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Grifolin is a volatile compound contained in essential oils of several medicinal plants. Several studies show that this substance has been the subject of numerous pharmacological investigations, which have yielded interesting results. Grifolin demonstrated beneficial effects for health via its multiple pharmacological activities. It has anti-microbial properties against bacteria, fungi, and parasites. In addition, grifolin exhibited remarkable anti-cancer effects on different human cancer cells. The anticancer action of this molecule is related to its ability to act at cellular and molecular levels on different checkpoints controlling the signaling pathways of human cancer cell lines. Grifolin can induce apoptosis, cell cycle arrest, autophagy, and senescence in these cells. Despite its major pharmacological properties, grifolin has only been investigated in vitro and in vivo. Therefore, further investigations concerning pharmacodynamic and pharmacokinetic tests are required for any possible pharmaceutical application of this substance. Moreover, toxicological tests and other investigations involving humans as a study model are required to validate the safety and clinical applications of grifolin.

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Section: Resultsmentioning

confidence: 99%

Pharmacological Effects of Grifolin: Focusing on Anticancer Mechanisms

Bouyahya

Allam

Zeouk³

et al. 2022

Molecules

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“…Grifolin and neogrifolin, isolated from Peperomia galioides, Rhododendron dauricum and Albatrellus sp., inhibited TRPV1 receptor in the low micromolar range. The IC50 binding values for grifolin and neogrifolin are 18.8 µM and 30.8 µM, respectively [ 148 ]. However, we found no information on the mode of binding of these triprenylphenols with the receptor or on their effect on Tb.…”

Section: Natural Modulators Of Trpv1 Channelmentioning

confidence: 99%

Natural Active Ingredients and TRPV1 Modulation: Focus on Key Chemical Moieties Involved in Ligand–Target Interaction

Andrei

Zanfirescu

Nițulescu

et al. 2023

Plants

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Diseases such as cancer, neurological pathologies and chronic pain represent currently unmet needs. The existing pharmacotherapeutic options available for treating these conditions are limited by lack of efficiency and/or side effects. Transient receptor potential vanilloid 1 ion channel emerged as an attractive therapeutic target for developing new analgesic, anti-cancer and antiepileptic agents. Furthermore, various natural ingredients were shown to have affinity for this receptor. The aim of this narrative review was to summarize the diverse natural scaffolds of TRPV1 modulators based on their agonistic/antagonistic properties and to analyze the structure–activity relationships between the ligands and molecular targets based on the results of the existing molecular docking, mutagenesis and in vitro studies. We present here an exhaustive collection of TRPV1 modulators grouped by relevant chemical features: vanilloids, guaiacols, phenols, alkylbenzenes, monoterpenes, sesquiterpenoids, alkaloids, etc. The information herein is useful for understanding the key structural elements mediating the interaction with TRPV1 and how their structural variation impacts the interaction between the ligand and receptor. We hope this data will contribute to the design of novel effective and safe TRPV1 modulators, to help overcome the lack of effective therapeutic agents against pathologies with high morbidity and mortality.

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“…DEFENSIL ® -SOFT by RAHN AG is a neuro-soother formulation based on the extract of an edible mushroom Albatrellus ovinus, and proposed as a functional ingredient [227]. Due to the presence of the bioactive phenolic compounds grifolin, neogrifolin, and scutigeral in this extract, the effective inhibition of the TRPV1 receptor was observed during in vitro studies [203,228,229]. Furthermore, when applied to the skin, DEFENSIL ® -SOFT provides soothing (in vivo study) and anti-aging effects [230].…”

Section: Providing Solutions For Sensitive Skin: Neurocosmetic Ingredientsmentioning

confidence: 99%

Neurocosmetics in Skincare—The Fascinating World of Skin–Brain Connection: A Review to Explore Ingredients, Commercial Products for Skin Aging, and Cosmetic Regulation

et al. 2021

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The “modern” cosmetology industry is focusing on research devoted to discovering novel neurocosmetic functional ingredients that could improve the interactions between the skin and the nervous system. Many cosmetic companies have started to formulate neurocosmetic products that exhibit their activity on the cutaneous nervous system by affecting the skin’s neuromediators through different mechanisms of action. This review aims to clarify the definition of neurocosmetics, and to describe the features of some functional ingredients and products available on the market, with a look at the regulatory aspect. The attention is devoted to neurocosmetic ingredients for combating skin stress, explaining the stress pathways, which are also correlated with skin aging. “Neuro-relaxing” anti-aging ingredients derived from plant extracts and neurocosmetic strategies to combat inflammatory responses related to skin stress are presented. Afterwards, the molecular basis of sensitive skin and the suitable neurocosmetic ingredients to improve this problem are discussed. With the aim of presenting the major application of Botox-like ingredients as the first neurocosmetics on the market, skin aging is also introduced, and its theory is presented. To confirm the efficacy of the cosmetic products on the market, the concept of cosmetic claims is discussed.

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Grifolin derivatives from Albatrellus ovinus as TRPV1 receptor blockers for cosmetic applications

Abstract: Grifolin derivatives from Albatrellus ovinus are able to serve as fungal-derived TRPV1 receptor blockers with capability to serve as a cosmetic active ingredient on sensitive skin.

Cited by 7 publications

References 23 publications

Pharmacological Effects of Grifolin: Focusing on Anticancer Mechanisms

Pharmacological Effects of Grifolin: Focusing on Anticancer Mechanisms

Natural Active Ingredients and TRPV1 Modulation: Focus on Key Chemical Moieties Involved in Ligand–Target Interaction

Neurocosmetics in Skincare—The Fascinating World of Skin–Brain Connection: A Review to Explore Ingredients, Commercial Products for Skin Aging, and Cosmetic Regulation

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