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Grifolin derivatives from Albatrellus ovinus as TRPV1 receptor blockers for cosmetic applications
Objective Blocking the TRPV1 receptor is an interesting approach for the treatment of sensitive skin. Here we investigated the potential of grifolin derivatives from Albatrellus ovinus to act as TRPV1 receptor blockers and their potential to serve as cosmetic active ingredients. Methods Binding char...
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Published in: | International journal of cosmetic science 2017-08, Vol.39 (4), p.379-385 |
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container_title | International journal of cosmetic science |
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creator | Hettwer, S. Bänziger, S. Suter, B. Obermayer, B. |
description | Objective
Blocking the TRPV1 receptor is an interesting approach for the treatment of sensitive skin. Here we investigated the potential of grifolin derivatives from Albatrellus ovinus to act as TRPV1 receptor blockers and their potential to serve as cosmetic active ingredients.
Methods
Binding characteristics of grifolin derivatives from Albatrellus ovinus were determined in competitive and functional in vitro assays to achieve IC50 values. The TRPV1 receptor was activated in vivo with capsaicin and noxious heat to investigate skin reddening, microcirculation, skin sensations and heat pain thresholds.
Results
Grifolin derivatives extracted from Albatrellus ovinus proved to inhibit the TRPV1 receptor in vitro and in vivo. Besides suppression of the TRPV1 receptor activity upon chemical stimulation with capsaicin, thermal activation was shown to be inhibited as well by application of cosmetic formulations containing 3% Albatrellus ovinus extract. The reduction of stinging and burning sensations as well as reduction of reddening and microcirculation upon irritation with capsaicin or thermal stress proved efficacy in vivo.
Conclusion
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.
Résumé
Objectif
Le blocage du récepteur TRPV1 est une approche intéressante pour le traitement des peaux sensibles. Ici, nous avons étudié le potentiel des dérivés de grifolin d'Albatrellus ovinus pour agir comme bloqueurs des récepteurs TRPV1 et leur potentiel pour servir d'ingrédients actifs cosmétiques.
Methodes
Les caractéristiques de liaison de dérivés de grifoline d’Albatrellus ovinus ont été déterminées dans des essais in vitro compétitifs et fonctionnels pour obtenir les valeurs de CI50. Le récepteur TRPV1 a été activé in vivo avec de la capsaïcine et de la chaleur nocive pour étudier la rougeur de la peau, la microcirculation, les sensations cutanées et les seuils de douleur thermique.
Resultats
Les dérivés de grifoline extraits d'Albatrellus ovinus ont montré une inhibition in vitro et in vivo du récepteur TRPV1. Outre la suppression de l'activité du récepteur TRPV1 par stimulation chimique avec la capsaïcine, on a montré que l'activation thermique était également inhibée par l'application de formulations cosmétiques contenant 3% d'extrait d'Albatrellus ovinus. La réduction des sensations de picotemente et de brûlure, ainsi que la réduction d |
doi_str_mv | 10.1111/ics.12385 |
format | article |
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Blocking the TRPV1 receptor is an interesting approach for the treatment of sensitive skin. Here we investigated the potential of grifolin derivatives from Albatrellus ovinus to act as TRPV1 receptor blockers and their potential to serve as cosmetic active ingredients.
Methods
Binding characteristics of grifolin derivatives from Albatrellus ovinus were determined in competitive and functional in vitro assays to achieve IC50 values. The TRPV1 receptor was activated in vivo with capsaicin and noxious heat to investigate skin reddening, microcirculation, skin sensations and heat pain thresholds.
Results
Grifolin derivatives extracted from Albatrellus ovinus proved to inhibit the TRPV1 receptor in vitro and in vivo. Besides suppression of the TRPV1 receptor activity upon chemical stimulation with capsaicin, thermal activation was shown to be inhibited as well by application of cosmetic formulations containing 3% Albatrellus ovinus extract. The reduction of stinging and burning sensations as well as reduction of reddening and microcirculation upon irritation with capsaicin or thermal stress proved efficacy in vivo.
Conclusion
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.
Résumé
Objectif
Le blocage du récepteur TRPV1 est une approche intéressante pour le traitement des peaux sensibles. Ici, nous avons étudié le potentiel des dérivés de grifolin d'Albatrellus ovinus pour agir comme bloqueurs des récepteurs TRPV1 et leur potentiel pour servir d'ingrédients actifs cosmétiques.
Methodes
Les caractéristiques de liaison de dérivés de grifoline d’Albatrellus ovinus ont été déterminées dans des essais in vitro compétitifs et fonctionnels pour obtenir les valeurs de CI50. Le récepteur TRPV1 a été activé in vivo avec de la capsaïcine et de la chaleur nocive pour étudier la rougeur de la peau, la microcirculation, les sensations cutanées et les seuils de douleur thermique.
Resultats
Les dérivés de grifoline extraits d'Albatrellus ovinus ont montré une inhibition in vitro et in vivo du récepteur TRPV1. Outre la suppression de l'activité du récepteur TRPV1 par stimulation chimique avec la capsaïcine, on a montré que l'activation thermique était également inhibée par l'application de formulations cosmétiques contenant 3% d'extrait d'Albatrellus ovinus. La réduction des sensations de picotemente et de brûlure, ainsi que la réduction des rougeurs et de la microcirculation lors de l'irritation par la capsaïcine ou le stress thermique, ont prouvé leur efficacité in vivo.
Conclusion
Les dérivés de grifolin du champignon Albatrellus ovinus sont capables de servir de bloqueurs des récepteurs TRPV1, capables de servir d'ingrédient actif cosmétique sur les peaux sensibles.
The TRPV1 receptor is a nociceptor activated by heat and chemical stimuli. Albatrellus ovinus extract is a source of grifolin derivatives capable of TRPV1 receptor inhibition. Topical application of the extract leads to amelioration of unpleasing perceptions on normal and sensitive skin.</description><identifier>ISSN: 0142-5463</identifier><identifier>EISSN: 1468-2494</identifier><identifier>DOI: 10.1111/ics.12385</identifier><identifier>PMID: 27883196</identifier><language>eng</language><publisher>England: Wiley Subscription Services, Inc</publisher><subject>Activation ; Adolescent ; Adult ; Animals ; Assaying ; Basidiomycota - chemistry ; Burning ; Capsaicin ; Capsaicin receptors ; chemical analysis ; CHO Cells ; claim substantiation in vivo/in vitro ; Combustion ; Cosmetics ; Cricetulus ; Cross-Over Studies ; Derivatives ; Double-Blind Method ; Formulations ; Fungi ; Heat ; Humans ; In vitro methods and tests ; In vivo methods and tests ; Ingredients ; Inhibition ; Irritation ; Middle Aged ; Pain ; Pain perception ; Placebos ; sensitive skin/inflammation/allergy ; Skin ; Stimulation ; Terpenes - pharmacology ; Thermal stress ; Thresholds ; TRPV Cation Channels - antagonists & inhibitors ; TRPV1 ; Young Adult</subject><ispartof>International journal of cosmetic science, 2017-08, Vol.39 (4), p.379-385</ispartof><rights>2016 RAHN AG. published by John Wiley & Sons Ltd on behalf of Society of Cosmetic Scientists and the Société Française de Cosmétologie</rights><rights>2016 RAHN AG. International Journal of Cosmetic Science published by John Wiley & Sons Ltd on behalf of Society of Cosmetic Scientists and the Société Française de Cosmétologie.</rights><rights>Copyright © 2017 Society of Cosmetic Scientists and the Société Française de Cosmétologie</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27883196$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Hettwer, S.</creatorcontrib><creatorcontrib>Bänziger, S.</creatorcontrib><creatorcontrib>Suter, B.</creatorcontrib><creatorcontrib>Obermayer, B.</creatorcontrib><title>Grifolin derivatives from Albatrellus ovinus as TRPV1 receptor blockers for cosmetic applications</title><title>International journal of cosmetic science</title><addtitle>Int J Cosmet Sci</addtitle><description>Objective
Blocking the TRPV1 receptor is an interesting approach for the treatment of sensitive skin. Here we investigated the potential of grifolin derivatives from Albatrellus ovinus to act as TRPV1 receptor blockers and their potential to serve as cosmetic active ingredients.
Methods
Binding characteristics of grifolin derivatives from Albatrellus ovinus were determined in competitive and functional in vitro assays to achieve IC50 values. The TRPV1 receptor was activated in vivo with capsaicin and noxious heat to investigate skin reddening, microcirculation, skin sensations and heat pain thresholds.
Results
Grifolin derivatives extracted from Albatrellus ovinus proved to inhibit the TRPV1 receptor in vitro and in vivo. Besides suppression of the TRPV1 receptor activity upon chemical stimulation with capsaicin, thermal activation was shown to be inhibited as well by application of cosmetic formulations containing 3% Albatrellus ovinus extract. The reduction of stinging and burning sensations as well as reduction of reddening and microcirculation upon irritation with capsaicin or thermal stress proved efficacy in vivo.
Conclusion
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.
Résumé
Objectif
Le blocage du récepteur TRPV1 est une approche intéressante pour le traitement des peaux sensibles. Ici, nous avons étudié le potentiel des dérivés de grifolin d'Albatrellus ovinus pour agir comme bloqueurs des récepteurs TRPV1 et leur potentiel pour servir d'ingrédients actifs cosmétiques.
Methodes
Les caractéristiques de liaison de dérivés de grifoline d’Albatrellus ovinus ont été déterminées dans des essais in vitro compétitifs et fonctionnels pour obtenir les valeurs de CI50. Le récepteur TRPV1 a été activé in vivo avec de la capsaïcine et de la chaleur nocive pour étudier la rougeur de la peau, la microcirculation, les sensations cutanées et les seuils de douleur thermique.
Resultats
Les dérivés de grifoline extraits d'Albatrellus ovinus ont montré une inhibition in vitro et in vivo du récepteur TRPV1. Outre la suppression de l'activité du récepteur TRPV1 par stimulation chimique avec la capsaïcine, on a montré que l'activation thermique était également inhibée par l'application de formulations cosmétiques contenant 3% d'extrait d'Albatrellus ovinus. La réduction des sensations de picotemente et de brûlure, ainsi que la réduction des rougeurs et de la microcirculation lors de l'irritation par la capsaïcine ou le stress thermique, ont prouvé leur efficacité in vivo.
Conclusion
Les dérivés de grifolin du champignon Albatrellus ovinus sont capables de servir de bloqueurs des récepteurs TRPV1, capables de servir d'ingrédient actif cosmétique sur les peaux sensibles.
The TRPV1 receptor is a nociceptor activated by heat and chemical stimuli. Albatrellus ovinus extract is a source of grifolin derivatives capable of TRPV1 receptor inhibition. Topical application of the extract leads to amelioration of unpleasing perceptions on normal and sensitive skin.</description><subject>Activation</subject><subject>Adolescent</subject><subject>Adult</subject><subject>Animals</subject><subject>Assaying</subject><subject>Basidiomycota - chemistry</subject><subject>Burning</subject><subject>Capsaicin</subject><subject>Capsaicin receptors</subject><subject>chemical analysis</subject><subject>CHO Cells</subject><subject>claim substantiation in vivo/in vitro</subject><subject>Combustion</subject><subject>Cosmetics</subject><subject>Cricetulus</subject><subject>Cross-Over Studies</subject><subject>Derivatives</subject><subject>Double-Blind Method</subject><subject>Formulations</subject><subject>Fungi</subject><subject>Heat</subject><subject>Humans</subject><subject>In vitro methods and tests</subject><subject>In vivo methods and tests</subject><subject>Ingredients</subject><subject>Inhibition</subject><subject>Irritation</subject><subject>Middle Aged</subject><subject>Pain</subject><subject>Pain perception</subject><subject>Placebos</subject><subject>sensitive skin/inflammation/allergy</subject><subject>Skin</subject><subject>Stimulation</subject><subject>Terpenes - pharmacology</subject><subject>Thermal stress</subject><subject>Thresholds</subject><subject>TRPV Cation Channels - antagonists & inhibitors</subject><subject>TRPV1</subject><subject>Young Adult</subject><issn>0142-5463</issn><issn>1468-2494</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>24P</sourceid><recordid>eNpdkU1LxDAQhoMoun4c_ANS8OKlmknSNjnK4hcIiq5eQ5rOQrRtatKu-O-NrnpwLjPDPPMyzEvIIdBTSHHmbDwFxmWxQWYgSpkzocQmmVEQLC9EyXfIbowvlFKhJN8mO6ySkoMqZ8RcBbf0reuzBoNbmdGtMGbL4LvsvK3NGLBtp5j5letTMjFbPNw_QxbQ4jD6kNWtt68Y0kpqrI8djs5mZhhaZ5OY7-M-2VqaNuLBT94jT5cXi_l1fnt3dTM_v80HDqLIK0RQBljVcMsMq8GqssCipNxQWjGLHBu1lJxbSnmjgAuGrOKAoilkDZTvkZO17hD824Rx1J2LNp1vevRT1CAFV2XFABJ6_A998VPo03UaFFRSlIVgiTr6oaa6w0YPwXUmfOjf5yXgbA28uxY__uZA9ZcrOrmiv13RN_PH74J_Amsrfjk</recordid><startdate>201708</startdate><enddate>201708</enddate><creator>Hettwer, S.</creator><creator>Bänziger, S.</creator><creator>Suter, B.</creator><creator>Obermayer, B.</creator><general>Wiley Subscription Services, Inc</general><scope>24P</scope><scope>WIN</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7QR</scope><scope>7U7</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>201708</creationdate><title>Grifolin derivatives from Albatrellus ovinus as TRPV1 receptor blockers for cosmetic applications</title><author>Hettwer, S. ; Bänziger, S. ; Suter, B. ; Obermayer, B.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p3145-7ee19a127d3c2a2b1c965e5603a0072ce3ed9f833c003d91342e2731e4d58b103</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Activation</topic><topic>Adolescent</topic><topic>Adult</topic><topic>Animals</topic><topic>Assaying</topic><topic>Basidiomycota - chemistry</topic><topic>Burning</topic><topic>Capsaicin</topic><topic>Capsaicin receptors</topic><topic>chemical analysis</topic><topic>CHO Cells</topic><topic>claim substantiation in vivo/in vitro</topic><topic>Combustion</topic><topic>Cosmetics</topic><topic>Cricetulus</topic><topic>Cross-Over Studies</topic><topic>Derivatives</topic><topic>Double-Blind Method</topic><topic>Formulations</topic><topic>Fungi</topic><topic>Heat</topic><topic>Humans</topic><topic>In vitro methods and tests</topic><topic>In vivo methods and tests</topic><topic>Ingredients</topic><topic>Inhibition</topic><topic>Irritation</topic><topic>Middle Aged</topic><topic>Pain</topic><topic>Pain perception</topic><topic>Placebos</topic><topic>sensitive skin/inflammation/allergy</topic><topic>Skin</topic><topic>Stimulation</topic><topic>Terpenes - pharmacology</topic><topic>Thermal stress</topic><topic>Thresholds</topic><topic>TRPV Cation Channels - antagonists & inhibitors</topic><topic>TRPV1</topic><topic>Young Adult</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hettwer, S.</creatorcontrib><creatorcontrib>Bänziger, S.</creatorcontrib><creatorcontrib>Suter, B.</creatorcontrib><creatorcontrib>Obermayer, B.</creatorcontrib><collection>Open Access: Wiley-Blackwell Open Access Journals</collection><collection>Wiley-Blackwell Backfiles (Open access)</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>Chemoreception Abstracts</collection><collection>Toxicology Abstracts</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>International journal of cosmetic science</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Hettwer, S.</au><au>Bänziger, S.</au><au>Suter, B.</au><au>Obermayer, B.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Grifolin derivatives from Albatrellus ovinus as TRPV1 receptor blockers for cosmetic applications</atitle><jtitle>International journal of cosmetic science</jtitle><addtitle>Int J Cosmet Sci</addtitle><date>2017-08</date><risdate>2017</risdate><volume>39</volume><issue>4</issue><spage>379</spage><epage>385</epage><pages>379-385</pages><issn>0142-5463</issn><eissn>1468-2494</eissn><abstract>Objective
Blocking the TRPV1 receptor is an interesting approach for the treatment of sensitive skin. Here we investigated the potential of grifolin derivatives from Albatrellus ovinus to act as TRPV1 receptor blockers and their potential to serve as cosmetic active ingredients.
Methods
Binding characteristics of grifolin derivatives from Albatrellus ovinus were determined in competitive and functional in vitro assays to achieve IC50 values. The TRPV1 receptor was activated in vivo with capsaicin and noxious heat to investigate skin reddening, microcirculation, skin sensations and heat pain thresholds.
Results
Grifolin derivatives extracted from Albatrellus ovinus proved to inhibit the TRPV1 receptor in vitro and in vivo. Besides suppression of the TRPV1 receptor activity upon chemical stimulation with capsaicin, thermal activation was shown to be inhibited as well by application of cosmetic formulations containing 3% Albatrellus ovinus extract. The reduction of stinging and burning sensations as well as reduction of reddening and microcirculation upon irritation with capsaicin or thermal stress proved efficacy in vivo.
Conclusion
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.
Résumé
Objectif
Le blocage du récepteur TRPV1 est une approche intéressante pour le traitement des peaux sensibles. Ici, nous avons étudié le potentiel des dérivés de grifolin d'Albatrellus ovinus pour agir comme bloqueurs des récepteurs TRPV1 et leur potentiel pour servir d'ingrédients actifs cosmétiques.
Methodes
Les caractéristiques de liaison de dérivés de grifoline d’Albatrellus ovinus ont été déterminées dans des essais in vitro compétitifs et fonctionnels pour obtenir les valeurs de CI50. Le récepteur TRPV1 a été activé in vivo avec de la capsaïcine et de la chaleur nocive pour étudier la rougeur de la peau, la microcirculation, les sensations cutanées et les seuils de douleur thermique.
Resultats
Les dérivés de grifoline extraits d'Albatrellus ovinus ont montré une inhibition in vitro et in vivo du récepteur TRPV1. Outre la suppression de l'activité du récepteur TRPV1 par stimulation chimique avec la capsaïcine, on a montré que l'activation thermique était également inhibée par l'application de formulations cosmétiques contenant 3% d'extrait d'Albatrellus ovinus. La réduction des sensations de picotemente et de brûlure, ainsi que la réduction des rougeurs et de la microcirculation lors de l'irritation par la capsaïcine ou le stress thermique, ont prouvé leur efficacité in vivo.
Conclusion
Les dérivés de grifolin du champignon Albatrellus ovinus sont capables de servir de bloqueurs des récepteurs TRPV1, capables de servir d'ingrédient actif cosmétique sur les peaux sensibles.
The TRPV1 receptor is a nociceptor activated by heat and chemical stimuli. Albatrellus ovinus extract is a source of grifolin derivatives capable of TRPV1 receptor inhibition. Topical application of the extract leads to amelioration of unpleasing perceptions on normal and sensitive skin.</abstract><cop>England</cop><pub>Wiley Subscription Services, Inc</pub><pmid>27883196</pmid><doi>10.1111/ics.12385</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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language | eng |
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source | Wiley-Blackwell Read & Publish Collection |
subjects | Activation Adolescent Adult Animals Assaying Basidiomycota - chemistry Burning Capsaicin Capsaicin receptors chemical analysis CHO Cells claim substantiation in vivo/in vitro Combustion Cosmetics Cricetulus Cross-Over Studies Derivatives Double-Blind Method Formulations Fungi Heat Humans In vitro methods and tests In vivo methods and tests Ingredients Inhibition Irritation Middle Aged Pain Pain perception Placebos sensitive skin/inflammation/allergy Skin Stimulation Terpenes - pharmacology Thermal stress Thresholds TRPV Cation Channels - antagonists & inhibitors TRPV1 Young Adult |
title | Grifolin derivatives from Albatrellus ovinus as TRPV1 receptor blockers for cosmetic applications |
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