{"id":2420,"date":"2021-12-17T09:42:28","date_gmt":"2021-12-17T00:42:28","guid":{"rendered":"https:\/\/misterx95.myds.me\/?p=2420"},"modified":"2021-12-17T09:42:31","modified_gmt":"2021-12-17T00:42:31","slug":"journal-club-2021-12-17","status":"publish","type":"post","link":"https:\/\/misterx95.myds.me\/wordpress\/?p=2420","title":{"rendered":"Journal Club-2021.12.17"},"content":{"rendered":"\n<figure class=\"wp-block-pullquote\"><blockquote><p><strong>A plant-derived TRPV3 inhibitor suppresses pain and itch<\/strong><\/p><\/blockquote><\/figure>\n\n\n\n<p>PUBLISHED IN:- JOURNAL OF BRITISH PHARMACOLOGY.                     DOI: 10.1111\/BPH.15390<\/p>\n\n\n\n<h2>Abstract<\/h2>\n\n\n\n<p><strong>Background and Purpose:<\/strong>\u00a0Itching is the most frequent pathology in dermatology that has significant impacts on people&#8217;s mental health and social life. Transient receptor potential vanilloid 3 (TRPV3) channel is a promising target for treating pruritus. However, few selecetive and potent antagonists have been reported. This study was designed to identify selective TRPV3 antagonist and elucidate its anti-pruritus pharmacology.<\/p>\n\n\n\n<p><strong>Experimental Approach:<\/strong>\u00a0FlexStation and calcium fluorescence imaging were conducted to track the functional compounds. Whole-cell patch clamp was used to record itch-related ion channel currents. Homologous recombination and site-directed mutagenesis were employed to construct TRPV3 channel chimeras and point mutations for exploring pharmacological mechanism. Mouse models were used for\u00a0in vivo\u00a0anti-pruritus assay.<\/p>\n\n\n\n<p><strong>Key Results:<\/strong>\u00a0An acridone alkaloid (citrusinine-II) was purified and characterized from\u00a0Atalantia monophylla. It directly interacts with Y564 within S4 helix of TRPV3 to selectively inhibit the channel with a half maximal inhibitory concentration (IC50) of 12.43\u00a0\u03bcM. Citrusinine-II showed potential efficacy to attenuate both chronic and acute itch. Intradermal administration of citrusinine-II (143 ng\/skin site) nearly completely inhibited itch behaviours. It also shows significant analgesic effects. Little side effects of the compound are observed.<\/p>\n\n\n\n<p><strong>Conclusion and Implications:<\/strong>\u00a0By acting as a selective and potent inhibitor of TRPV3 channel, citrusinine-II shows valuable therapeutic effects in pruritus animal models and is a promising candidate drug and\/or lead molecule for the development of anti- pruritus drugs.<\/p>\n\n\n\n<p><strong>KEYWORDS<\/strong>: citrusinine-II, Inhibition, Itch, Pain, TRPV3<\/p>\n\n\n\n<div class=\"wp-block-file\"><a href=\"https:\/\/misterx95.myds.me\/wordpress\/wp-content\/uploads\/2021\/12\/TRPV3-inhibitor.pdf\">TRPV3-inhibitor<\/a><a href=\"https:\/\/misterx95.myds.me\/wordpress\/wp-content\/uploads\/2021\/12\/TRPV3-inhibitor.pdf\" class=\"wp-block-file__button\" download>Download<\/a><\/div>\n\n\n\n<p><\/p>\n","protected":false},"excerpt":{"rendered":"<p>A plant-derived TRPV3 inhibitor suppresses pain and itch PUBLISHED IN:- JOURNAL OF BRITISH PHARMACOLOGY. DOI: 10.1111\/BPH.15390 Abstract Background and Purpose:\u00a0Itching is the most frequent pathology in dermatology that has significant impacts on people&#8217;s mental health and social life. Transient receptor potential vanilloid 3 (TRPV3) channel is a promising target for treating pruritus. However, few selecetive [&hellip;]<\/p>\n","protected":false},"author":11,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"site-sidebar-layout":"default","site-content-layout":"","ast-site-content-layout":"","site-content-style":"default","site-sidebar-style":"default","ast-global-header-display":"","ast-banner-title-visibility":"","ast-main-header-display":"","ast-hfb-above-header-display":"","ast-hfb-below-header-display":"","ast-hfb-mobile-header-display":"","site-post-title":"","ast-breadcrumbs-content":"","ast-featured-img":"","footer-sml-layout":"","theme-transparent-header-meta":"","adv-header-id-meta":"","stick-header-meta":"","header-above-stick-meta":"","header-main-stick-meta":"","header-below-stick-meta":"","astra-migrate-meta-layouts":"default","ast-page-background-enabled":"default","ast-page-background-meta":{"desktop":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"tablet":{"background-color":"","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"mobile":{"background-color":"","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""}},"ast-content-background-meta":{"desktop":{"background-color":"var(--ast-global-color-5)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"tablet":{"background-color":"var(--ast-global-color-5)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"mobile":{"background-color":"var(--ast-global-color-5)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""}}},"categories":[1],"tags":[],"_links":{"self":[{"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/posts\/2420"}],"collection":[{"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/users\/11"}],"replies":[{"embeddable":true,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=2420"}],"version-history":[{"count":3,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/posts\/2420\/revisions"}],"predecessor-version":[{"id":2424,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/posts\/2420\/revisions\/2424"}],"wp:attachment":[{"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=2420"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=2420"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=2420"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}