{"id":8158,"date":"2022-03-10T09:22:35","date_gmt":"2022-03-10T08:22:35","guid":{"rendered":"https:\/\/www.iqac.csic.es\/patentades-unes-molecules-que-contraresten-lefecte-del-farmac-anticoagulant-mes-comu\/"},"modified":"2026-06-16T10:47:09","modified_gmt":"2026-06-16T08:47:09","slug":"patentades-unes-molecules-que-contraresten-lefecte-del-farmac-anticoagulant-mes-comu","status":"publish","type":"post","link":"https:\/\/www.iqac.csic.es\/ca\/patentades-unes-molecules-que-contraresten-lefecte-del-farmac-anticoagulant-mes-comu\/","title":{"rendered":"Patentades unes mol\u00e8cules que contraresten l&#8217;efecte del f\u00e0rmac anticoagulant m\u00e9s com\u00fa"},"content":{"rendered":"<p>Un estudi liderat per cient\u00edfics de<strong> l&#8217;Institut de Qu\u00edmica Avan\u00e7ada de Catalunya (IQAC-CSIC)<\/strong> del <strong><a href=\"https:\/\/www.csic.es\/es\" target=\"_blank\" rel=\"noopener\">Consell Superior de Recerques Cient\u00edfiques (CSIC)<\/a> <\/strong>han descobert i sintetitzat diverses mol\u00e8cules que inhibeixen l&#8217;efecte del f\u00e0rmac anticoagulant m\u00e9s com\u00fa. Aquest f\u00e0rmac \u00e9s molt \u00fatil per a tractar a malalts en risc de sofrir trombes, per\u00f2 en moltes ocasions \u00e9s imprescindible bloquejar la seva actuaci\u00f3 quan aquests pacients s&#8217;enfronten a intervencions quir\u00fargiques per a evitar sagnats descontrolats. Dos d&#8217;aquestes mol\u00e8cules s&#8217;han provat, amb molt bons resultats, en assajos amb ratolins, la qual cosa podria ser el pas previ per a dissenyar possibles f\u00e0rmacs. Els resultats de la recerca han estat patentats i publicats en la revista <em>The Journal of Medicinal Chemistry<\/em> (ACS).<\/p>\n<p>En el 2018 la prova de concepte es va publicar com <em>hot paper<\/em> en la revista <em>Angewandte Chemie International Edition<\/em>, en la qual els investigadors van utilitzar sistemes qu\u00edmics combinatoris din\u00e0mics i van aconseguir una mol\u00e8cula senzilla que <a href=\"https:\/\/www.csic.es\/es\/actualidad-del-csic\/identificada-una-molecula-sencilla-que-inhibe-el-efecto-del-farmaco\" target=\"_blank\" rel=\"noopener\">inhibia in vitro l&#8217;efecte de l&#8217;heparina<\/a>, el f\u00e0rmac anticoagulant m\u00e9s usat. En aquest treball, l&#8217;equip liderat per <strong>Ignacio Alfonso<\/strong>, de l&#8217;Institut de Qu\u00edmica Avan\u00e7ada de Catalunya, ha utilitzat aquesta mateixa metodologia per a un garbellat m\u00e9s ampli, la qual cosa els ha portat a descobrir mol\u00e8cules amb major potencial que han pogut fer el salt a assajos ex viu i in vivo amb ratolins. \u201cEls assajos de coagulaci\u00f3 amb ratolins mostren que les mol\u00e8cules optimitzades s\u00f3n potents ant\u00eddots amb \u00fas potencial com a f\u00e0rmacs de reversi\u00f3 de l&#8217;heparina\u201d, explica l&#8217;investigador.<\/p>\n<p>L&#8217;heparina s&#8217;utilitza \u00e0mpliament en cl\u00ednica principalment com a anticoagulant, per\u00f2 tamb\u00e9 com a antiviral i anticancer\u00f3s. A m\u00e9s, el seu \u00fas s&#8217;ha revitalitzat encara m\u00e9s amb la pand\u00e8mia de la covid-19, ja que actualment s&#8217;est\u00e0 usant com a tractament preventiu dels trombes produ\u00efts en malalts de coronavirus i en embarassades. \u201cEncara que \u00e9s un dels f\u00e0rmacs anticoagulants m\u00e9s comuns, no est\u00e0 lliure de perills, i \u00e9s fonamental comptar amb una eficient i variada bateria d&#8217;ant\u00eddots\u201d assenyala Alfonso.<\/p>\n<p>\u201cEl tractament amb heparina \u00e9s molt comuna en malalts amb el risc de presentar trombes sanguinis. No obstant aix\u00f2, en alguns casos es donen reaccions al\u00b7l\u00e8rgiques o sobredosis, que produeixen l&#8217;aparici\u00f3 d&#8217;importants hematomes o fins i tot hemorr\u00e0gies incontrolades\u201d, destaca l&#8217;investigador. \u201cAix\u00f2 \u00e9s especialment cr\u00edtic en malalts sota tractament amb heparina que necessiten ser intervinguts quir\u00fargicament de manera urgent o imprevista (per exemple, despr\u00e9s d&#8217;un traumatisme sever o un accident cardiovascular). En aquests casos la inhibici\u00f3 de l&#8217;heparina circulant en el torrent sanguini \u00e9s imprescindible per a evitar complicacions per sagnat excessiu\u201d, afegeix.<\/p>\n<p>Actualment el sulfat de protamina \u00e9s l&#8217;ant\u00eddot que existeix per a neutralitzar l&#8217;acci\u00f3 de l&#8217;heparina, per\u00f2 es tracta d&#8217;un f\u00e0rmac d&#8217;alt pes molecular, per la qual cosa pot comportar inconvenients. No existeix fins avui en el mercat cap mol\u00e8cula petita que inhibeixi l&#8217;efecte anticoagulant de l&#8217;heparina. \u201cLa cerca d&#8217;ant\u00eddots d&#8217;heparina basats en mol\u00e8cules petites continua sent un desafiament degut a les propietats fisicoqu\u00edmiques d&#8217;aquest polisac\u00e0rid ani\u00f2nic\u201d, assenyala Alfonso.<\/p>\n<p>En aquest treball s&#8217;ha utilitzat de nou la metodologia basada en la qu\u00edmica combinat\u00f2ria din\u00e0mica que conjumina en un \u00fanic proc\u00e9s la selecci\u00f3, identificaci\u00f3 i preparaci\u00f3 de mol\u00e8cules per a una determinada aplicaci\u00f3, accelerant el desenvolupament de nous compostos funcionals. La limitada informaci\u00f3 estructural i l&#8217;heterogene\u00eftat de la mol\u00e8cula d&#8217;heparina la converteixen en una bona candidata com a model en qu\u00edmica combinat\u00f2ria din\u00e0mica, ja que aquesta metodologia no requereix un coneixement detallat de l&#8217;estructura de la mol\u00e8cula diana.<\/p>\n<p>\u201cEls resultats obtinguts d&#8217;aquesta recerca subratllen l&#8217;\u00e8xit d&#8217;aquesta metodologia. A m\u00e9s, s&#8217;ha trobat una excel\u00b7lent correlaci\u00f3 entre els resultats del garbellat i la inhibici\u00f3 de l&#8217;heparina amb assajos enzim\u00e0tics in vitro, dels que es van obtenir una petita col\u00b7lecci\u00f3 de mol\u00e8cules amb bona activitat. D&#8217;aquesta bateria de mol\u00e8cules, dues d&#8217;elles presentaven activitats in vitro significativament millors que les obtingudes en 2018, i per tant es van provar en assajos in vivo obtenint excel\u00b7lents resultats\u201d, explica l&#8217;investigador. \u201cAquest estudi representa una validaci\u00f3 definitiva del nostre enfocament\u201d, conclou Alfonso.<\/p>\n<p>Per tant, la projecci\u00f3 de la qu\u00edmica combinat\u00f2ria din\u00e0mica demostra ser una eina molt potent per al descobriment de noves fites en el desenvolupament de futurs medicaments on els enfocaments convencionals han trobat moltes dificultats per a triomfar.<\/p>\n<p>&nbsp;<\/p>\n<p>Daniel Carbajo, Yolanda P\u00e9rez, Jordi Bujons, and Ignacio Alfonso. <strong>Live-Cell-Templated Dynamic Combinatorial Chemistry<\/strong>. <em>Angewandte Chemie. Int. Ed<\/em>. <a href=\"https:\/\/pubs.acs.org\/doi\/abs\/10.1021\/acs.jmedchem.1c02054\" target=\"_blank\" rel=\"noopener\">DOI: 10.1002\/anie.202004745<\/a><\/p>\n<p style=\"text-align: right;\"><strong>Ana Sotres \/ IQAC-CSIC Comunicaci\u00f3<\/strong><\/p>\n","protected":false},"excerpt":{"rendered":"<p>Un estudi liderat per cient\u00edfics de l&#8217;Institut de Qu\u00edmica Avan\u00e7ada de Catalunya (IQAC-CSIC) del Consell Superior de Recerques Cient\u00edfiques (CSIC) han descobert i sintetitzat diverses mol\u00e8cules que inhibeixen l&#8217;efecte del f\u00e0rmac anticoagulant m\u00e9s com\u00fa. Aquest f\u00e0rmac \u00e9s molt \u00fatil per a tractar a malalts en risc de sofrir trombes, per\u00f2 en moltes ocasions \u00e9s imprescindible<a class=\"more-link\" href=\"https:\/\/www.iqac.csic.es\/ca\/patentades-unes-molecules-que-contraresten-lefecte-del-farmac-anticoagulant-mes-comu\/\">Continue reading <span class=\"screen-reader-text\">\u00abPatentades unes mol\u00e8cules que contraresten l&#8217;efecte del f\u00e0rmac anticoagulant m\u00e9s com\u00fa\u00bb<\/span><\/a><\/p>\n","protected":false},"author":3,"featured_media":4292,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"footnotes":""},"categories":[73],"tags":[],"class_list":["post-8158","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-news","entry"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v28.7 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Patentades unes mol\u00e8cules que contraresten l&#039;efecte del f\u00e0rmac anticoagulant m\u00e9s com\u00fa | IQAC - Institut de Qu\u00edmica Avan\u00e7ada de Catalunya - CSIC<\/title>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/www.iqac.csic.es\/patentadas-unas-moleculas-que-contrarrestan-el-efecto-del-farmaco-anticoagulante-mas-comun\/\" \/>\n<meta property=\"og:locale\" content=\"ca_ES\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Patentades unes mol\u00e8cules que contraresten l&#039;efecte del f\u00e0rmac anticoagulant m\u00e9s com\u00fa | IQAC - Institut de Qu\u00edmica Avan\u00e7ada de Catalunya - CSIC\" \/>\n<meta property=\"og:description\" content=\"Un estudi liderat per cient\u00edfics de l&#8217;Institut de Qu\u00edmica Avan\u00e7ada de Catalunya (IQAC-CSIC) del Consell Superior de Recerques Cient\u00edfiques (CSIC) han descobert i sintetitzat diverses mol\u00e8cules que inhibeixen l&#8217;efecte del f\u00e0rmac anticoagulant m\u00e9s com\u00fa. 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