{"id":45265,"date":"2020-12-22T02:30:57","date_gmt":"2020-12-22T01:30:57","guid":{"rendered":"https:\/\/rina.naturopatiadigital.eu\/?p=45265"},"modified":"2020-12-24T12:24:48","modified_gmt":"2020-12-24T11:24:48","slug":"area-de-conocimiento-naturopatia-experimental-sustancias-bioactivas-la-flavona-hispidulina-un-ligando-del-receptor-de-benzodiazepinas-con-propiedades-alostericas-positivas-atraviesa-la-barrera","status":"publish","type":"post","link":"https:\/\/rina.naturopatiadigital.eu\/?p=45265","title":{"rendered":"\u00c1rea de conocimiento: Naturopat\u00eda Experimental: Sustancias Bioactivas: \u00abLa flavona hispidulina, un ligando del receptor de benzodiazepinas con propiedades alost\u00e9ricas positivas, atraviesa la barrera hematoencef\u00e1lica y exhibe efectos anticonvulsivos\u00bb"},"content":{"rendered":"<p><a href=\"https:\/\/1.bp.blogspot.com\/-AqClAU5w8tY\/X-R5_Sr25aI\/AAAAAAAAhU8\/KvvX1dLWyGMLOnrzGSPTWq8B5TJfkhI_gCLcBGAsYHQ\/s258\/British_journal%2Bof%2Bpharmacology.jpg\"><img decoding=\"async\" class=\"alignleft\" src=\"https:\/\/1.bp.blogspot.com\/-AqClAU5w8tY\/X-R5_Sr25aI\/AAAAAAAAhU8\/KvvX1dLWyGMLOnrzGSPTWq8B5TJfkhI_gCLcBGAsYHQ\/s0\/British_journal%2Bof%2Bpharmacology.jpg\" border=\"0\" data-original-height=\"258\" data-original-width=\"195\" \/><\/a>Kavvadias, D., Sand, P., Youdim, K. A., Qaiser, M. Z., Rice\u2010Evans, C., Baur, R., &#8230; &amp; Schreier, P. (2004). <a href=\"https:\/\/bpspubs.onlinelibrary.wiley.com\/doi\/pdf\/10.1038\/sj.bjp.0705828\">The flavone hispidulin, a benzodiazepine receptor ligand with positive allosteric properties, traverses the blood\u2013brain barrier and exhibits anticonvulsive effects<\/a>.\u00a0<i>British journal of pharmacology<\/i>, 142(5), 811-820.<\/p>\n<p>OBJETIVO: Se inici\u00f3 la caracterizaci\u00f3n funcional de la hispidulina (4 &#8216;, 5,7-trihidroxi-6-metoxiflavona), un potente ligando del receptor de benzodiazepinas (BZD), para determinar su potencial como modulador de la actividad del sistema nervioso central.<\/p>\n<p>METODOLOG\u00cdA \/ RESULTADOS: Despu\u00e9s de la s\u00edntesis qu\u00edmica, se investig\u00f3 la hispidulina en los receptores GABA (A) \/ BZD recombinantes expresados \u200b\u200bpor ovocitos de Xenopus laevis. Las concentraciones de 50 nm y superiores estimularon las corrientes de cloruro inducidas por GABA en los subtipos de receptores probados (alfa (1-3,5,6) beta (2) gamma (2) S), lo que indica propiedades alost\u00e9ricas positivas. Se observ\u00f3 una estimulaci\u00f3n m\u00e1xima en alfa (1) beta (2) gamma (2) S con 10 micras de hispidulina. A diferencia del diazepam, la hispidulina modul\u00f3 el subtipo de receptor alfa (6) beta (2) gamma (2) S-GABA (A).\u00a0Cuando se administra a jerbos mongoles propensos a convulsiones (Meriones unguiculatus) en un modelo de epilepsia, hispidulina (10 mg kg (-1) de peso corporal (BW) por d\u00eda) y diazepam (2 mg kg (-1) BW por d\u00eda) marcadamente redujo el n\u00famero de animales que padec\u00edan convulsiones despu\u00e9s de 7 d\u00edas de tratamiento (30 y 25% de animales en los respectivos grupos de tratamiento, frente al 80% en el grupo de veh\u00edculo). La permeabilidad a trav\u00e9s de la barrera hematoencef\u00e1lica para la hispidulina marcada con (14) C sintetizada qu\u00edmicamente se confirm\u00f3 mediante un modelo de perfusi\u00f3n in situ de rata. Con una tasa de absorci\u00f3n (K (in)) de 1,14 ml min (-1) g (-1), las medidas se acercaron a los valores obtenidos con compuestos de alta penetraci\u00f3n como el diazepam.<\/p>\n<p>CONCLUSIONES: Los experimentos con c\u00e9lulas Caco-2 predicen que la hispidulina administrada por v\u00eda oral entra en la circulaci\u00f3n en su forma intacta. A una concentraci\u00f3n de 30 micras, la flavona cruz\u00f3 la monocapa sin degradarse, como lo verifica la ausencia de metabolitos glucuronidados.<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Kavvadias, D., Sand, P., Youdim, K. A., Qaiser, M. Z., Rice\u2010Evans, C., Baur, R., &#8230; &amp; Schreier, P. (2004). The flavone hispidulin, a benzodiazepine receptor ligand with positive allosteric properties, traverses the blood\u2013brain barrier and exhibits anticonvulsive effects.\u00a0British journal of pharmacology, 142(5), 811-820. OBJETIVO: Se inici\u00f3 la caracterizaci\u00f3n funcional de la hispidulina (4 &#8216;, 5,7-trihidroxi-6-metoxiflavona), [&hellip;]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[8],"tags":[],"class_list":["post-45265","post","type-post","status-publish","format-standard","hentry","category-sustancias-bioactivas"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v21.8 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>\u00c1rea de conocimiento: Naturopat\u00eda Experimental: Sustancias Bioactivas: &quot;La flavona hispidulina, un ligando del receptor de benzodiazepinas con propiedades alost\u00e9ricas positivas, atraviesa la barrera hematoencef\u00e1lica y exhibe efectos anticonvulsivos&quot; -<\/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:\/\/rina.naturopatiadigital.eu\/?p=45265\" \/>\n<meta property=\"og:locale\" content=\"es_ES\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"\u00c1rea de conocimiento: Naturopat\u00eda Experimental: Sustancias Bioactivas: &quot;La flavona hispidulina, un ligando del receptor de benzodiazepinas con propiedades alost\u00e9ricas positivas, atraviesa la barrera hematoencef\u00e1lica y exhibe efectos anticonvulsivos&quot; -\" \/>\n<meta property=\"og:description\" content=\"Kavvadias, D., Sand, P., Youdim, K. A., Qaiser, M. Z., Rice\u2010Evans, C., Baur, R., &#8230; &amp; Schreier, P. (2004). The flavone hispidulin, a benzodiazepine receptor ligand with positive allosteric properties, traverses the blood\u2013brain barrier and exhibits anticonvulsive effects.\u00a0British journal of pharmacology, 142(5), 811-820. 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