{"id":5017,"date":"2024-08-04T16:50:34","date_gmt":"2024-08-04T16:50:34","guid":{"rendered":"https:\/\/longchangextracts.com\/?p=5017"},"modified":"2024-08-04T16:50:34","modified_gmt":"2024-08-04T16:50:34","slug":"pixiu-grass","status":"publish","type":"post","link":"https:\/\/longchangextracts.com\/da\/pixiu-graes\/","title":{"rendered":"Unders\u00f8gelse af den strukturelle modifikation af Pixiu-alkohol og dens antikoagulerende faktor Xa-aktivitet"},"content":{"rendered":"<p>Unders\u00f8gelse af den strukturelle modifikation af Pixiu-alkohol og dens antikoagulerende faktor Xa-aktivitet<br \/>\nPixiu-gr\u00e6s er en et\u00e5rig urteagtig plante af Pixiu-sl\u00e6gten i Asteraceae-familien. 2020-udgaven af Pharmacopoeia of the People's Republic of China inkluderer t\u00f8rrede overjordiske dele af tre planter i Asteraceae-familien, nemlig Siegesbeckia orientalis L., Siegesbeckia pubescens Makino og Siegesbeckia glabrescent Makino, som traditionel kinesisk medicin \"Siegesbeckia\". Den virker ved at fordrive vind og fugt, fremme udviklingen af leddene og afgifte. Den bruges mod gigt og smerter, muskel- og knoglesvaghed, \u00f8mhed og svaghed i talje og kn\u00e6, lammelse af lemmer, hemiplegi, r\u00f8de hunde og v\u00e5de s\u00e5r. Moderne farmakologiske eksperimenter har vist, at ekstraktet af Polygonatum sibiricum har antiinflammatoriske, antiallergiske, antitrombotiske og antihistamin-frig\u00f8rende aktiviteter. Unders\u00f8gelser af kemisk sammens\u00e6tning og farmakologisk aktivitet har vist, at de rigelige diterpenoidforbindelser i Polygonatum sibiricum er det materielle grundlag for dets forskellige virkninger, is\u00e6r inden for antiinflammatoriske, smertestillende og blodaktiverende og stasefjernende aspekter.<br \/>\nDarutigenol er en diterpenoidforbindelse, der udvindes af planten Scutellaria baicalensis. Moderne farmakologiske eksperimenter har vist, at Darutigenol signifikant kan h\u00e6mme den maksimale blodpladeaggregeringshastighed og adh\u00e6sionshastighed hos rotter, forl\u00e6nge opl\u00f8sningstiden for euglobulin og bl\u00f8dnings- og koagulationstiden hos mus, reducere fuldblodsviskositeten og plasmaviskositeten i blodstasemodellrotter betydeligt, forbedre unormal blodreologi og h\u00e6mme TXB2-syntese i blodstasemodellrotter. Det har tydelige antitrombotiske, trombolytiske, antikoagulerende og h\u00e6morologiske virkninger. Koagulationsfaktoren Xa (FXa) er placeret i sk\u00e6ringspunktet mellem endogene og eksogene koagulationsveje og spiller en vigtig rolle i koagulationsvejen, hvilket g\u00f8r det til et af hotspots i antikoagulerende l\u00e6gemiddelforskning i de senere \u00e5r. Derfor udf\u00f8rte denne artikel strukturelle modifikationsunders\u00f8gelser af den aktive forbindelse Pixiu-alkohol isoleret fra Pixiu-gr\u00e6s af vores forskningsgruppe i den tidlige fase og unders\u00f8gte dens virkning p\u00e5 koagulationsfaktor Xa for at opdage ledende forbindelsesmolekyler med bedre aktivitet. Denne unders\u00f8gelse vil fungere som reference for opdagelsen af nye antitrombotiske l\u00e6gemidler med sm\u00e5 molekyler og udviklingen af l\u00e6geplanter som Hedyotis diffusa.<\/p>\n<p>&nbsp;<\/p>\n<p><img loading=\"lazy\" decoding=\"async\" class=\"alignnone size-full wp-image-5018\" src=\"https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/1-110.png\" alt=\"\" width=\"776\" height=\"376\" srcset=\"https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/1-110.png 776w, https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/1-110-768x372.png 768w\" sizes=\"(max-width: 776px) 100vw, 776px\" \/><img loading=\"lazy\" decoding=\"async\" class=\"alignnone size-full wp-image-5019\" src=\"https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/2-96.png\" alt=\"\" width=\"782\" height=\"179\" srcset=\"https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/2-96.png 782w, https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/2-96-768x176.png 768w\" sizes=\"(max-width: 782px) 100vw, 782px\" \/><img loading=\"lazy\" decoding=\"async\" class=\"alignnone size-full wp-image-5020\" src=\"https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/3-92.png\" alt=\"\" width=\"776\" height=\"352\" srcset=\"https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/3-92.png 776w, https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/3-92-768x348.png 768w\" sizes=\"(max-width: 776px) 100vw, 776px\" \/><img loading=\"lazy\" decoding=\"async\" class=\"alignnone size-full wp-image-5021\" src=\"https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/4-81.png\" alt=\"\" width=\"353\" height=\"328\" \/><img loading=\"lazy\" decoding=\"async\" class=\"alignnone size-full wp-image-5022\" src=\"https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/5-75.png\" alt=\"\" width=\"779\" height=\"580\" srcset=\"https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/5-75.png 779w, https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/5-75-768x572.png 768w\" sizes=\"(max-width: 779px) 100vw, 779px\" \/><img loading=\"lazy\" decoding=\"async\" class=\"alignnone size-full wp-image-5023\" src=\"https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/6-67.png\" alt=\"\" width=\"774\" height=\"302\" srcset=\"https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/6-67.png 774w, https:\/\/longchangextracts.com\/wp-content\/uploads\/2024\/08\/6-67-768x300.png 768w\" sizes=\"(max-width: 774px) 100vw, 774px\" \/>Ud fra den kliniske effekt af FXa-h\u00e6mmere repr\u00e6senteret af iduban kan man se, at det har en god antikoagulerende effekt, et bredt behandlingsvindue og ikke er tilb\u00f8jeligt til at for\u00e5rsage hyperkoagulerbare reaktioner med h\u00f8j sikkerhed. Det er blevet et varmt emne inden for forskning i antikoagulerende l\u00e6gemidler i dag. Naturprodukter har unikke fordele inden for antikoagulation, og opdagelse af aktive ingredienser fra traditionel kinesisk medicin med pr\u00e6cis klinisk effekt og forskning i strukturelle \u00e6ndringer kan v\u00e6re en vigtig m\u00e5de at opdage nye antikoagulantia p\u00e5. Pixiu-alkohol er en aktiv forbindelse, der er isoleret fra den traditionelle kinesiske medicin Pixiu-gr\u00e6s. Tidligere unders\u00f8gelser har vist, at det har en betydelig antikoagulerende aktivitet. Derfor udf\u00f8rte denne unders\u00f8gelse strukturel modifikationsforskning p\u00e5 Pixiu-alkohol og screenede for FXa-h\u00e6mmende aktivitet med det form\u00e5l at opdage nye FXa-h\u00e6mmere med udviklingsv\u00e6rdi.<\/p>\n<p>Baseret p\u00e5 berberins strukturelle egenskaber blev der indf\u00f8rt en heterocyklisk ring i den oprindelige struktur for at forbedre hydrofiliciteten og aktiviteten af denne type forbindelse. Derfor blev flere derivater designet og syntetiseret ved at indf\u00f8re en femleddet heterocyklisk ring p\u00e5 A-ringen af berberin. Ved at udf\u00f8re in vitro FXa-h\u00e6mningseksperimenter p\u00e5 berberin og dets derivater blev der opn\u00e5et syv forbindelser med god aktivitet (IC50&lt;10 \u03bc mol\/L). Sammenlignet med berberin viste de fleste derivater en vis forbedring i den h\u00e6mmende aktivitet af koagulationsfaktor FXa, blandt hvilke forbindelser 9 og 11 var de mest betydningsfulde med IC50-v\u00e6rdier p\u00e5 henholdsvis 0,71 \u00b1 0,07 og 0,22 \u00b1 0,03 \u03bc mol\/L. Forel\u00f8bige unders\u00f8gelser af forholdet mellem struktur og aktivitet har vist, at introduktion af methylengrupper p\u00e5 15,16-diolerne i den oprindelige struktur og introduktion af heterocykler i A-ringen kan forbedre forbindelsernes aktivitet, og den elektroniske effekt p\u00e5 de heterocykliske substituenter spiller en vigtig rolle i forbedringen af aktiviteten. If\u00f8lge analysen af ligandproteininteraktionsm\u00f8nstre i computerst\u00f8ttet l\u00e6gemiddeldesign fungerer hydroxylgruppen p\u00e5 imidazolringen af forbindelse 9 og aminogruppen p\u00e5 thiophenringen af forbindelse 11 som hydrogenbindingsdonorer til at danne hydrogenbindinger med FXa og derved forbedre affiniteten mellem forbindelsen og receptoren. Dette kan v\u00e6re \u00e5rsagen til den st\u00e6rke aktivitet. Derudover kan svovl-heterocyklen i strukturen af forbindelse 11 bidrage til forbedring af forbindelsens aktivitet, og yderligere udforskning er n\u00f8dvendig. Ovenst\u00e5ende vil give nye ideer til yderligere optimering af strukturen af derivater af berberin.<\/p>","protected":false},"excerpt":{"rendered":"<p>Study on the structural modification of Pixiu alcohol and its anticoagulant factor Xa activity Pixiu grass is an annual herbaceous plant of the Pixiu genus in the Asteraceae family. The 2020 edition of the Pharmacopoeia of the People&#8217;s Republic of China includes dried aboveground parts of three plants in the Asteraceae family, namely Siegesbeckia orientalis [&hellip;]<\/p>","protected":false},"author":1,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[20],"tags":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v23.0 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Study on the structural modification of Pixiu alcohol and its anticoagulant factor Xa activity - China Chemical Manufacturer<\/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:\/\/longchangextracts.com\/da\/pixiu-graes\/\" \/>\n<meta property=\"og:locale\" content=\"da_DK\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Study on the structural modification of Pixiu alcohol and its anticoagulant factor Xa activity - China Chemical Manufacturer\" \/>\n<meta property=\"og:description\" content=\"Study on the structural modification of Pixiu alcohol and its anticoagulant factor Xa activity Pixiu grass is an annual herbaceous plant of the Pixiu genus in the Asteraceae family. 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