{"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\/hu\/pixiu-grass\/","title":{"rendered":"A Pixiu alkohol szerkezeti m\u00f3dos\u00edt\u00e1s\u00e1nak \u00e9s Xa faktor Xa antikoagul\u00e1ns aktivit\u00e1s\u00e1nak vizsg\u00e1lata"},"content":{"rendered":"<p>A Pixiu alkohol szerkezeti m\u00f3dos\u00edt\u00e1s\u00e1nak \u00e9s Xa faktor Xa antikoagul\u00e1ns aktivit\u00e1s\u00e1nak vizsg\u00e1lata<br \/>\nA Pixiu f\u0171 az Asteraceae csal\u00e1dba tartoz\u00f3 Pixiu nemzets\u00e9ghez tartoz\u00f3 egy\u00e9ves l\u00e1gysz\u00e1r\u00fa n\u00f6v\u00e9ny. A K\u00ednai N\u00e9pk\u00f6zt\u00e1rsas\u00e1g gy\u00f3gyszerk\u00f6nyv\u00e9nek 2020-as kiad\u00e1sa az Asteraceae csal\u00e1dba tartoz\u00f3 h\u00e1rom n\u00f6v\u00e9ny, nevezetesen a Siegesbeckia orientalis L., a Siegesbeckia pubescens Makino \u00e9s a Siegesbeckia glabrescent Makino sz\u00e1r\u00edtott f\u00f6ld feletti r\u00e9szeit tartalmazza hagyom\u00e1nyos k\u00ednai gy\u00f3gyszerk\u00e9nt \"Siegesbeckia\" n\u00e9ven. Sz\u00e9l- \u00e9s nedvess\u00e9geloszlat\u00f3, \u00edz\u00fcletfejl\u0151d\u00e9st el\u0151seg\u00edt\u0151 \u00e9s m\u00e9regtelen\u00edt\u0151 hat\u00e1s\u00fa. Reuma \u00e9s f\u00e1jdalom, izom- \u00e9s csontgyenges\u00e9g, der\u00e9k \u00e9s t\u00e9rd f\u00e1jdalma \u00e9s gyenges\u00e9ge, v\u00e9gtagb\u00e9nul\u00e1s, f\u00e9loldali b\u00e9nul\u00e1s, f\u00e9loldali b\u00e9nul\u00e1s, rubeola \u00e9s nedves sebek eset\u00e9n alkalmazz\u00e1k. A modern farmakol\u00f3giai k\u00eds\u00e9rletek kimutatt\u00e1k, hogy a Polygonatum sibiricum kivonata gyullad\u00e1scs\u00f6kkent\u0151, antiallergi\u00e1s, tromb\u00f3zisellenes \u00e9s hisztamin felszabadul\u00e1st g\u00e1tl\u00f3 hat\u00e1s\u00fa. A k\u00e9miai \u00f6sszet\u00e9tel \u00e9s a farmakol\u00f3giai aktivit\u00e1s vizsg\u00e1latai kimutatt\u00e1k, hogy a Polygonatum sibiricumban tal\u00e1lhat\u00f3 b\u0151s\u00e9ges diterpenoid vegy\u00fcletek k\u00e9pezik a k\u00fcl\u00f6nb\u00f6z\u0151 hat\u00e1sok anyagi alapj\u00e1t, k\u00fcl\u00f6n\u00f6sen a gyullad\u00e1scs\u00f6kkent\u0151, f\u00e1jdalomcsillap\u00edt\u00f3, v\u00e9raktiv\u00e1l\u00f3 \u00e9s szt\u00e1zisold\u00f3 vonatkoz\u00e1sokban.<br \/>\nA darutigenol a Scutellaria baicalensis n\u00f6v\u00e9nyb\u0151l kivont diterpenoid vegy\u00fclet. A modern farmakol\u00f3giai k\u00eds\u00e9rletek kimutatt\u00e1k, hogy a darutigenol jelent\u0151sen g\u00e1tolja a maxim\u00e1lis v\u00e9rlemezke-aggreg\u00e1ci\u00f3s sebess\u00e9get \u00e9s az adh\u00e9zi\u00f3s sebess\u00e9get patk\u00e1nyokban, meghosszabb\u00edtja az euglobulin old\u00f3d\u00e1si idej\u00e9t \u00e9s a v\u00e9rz\u00e9si \u00e9s koagul\u00e1ci\u00f3s id\u0151t egerekben, jelent\u0151sen cs\u00f6kkenti a teljes v\u00e9r viszkozit\u00e1s\u00e1t \u00e9s a plazma viszkozit\u00e1s\u00e1t v\u00e9rstasis modell patk\u00e1nyokban, jav\u00edtja a k\u00f3ros v\u00e9rreol\u00f3gi\u00e1t, \u00e9s g\u00e1tolja a TXB2 szint\u00e9zist v\u00e9rstasis modell patk\u00e1nyokban. Nyilv\u00e1nval\u00f3 antitrombotikus, trombolytikus, antikoagul\u00e1ns \u00e9s hemorheol\u00f3giai hat\u00e1sa van. A Xa alvad\u00e1si faktor (FXa) az endog\u00e9n \u00e9s exog\u00e9n alvad\u00e1si \u00fatvonalak metsz\u00e9spontj\u00e1ban helyezkedik el, \u00e9s fontos szerepet j\u00e1tszik az alvad\u00e1si \u00fatvonalban, \u00edgy az ut\u00f3bbi \u00e9vekben az antikoagul\u00e1ns gy\u00f3gyszerek kutat\u00e1s\u00e1nak egyik forr\u00f3 pontj\u00e1v\u00e1 v\u00e1lt. Ez\u00e9rt ez a tanulm\u00e1ny szerkezeti m\u00f3dos\u00edt\u00e1si vizsg\u00e1latokat v\u00e9gzett a Pixiu-f\u0171b\u0151l a kutat\u00f3csoportunk \u00e1ltal korai szakaszban izol\u00e1lt Pixiu alkohol hat\u00f3anyagon, \u00e9s felt\u00e1rta a Xa alvad\u00e1si faktorra gyakorolt hat\u00e1s\u00e1t, hogy jobb aktivit\u00e1s\u00fa vezet\u0151 vegy\u00fcletmolekul\u00e1kat fedezzen fel. Ez a tanulm\u00e1ny referenci\u00e1t ny\u00fajt az \u00faj kismolekul\u00e1j\u00fa antitrombotikus gy\u00f3gyszerek felfedez\u00e9s\u00e9hez \u00e9s az olyan gy\u00f3gyn\u00f6v\u00e9nyek fejleszt\u00e9s\u00e9hez, mint a 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\" \/>Az iduban \u00e1ltal k\u00e9pviselt FXa-g\u00e1tl\u00f3k klinikai hat\u00e9konys\u00e1g\u00e1b\u00f3l l\u00e1that\u00f3, hogy j\u00f3 v\u00e9ralvad\u00e1sg\u00e1tl\u00f3 hat\u00e1ssal rendelkezik, sz\u00e9les kezel\u00e9si ablakkal rendelkezik, \u00e9s nem hajlamos hiperkoagul\u00e1ci\u00f3s reakci\u00f3kat okozni, nagy biztons\u00e1ggal. Napjainkban az antikoagul\u00e1ns gy\u00f3gyszerek kutat\u00e1s\u00e1ban forr\u00f3 t\u00e9m\u00e1v\u00e1 v\u00e1lt. A term\u00e9szetes term\u00e9keknek egyed\u00fcl\u00e1ll\u00f3 el\u0151nyei vannak az alvad\u00e1sg\u00e1tl\u00e1sban, \u00e9s a hagyom\u00e1nyos k\u00ednai gy\u00f3gy\u00e1szatb\u00f3l sz\u00e1rmaz\u00f3, pontos klinikai hat\u00e9konys\u00e1ggal rendelkez\u0151 hat\u00f3anyagok felfedez\u00e9se \u00e9s a szerkezeti m\u00f3dos\u00edt\u00e1si kutat\u00e1sok elv\u00e9gz\u00e9se fontos \u00fat lehet az \u00faj v\u00e9ralvad\u00e1sg\u00e1tl\u00f3k felfedez\u00e9s\u00e9hez. A Pixiu alkohol a hagyom\u00e1nyos k\u00ednai gy\u00f3gy\u00e1szatban haszn\u00e1lt Pixiu f\u0171b\u0151l izol\u00e1lt akt\u00edv vegy\u00fclet. Kor\u00e1bbi vizsg\u00e1latok kimutatt\u00e1k, hogy jelent\u0151s v\u00e9ralvad\u00e1sg\u00e1tl\u00f3 hat\u00e1ssal rendelkezik. Ez\u00e9rt ebben a tanulm\u00e1nyban a Pixiu alkohol szerkezeti m\u00f3dos\u00edt\u00e1si kutat\u00e1s\u00e1t v\u00e9gezt\u00fck el, \u00e9s az FXa g\u00e1tl\u00f3 aktivit\u00e1st vizsg\u00e1ltuk, azzal a c\u00e9llal, hogy \u00faj, fejleszt\u00e9si \u00e9rt\u00e9kkel b\u00edr\u00f3 FXa-g\u00e1tl\u00f3kat fedezz\u00fcnk fel.<\/p>\n<p>A berberin szerkezeti jellemz\u0151i alapj\u00e1n egy heterociklusos gy\u0171r\u0171t vezettek be az eredeti szerkezetbe, hogy jav\u00edts\u00e1k az ilyen t\u00edpus\u00fa vegy\u00fcletek hidrofilit\u00e1s\u00e1t \u00e9s aktivit\u00e1s\u00e1t. Ez\u00e9rt sz\u00e1mos sz\u00e1rmaz\u00e9kot terveztek \u00e9s szintetiz\u00e1ltak \u00fagy, hogy a berberin A gy\u0171r\u0171j\u00e9be egy \u00f6ttag\u00fa heterociklusos gy\u0171r\u0171t vezettek be. A berberinnel \u00e9s sz\u00e1rmaz\u00e9kaival v\u00e9gzett in vitro FXa-g\u00e1tl\u00e1si k\u00eds\u00e9rletekkel h\u00e9t j\u00f3 aktivit\u00e1s\u00fa (IC50&lt;10 \u03bc mol\/L) vegy\u00fcletet kaptunk. A berberinnel \u00f6sszehasonl\u00edtva a legt\u00f6bb sz\u00e1rmaz\u00e9k bizonyos fokozotts\u00e1got mutatott az FXa v\u00e9ralvad\u00e1si faktor g\u00e1tl\u00f3 hat\u00e1s\u00e1ban, amelyek k\u00f6z\u00fcl a 9. \u00e9s 11. vegy\u00fclet volt a legjelent\u0151sebb, 0,71 \u00b1 0,07 \u00e9s 0,22 \u00b1 0,03 \u03bc mol\/L IC50 \u00e9rt\u00e9kkel. El\u0151zetes szerkezet-aktivit\u00e1s \u00f6sszef\u00fcgg\u00e9s vizsg\u00e1latok kimutatt\u00e1k, hogy az eredeti szerkezetben a 15,16-diolokra metil\u00e9ncsoportok bevezet\u00e9se \u00e9s a heterociklusok bevezet\u00e9se az A gy\u0171r\u0171be fokozhatja a vegy\u00fcletek aktivit\u00e1s\u00e1t, \u00e9s a heterociklusos szubsztituensekre gyakorolt elektronikus hat\u00e1s fontos szerepet j\u00e1tszik az aktivit\u00e1s jav\u00edt\u00e1s\u00e1ban. A ligandum-feh\u00e9rje k\u00f6lcs\u00f6nhat\u00e1si mint\u00e1zatok sz\u00e1m\u00edt\u00f3g\u00e9pes gy\u00f3gyszertervez\u00e9sben v\u00e9gzett elemz\u00e9se szerint a 9. vegy\u00fclet imidazolgy\u0171r\u0171n l\u00e9v\u0151 hidroxilcsoportja \u00e9s a 11. vegy\u00fclet tiofengy\u0171r\u0171n l\u00e9v\u0151 aminocsoportja hidrog\u00e9nk\u00f6t\u00e9s-donork\u00e9nt viselkedik, hogy hidrog\u00e9nk\u00f6t\u00e9seket alak\u00edtson ki az FXa-val, ez\u00e1ltal fokozva a vegy\u00fclet \u00e9s a receptor k\u00f6z\u00f6tti affinit\u00e1st. Ez lehet az oka az er\u0151s aktivit\u00e1snak. Ezenk\u00edv\u00fcl a 11. vegy\u00fclet szerkezet\u00e9ben l\u00e9v\u0151 k\u00e9n heterociklus hozz\u00e1j\u00e1rulhat a vegy\u00fclet aktivit\u00e1s\u00e1nak jav\u00edt\u00e1s\u00e1hoz, \u00e9s tov\u00e1bbi vizsg\u00e1latokra van sz\u00fcks\u00e9g. A fentiek \u00faj \u00f6tletekkel szolg\u00e1lnak a berberin sz\u00e1rmaz\u00e9kok szerkezet\u00e9nek tov\u00e1bbi optimaliz\u00e1l\u00e1s\u00e1hoz.<\/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\/hu\/pixiu-grass\/\" \/>\n<meta property=\"og:locale\" content=\"hu_HU\" \/>\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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