{"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\/tr\/pixiu-cim\/","title":{"rendered":"Pixiu alkol\u00fcn yap\u0131sal modifikasyonu ve antikoag\u00fclan fakt\u00f6r Xa aktivitesi \u00fczerine \u00e7al\u0131\u015fma"},"content":{"rendered":"<p>Pixiu alkol\u00fcn yap\u0131sal modifikasyonu ve antikoag\u00fclan fakt\u00f6r Xa aktivitesi \u00fczerine \u00e7al\u0131\u015fma<br \/>\nPixiu otu, Asteraceae familyas\u0131ndaki Pixiu cinsinin y\u0131ll\u0131k otsu bir bitkisidir. \u00c7in Halk Cumhuriyeti Farmakopesi'nin 2020 bask\u0131s\u0131, Asteraceae familyas\u0131ndaki Siegesbeckia orientalis L., Siegesbeckia pubescens Makino ve Siegesbeckia glabrescent Makino adl\u0131 \u00fc\u00e7 bitkinin kurutulmu\u015f toprak \u00fcst\u00fc k\u0131s\u0131mlar\u0131n\u0131 geleneksel \u00c7in t\u0131bb\u0131 \"Siegesbeckia\" olarak i\u00e7ermektedir. R\u00fczgar ve rutubeti giderme, eklem geli\u015fimini te\u015fvik etme ve detoksifiye etme etkilerine sahiptir. Romatizma ve a\u011fr\u0131, kas ve kemik zay\u0131fl\u0131\u011f\u0131, bel ve dizlerde a\u011fr\u0131 ve g\u00fc\u00e7s\u00fczl\u00fck, uzuv felci, hemipleji, k\u0131zam\u0131k\u00e7\u0131k ve \u0131slak yaralar i\u00e7in kullan\u0131l\u0131r. Modern farmakolojik deneyler, Polygonatum sibiricum ekstrakt\u0131n\u0131n anti-enflamatuar, anti alerjik, anti trombotik ve anti histamin sal\u0131n\u0131m aktivitelerine sahip oldu\u011funu g\u00f6stermi\u015ftir. Kimyasal bile\u015fim ve farmakolojik aktivite \u00e7al\u0131\u015fmalar\u0131, Polygonatum sibiricum'daki bol miktarda diterpenoid bile\u015fiklerin, \u00f6zellikle anti-enflamatuar, analjezik ve kan aktive edici ve staz giderici y\u00f6nlerdeki \u00e7e\u015fitli etkilerinin maddi temeli oldu\u011funu g\u00f6stermi\u015ftir.<br \/>\nDarutigenol, Scutellaria baicalensis bitkisinden elde edilen bir diterpenoid bile\u015fi\u011fidir. Modern farmakolojik deneyler, Darutigenol'\u00fcn s\u0131\u00e7anlarda maksimum trombosit agregasyon oran\u0131n\u0131 ve yap\u0131\u015fma oran\u0131n\u0131 \u00f6nemli \u00f6l\u00e7\u00fcde inhibe edebildi\u011fini, \u00f6globulinin \u00e7\u00f6z\u00fcnme s\u00fcresini ve farelerde kanama ve p\u0131ht\u0131la\u015fma s\u00fcresini uzatt\u0131\u011f\u0131n\u0131, kan staz modeli s\u0131\u00e7anlarda tam kan viskozitesini ve plazma viskozitesini \u00f6nemli \u00f6l\u00e7\u00fcde azaltt\u0131\u011f\u0131n\u0131, anormal kan reolojisini iyile\u015ftirdi\u011fini ve kan staz modeli s\u0131\u00e7anlarda TXB2 sentezini inhibe etti\u011fini g\u00f6stermi\u015ftir. Belirgin antitrombotik, trombolitik, antikoag\u00fclan ve hemoreolojik etkileri vard\u0131r. Koag\u00fclasyon fakt\u00f6r\u00fc Xa (FXa), endojen ve eksojen koag\u00fclasyon yollar\u0131n\u0131n kesi\u015fti\u011fi noktada bulunur ve koag\u00fclasyon yolunda \u00f6nemli bir rol oynar, bu da onu son y\u0131llarda antikoag\u00fclan ila\u00e7 ara\u015ft\u0131rmalar\u0131nda s\u0131cak noktalardan biri haline getirir. Bu nedenle, bu makale, ara\u015ft\u0131rma grubumuz taraf\u0131ndan Pixiu otundan izole edilen aktif bile\u015fik Pixiu alkol \u00fczerinde erken a\u015famada yap\u0131sal modifikasyon \u00e7al\u0131\u015fmalar\u0131 y\u00fcr\u00fctm\u00fc\u015f ve daha iyi aktiviteye sahip \u00f6nc\u00fc bile\u015fik molek\u00fclleri ke\u015ffetmek i\u00e7in p\u0131ht\u0131la\u015fma fakt\u00f6r\u00fc Xa \u00fczerindeki etkisini ara\u015ft\u0131rm\u0131\u015ft\u0131r. Bu \u00e7al\u0131\u015fma, yeni k\u00fc\u00e7\u00fck molek\u00fcll\u00fc antitrombotik ila\u00e7lar\u0131n ke\u015ffi ve Hedyotis diffusa gibi t\u0131bbi bitkilerin geli\u015ftirilmesi i\u00e7in referans sa\u011flayacakt\u0131r.<\/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\" \/>\u0130duban taraf\u0131ndan temsil edilen FXa inhibit\u00f6rlerinin klinik etkinli\u011finden, iyi bir antikoag\u00fclan etkiye, geni\u015f bir tedavi penceresine sahip oldu\u011fu ve y\u00fcksek g\u00fcvenlikle hiperkoag\u00fclabil reaksiyonlara neden olmaya e\u011filimli olmad\u0131\u011f\u0131 g\u00f6r\u00fclebilir. G\u00fcn\u00fcm\u00fczde antikoag\u00fclan ila\u00e7 ara\u015ft\u0131rmalar\u0131nda s\u0131cak bir konu haline gelmi\u015ftir. Do\u011fal \u00fcr\u00fcnler antikoag\u00fclasyonda benzersiz avantajlara sahiptir ve geleneksel \u00c7in t\u0131bb\u0131ndan kesin klinik etkinli\u011fe sahip aktif bile\u015fenleri ke\u015ffetmek ve yap\u0131sal modifikasyon ara\u015ft\u0131rmalar\u0131 yapmak yeni antikoag\u00fclanlar ke\u015ffetmek i\u00e7in \u00f6nemli bir yol olabilir. Pixiu alkol, geleneksel \u00c7in t\u0131bb\u0131 Pixiu otundan izole edilen aktif bir bile\u015fiktir. \u00d6nceki \u00e7al\u0131\u015fmalar \u00f6nemli antikoag\u00fclan aktiviteye sahip oldu\u011funu g\u00f6stermi\u015ftir. Bu nedenle, bu \u00e7al\u0131\u015fma Pixiu alkol \u00fczerinde yap\u0131sal modifikasyon ara\u015ft\u0131rmas\u0131 y\u00fcr\u00fctm\u00fc\u015f ve geli\u015ftirme de\u011feri olan yeni FXa inhibit\u00f6rlerini ke\u015ffetmeyi ama\u00e7layarak FXa inhibit\u00f6r aktivitesi i\u00e7in taram\u0131\u015ft\u0131r.<\/p>\n<p>Berberinin yap\u0131sal \u00f6zelliklerine dayanarak, bu t\u00fcr bile\u015fiklerin hidrofilikli\u011fini ve aktivitesini geli\u015ftirmek i\u00e7in orijinal yap\u0131ya bir heterosiklik halka eklenmi\u015ftir. Bu nedenle, berberinin A halkas\u0131na be\u015f \u00fcyeli bir heterosiklik halka eklenerek \u00e7e\u015fitli t\u00fcrevler tasarlanm\u0131\u015f ve sentezlenmi\u015ftir. Berberin ve t\u00fcrevleri \u00fczerinde in vitro FXa inhibisyon deneyleri yap\u0131larak, iyi aktiviteye sahip (IC50&lt;10 \u03bc mol\/L) yedi bile\u015fik elde edilmi\u015ftir. Berberin ile kar\u015f\u0131la\u015ft\u0131r\u0131ld\u0131\u011f\u0131nda, \u00e7o\u011fu t\u00fcrev, p\u0131ht\u0131la\u015fma fakt\u00f6r\u00fc FXa&#039;n\u0131n inhibit\u00f6r aktivitesinde belirli bir art\u0131\u015f g\u00f6stermi\u015ftir; bunlar aras\u0131nda 9 ve 11 numaral\u0131 bile\u015fikler, s\u0131ras\u0131yla 0,71 \u00b1 0,07 ve 0,22 \u00b1 0,03 \u03bc mol\/L IC50 de\u011ferleri ile en \u00f6nemlileridir. \u00d6n yap\u0131-aktivite ili\u015fkisi \u00e7al\u0131\u015fmalar\u0131, orijinal yap\u0131daki 15,16-diollere metilen gruplar\u0131n\u0131n eklenmesinin ve A halkas\u0131na heterosikllerin eklenmesinin bile\u015fiklerin aktivitesini art\u0131rabilece\u011fini ve heterosiklik s\u00fcbstit\u00fcentler \u00fczerindeki elektronik etkinin aktiviteyi art\u0131rmada \u00f6nemli bir rol oynad\u0131\u011f\u0131n\u0131 g\u00f6stermi\u015ftir. Bilgisayar destekli ila\u00e7 tasar\u0131m\u0131nda ligand protein etkile\u015fim modellerinin analizine g\u00f6re, bile\u015fik 9&#039;un imidazol halkas\u0131 \u00fczerindeki hidroksil grubu ve bile\u015fik 11&#039;in tiyofen halkas\u0131 \u00fczerindeki amino grubu, FXa ile hidrojen ba\u011flar\u0131 olu\u015fturmak i\u00e7in hidrojen ba\u011f\u0131 don\u00f6rleri olarak hareket eder, b\u00f6ylece bile\u015fik ve resept\u00f6r aras\u0131ndaki afiniteyi artt\u0131r\u0131r. G\u00fc\u00e7l\u00fc aktivitesinin nedeni bu olabilir. Ayr\u0131ca, bile\u015fik 11&#039;in yap\u0131s\u0131ndaki s\u00fclf\u00fcr heterosikl bile\u015fik aktivitesinin iyile\u015ftirilmesine katk\u0131da bulunabilir ve daha fazla ara\u015ft\u0131rmaya ihtiya\u00e7 vard\u0131r. Yukar\u0131dakiler, berberin t\u00fcrevlerinin yap\u0131s\u0131n\u0131 daha da optimize etmek i\u00e7in yeni fikirler sa\u011flayacakt\u0131r.<\/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\/tr\/pixiu-cim\/\" \/>\n<meta property=\"og:locale\" content=\"tr_TR\" \/>\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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