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首页> 外文期刊>RSC Advances >Mechanism in the existent difference in form of wogonin/wogonoside between plasma and intestine/liver in rats
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Mechanism in the existent difference in form of wogonin/wogonoside between plasma and intestine/liver in rats

机译：大鼠血浆与肠/肝中伍格宁/牛磺酸皂甙形式存在差异的机制

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Wogonin (WO) and its glucuronide, wogonoside (WG) exhibit various beneficial bioactivities that may have potential for the development of novel drugs. In this study, we determined their pharmacokinetic characteristics in rats after intragastric administration of WO and intraportal vein injection of WG. WG was the predominant form in the portal vein and body plasma, and in bile; WO was detected only in the small intestine and liver. WG is a substrate of the multidrug resistance-associated protein (MRP) 1, 2, 3, and 4, and organic anion-transporting polypeptide (OATP) 2B1 and OATP1B3. Metabolism studies indicated that WG formation and WO decrease had similar CLint values in rat intestine S9 (RIS9) and rat liver microsome (RLM), and that the hydrolysis rate of WG in RIS9 and rat liver S9 (RLS9) was fast. Thus, WG could be excreted into the intestinal tract by MRP2, and transported into mesenteric blood by MRP1, 3, and 4. OATP2B1 and OATP1B3 mediated the hepatic uptake of WG and MRPs mediated WG efflux to the bile and circulation. The high transport capability of MRPs for WG and the fast hydrolysis in the small intestine and liver may be responsible for the presence of WO in these tissues.
机译：Wogonin（WO）及其葡糖醛酸苷，wogonoside（WG）表现出各种有益的生物活性，可能对开发新药具有潜力。在这项研究中，我们确定了它们在大鼠胃内施用WO和门静脉内注射WG后在大鼠中的药代动力学特征。 WG是门静脉和体内血浆以及胆汁中的主要形式。仅在小肠和肝脏中检测到WO。 WG是多药耐药相关蛋白（MRP）1、2、3和4，以及有机阴离子转运多肽（OATP）2B1和OATP1B3的底物。代谢研究表明，在大鼠小肠S9（RIS9）和大鼠肝微粒体（RLM）中WG的形成和WO的降低具有相似的CL int 值，并且WG的水解速率在RIS9和大鼠肝脏S9（RLS9）中的速度很快。因此，WG可以通过MRP2排入肠道，并通过MRP1、3和4转运到肠系膜血液中。OATP2B1和OATP1B3介导肝对WG的吸收，而MRPs介导WG向胆汁和循环的外排。 MRP对WG的高运输能力以及在小肠和肝脏中的快速水解可能是这些组织中WO的存在的原因。

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