Osthenol, a prenylated coumarin, is a C8-prenylated derivative of umbelliferone isolated from the root of Angelica koreana and Angelica dahurica, an intermediate and is known as a major metabolite of desmethyl-osthole.The various pharmacological effects of osthenol have been reported. In previous studies, we investigated five hydroxylated metabolites by cytochromes P450 (CYP) and glucuronide conjugates of osthenol by uridine diphosphate-glucuronosyltransferases (UGTs). However, osthenol have very few studies have been reported on its pharmacokinetic (PK) profiling, we reported the PK parameters in mouse of osthenol through this study.After oral (5 and 20 mg/kg) and intravenous (5 mg/kg) administration, the concentration of osthenol in plasma was determined by LC-MS/MS. The quantitative method was validated in terms of linearity, accuracy, and precision. When 5 and 20 mg/kg of osthenol were orally administered, the bioavailability (BA) was found to be very low at 0.43 and 0.02%, respectively.In fact, osthenol was mostly metabolized to a two-Phase II conjugates, a sulfonyl and glucuronyl-osthenol, in the blood, which was determined by LC-HR/MS analysis of the blood sample. Because osthenol is rapidly metabolized to two conjugates by first-pass effect the BA of osthenol is low after oral administration.

中文翻译：

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体内邻苯二酚代谢的表征及其药代动力学。

Osthenol是一种烯丙基香豆素，是从当归和当归的根中分离出的伞形酮的C8烯丙基化衍生物，被称为去甲基-osthole的主要代谢产物.osthenol有多种药理作用。在以前的研究中，我们通过尿苷二磷酸-葡萄糖醛酸转移酶（UGT）研究了细胞色素P450（CYP）和邻苯二酚的葡萄糖醛酸苷共轭物的五个羟基化代谢产物。然而，关于雌二醇的药代动力学（PK）分布图的研究很少，我们通过这项研究报告了雌二醇在小鼠中的PK参数。口服（5和20 mg / kg）和静脉内（5 mg / kg）给药后，通过LC-MS / MS测定血浆中邻苯二酚的浓度。定量方法在线性，准确性，和精度。当口服5和20 mg / kg的邻苯二酚时，其生物利​​用度（BA）分别很低，分别为0.43和0.02％。事实上，邻苯二酚主要代谢为两相II结合物，磺酰基和通过血样的LC-HR / MS分析确定血液中的葡糖醛酸-雌二醇。由于邻苯二酚通过首过效应迅速代谢为两种结合物，口服后邻苯二酚的BA较低。