Pharmacokinetics, Bioavailability, and Tissue Distribution Study of Angoroside C and Its Metabolite Ferulic Acid in Rat Using UPLC-MS/MS.
Pharmacokinetics, Bioavailability, and Tissue Distribution Study of Angoroside C and Its Metabolite Ferulic Acid in Rat Using UPLC-MS/MS.
复制标题
采用 UPLC-MS/MS 进行安果苷 C 及其代谢物阿魏酸在大鼠体内的药代动力学、生物利用度和组织分布研究
DOI：
10.3389/fphar.2018.01186
复制
发表时间：
2018
影响因子：
5.6
通讯作者：
Zheng T
中科院分区：
文献类型：
--
作者：
Zhang C;Ma W;Zhang Y;Wang Q;Qin C;Du S;Huang L;Ye F;Chen L;Zheng T
樟脑苷C是一种从樟脑干根中分离得到的苯丙苷类化合物。，具有防止心室重构、减轻肺水肿、降低血压的作用，并具有抗血小板聚集、保肝、抗肾炎等特性。然而，对鹿皮苷C的吸收、分布、代谢和排泄（ADME）研究较少。为此，建立了一种超高效液相色谱-串联四极杆质谱（UPLC-MS/MS）快速测定大鼠血浆和组织匀浆中鹿皮苷C及其代谢物阿魏酸的方法。这两种分析物是用简单的蛋白质沉淀和乙腈从生物样品中提取的。验证了该方法的有效性，并成功应用于鹿皮苷C灌胃（100mg /kg）和静脉给药（5mg /kg）后的药代动力学、生物利用度和组织分布研究。结果表明，鹿皮苷C吸收极快（Tmax = 15 min），清除极快（t1/2 = 1.26 h），口服生物利用度仅为2.1%左右。此外，鹿皮苷C广泛分布于各主要脏器（肝、心、脾、肺、肾、脑），并在口服15 min后肺中检测到最高浓度。本文还表明，鹿皮苷C在体内可转化为活性代谢物阿魏酸。阿魏酸在肾脏中的最高浓度出现在口服给药后6小时。综上所述，本研究探讨了赤罗苷C在体内的一些药动学特征，所得数据可为进一步研究赤罗苷C提供依据。
Angoroside C is a phenylpropanoid glycoside compound isolated from the dried root of Scrophularia ningpoensis Hemsl., which possesses the effects of preventing ventricular remodeling, reducing pulmonary oedema, and reducing blood pressure, as well as having the properties of anti-platelet aggregation, hepatoprotection and anti-nephritis, etc. However, few investigations have been conducted on the absorption, distribution, metabolism, and excretion (ADME) study of angoroside C. Thus, a fast ultra-high performance liquid chromatography-tandem quadrupole mass spectrometry (UPLC-MS/MS) method was established for the determination of angoroside C and its metabolite ferulic acid in rat plasma and tissue homogenate. The two analytes were extracted from the biosamples using a simple protein precipitation with acetonitrile. The developed method was validated and successfully applied to the pharmacokinetics, bioavailability and tissue distribution study after the intragastric administration of angoroside C (100 mg/kg) or the intravenous administration of angoroside C (5 mg/kg), respectively. The results showed that angoroside C can be absorbed extremely quickly (Tmax = 15 min), can be eliminated very rapidly (t1/2 = 1.26 h), and its oral bioavailability is only about 2.1%. Furthermore, angoroside C was extensively distributed in all main organs (liver, heart, spleen, lung, kidney, and brain), and the highest concentration was detected in the lung 15 min after oral administration. This paper also indicated that angoroside C could be converted to the active metabolite ferulic acid in vivo. The maximum concentrations of ferulic acid in the kidney occurred at 6 h after oral administration. In summary, this study explored some of the pharmacokinetic characteristics of angoroside C in vivo, and the data produced could provide a basis for the further investigation of angoroside C.
登录
查看更多内容
DOI：
10.3390/molecules22111937
发表时间：
2017-11-09
期刊：
Molecules (Basel, Switzerland)
影响因子：
--
作者：
Liu Y;Chi S;Wang W;Su L;Liu B
通讯作者：
Liu B
影响因子：
4.6
作者：
Liu H;Zheng YF;Li CY;Zheng YY;Wang DQ;Wu Z;Huang L;Wang YG;Li PB;Peng W;Su WW
通讯作者：
Su WW
影响因子：
7.9
作者：
Huang, Xiao Yan;Chen, Chang Xun;Li, Yi Ming
通讯作者：
Li, Yi Ming
影响因子：
3.8
作者：
Li, YM;Jiang, SH;Zhu, DY
通讯作者：
Zhu, DY
影响因子：
2.7
作者：
Qian, J.;Hunkler, D.;Rimpler, H.
通讯作者：
Rimpler, H.