Li Fei, Yang Xiu-Wei
State Key Laboratory of Natural and Biomimetic Drugs and Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University, Beijing, China.
Biomed Chromatogr. 2012 Jun;26(6):703-7. doi: 10.1002/bmc.1717. Epub 2011 Sep 19.
Dehydrodiisoeugenol (DDIE) is a lignan in the fruit of Myristica fragrans. It can be converted into several metabolites in in vitro and in vivo metabolism. In this study, the excretion of DDIE in urine and feces was investigated after intravenous (i.v.) and intragastric (i.g.) administration to rats. DDIE and its metabolites (M-1 and M-2) were measured using HPLC. The amount of DDIE and its metabolites excreted was higher in feces than in urine, suggesting that DDIE and its metabolites are eliminated primarily in the feces. Significant differences in the excretion levels of DDIE and its metabolites were seen between i.v. and i.g. administration. Greater amounts of DDIE and its metabolites were excreted following i.v. administration, suggesting that DDIE can exert a longer period of anti-inflammatory activity following i.g. administration. The accuracy, precision, recovery and stability of the analytical method in this study were satisfactory for the measurement of DDIE and its metabolites in rat urine and feces. Observations made in this study will contribute to understanding of the absorption, distribution, metabolism and excretion pathway of DDIE and will aid decision-making regarding the best mode of DDIE administration during treatment to maximize its anti-inflammatory effects.
脱氢二异丁香酚（DDIE）是肉豆蔻果实中的一种木脂素。它在体外和体内代谢过程中可转化为多种代谢产物。在本研究中，对大鼠静脉注射（i.v.）和灌胃（i.g.）给药后，DDIE在尿液和粪便中的排泄情况进行了研究。使用高效液相色谱法（HPLC）测定DDIE及其代谢产物（M-1和M-2）。DDIE及其代谢产物在粪便中的排泄量高于尿液，这表明DDIE及其代谢产物主要通过粪便排出。静脉注射和灌胃给药后，DDIE及其代谢产物的排泄水平存在显著差异。静脉注射给药后，DDIE及其代谢产物的排泄量更大，这表明灌胃给药后DDIE可发挥更长时间的抗炎活性。本研究中分析方法的准确性、精密度、回收率和稳定性对于测定大鼠尿液和粪便中的DDIE及其代谢产物而言令人满意。本研究中的观察结果将有助于了解DDIE的吸收、分布代谢和排泄途径，并有助于在治疗期间就DDIE的最佳给药方式做出决策，以最大限度地发挥其抗炎作用。
