Chen Cong, Feng Yanbo, Li Han, Lin Hao, Jing Shu, Li He, Wang Chunmei, Chen Jianguang, Sun Jinghui
College of Pharmacy, Beihua University, Jilin, China.
Front Pharmacol. 2022 Jul 5;13:929177. doi: 10.3389/fphar.2022.929177. eCollection 2022.
Anwulignan is a representative component of Chinese traditional medicine , with strong pharmacological activities. However, there are few reports on its pharmacokinetics and metabolites in the body. In this study, a metabolomic method based on UHPLC-Q-Orbitrap-MS was used to study the pharmacokinetics of anwulignan in the blood, organs, urine, and feces samples of mice after the intragastric administration of anwulignan (10 mg/kg). The pharmacokinetic parameters were calculated, and the distribution characteristics and main metabolites of anwulignan in the body of mice were analyzed. The results showed that the retention time of anwulignan in the body of mice was longer ( = 7.1 h), and anwulignan was widely distributed in the body (V = 32.81 L/kg), especially in the liver. The order of anwulignan concentration in the tissues of mice from high to low was the liver > heart > brain > kidney > lung > spleen. Anwulignan was mainly excreted through the digestive tract in the form of its prototype and metabolites, indicating that it might experience an enterohepatic circulation. A total of seven metabolites were identified, and the demethylation, hydroxylation, dehydroxylation, and demethoxylation were considered to be the main metabolic ways of anwulignan in the body of mice.
暗物质是中药的代表性成分，具有较强的药理活性。然而，关于其体内药代动力学和代谢产物的报道较少。本研究采用基于超高效液相色谱-四极杆-轨道阱质谱联用（UHPLC-Q-Orbitrap-MS）的代谢组学方法，研究了暗物质（10 mg/kg）灌胃给药后在小鼠血液、器官、尿液和粪便样本中的药代动力学。计算了药代动力学参数，分析了暗物质在小鼠体内的分布特征和主要代谢产物。结果表明，暗物质在小鼠体内的保留时间较长（t1/2 = 7.1 h），且在体内广泛分布（V = 32.81 L/kg），尤其在肝脏中。暗物质在小鼠组织中的浓度由高到低的顺序为肝脏>心脏>大脑>肾脏>肺>脾脏。暗物质主要以原型和代谢产物的形式通过消化道排泄，表明其可能存在肠肝循环。共鉴定出7种代谢产物，去甲基化、羟基化、去羟基化和去甲氧基化被认为是暗物质在小鼠体内的主要代谢途径。
