Wang Junjun, Yu Xuejin, Zhang Ling, Wang Ling, Peng Zhihong, Chen Yong
Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, Hubei Collaborative Innovation Center for Green Transformation of Bio-resources, Hubei University, Wuhan, China.
Research Chemicals, Honeywell Integrated Technology (China) Co. Ltd, Shanghai, China.
Biomed Chromatogr. 2018 Apr 24:e4267. doi: 10.1002/bmc.4267.
Curcumin (CUR) is the major active component of turmeric and plays an important role in the prevention and treatment of many chronic diseases such as respiratory and neurodegenerative disease. In the present work, a rapid and simple LC-MS/MS method was developed to investigate the pharmacokinetics and tissue distribution of CUR and its metabolites in mice after intravenous administration of CUR (20 mg/kg). The results showed that the values of AUC were 107.0 ± 18.3, 6.0 ± 1.2 and 12.0 ± 4.0 (mg/L) min, and those for t were 32.4 ± 10.8, 6.4 ± 2.4 and 5.6 ± 1.8 min for CUR, dihydrocurcumin (DHC) and tetrahydrocurcumin (THC) in plasma, respectively. CUR and THC could be detected in liver while CUR and DHC were detected in kidney. Only CUR was detected in brain. These findings indicated that THC was the main metabolite of CUR in plasma. The exposure of CUR in plasma was 6-fold greater than that in liver, kidney and brain.
姜黄素（CUR）是姜黄的主要活性成分，在预防和治疗许多慢性疾病（如呼吸系统疾病和神经退行性疾病）中发挥着重要作用。在本研究中，开发了一种快速简便的液相色谱-串联质谱法（LC-MS/MS），用于研究静脉注射CUR（20 mg/kg）后小鼠体内CUR及其代谢产物的药代动力学和组织分布。结果表明，血浆中CUR、二氢姜黄素（DHC）和四氢姜黄素（THC）的AUC值分别为107.0±18.3、6.0±1.2和12.0±4.0（mg/L）·min，t值分别为32.4±10.8、6.4±2.4和5.6±1.8 min。肝脏中可检测到CUR和THC，肾脏中可检测到CUR和DHC。脑中仅检测到CUR。这些发现表明，THC是血浆中CUR的主要代谢产物。CUR在血浆中的暴露量比在肝脏、肾脏和脑中高6倍。
