Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100193, People's Republic of China.
J Agric Food Chem. 2017 May 24;65(20):4066-4073. doi: 10.1021/acs.jafc.7b00743. Epub 2017 May 16.
As a major active stilbene from the leaves of pigeon pea (Cajanus cajan), cajaninstilbene acid (CSA) exerts various pharmacological activities. The present study aimed to investigate the pharmacokinetics of CSA and one of its main metabolites (M1) to explore their fate in the body and provide a pharmacokinetic foundation for their in vivo biological activities and functional food or complementary medicine application. M1 was characterized as CSA-3-O-glucuronide using the multiple reaction monitoring-information-dependent acquisition-enhanced product ion technique. After oral and intravenous administration, plasma, urine, and bile were collected and analyzed to estimate pharmacokinetic properties of CSA and M1 and to explore the main excretion route. The oral bioavailability of CSA was estimated to be 44.36%. This study first reported that CSA is mainly metabolized to CSA-3-O-glucuronide via the first-pass effect to limit its oral bioavailability and excreted predominantly through the biliary route, while the enterohepatic circulation, extravascular distribution, and renal reabsorption characteristics of CSA might delay its elimination.
作为落花生（Cajanus cajan）叶中的一种主要的活性二苯乙烯，鸡纳酸（CSA）发挥着各种药理活性。本研究旨在研究 CSA 及其主要代谢物（M1）的药代动力学，以探索它们在体内的命运，并为其体内生物活性和功能性食品或补充药物应用提供药代动力学基础。采用多重反应监测-信息依赖性采集-增强子离子技术，将 M1 鉴定为 CSA-3-O-葡萄糖醛酸苷。口服和静脉给药后，收集并分析血浆、尿液和胆汁，以评估 CSA 和 M1 的药代动力学特性，并探索主要的排泄途径。CSA 的口服生物利用度估计为 44.36%。本研究首次报道 CSA 主要通过首过效应代谢为 CSA-3-O-葡萄糖醛酸苷，从而限制其口服生物利用度，并主要通过胆汁途径排泄，而 CSA 的肠肝循环、血管外分布和肾重吸收特征可能会延迟其消除。
