Cheng Wenhao, Wu Siyang, Yuan Zheng, Hu Weiyu, Yu Xin, Kang Nianxin, Wang Qiutao, Zhu Mingying, Xia Kexin, Yang Wei, Kang Chen, Zhang Shuofeng, Li Yingfei
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China.
Center for DMPK Research of Herbal Medicines, Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, China.
Front Pharmacol. 2022 Feb 21;13:827668. doi: 10.3389/fphar.2022.827668. eCollection 2022.
Although progress has been achieved in the pharmacological activity and toxicity of Radix Polygoni Multiflori (RPM), the chemical basis of its toxicity is still unclear. Here, we performed a multicompound pharmacokinetic analysis and investigated the tissue distribution and excretion characteristics of RPM components after oral administration in rats. The findings demonstrated that the active ingredients of the RPM extract were quickly absorbed after oral administration, with high exposure levels of emodin, 2,3,5,4'-teterahydroxystilbene-2-O-β-D-glucoside (TSG), citreorosein, torachrysone-8-O-glucoside (TG), emodin-8-O-β-D-glucoside (EG), and physcion-8-O-β-D-glucoside (PG). The tissue distributions of emodin, TSG, TG, EG, and PG were high in the liver and kidney. These components were the key contributors to the effectiveness and toxicity of RPM on the liver and kidney. Most of the active ingredients were mainly excreted through feces and bile, while a few were converted into other products in the body and excreted through urine and feces.
尽管何首乌在药理活性和毒性方面已取得进展，但其毒性的化学基础仍不清楚。在此，我们进行了多化合物药代动力学分析，并研究了大鼠口服何首乌成分后的组织分布和排泄特征。研究结果表明，何首乌提取物的活性成分口服后迅速吸收，大黄素、2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷（TSG）、橙黄决明素、大黄素甲醚-8-O-葡萄糖苷（TG）、大黄素-8-O-β-D-葡萄糖苷（EG）和大黄酚-8-O-β-D-葡萄糖苷（PG）的暴露水平较高。大黄素、TSG、TG、EG和PG在肝脏和肾脏中的组织分布较高。这些成分是何首乌对肝脏和肾脏有效性和毒性的关键因素。大多数活性成分主要通过粪便和胆汁排泄，而少数在体内转化为其他产物并通过尿液和粪便排泄。
