Department of Pharmacology, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Beijing 100193, China.
Phytomedicine. 2010 Jul;17(8-9):640-5. doi: 10.1016/j.phymed.2009.12.010. Epub 2010 Jan 21.
Hawthorn leaf flavonoids (HLF) are used in the treatment of cardiovascular diseases. Various potential pharmacodynamic effects have been observed for vitexin-4''-O-glucoside (VOG) and vitexin-2''-O-rhamnoside (VOR) which are the main constituents of HLF. The aim of this study was to investigate the pharmacokinetics of VOG and VOR when a single dose of HLF was administrated orally. The levels of VOG and VOR in plasma, tissues (heart, liver, spleen, lung, kidney and brain), bile, urine and feces were measured by HPLC-UV. The results showed that VOG and VOR have the similar pharmacokinetics. Both of them were absorbed quickly into plasma with maximal plasma concentrations of VOG and VOR being reached within 0.75 h. The mean elimination half-life (t(1/2)) of VOG and VOR were 2.53 h and 2.32 h, respectively. High levels of tissue distribution of VOG and VOR were observed in liver and kidney. No VOG and VOR were detected in brain tissue. There was no long-term accumulation of VOG and VOR in rat tissues examined. The total recovery of the dose in 24 hours was 64.91% (0.70% in urine; 64.21% in feces) for VOG and 89.01% (0.72% in urine; 88.29% in feces) for VOR. The cumulative VOG and VOR excreted in bile represented 0.58% and 13.38% of the doses, respectively. VOG and VOR in HLF were not efficiently absorbed in the rodent gastrointestinal tract.
山楂叶总黄酮（HLF）被用于治疗心血管疾病。牡荆素-4''-O-葡萄糖苷（VOG）和牡荆素-2''-O-鼠李糖苷（VOR）是 HLF 的主要成分，它们具有多种潜在的药效学作用。本研究旨在研究单次口服 HLF 时 VOG 和 VOR 的药代动力学。采用 HPLC-UV 法测定血浆、组织（心、肝、脾、肺、肾、脑）、胆汁、尿液和粪便中 VOG 和 VOR 的浓度。结果表明，VOG 和 VOR 的药代动力学特征相似。它们均迅速被吸收进入血浆，VOG 和 VOR 的最大血浆浓度分别在 0.75 h 时达到。VOG 和 VOR 的平均消除半衰期（t(1/2)）分别为 2.53 h 和 2.32 h。VOG 和 VOR 在肝和肾组织中有较高的分布水平。脑组织中未检测到 VOG 和 VOR。在检测的大鼠组织中，未发现 VOG 和 VOR 有长期蓄积。24 小时内 VOG 的总回收率为 64.91%（尿液中 0.70%；粪便中 64.21%），VOR 的总回收率为 89.01%（尿液中 0.72%；粪便中 88.29%）。胆汁中累积的 VOG 和 VOR 分别占剂量的 0.58%和 13.38%。HLF 中的 VOG 和 VOR 在啮齿动物胃肠道中吸收效率不高。
