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Steady-state pharmacokinetics and tissue distribution of anthraquinones of Rhei Rhizoma in rats

Shia, Chi-Sheng, Tsai, Shang-Yuan, Lin, Jung-Chih, Li, Ming-Li, Ko, Miau-Hwa, Chao, Pei-Dawn Lee, Huang, Yu-Ching, Hou, Yu-Chi
Journal of ethnopharmacology 2011 v.137 no.3 pp. 1388-1394
Rheum palmatum, blood sampling, brain, emodin, high performance liquid chromatography, kidneys, liver, lungs, medicine, pharmacokinetics, rats, sulfates, tissue analysis, tissue distribution
AIM OF THE STUDY: Rhei Rhizoma, the rhizome of Rheum palmatum L. (RP), is a popular herb in clinical Chinese medicine. RP is abundant in polyphenolic anthraquinones, which have been reported to show various beneficial bioactivities. This study investigated the pharmacokinetics and tissue distribution of anthraquinones following seven-dose administration of RP decoction to rats. MATERIALS AND METHODS: Six Sprague-Dawley rats were given 2.0g/kg of RP twice daily for seven doses and blood samples were collected at designated time after the 7th dose. Another six rats were sacrificed at 30min after the 7th dose and organs including liver, kidney, lung and brain were collected. Serum and tissue specimens were assayed by HPLC before and after hydrolysis with β-glucuronidase and sulfatase, respectively. RESULTS: Pharmacokinetic analysis indicated that the anthraquinones in serum mainly presented as glucuronides/sulfates and contained higher ratio of sulfates when compared with single-dose administration of RP. Contrary to the finding in serum, tissue analysis discovered mainly free form of anthraquinone in most organs assayed, such as aloe-emodin and rhein in kidney, liver, lung; emodin in liver, lung; trace of chrysophanol in kidney and liver. In all brains, neither free forms nor their glucuronides/sulfates have been detected. CONCLUSIONS: The glucuronides/sulfates of anthraquinones were the major forms in bloodstream, whereas the free forms of most anthraquinones were predominant in kidney and liver.