Analysis of the pharmacokinetics and metabolism of aloe-emodin following intravenous and oral administrations in rats

被引:29
作者
Yu, Chung-Ping [1 ]
Shia, Chi-Sheng [2 ]
Lin, Hui-Ju [1 ,3 ]
Hsieh, Yow-Wen [2 ,4 ]
Lin, Shiuan-Pey [2 ]
Hou, Yu-Chi [2 ,4 ]
机构
[1] China Med Univ, Sch Chinese Med, Taichung 404, Taiwan
[2] China Med Univ, Sch Pharm, Taichung 404, Taiwan
[3] China Med Univ Hosp, Dept Ophthalmol, Taichung 404, Taiwan
[4] China Med Univ Hosp, Dept Pharm, Taichung 404, Taiwan
关键词
aloe-emodin; rhein; pharmacokinetics; metabolism; LC; MS; PERFORMANCE LIQUID-CHROMATOGRAPHY; VIVO ANTIOXIDANT ACTIVITY; MASS-SPECTROMETRY; P-GLYCOPROTEIN; ANTHRAQUINONES; BIOAVAILABILITY; RHUBARB; POLYPHENOLS; MACROPHAGES; DERIVATIVES;
D O I
10.1002/bmc.3735
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Aloe-emodin, a natural polyphenolic anthraquinone, has shown various beneficial bioactivities in vitro. The aim of this study was to investigate the pharmacokinetics and metabolism of aloe-emodin. Aloe-emodin was intravenously and orally administered to rats. The concentrations of aloe-emodin and rhein, a metabolite of aloe-emodin, were determined by HPLC method prior to and after hydrolysis with -glucuronidase and sulfatase/-glucuronidase. The results showed that the systemic exposures of aloe-emodin and its metabolites were ranked as aloe-emodin glucuronides (G)>rhein sulfates (S)>aloe-emodin > rhein and rhein G when aloe-emodin was given intravenously. In contrast, when aloe-emodin was administered orally, the parent form of aloe-emodin was not absorbed per se, and the systemic exposures of its metabolites were ranked as aloe-emodin G>rhein G>rhein. In conclusion, the metabolites of aloe-emodin are more important than the parent form for the bioactivities in vivo. Copyright (c) 2016 John Wiley & Sons, Ltd.
引用
收藏
页码:1641 / 1647
页数:7
相关论文
共 28 条
[1]   Evaluation of the anti-angiogenic effect of aloe-emodin [J].
Cardenas, C. ;
Quesada, A. R. ;
Medina, M. A. .
CELLULAR AND MOLECULAR LIFE SCIENCES, 2006, 63 (24) :3083-3089
[2]   Evaluation of the anti-inflammatory and cytotoxic effects of anthraquinones and anthracenes derivatives in human leucocytes [J].
Chen, RF ;
Shen, YC ;
Huang, HS ;
Liao, JF ;
Ho, LK ;
Chou, YC ;
Wang, WY ;
Chen, CF .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 2004, 56 (07) :915-919
[3]   Potential Antineoplastic Effects of Aloe-emodin: A Comprehensive Review [J].
Chen, Ruie ;
Zhang, Jinming ;
Hu, Yangyang ;
Wang, Shengpeng ;
Chen, Meiwan ;
Wang, Yitao .
AMERICAN JOURNAL OF CHINESE MEDICINE, 2014, 42 (02) :275-288
[4]   Anti-inflammatory properties of anthraquinones and their relationship with the regulation of p-glycoprotein function and expression [J].
Choi, Ran Joo ;
Tran Minh Ngoc ;
Bae, KiHwan ;
Cho, Hyun-Jong ;
Kim, Dae-Duk ;
Chun, Jaemoo ;
Khan, Salman ;
Kim, Yeong Shik .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2013, 48 (1-2) :272-281
[5]   A good practice guide to the administration of substances and removal of blood, including routes and volumes [J].
Diehl, KH ;
Hull, R ;
Morton, D ;
Pfister, R ;
Rabemampianina, Y ;
Smith, D ;
Vidal, JM ;
van de Vorstenbosch, C .
JOURNAL OF APPLIED TOXICOLOGY, 2001, 21 (01) :15-23
[6]   Improving the Dissolution and Oral Bioavailability of the Poorly Water-soluble Drug Aloe-Emodin by Solid Dispersion With Polyethylene Glycol 6000 [J].
Duan, Hao-gang ;
Wei, Yu-hui ;
Li, Bo-xia ;
Qin, Hong-yan ;
Wu, Xin-an .
DRUG DEVELOPMENT RESEARCH, 2009, 70 (05) :363-369
[7]   Peptidyl anthraquinones as potential antineoplastic drugs: Synthesis, DNA binding, redox cycling, and biological activity [J].
Gatto, B ;
Zagotto, G ;
Sissi, C ;
Cera, C ;
Uriarte, E ;
Palu, G ;
Capranico, G ;
Palumbo, M .
JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (16) :3114-3122
[8]   Anticancer effect of aloe-emodin on cervical cancer cells involves G2/M arrest and induction of differentiation [J].
Guo, Jun-ming ;
Xiao, Bing-xiu ;
Liu, Qiong ;
Zhang, Shun ;
Liu, Dong-hai ;
Gong, Zhao-hui .
ACTA PHARMACOLOGICA SINICA, 2007, 28 (12) :1991-1995
[9]   Aloe-emodin from rhubarb (Rheum rhabarbarum) inhibits lipopolysaccharide-induced inflammatory responses in RAW264.7 macrophages [J].
Hu, Boyang ;
Zhang, Hai ;
Meng, Xianli ;
Wang, Fei ;
Wang, Ping .
JOURNAL OF ETHNOPHARMACOLOGY, 2014, 153 (03) :846-853
[10]   Anti-cancer properties of anthraquinones from rhubarb [J].
Huang, Qing ;
Lu, Guodong ;
Sben, Han-Ming ;
Cbung, Maxey C. M. ;
Ong, Choon Nam .
MEDICINAL RESEARCH REVIEWS, 2007, 27 (05) :609-630