Asian Journal of Pharmacodynamics and Pharmacokinetics

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Xu HY et al. Asian Journal of Pharmacodynamics and Pharmacokinetics 2009; 9(1):11-25 Asian Journal of Pharmacodynamics and Pharmacokinetics ISSN 1608-2281 Copyright by Hong Kong Medical Publisher Publisher Homepage: www.hktmc.com Recent advance on chemical compositions and pharmacodynamic and pharmacokinetic studies of Rhizoma Coptidis Hai-Yu Xu 1,3 , Tie-Jun Zhang 2 , Xue-Yu Zhu 2 ,Yu-Bo Li 1,3 1 Tianjin State Key Laboratory of Pharmacidymanamics and Pharmcokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China 2 Tianjin Research Center of Modern Chinese Medicines, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China 3 Tianjin University of Traditional Chinese Medicine, Tianjing, 300193, China. Abstract Key words Rhizoma Coptidis has long been used for the treatment of gastrointestinal disorders, pyretic toxicity, abdominal typhus, bacillary dysentery, Swelling of throat in traditional oriental medicine in china. Recent studies found that its active constituents are alkaloids comprising berberine, coptisine, palmaine, jatrorrhizine etc. And also Rhizoma Coptidis has been proved to have extensive pharmacological activities including anti-cancer, anti-microbial activity, hypoglycemic activity, LDL-lowering activity, anti-inflammatory potential and antioxygen and free radicals scavenging etc.. In order to improve its therapeutic value and reduce its side effects, it is necessary to study the relationship between its activity and pharmacokinetics in vitro and in vivo. Some studies have been showed that berberine, an important ingredient in Coptis chinensis Franch displays a linear pharmacokinetic phenomenon and has poor bioavailability. This article summarizes chemical compositions, pharmacological actions and pharmacokinetics of Rhizoma Coptidis. Rhizoma Coptidis; chemical constituents; antimicrobial activity; hypoglycemic Activity; anticancer action; anti-inflammatory; antioxygen; cardiovascular action; free radicals scavenging; pharmacokinetics Article history Received 22 June 2008; Accepted 30 December 2008 Publication data Pages: 15; Tables: 0; Figures: 4; References: 58; Paper ID: 1608-2281-2009-0901011-15 Corresponding author Professor Zhang Tie-Jun, Tianjin Institute of Pharmaceutical Research,308 An-Shan West Road, Tianjin, 300193, China. E-mail: tiezheng4@sina.com. Introduction Herbs have been widely employed as important remedies all over the world [1] . Progress in science and technology in recent decades has been made possibly not only to isolate and to characterize the biologically active constituents of herbs, but also to evaluate their biological activities. Rhizoma Coptidis, the dried root and rhizome of “Huang-lian” named in Chinese, has long been used for the treatment of gastrointestinal disorders, pyretic toxicity, abdominal typhus, bacillary dysentery, Swelling of throat in traditional oriental medicine. Ethnopharmacologically, the property and taste of Rhizoma Coptidis are bitter and 11
Xu HY et al. Asian Journal of Pharmacodynamics and Pharmacokinetics 2009; 9(1):11-25 cold; the meridians are into heart, liver, stomach and large intestine. The functions are to clear heat and dry dampness, and to reduce fire and dispel toxins. It is used to eliminate heat in the heart for insomnia, fidget, delirium due to high fever, inflammation of the month and tongue, and to stop diarrhea for acute enteritis and dysentery. [2] It can be devided into 3 spicies which are Coptis chinensis Franch, (Fig 1, www.newdruginfo.com) Coptis deltoidea C.Y. Cheng et Hsiao and C. teeta Wall. Rhizoma Coptidis (Fig 2, www.zgycsc.com) is thought as high grade which has good effect and little toxin, recorded in TCM Classic Shennong Bencaojing. Recent in the chemical Constituents and pharmacological studies,it indicate that the total alkaloids is thought as main active ingredients and berberine is the highest in the total alkaloids of Rhizoma Coptidis. Rhizoma Coptidis and berberine have been proved to have extensive pharmacological activities, such as antibacterial effect, antiinflammatory effects, antioxygen and free radicals scavenging ect. and new pharmacological activities, such as hypoglycemic and hypolipidemic effects, anticancer and effects on cardiovascular system etc.. In order to improve its therapeutic value and reduce its side effects, it is necessary to study the relationship between its activity and pharmacokinetics in vitro and in vivo. Some studies have been showed that berberine ,an important ingredient in Coptis chinensis Franch displays a linear pharmacokinetic phenomenon and have poor bioavailability. In this review paper, we collected some information about chemical instistuents, pharmacological actions and pharmacokinetics of Rhizoma Coptidis. The introduced information on Rhizoma Coptidis will help us to know pharmacological actions, the mechanism of TCM, secondary exploitation for Rhizoma Coptidis and its be value for studies on TCM Chemical Constituents In Rhizoma Coptidis, major chemical constituents are several alkaloids such as berberine,coptisine, palmaine, jatrorrhizine, worenine, epiberberine (Fig 3) which of all are both protoberberine and quaternary-amine alkaloid. the content of berberine is approximately 5 percent to 8 percent ,which is the most constituent of the total alkaloids. In addition, Rhizoma Coptidis may contain magnoflorine, ferulaic acid (Fig 4) and so on [3] . Fig 1. Coptis chinensis Franch Fig 2. Rhizoma Coptidis Kobayashi [4] et al had reported that inhibitors of topoismerase I and topoismerase II were separated from Rhizoma Coptidis which could duplicate, transcribe and recombine DNA in the cell. Aqueous extract of Rhizoma Coptidis may make cleavable-complex of DNA Topoismerase steadily in mammal. Both epiberberine and groenlandicine are active constitutents of topoismerase I mediating DNA cleavage and berberrubine is a specific inductor of topoismeras I mediating DNA cleavage. Hirano [4] et al had separated lariciresinol and anti-ferulaic acid-duplet hydroxyl-benzene-ethyl ester. 12
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