Influences of Fructus evodiae pretreatment on the pharmacokinetics of Rhizoma coptidis alkaloids

Ma, Bing-Liang; Yao, Meng-Kan; Han, Xin; Ma, Yueming; Wu, Jiasheng; Wang, Changhong

doi:10.1016/j.jep.2011.08.002

Cited by 11 publications

(6 citation statements)

References 26 publications

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“…The QPAs like coptisine, palmatine and berberine were P -gp substrates [ 63 , 67 ], and their efflux ratio could be reduced by EF on the Caco-2 transport model [ 68 ], so EF may possibly promote the absorption of QPAs by inhibiting P -gp. On the other hand, EF could also induce hepatic UDP-glucuronosyltransferase 1A1 and then accelerate the elimination of QPAs [ 69 ]. In the present study, QPAs’ systemic exposure (AUC 0→∞ /D) were finally increased when the proportion of EF increased, suggesting that EF had a greater influence on the absorption than on the elimination of QPAs after the compatibility of CR and EF.…”

Section: Resultsmentioning

confidence: 99%

Pharmacokinetics Studies of 12 Alkaloids in Rat Plasma after Oral Administration of Zuojin and Fan-Zuojin Formulas

Qian

Zhang²,

Yang³

et al. 2017

Molecules

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Zuojin formula (ZJ) is a traditional Chinese medicine (TCM) prescription consisted of Coptidis Rhizoma (CR) and Euodiae Fructus (EF), and has been used to treat gastrointestinal (GI) disease for more than 700 years. Fan-Zuojin formula (FZJ) is a related TCM prescription also consisted of CR and EF with the opposite proportion. In recent years, ZJ was getting more attention for its antitumor potential, but the indeterminate pharmacokinetic (PK) behavior restricted its clinical applications, and the PK differences between ZJ and FZJ were also largely unknown. Consequently it is necessary to carry out a full-scale PK study to demonstrate the physiological disposition of ZJ, as well as the comparative PK study between ZJ and FZJ to illustrate the compatibility dose effects. Therefore a liquid chromatographic–tandem mass spectrometry (LC–MS/MS) method was established and validated for the determinations of coptisine, epiberberine, palmatine, berberine, 8-oxocoptisine, 8-oxoepiberberine, noroxyhydrastinine, corydaldine, dehydroevodiamine, evodiamine, wuchuyuamide-I, and evocarpine in rat plasma. PK characteristics of 12 alkaloids after oral administration of ZJ and FZJ were compared, and the result was analyzed and discussed with the help of an in silico study. Then an integrated PK study was carried out with the AUC-based weighting method and the total drug concentration method. The established method has been successfully applied to reveal the PK profiles of the 12 alkaloids in rat plasma after oral administration of ZJ and FZJ. The results showed that: (1) double peaks were observed in the plasma concentration-time (C–T) curves of the alkaloids after ZJ administration; but the C–T curves approximately matched the two-compartment model after FZJ administration; (2) There were wide variations in the absorption levels of these alkaloids; and even for a certain alkaloid, the dose modified systemic exposure levels and elimination rate also varied significantly after administration of ZJ and FZJ extracts. The results could be interpreted as follows: firstly, inhibition effect on GI motility caused by the high content CR alkaloids (especially berberine) in ZJ could delay the Tmax, and increase the absorption and systemic exposure levels of the other alkaloids, and also lead to the double peak phenomenon of these alkaloids. However, for quaternary protoberberine alkaloids (QPA), double peaks were primarily caused by the different Ka value in two intestinal absorption sites; Secondly, absorption was the major obstacle to the systemic exposure level of the alkaloids from CR and EF. In silico and PK studies suggested that the absorption of these alkaloids, except QPAs, mainly depended on their solubility rather than permeability; Thirdly, EF could promote the absorption and accelerate the elimination of QPAs, and had a greater influence on the former than the latter. At last the integrated PK analysis suggested that berberine and dehydroevodiamine could be regarded as the representative components to reflect the PK behaviors o...

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Section: Resultsmentioning

confidence: 99%

Pharmacokinetics Studies of 12 Alkaloids in Rat Plasma after Oral Administration of Zuojin and Fan-Zuojin Formulas

Qian

Zhang²,

Yang³

et al. 2017

Molecules

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“…89,90 Pretreatment of rats with T. rutaecarpa fruit aqueous extract for 2 weeks also resulted in significant reduction in berberine bioavailability from C. chinensis. 91 The mechanism appeared to be through the constituents of T. rutaecarpa inducing hepatic UGT1A1, increasing first pass metabolism of berberine. C. chinensis is commonly combined with T. rutaecarpa as a corrective assistant because C. chinensis is "cold" while T. rutaecarpa is "hot."…”

Section: Coptis Chinensis (Goldthread)mentioning

confidence: 99%

Synergy in Herbal Medicines: Part 1

Yarnell¹

2015

j restorat med

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In the following paper, we will review the available literature on synergy and additive effects involving medicinal herbs and herbal extracts. Several types of synergistic interactions are discussed, including apparently inactive constituents enhancing the effects of apparently active constituents within and between herbal medicines, various herbal compounds altering the absorption of others, reduction in toxicity of some herbal constituents by others, and direct synergistic therapeutic effects when active constituents are combined within and between many medicinal herbs. Species discussed include Artemisia annua (sweet Annie, q ng h o), Ammi visnaga (khella), Glycyrrhiza glabra (licorice), G. uralensis (Chinese licorice, g n c o), Panax ginseng (Asian ginseng, rén sh n), Mahonia aquifolium (Oregon grape), Berberis aetnensis (Mt. Etna barberry), B. trifoliolata (algerita), B. fendleri (Colorado barberry), and Coptis chinensis (goldthread, huáng lián). Part 2 of this article will continue this review on other medicinal herb species.

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“…In the in vitro experiments with monolayers of Caco-2 cells under and semi-physiologic conditions, the dissolution of eight components from TR increased with the increasing proportions of Coptidis Rhizoma, whereas the dissolution of main alkaloids from TR increased along with the components of Coptidis Rhizoma decreased (Deng, 2008;. Pretreatment with TR in rats suggests that its mechanism of action involves induction of hepatic expression of uridine 5′diphospho-glucuronosyltransferase (UGT)1A1 (Ma et al, 2011;Yan et al, 2011). Mechanism involved may be the increasing efflux of the main bioactive alkaloids of Coptidis Rhizoma when prescribed with TR.…”

Section: Pharmacokinetic Parametersmentioning

confidence: 99%

“…Therefore, the fruit of TR could induce drug interactions via CYP3A4 in the small intestine, thereby demonstrating a potential for alteration of efficacy before and after processing. Besides, according to studies using rat liver microsomes, hepatic UGT1A1 is believed to induce decreased exposure to the alkaloids of Coptidis Rhizoma, with the activity and expression of UGT1A1 being identified after TR pretreatment for 2 weeks (Ma et al, 2011). This action could explain why the dissolution of Coptidis Rhizoma declined after combination with TR.…”

Section: Metabolismmentioning

confidence: 99%

Processing and Polyherbal Formulation of Tetradium ruticarpum (A. Juss.) Hartley: Phytochemistry, Pharmacokinetics, and Toxicity

et al. 2020

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Herbal medicine is a major part of traditional Chinese medicine (TCM), which is evolved as a system of medical practice from ancient China. The use of herbal medicine is mainly based on practice and theories and concepts rooted in ancient philosophy. In the era of evidence-based medicine, it is essential to accurately evaluate herbal remedy with standard/modern medical practice approaches. Tetradium ruticarpum (A. Juss.) Hartley (TR), a medicinal plant with diversify bioactive components, has been broadly used to treat pain and gastrointestinal disorders in TCM. However, TR has also been reported to have potential toxicity by long-term use or excessive doses, though the associated compounds are yet to be identified. TR is usually processed, and/or combined with other herbs in TCM formulas in order to achieve a synergistic effect or reduce its toxicity. Since processing or polyherbal formulation of TR may lead to changes in its chemical composition and contents, quality, efficacy and toxicity, comparison of TR samples before and after processing, as well as its combination with other medicines, would provide useful knowledge of bioactive compounds, efficacy and toxicity of this valuable medicinal plant. Here we reviewed the recent studies about the phytochemistry, pharmacokinetic behaviors and toxicity of TR under various processing or polyherbal formulation conditions, which would expand our understanding of mechanisms of TR's efficacy and toxicity and be valuable for quality control in industrial manufacturing, future medicinal research, and safety and rational use of TR in TCM.

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Influences of Fructus evodiae pretreatment on the pharmacokinetics of Rhizoma coptidis alkaloids

Cited by 11 publications

References 26 publications

Pharmacokinetics Studies of 12 Alkaloids in Rat Plasma after Oral Administration of Zuojin and Fan-Zuojin Formulas

Pharmacokinetics Studies of 12 Alkaloids in Rat Plasma after Oral Administration of Zuojin and Fan-Zuojin Formulas

Synergy in Herbal Medicines: Part 1

Processing and Polyherbal Formulation of Tetradium ruticarpum (A. Juss.) Hartley: Phytochemistry, Pharmacokinetics, and Toxicity

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