Cellular Absorption of Anthraquinones Emodin and Chrysophanol in Human Intestinal Caco-2 Cells

Teng, Zhaogang; Zhou, Siyuan; Ran, Yu-Hua; Liu, Xinyou; Yang, Run-tao; Yang, Xi; Yuan, Chengjun; Mei, Qibing

doi:10.1271/bbb.70025

Cited by 37 publications

(22 citation statements)

References 23 publications

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“…This data suggests that aloin is a substrate of both SGLT1 and GLUT2 located in intestinal membrane. Teng et al. (2007) recently reported a similar result that phloridzin inhibited cellular accumulation of anthraquinon across the apical membrane of caco‐2 cell.…”

Section: Resultssupporting

confidence: 52%

“…2005). Teng et al. (2007) reported that the presence of an inhibitor of P‐glycoprotein, verapamil, increased the intestinal absorption of phenolic glycosides in aloe.…”

Section: Resultsmentioning

confidence: 99%

“…Contrary to numerous studies on medicinal properties of phenolic compounds in aloe, there is limited information regarding the bioavailability and intestinal transport mechanism of these compounds. It was reported that the intestinal cellular absorption of phenolic compounds were inhibited by some transport proteins existed in epithelial membrane (Teng et al. 2007).…”

Section: Introductionmentioning

confidence: 99%

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ASSESSING ABSORBABILITY OF BIOACTIVE COMPONENTS IN ALOE USINGIN VITRODIGESTION MODEL WITH HUMAN INTESTINAL CELL

Shim¹,

Kwon

2010

Journal of Food Biochemistry

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This study used a simulated in vitro digestion model coupled with caco‐2 cell to assess the digestive stability and absorption of aloin, aloe‐emodin and aloenin A. Aloenin A and aloe‐emodin were stable and entirely recovered during simulated digestion, but 50% of aloin was lost. Approximately 53.2, 7.3 and 28.7% of aloe‐emodin, aloenin A and aloin, respectively, was transported into both apical and basolateral compartments after 1 h incubation in caco‐2 cell. The involvement of several transporter proteins for aloin and aloenin A was examined. An inhibitor of SGLT1 on apical surface (phloridzin) or that of GLUT2 on basolateral membrane (cytochalasin B) reduced the absorption of aloin by 40 or 60%, respectively, indicating that aloin is likely to be a partial substrate of SGLT1. In the presence of an efflux transporter inhibitor (verapamil), the transport of aloenin A through an intentinal apical membrane increased up to 2.1 times compared with the control (without verapamil). PRACTICAL APPLICATIONS Our results on both digestive stability and intestinal absorption characteristics of bioactive components in aloe could be of helpful information for promoting its bioavailability. The in vitro technique described in this study provides a rapid and cost‐effective alternative for predicting bioavailability of biomarkers in aloe functional food.

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Section: Resultssupporting

confidence: 52%

“…2005). Teng et al. (2007) reported that the presence of an inhibitor of P‐glycoprotein, verapamil, increased the intestinal absorption of phenolic glycosides in aloe.…”

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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ASSESSING ABSORBABILITY OF BIOACTIVE COMPONENTS IN ALOE USINGIN VITRODIGESTION MODEL WITH HUMAN INTESTINAL CELL

Shim¹,

Kwon

2010

Journal of Food Biochemistry

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“…The lower % absorption of aloin compared to aloe-emodin may be explained by a limited number of receptors/transporters capable of handling the molecule. In a recent study, Teng et al (2007) reported that the SGLT1 blocker can inhibit the cellular accumulation of emodin across the apical membrane of Caco-2 cells. This suggests that partial intestinal absorption of emodin may be transported by SGLT1.…”

Section: Discussionmentioning

confidence: 99%

Intestinal absorption of aloin, aloe-emodin, and aloesin; A comparative study using two in vitro absorption models

2009

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Aloe products are one of the top selling health-functional foods in Korea, however the adequate level of intake to achieve desirable effects are not well understood. The objective of this study was to determine the intestinal uptake and metabolism of physiologically active aloe components using in vitro intestinal absorption model. The Caco-2 cell monolayer and the everted gut sac were incubated with 5-50 µM of aloin, aloe-emodin, and aloesin. The basolateral appearance of test compounds and their glucuronosyl or sulfated forms were quantified using HPLC. The % absorption of aloin, aloe-emodin, and aloesin was ranged from 5.51% to 6.60%, 6.60% to 11.32%, and 7.61% to 13.64%, respectively. Up to 18.15%, 18.18%, and 38.86% of aloin, aloe-emodin, and aloesin, respectively, was absorbed as glucuronidated or sulfated form. These results suggest that a significant amount is transformed during absorption. The absorption rate of test compounds except aloesin was similar in two models; more aloesin was absorbed in the everted gut sac than in the Caco-2 monolayer. These results provide information to establish adequate intake level of aloe supplements to maintain effective plasma level.

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“…Caco-2 monolayers [185,186] Chrysophanol Plant anthraquinone Caco-2 monolayers [187] Cryptotanshinone S. miltiorrhiza Caco-2 monolayers, MDR1 overexpressing cell line [188] Emodin Rhubarb Caco-2 monolayers [187] Ginsenoside Rh2 Ginseng Caco-2 monolayers [189] Glabridin Glycyrrhiza glabra (licorice) Caco-2 monolayers, MDR1 overexpressing cell line [190] Isorhamnetin Plant flavonoid Caco-2 monolayers [191] Kaempferol Plant flavonoid Caco-2 monolayers [191] Protopanaxadiol Ginseng Caco-2 monolayers [189] Quercetin Plant flavonoid (e.g. ginkgo & St John's wort)…”

Section: Intestinal Absorption Of Herbal Medici-nesmentioning

confidence: 99%

Disposition Pathways and Pharmacokinetics of Herbal Medicines in Humans

He¹,

Li²,

Liu³

et al. 2012

CMC

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Pharmacokinetic studies have become an integral part of modern drug development, but these studies are not regulatory needs for herbal remedies. This paper updates our current knowledge on the disposition pathways and pharmacokinetic properties of commonly used herbal medicines in humans. To retrieve relevant data, the authors have searched through computer-based literatures by full text search in Medline (via Pubmed), ScienceDirect, Current Contents Connect (ISI), Cochrance Library, CINAHL (EBSCO), CrossRef Search and Embase (all from inception to May 2010). Many herbal compounds undergo Phase I and/or Phase II metabolism in vivo, with cytochrome P450s (CYPs) and uridine diphosphate glucuronosyltransferases (UGTs) playing a major role. Some herbal ingredients are substrates of P-glycoprotein (P-gp) which is highly expressed in the intestine, liver, brain and kidney. As such, the activities of these drug metabolizing enzymes and drug transporters are determining factors for the in vivo bioavailability, disposition and distribution of herbal remedies. There are increasing pharmacokinetic studies of herbal remedies, but these studies are mainly focused on a small number of herbal remedies including St John's wort, milk thistle, sculcap, curcumin, echinacea, ginseng, ginkgo, and ginger. The pharmacokinetic data of a small number of purified herbal ingredients, including anthocyanins, berberine, catechins, curcumin, lutein and quercetin, are available. For the majority of herbal remedies used in folk medicines, data on their disposition and biological fate in humans are lacking or in paucity. For a herbal medicine, the pharmacological effect is achieved when the bioactive agents or the metabolites reach and sustain proper levels at their sites of action. Both the dose levels and fates of active components in the body govern their target-site concentrations after administration of an herbal remedy. In this regard, a safe and optimal use of herbal medicines requires a full understanding of their pharmacokinetic profiles. To optimize the use of herbal remedies, further clinical studies to explore their biological fate including the disposition pathways and kinetics in the human body are certainly needed.

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Cellular Absorption of Anthraquinones Emodin and Chrysophanol in Human Intestinal Caco-2 Cells

Cited by 37 publications

References 23 publications

ASSESSING ABSORBABILITY OF BIOACTIVE COMPONENTS IN ALOE USINGIN VITRODIGESTION MODEL WITH HUMAN INTESTINAL CELL

ASSESSING ABSORBABILITY OF BIOACTIVE COMPONENTS IN ALOE USINGIN VITRODIGESTION MODEL WITH HUMAN INTESTINAL CELL

Intestinal absorption of aloin, aloe-emodin, and aloesin; A comparative study using two in vitro absorption models

Disposition Pathways and Pharmacokinetics of Herbal Medicines in Humans

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