Possible inhibitory mechanism of Curcuma drugs on CYP3A4 in 1α,25 dihydroxyvitamin D3 treated Caco-2 cells

Hou, Xiao-Long; Takahashi, Kyoko; Kinoshita, Natsumi; Qiu, Feng; Tanaka, Ken; Komatsu, Kenshi; Azuma, Jun-ichi

doi:10.1016/j.ijpharm.2006.12.035

Cited by 39 publications

(33 citation statements)

References 35 publications

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“…3,11,37 The poor bioavailability of curcumin also drew many scientists' attention, and enhancing bioavailability has been the objective of several studies. 31,34,38 In the present study, the transport of curcumin was investigated using the in vitro Caco-2 cell monolayer model. A simple hypothesis was verified in this wellestablished and widely used model.…”

Section: Discussionmentioning

confidence: 99%

The Role of Turmerones on Curcumin Transportation and P-Glycoprotein Activities in Intestinal Caco-2 Cells

Yue

Cheng

et al. 2012

Journal of Medicinal Food

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The rhizome of Curcuma longa (turmeric) is often used in Asia as a spice and as a medicine. Its most well-studied component, curcumin, has been shown to exhibit poor bioavailability in animal studies and clinical trials. We hypothesized that the presence of lipophilic components (e.g., turmerones) in turmeric extract would affect the absorption of curcumin. The effects of turmerones on curcumin transport were evaluated in human intestinal epithelial Caco-2 cells. The roles of turmerones on P-glycoprotein (P-gp) activities and mRNA expression were also evaluated. Results showed that in the presence of α- and aromatic turmerones, the amount of curcumin transported into the Caco-2 cells in 2 hours was significantly increased. α-Turmerone and verapamil (a P-gp inhibitor) significantly inhibited the efflux of rhodamine-123 and digoxin (i.e., inhibited the activity of P-gp). It is interesting that aromatic turmerone significantly increased the rhodamine-123 efflux and P-gp (MDR1 gene) mRNA expression levels. The effects of α- and aromatic turmerones on curcumin transport as well as P-gp activities were shown here for the first time. The presence of turmerones did affect the absorption of curcumin in vitro. These findings suggest the potential use of turmeric extract (including curcumin and turmerones), rather than curcumin alone, for treating diseases.

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Section: Discussionmentioning

confidence: 99%

The Role of Turmerones on Curcumin Transportation and P-Glycoprotein Activities in Intestinal Caco-2 Cells

Yue

Cheng

et al. 2012

Journal of Medicinal Food

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“…These modified cells have become an accepted tool to detect inhibition/induction of intestinal CYP3A4. In a previous report, we used the model to examine the effects of Curcumas on intestinal CYP3A4 activity (Hou et al, 2007).…”

Section: Discussionmentioning

confidence: 99%

“…In the study, testosterone and nifedipine were used to assay CYP3A4 catalytic activity (Hou et al, 2007). As the positive control, ketoconazole (KTZ, 1 M) significantly inhibited the 6␤-hydroxylation of testosterone and the oxidation of nifedipine by almost 100% and 60%, respectively.…”

Section: Inhibitory Effects Of Andrographolide On Cyp3a4 Catalytic Acmentioning

confidence: 99%

Andrographolide inhibits the expression and metabolic activity of cytochrome P450 3A4 in the modified Caco-2 cells

Qiu

Hou

Takahashi

et al. 2012

Journal of Ethnopharmacology

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“…Curcumin is the most studied of the curcuminoids and shows a broad range of biological activities, including anti-inflammatory, anti-carcinogenic, and anti-oxidant activities [5]. In contrast, no curcumin content was detected in Japanese C. zedoaria [6], which contains various sesquiterpenes. However, various sesquiterpenes and curcuminoids have been identified from the rhizomes of C. aromatica.…”

Section: Introductionmentioning

confidence: 99%

Compounds isolated from Curcuma aromatica Salisb. inhibit human P450 enzymes

et al. 2011

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Curcuma species (Zingiberaceae) are used as both food and medicine in Asia. Ten sesquiterpenes (1-10) and two curcuminoids (11 and 12) were isolated from the rhizomes of Curcuma aromatica Salisb. and identified. The compounds were evaluated for their ability to inhibit cytochrome P450 (CYP). Among them, the sesquiterpene (4S,5S)-(+)-germacrone-4,5-epoxide (7) inhibited certain subtypes of CYP more potently than or at levels comparable to the curcuminoids curcumin (11) and demethoxycurcumin (12); 7 (IC(50) = 1.0 ± 0.2 μM) > 12 (IC(50) = 7.0 ± 1.7 μM) > 11 (IC(50) = 14.9 ± 1.4 μM) for CYP3A4 inhibition; 12 (IC(50) = 1.4 ± 0.2 μM) > 11 (IC(50) = 6.0 ± 1.4 μM) > 7 (IC(50) = 7.6 ± 2.5 μM) for CYP2C9 inhibition; and 7 (IC(50) = 33.2 ± 3.6 μM) = 12 (IC(50) = 34.0 ± 14.2 μM) > 11 (IC(50) > 100 μM) for CYP1A2 inhibition. These results suggest the possibility that Curcuma aromatica Salisb. may cause food-drug interactions via cytochrome P450 inhibition by sesquiterpene 7 and curcuminoids 11 and 12.

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Possible inhibitory mechanism of Curcuma drugs on CYP3A4 in 1α,25 dihydroxyvitamin D3 treated Caco-2 cells

Cited by 39 publications

References 35 publications

The Role of Turmerones on Curcumin Transportation and P-Glycoprotein Activities in Intestinal Caco-2 Cells

The Role of Turmerones on Curcumin Transportation and P-Glycoprotein Activities in Intestinal Caco-2 Cells

Andrographolide inhibits the expression and metabolic activity of cytochrome P450 3A4 in the modified Caco-2 cells

Compounds isolated from Curcuma aromatica Salisb. inhibit human P450 enzymes

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