Effects of Capsaicin on Cellular Damage and Monolayer Permeability in Human Intestinal Caco-2 Cells

Tsukura, Yuri; Mori, Masao; Hirotani, Yoshihiko; Ikeda, Kenji; Amano, Fumio; Kato, Ryuichi; Ijiri, Yoshio; Tanaka, Kazuhiko

doi:10.1248/bpb.30.1982

Cited by 34 publications

(27 citation statements)

References 24 publications

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“…lial Caco-2 cells grown on permeable inserts have been shown to possess many of the morphological and functional characteristics of intestinal enterocytes and to enable intestinal permeability to be evaluated [17]. Furthermore, they have already been used as an in vitro model in studies of the absorption of natural bioactive compounds [13,[17][18][19][20]. They have also been assayed in a doublelayered system that reproduces absorption in the intestine.…”

Section: Development Of a Coculture System To Evaluate The Bioactivitmentioning

confidence: 99%

Development of a Coculture System to Evaluate the Bioactivity of Plant Extracts on Pancreaticβ-Cells

Castell-Auví¹,

Cedó²,

Pallarès³

et al. 2010

Planta Med

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Natural plant extracts are candidates for the development of new functional foods. Most of them are usually complex mixtures of molecules of uncertain bioavailability that are often partially metabolized before they finally reach the target cells IN VIVO. IN VITRO studies of the bioactivity of these extracts suggest that their direct application to some cell cultures might be a long way from becoming a reality. To overcome this limitation, we seeded Caco-2 cells onto culture inserts and after 21 days, cocultured these with INS-1E on the base of the well. After 24 hours of coculture, TEER (transepithelium electrical resistance) measurements indicated no changes in the permeability of the Caco-2 barrier. We also found no changes in either the ability of Caco-2 cells to metabolize the flavan-3-ol component of a grape-seed procyanidin-rich extract, or in the flavanols' ability to pass through the barrier. However, the expression of the Caco-2 SGLT-1 gene increased due to the coculture. GSIS (glucose stimulated insulin secretion) was maintained in the INS-1E cells with higher levels of insulin secretion despite the fact that the insulin gene expression was unmodified by the cocultivation. Furthermore, we found that in some of the assays requiring several medium changes there was a tendency to lose β-cells. Neutral red assay showed that seeded cells should only be cocultured for a short time to obtain a higher consistency. In conclusion, four hours coculture with Caco-2 cells and INS-1E is a suitable method for checking the bioactivity of natural plant extracts of unknown bioavailability on β-cells.

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Section: Development Of a Coculture System To Evaluate The Bioactivitmentioning

confidence: 99%

Development of a Coculture System to Evaluate the Bioactivity of Plant Extracts on Pancreaticβ-Cells

Castell-Auví¹,

Cedó²,

Pallarès³

et al. 2010

Planta Med

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“…Another group of compounds that have been shown to induce epithelial resistance in the Caco‐2 model system are polyunsaturated fatty acids (PUFAs), which were able to alleviate interleukin‐4 induced epithelial leakage 10. In contrast, capsaicin has shown to reduce TEER,11, 12 although a reduction in TEER is more difficult to interpret since the reduction might also be caused by cell damage due to toxicity 12…”

Section: Introductionmentioning

confidence: 99%

Apple extract induces increased epithelial resistance and claudin 4 expression in Caco‐2 cells

et al. 2011

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BACKGROUND: The small intestinal epithelium functions both to absorb nutrients, and to provide a barrier between the outside, luminal, world and the human body. One of the passageways across the intestinal epithelium is paracellular diffusion, which is controlled by the properties of tight junction complexes. We used a differentiated Caco-2 monolayer as a model for small intestinal epithelium to study the effect of crude apple extracts on paracellular permeability.

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“…CAP was shown to be an inhibitor of CYP3A in in vitro studies . Moreover, there are several reports indicating that CAP exhibited inhibitory effects on P‐gp .…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetic effects of capsaicin on vinblastine in rats mediated by CYP3A and Mrp2

Zhai

Feng

Liu

et al. 2019

Fundamemntal Clinical Pharma

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Capsaicin (trans‐8‐methyl‐N‐vanillyl‐6‐nonenamide, CAP) is an important ingredient in spicy foods consumed throughout the world. Vinblastine (VBL) is a naturally occurring alkaloid prescribed to cancer patients. Many cancer patients treated with VBL were taking CAP at the same time. This study attempted to investigate the effect of CAP on the pharmacokinetics of VBL, which is the substrate of CYP3A, P‐gp, and Mrp2. CAP, cyclosporine (CsA) or olive oil was given to rats for seven consecutive days, and on the seventh day, VBL (1.3 mg/kg) was administered intravenously. CsA was used as a CYP3A1/2 and transporter inhibitor, and olive oil was used as a vehicle. The results showed that pretreatment of rats with CAP (3.0 mg/kg) for seven consecutive days resulted in an increase in the AUC0–t of VBL of about 29.8% (P < 0.05) compared with the control group. Moreover, CAP decreased the CL of VBL to 75.5% (P < 0.05). At this time, CYP3A1/2 and Mrp2/Abcc2 in the liver was decreased at the mRNA and protein levels. These results demonstrate that chronic ingestion of CAP will increase systemic exposure and reduce clearance of VBL in rats. The food–drug interaction between CAP and VBL appears to be due to modulation of CYP3A1/2 and Mpr2 expression by CAP.

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Effects of Capsaicin on Cellular Damage and Monolayer Permeability in Human Intestinal Caco-2 Cells

Cited by 34 publications

References 24 publications

Development of a Coculture System to Evaluate the Bioactivity of Plant Extracts on Pancreaticβ-Cells

Development of a Coculture System to Evaluate the Bioactivity of Plant Extracts on Pancreaticβ-Cells

Apple extract induces increased epithelial resistance and claudin 4 expression in Caco‐2 cells

Pharmacokinetic effects of capsaicin on vinblastine in rats mediated by CYP3A and Mrp2

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