Transport of active flavonoids, based on cytotoxicity and lipophilicity: An evaluation using the blood–brain barrier cell and Caco-2 cell models

Yang, Yuya; Bai, Lu; Li, Xiaorong; Xiong, Jie; Xu, Pinxiang; Guo, Chenyang; Xue, Ming

doi:10.1016/j.tiv.2013.12.002

Cited by 108 publications

(73 citation statements)

References 31 publications

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“…As shown in Figure , rutin, pure and from BF, was susceptible to being transported outside of the cells, but when HEE was tested, the efflux of the marker was practically reversed. According to our results and previous reports, P‐gp will be involved in this efflux. Hence, the lower ER of rutin from HEE could be a consequence of the saturation of this transporter, that would be favoured by the more complex mixture of compounds present in crude extracts (comparatively to fractions) and by the higher starting concentration of HEE used in the experiments (equivalent to 10 μ m for HEE vs 5 μ m for BF).…”

Section: Discussionsupporting

confidence: 90%

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces from Physalis peruviana L. on the biopharmaceutics classification of rutin

Moré

Feltrin

Brambila

et al. 2020

Journal of Pharmacy and Pharmacology

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Objectives The Biopharmaceutics Classification System (BCS) categorizes active pharmaceutical ingredients according to their solubility and permeability properties, which are susceptible to matrix or formulation effects. The aim of this research was to evaluate the matrix effects of a hydroethanolic extract of calyces from Physalis peruviana L. (HEE) and its butanol fraction (BF), on the biopharmaceutics classification of their major compound, quercetin‐3‐O‐rutinoside (rutin, RU). Methods Rutin was quantified by HPLC‐UV, and Caco‐2 cell monolayer transport studies were performed to obtain the apparent permeability values (Papp). Aqueous solubility was determined at pH 6.8 and 7.4. Key findings The Papp values followed this order: BF > HEE > RU (1.77 ± 0.02 > 1.53 ± 0.07 > 0.90 ± 0.03 × 10−5 cm/s). The lowest solubility values followed this order: HEE > RU > BF (2.988 ± 0.07 > 0.205 ± 0.002 > 0.189 ± 0.005 mg/ml). Conclusions According to these results, rutin could be classified as BCS classes III (high solubility/low permeability) and IV (low solubility/low permeability), depending on the plant matrix. Further work needs to be done in order to establish how apply the BCS for research and development of new botanical drugs or for bioequivalence purposes.

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Section: Discussionsupporting

confidence: 90%

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces from Physalis peruviana L. on the biopharmaceutics classification of rutin

Moré

Feltrin

Brambila

et al. 2020

Journal of Pharmacy and Pharmacology

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“…23 This barrier has a high transendothelial resistance that prohibits the diffusion and transport of some therapeutic agents from the blood to the brain. However, the tight junctions in the BBB have gaps of within 4-6 nm.…”

Section: Bbb-penetration Ability Of the N-cdsmentioning

confidence: 99%

Hydrothermal synthesis of nitrogen-doped carbon dots with real-time live-cell imaging and blood–brain barrier penetration capabilities

Guo

et al. 2016

IJN

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116

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“…P app values of CAPE and CAPE-NO 2 exceeded 10 À6 cm/s, implying a relatively high intestinal permeability in vivo (Yee 1997). It has been reported that the P app values of taxifolin, caffeic acid, ferulic acid and isoliquirtigenin were less than 10 À6 , (1.4 ± 0.1) Â 10 À6 , (10 ± 0.2) Â 10 À6 and (11.77 ± 3.14) Â 10 À6 , respectively, and the lipophilicity and the membrane permeability coefficient of these compounds increased with the numbers of hydroxyl groups decreasing (Wang et al 2009a;Farrell et al 2012;Yang et al 2014). CAPE and CAPE-NO 2 are structurally similar with these above polyphenoliclike substances, and the P app value of CAPE-NO 2 (12.34 ± 1.6 Â 10 À6 ) was 2-to 4-fold higher than CAPE Figure 5.…”

Section: Discussionmentioning

confidence: 97%

Absorption properties and effects of caffeic acid phenethyl ester and its p-nitro-derivative on P-glycoprotein in Caco-2 cells and rats

Gou

Xiao

Tang

et al. 2016

Pharmaceutical Biology

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Context: Caffeic acid phenethyl ester (CAPE), isolated from honeybee propolis, has pharmacological applications. A synthesized CAPE derivative, p-nitro-caffeic acid phenethyl ester (CAPE-NO 2 ), showed similar activities with CAPE. The pharmacological activities of CAPE and CAPE-NO 2 are related to their absorption properties. Objective: To understand the pharmacokinetic profiles of CAPE and CAPE-NO 2 in rats and investigate the absorption mechanisms and effects on P-glycoprotein in Caco-2 cells. Materials and methods: The pharmacokinetic profiles of CAPE and CAPE-NO 2 were obtained after oral administration (10 mg/kg) to rats. Transport studies of CAPE and CAPE-NO 2 (5, 10, 20 lM) were performed in Caco-2 cell model. P-gp activities were assayed by rhodamine 123 cellular retention. Expression of P-gp was determined after the cells were administrated with CAPE and CAPE-NO 2 (5, 20 lM) for 48 and 72 h. Results: The AUC (0Àt) of CAPE-NO 2 (3239.9 ± 352 ng Â h/mL) was two-time greater than CAPE (1659.6 ± 152 ng Â h/mL) in rats. The P app values of CAPE and CAPE-NO 2 were (4.86 ± 0.90) Â 10 À6

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Transport of active flavonoids, based on cytotoxicity and lipophilicity: An evaluation using the blood–brain barrier cell and Caco-2 cell models

Cited by 108 publications

References 31 publications

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces from Physalis peruviana L. on the biopharmaceutics classification of rutin

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces from Physalis peruviana L. on the biopharmaceutics classification of rutin

Hydrothermal synthesis of nitrogen-doped carbon dots with real-time live-cell imaging and blood–brain barrier penetration capabilities

Absorption properties and effects of caffeic acid phenethyl ester and its p-nitro-derivative on P-glycoprotein in Caco-2 cells and rats

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Transport of active flavonoids, based on cytotoxicity and lipophilicity: An evaluation using the blood–brain barrier cell and Caco-2 cell models

Cited by 108 publications

References 31 publications

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces from Physalis peruviana L. on the biopharmaceutics classification of rutin

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces from Physalis peruviana L. on the biopharmaceutics classification of rutin

Hydrothermal synthesis of nitrogen-doped carbon dots with real-time live-cell imaging and blood&ndash;brain barrier penetration capabilities

Absorption properties and effects of caffeic acid phenethyl ester and its p-nitro-derivative on P-glycoprotein in Caco-2 cells and rats

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Product

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Hydrothermal synthesis of nitrogen-doped carbon dots with real-time live-cell imaging and blood–brain barrier penetration capabilities