Prediction of intestinal absorption and metabolism of pharmacologically active flavones and flavanones

Serra, Helena; Mendes, Tiago Antônio de Oliveira; Bronze, Maria Rosário; Simplı́cio, Ana Luı́sa

doi:10.1016/j.bmc.2008.01.028

Cited by 78 publications

(61 citation statements)

References 43 publications

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“…The least hydrophilic flavonol, galangin, produced the highest level of conjugates, followed by kaempferol and then quercetin, in general consistent with Caco-2 cells alone 27 . The overall yield of the flavonol aglycone and conjugates was 70-80%, indicating good stability in the medium over the incubation period, similar to that found for the flavonoid hesperetin 28 . No myricetin conjugates could be detected, even though we were able to synthesise enzymatically the conjugates and use them as standards in the analysis.…”

Section: Discussionsupporting

confidence: 73%

Effect of edible oils on quercetin, kaempferol and galangin transport and conjugation in the intestinal Caco-2/HT29-MTX co-culture model

Jailani

Williamson

2014

Food Funct.

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Section: Discussionsupporting

confidence: 73%

Effect of edible oils on quercetin, kaempferol and galangin transport and conjugation in the intestinal Caco-2/HT29-MTX co-culture model

Jailani

Williamson

2014

Food Funct.

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“…In Europe, it is prescribed for treatment of venous insufficiency while in the US, it is marketed as a food supplement [60,61]. A study in rat liver perfusate showed that diosmin was mainly excreted in the bile as a glucuronide conjugate [62].…”

Section: Diosminmentioning

confidence: 99%

“…A study in rat liver perfusate showed that diosmin was mainly excreted in the bile as a glucuronide conjugate [62]. Glucuronides of diosmetin (diosmin aglycone) were detected on the apical side of Caco-2 cell culture [61]. Specific UGT enzymes associated with diosmin glucuronidation have not been reported.…”

Section: Diosminmentioning

confidence: 99%

Effects of Herbal Supplements on Drug Glucuronidation. Review of Clinical, Animal, andIn VitroStudies

Mohamed

Frye

2010

Planta Med

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“…Other applications of PAMPA such as the prediction of protein binding, lipophilicity determination, and pH profiling have also been reported [10,12,21,22]. Despite the rapid industrial success of PAMPA in the last decade, papers mentioning the use of this HTS technique for studying the passive permeability potential of NPs are sparse [23][24][25][26][27]. The applicability of a modified version of the PAMPA-BBB technique was recently reported in the frame of a CNS-based HTS campaign in order to screen a library of chemically diverse plant extracts [18].…”

mentioning

confidence: 99%

Prediction of the Passive Intestinal Absorption of Medicinal Plant Extract Constituents with the Parallel Artificial Membrane Permeability Assay (PAMPA)

et al. 2016

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At the early drug discovery stage, the high-throughput parallel artificial membrane permeability assay is one of the most frequently used in vitro models to predict transcellular passive absorption. While thousands of new chemical entities have been screened with the parallel artificial membrane permeability assay, in general, permeation properties of natural products have been scarcely evaluated. In this study, the parallel artificial membrane permeability assay through a hexadecane membrane was used to predict the passive intestinal absorption of a representative set of frequently occurring natural products. Since natural products are usually ingested for medicinal use as components of complex extracts in traditional herbal preparations or as phytopharmaceuticals, the applicability of such an assay to study the constituents directly in medicinal crude plant extracts was further investigated. Three representative crude plant extracts with different natural product compositions were chosen for this study. The first extract was composed of furanocoumarins (Angelica archangelica), the second extract included alkaloids (Waltheria indica), and the third extract contained flavonoid glycosides (Pueraria montana var. lobata). For each medicinal plant, the effective passive permeability values Pe (cm/s) of the main natural products of interest were rapidly calculated thanks to a generic ultrahigh-pressure liquid chromatography-UV detection method and because Pe calculations do not require knowing precisely the concentration of each natural product within the extracts. The original parallel artificial membrane permeability assay through a hexadecane membrane was found to keep its predictive power when applied to constituents directly in crude plant extracts provided that higher quantities of the extract were initially loaded in the assay in order to ensure suitable detection of the individual constituents of the extracts. Such an approach is thus valuable for the high-throughput, cost-effective, and early evaluation of passive intestinal absorption of active principles in medicinal plants. In phytochemical studies, obtaining effective passive permeability values of pharmacologically active natural products is important to predict if natural products showing interesting activities in vitro may have a chance to reach their target in vivo.

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Prediction of intestinal absorption and metabolism of pharmacologically active flavones and flavanones

Cited by 78 publications

References 43 publications

Effect of edible oils on quercetin, kaempferol and galangin transport and conjugation in the intestinal Caco-2/HT29-MTX co-culture model

Effect of edible oils on quercetin, kaempferol and galangin transport and conjugation in the intestinal Caco-2/HT29-MTX co-culture model

Effects of Herbal Supplements on Drug Glucuronidation. Review of Clinical, Animal, andIn VitroStudies

Prediction of the Passive Intestinal Absorption of Medicinal Plant Extract Constituents with the Parallel Artificial Membrane Permeability Assay (PAMPA)

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