Comparative oral bioavailability of geniposide following oral administration of geniposide, <i>Gardenia jasminoides</i> Ellis fruits extracts and Gardenia herbal formulation in rats

Cheng, Sharleen; Lin, Lie Chwen; Lin, Chi; Tsai, Tung Hu

doi:10.1111/jphp.12185

Cited by 28 publications

(21 citation statements)

References 19 publications

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“…It is known that some dietary phytochemicals are poorly absorbed and the bioavailability of ingested bioactive food compounds is a complex and challenging process (Rein et al, 2013). Interestingly, some studies showed that the bioavailability of a single bioactive compound is much poorer than it is consumed with the whole plant extract (Cheng, Lin, Lin, & Tsai, 2014;Keung, Lazo, Kunze, & Vallee, 1996;Vissers, Bozonet, Pearson, & Braithwaite, 2011), suggesting that the consumption of whole herbal tea may show a greater bioavailability than that of saponins alone. The potential synergistic effects of saponins and other phytonutrients on gut microbiota would be of interest for further investigation.…”

Section: Discussionmentioning

confidence: 99%

Dietary saponins from four popular herbal tea exert prebiotic-like effects on gut microbiota in C57BL/6 mice

Chen

Tai

Hsiao

2015

Journal of Functional Foods

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Section: Discussionmentioning

confidence: 99%

Dietary saponins from four popular herbal tea exert prebiotic-like effects on gut microbiota in C57BL/6 mice

Chen

Tai

Hsiao

2015

Journal of Functional Foods

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“…Various chromatographic methods have been published for the determination of GE or GP in combination with other compounds in the biological matrix using HPLC‐UV or LC–MS/MS (Chen et al, ; Cheng, Lin, Lin, & Tsai, ; He et al, ; Hu et al, ; Huang et al, ; Peng et al, ; Qu et al, , ; Wang et al, ). Some methods have been established for simultaneous quantification of GE and GP.…”

Section: Introductionmentioning

confidence: 99%

A sensitive LC–MS/MS method for simultaneous quantification of geniposide and its active metabolite genipin in rat plasma and its application to a pharmacokinetic study

Shi

Pan

et al. 2017

Biomedical Chromatography

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Genipin (GP), an active metabolite of geniposide (GE), exhibits more potent pharmacological effects than its parent compound. In this paper, a sensitive LC-MS/MS method was developed and fully validated for the simultaneous determination of GE and GP in rat plasma. We found that GP degraded rapidly in rat plasma at room temperature as a result of irreversible binding with the endogenous nucleophiles in plasma. GP was stable when the sample's pH was ≤4.0. The degradation of GP in rat plasma was well prevented by immediate addition of 5% glacial acetic acid to the freshly collected plasma. The detection was performed on a tandem mass spectrometer coupled with electrospray ionization source in negative mode. Quantification was conducted by multiple reaction monitoring of the transitions [M + CH COO] m/z 447.3 → 225.3 for GE and [M - H] m/z 225.2 → 123.1 for GP. The method exhibited high sensitivity (LLOQ 1 ng/mL for GE and 0.2 ng/mL for GP) by selecting the acetate adduct ions as the precursor ions for GE. The robust developed method was successfully applied to a pharmacokinetic study in rats after oral administration of GE.

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“…In order to determine the concentration of GE, Caco-2 cells were incubated with a series of GE concentrations (1,2,5,10,25,50,100,200 µg/mL) at 37 ˚C with different durations (6,12,24,48 h). The survival rate of Caco-2 cells at different concentrations of GE was examined.…”

Section: Cytotoxicity Assaymentioning

confidence: 99%

“…The pharmacokinetics, bioavailability and tissue distribution of GE has been reported, and low oral bioavailability limits its clinical application [6,7] . The study of intestinal absorption of drugs can provide important informations such as absorption mechanism, absorption site and factors affecting absorption, and provide reference for drug development [8,9] .…”

Section: Introductionmentioning

confidence: 99%

Intestinal Absorption of Geniposide and Inhibition of Transporter-P-GP Across the Caco-2 Monolayer

Bu¹,

Wu²,

Sun³

et al. 2020

Preprint

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Background: Geniposide (GE) is the main bioactive component of Gardenia jasminoides Ellis, which has many pharmacological effects, such as anti-inflammatory, anti-oxidation, and anti-angiogenesis. GE has low absolute bioavailability after oral administration, and speculated that GE might have an effect on P-glycoprotein (P-gp) described in our previous study. However, intestinal absorption characteristics involved in the Caco-2 cells of GE are still unknown. Therefore, we aimed to investigate absorption mechanisms of GE and the effects on P-gp. Methods: By establishing the Caco-2 cells model and HPLC method, bidirectional transport of GE in the different conditions and the presence of P-gp inhibitors－verapamil were conducted to observe its absorption mechanisms. Transport assays of digoxin, a P-gp substrate, were also performed in the presence of GE or verapamil. The effects of GE on the function and expression of P-gp were analyzed by flow cytometry and Western blot using rhodamine-123 (rho-123) and the antibody, respectively. Results: Both absorption and secretion of GE were positively correlated with concentration and time at Caco-2 cell monolayer. The Papp of bidirectional transport was decreased in low temperature and the Papp(BL-AP) of GE decreased significantly in the presence of verapamil. Meanwhile, the ER value was higher than 1.5. In addition, in the bidirectional transport of digoxin, the values of Papp(BL-AP) and ER decreased significantly in the presence of GE, just like verapamil. GE increased the intracellular accumulation of rho-123 and also have a significant decrease on P-gp expression. Conclusion: Transepithelial transport mechanism of GE in Caco-2 cell monolayer is mainly passive diffusion and P-gp mediated active transportation. GE was a potential inhibitor of P-gp, can inhibit transport of digoxin and the function and expression of P-gp.

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Comparative oral bioavailability of geniposide following oral administration of geniposide, Gardenia jasminoides Ellis fruits extracts and Gardenia herbal formulation in rats

Abstract: The conclusion reveals that herbal ingredient-ingredient or herb-herb interaction may affect the oral absorption of geniposide-related herbal formulation.

Cited by 28 publications

References 19 publications

Dietary saponins from four popular herbal tea exert prebiotic-like effects on gut microbiota in C57BL/6 mice

Dietary saponins from four popular herbal tea exert prebiotic-like effects on gut microbiota in C57BL/6 mice

A sensitive LC–MS/MS method for simultaneous quantification of geniposide and its active metabolite genipin in rat plasma and its application to a pharmacokinetic study

Intestinal Absorption of Geniposide and Inhibition of Transporter-P-GP Across the Caco-2 Monolayer

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