Resveratrol in Human Hepatoma HepG2 Cells: Metabolism and Inducibility of Detoxifying Enzymes

Lançon, Allan; Hanet, Nathalie; Jannin, Brigitte; Delmas, Dominique; Heydel, Jean‐Marie; Lizard, Gérard; Chagnon, Marie‐Christine; Artur, Yves; Latruffe, Norbert

doi:10.1124/dmd.106.013664

Cited by 108 publications

(86 citation statements)

References 22 publications

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“…The highest concentration of the extract used in the study was at the limit of extract solubility in the final culture medium. Ethanol was used as a solubilizing enhancer and the final concentration of ethanol never exceeded 0.1% v/v (Lançon et al 2007). After incubation for 24, 48 or 72 h, 200 lL of serum free medium and 50 lL of XTT solution were added.…”

Section: Cell Viability Testmentioning

confidence: 99%

Ethanol extract ofTerminalia chebulafruit protects against UVB-induced skin damage

Yakaew

Itsarasook

Ngoenkam

et al. 2016

Pharmaceutical Biology

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Context: The fruit of Terminalia chebula Retz. (Combretaceae) has been used for several therapeutic purposes in Thai folk medicines. Currently, the ethanol extracts containing antioxidant compounds have shown the ability to promote collagen synthesis.Objective: This purpose of this work was to study the effects of the ethanol extract from T. chebula fruit on the inhibition of cutaneous photodamage. Materials and methods: The viability of human skin fibroblasts after incubation with T. chebula at concentration 0.5-50 lg/mL for 24, 48 and 72 h was assessed by using sodium 3 0 -[(phenyl-amino)-carbonyl]-3,4,tetrazolium-bis(4-methoxy-6-notro)benzene-sulphonic acid hydrate (XTT). The levels of type I procollagen and matrix metalloproteinases (MMP)-1 and MMP-13 produced by UVB-irradiated fibroblasts were determined by ELISA. Skin thickness and collagen content caused by long-term UVB irradiation in male ICR mice were determined from haematoxylin and eosin stained tissue sections and spectrophotometric measurement of hydroxyproline. Results: The extract (0.5-50 lg/mL) had no effect on cell viability or morphology of the human fibroblasts. In vitro studies showed that the T. chebula extract reduced the UVB-induced MMP-1 and MMP-13 expression, whereas an increased production of type I procollagen was observed. In a UVB-irradiated animal model, male ICR mice with hair shaved were chronically exposed to UVB which lead to epidermal thickness and loss of hydroxyproline. However, these effects were fully prevented by the topical application of the T.

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Section: Cell Viability Testmentioning

confidence: 99%

Ethanol extract ofTerminalia chebulafruit protects against UVB-induced skin damage

Yakaew

Itsarasook

Ngoenkam

et al. 2016

Pharmaceutical Biology

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“…A combination of resveratrol and another polyphenol, curcumin, had a synergistic effect on UGT1A1 induction, whereas a combination of resveratrol and chrysin, also a polyphenol, had an additive effect on UGT1A1 induction in Caco-2 cells (Iwuchukwu et al, 2011). In HepG2 cells treated with 10 or 30 mM resveratrol, mRNA and protein content of UGT1A1 and UGT2B7 increased after 24 and 48 hours (Lançon et al, 2007). Induction was observed in vivo in rats treated with 0.3, 1, or 3 mg/kg per day of resveratrol for 28 days.…”

Section: Case Study: Milk Thistlementioning

confidence: 99%

Herb–Drug Interactions: Challenges and Opportunities for Improved Predictions

et al. 2013

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Supported by a usage history that predates written records and the perception that "natural" ensures safety, herbal products have increasingly been incorporated into Western health care. Consumers often self-administer these products concomitantly with conventional medications without informing their health care provider(s). Such herb-drug combinations can produce untoward effects when the herbal product perturbs the activity of drug metabolizing enzymes and/or transporters. Despite increasing recognition of these types of herb-drug interactions, a standard system for interaction prediction and evaluation is nonexistent. Consequently, the mechanisms underlying herb-drug interactions remain an understudied area of pharmacotherapy. Evaluation of herbal product interaction liability is challenging due to variability in herbal product composition, uncertainty of the causative constituents, and often scant knowledge of causative constituent pharmacokinetics. These limitations are confounded further by the varying perspectives concerning herbal product regulation. Systematic evaluation of herbal product drug interaction liability, as is routine for new drugs under development, necessitates identifying individual constituents from herbal products and characterizing the interaction potential of such constituents. Integration of this information into in silico models that estimate the pharmacokinetics of individual constituents should facilitate prospective identification of herb-drug interactions. These concepts are highlighted with the exemplar herbal products milk thistle and resveratrol. Implementation of this methodology should help provide definitive information to both consumers and clinicians about the risk of adding herbal products to conventional pharmacotherapeutic regimens.

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“…Indeed, the modifications just mentioned have been long recognized and studied for representative members of this huge family of natural compounds, including resveratrol, which is of specific interest here. Rapid glucuronidation and sulfation in enterocytes, hepatocytes, and other cells (e.g., [14][15][16][17][18][19][20][21]) and re-export to the intestinal lumen by MDR proteins [15,22,23], or possibly OATPs [24], are thought to limit the potential impact of this celebrated "natural drug" in vivo. This is a pity, given the pleiotropic effects this dietary compound is reported to have in important pathophysiological respects (for recent reviews see, e.g., [25][26][27][28][29][30]).…”

Section: Introductionmentioning

confidence: 99%

N-Monosubstituted Methoxy-oligo(ethylene glycol) Carbamate Ester Prodrugs of Resveratrol

et al. 2015

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Abstract:Resveratrol is a natural polyphenol with many interesting biological activities. Its pharmacological exploitation in vivo is, however, hindered by its rapid elimination via phase II conjugative metabolism at the intestinal and, most importantly, hepatic levels. One approach to bypass this problem relies on prodrugs. We report here the synthesis, characterization, hydrolysis, and in vivo pharmacokinetic behavior of resveratrol prodrugs in which the OH groups are engaged in an N-monosubstituted carbamate ester linkage. As promoiety, methoxy-oligo(ethylene glycol) groups (m-OEG) (CH3-[OCH2CH2]n-) of defined chain length (n = 3, 4, 6) were used. These are expected to modulate the chemico-physical properties of the resulting derivatives, much like longer poly(ethylene glycol) (PEG) chains, while retaining a relatively low MW and, thus, a favorable drug loading capacity. Intragastric administration to rats resulted in the appearance in the bloodstream of the prodrug and of the products of its partial hydrolysis, confirming protection from first-pass metabolism during absorption.

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Resveratrol in Human Hepatoma HepG2 Cells: Metabolism and Inducibility of Detoxifying Enzymes

Cited by 108 publications

References 22 publications

Ethanol extract ofTerminalia chebulafruit protects against UVB-induced skin damage

Ethanol extract ofTerminalia chebulafruit protects against UVB-induced skin damage

Herb–Drug Interactions: Challenges and Opportunities for Improved Predictions

N-Monosubstituted Methoxy-oligo(ethylene glycol) Carbamate Ester Prodrugs of Resveratrol

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