Uptake and Transport Mechanism of Dihydromyricetin Across Human Intestinal Caco‐2 Cells

Fan, Lihua; Hou, Xiao-Long; Xiong, Wei; Shi, Chunyu; Wang, Wenqing; Fang, Jianguo

doi:10.1111/1750-3841.14112

Cited by 29 publications

(28 citation statements)

References 30 publications

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“…However, little information is available on DMY's absorption profiles, distribution, metabolism, and excretion in animal models and in human body. In a recent study (Xiang et al, 2018), a human intestinal Caco-2 cell model was used to investigate the uptake and transport mechanism of DMY. The effect of time, concentration, pH, temperature and efflux transporters on its uptake and transport were systematically evaluated.…”

Section: Absorption Metabolism and Elimination Of Dmymentioning

confidence: 99%

“…In addition, the pharmacokinetic characteristics of DMY in animal models and human body are also vital to the evaluation of their in vivo bioavailability efficacy. However, only partial information (Fan, Tong, & Dong, 2017;Xiang, Fan, & Hou, 2018;Zhang et al, 2007) is available on basic pharmacokinetic studies of DMY such as absorption, distribution, metabolism and excretion in organisms, biotransformation processes and metabolites.…”

Section: Introductionmentioning

confidence: 99%

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Dihydromyricetin: A review on identification and quantification methods, biological activities, chemical stability, metabolism and approaches to enhance its bioavailability

Liú

Mao

Ding

et al. 2019

Trends in Food Science & Technology

105

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Background: Dihydromyricetin (DMY) is an important plant flavonoid, which has received great attention due to its health-benefiting activities, including antioxidant, antimicrobial, anti-inflammatory, anticancer, antidiabetic and neuroprotective activities. DMY capsules have been sold in US as a nutraceutical supplement to prevent alcoholic hangovers. The major disadvantage associated with DMY is its chemical instability and poor bioavailability caused by the combined effects of its low solubility and poor membrane permeability. This limits its practical use in the food and pharmaceutical fields. Scope and approach: The present paper gives an overview of the current methods for the identification and quantification of DMY. Furthermore, recent findings regarding the main biological properties and chemical stability of DMY, the metabolism of DMY as well as different approaches to increase DMY bioavailability in both aqueous and lipid phases are discussed. Key findings and conclusions: Current trends on identification and quantification of DMY have been focused on spectral and chromatographic techniques. Many factors such as heat, pH, metal ions, could affect the chemical stability of DMY. Despite the diverse biological effects of DMY, DMY faces with the problem of poor bioavailability. Utilization of different delivery systems including solid dispersion, nanocapsule, microemuslion, cyclodextrin inclusion complexes, co-crystallization, phospholipid complexes, and chemical or enzymatic acylation has the potential to improve both the solubility and bioavailability. DMY digested in laboratory animals undergoes reduction, dehydroxylation, methylation, glucuronidation, and sulfation. Novel DMY delivery systems and basic pharmacokinetic studies of encapsulated DMY on higher animals and humans might be required in the future.

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Section: Absorption Metabolism and Elimination Of Dmymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Dihydromyricetin: A review on identification and quantification methods, biological activities, chemical stability, metabolism and approaches to enhance its bioavailability

Liú

Mao

Ding

et al. 2019

Trends in Food Science & Technology

105

View full text Add to dashboard Cite

show abstract

“…The plasma DHM concentration reached maximum (159 μg/L) at 1.5 h postadministration when DHM powder was given at a dosage of 115 mg/kg body weight in rabbits, indicating a low bioavailability of DHM [18]. Efflux transporters, multidrug resistance protein 2, and breast cancer resistance protein also played an important role in DHM uptake and transport processes [22]. A research group had investigated the distribution, excretion, and metabolic profile of DHM and found that most unconverted DHM forms were excreted in feces [23].…”

Section: Introductionmentioning

confidence: 99%

Dihydromyricetin Acts as a Potential Redox Balance Mediator in Cancer Chemoprevention

Chen

Shi

et al. 2021

Mediators of Inflammation

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Dihydromyricetin (DHM) is a flavonoid extracted from the leaves and stems of the edible plant Ampelopsis grossedentata that has been used for Chinese Traditional Medicine. It has attracted considerable attention from consumers due to its beneficial properties including anticancer, antioxidative, and anti-inflammatory activities. Continuous oxidative stress caused by intracellular redox imbalance can lead to chronic inflammation, which is intimately associated with the initiation, promotion, and progression of cancer. DHM is considered a potential redox regulator for chronic disease prevention, and its biological activities are abundantly evaluated by using diverse cell and animal models. However, clinical investigations are still scanty. This review summarizes the current potential chemopreventive effects of DHM, including its properties such as anticancer, antioxidative, and anti-inflammatory activities, and further discusses the underlying molecular mechanisms of DHM in cancer chemoprevention by targeting redox balance and influencing the gut microbiota.

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“…Furthermore, the time required for it reaches peak plasma concentration is 2.67 h after oral administration at a dose of 20 mg/kg (Liu et al, 2017). A recent in vitro study using the human intestinal Caco-2 cell model, a common tool used to predict, in vivo , the absorption of drugs in humans, showed that the uptake and transport of DHM occurs mainly through a passive diffusion mechanism, which can partially explain the low bioavailability of DHM after oral administration (Xiang et al, 2018).…”

Section: Introductionmentioning

confidence: 99%

Preclinical Research of Dihydromyricetin for Brain Aging and Neurodegenerative Diseases

et al. 2019

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Brain aging and neurodegenerative diseases share the hallmarks of slow and progressive loss of neuronal cells. Flavonoids, a subgroup of polyphenols, are broadly present in food and beverage and numerous studies have suggested that it could be useful for preventing or treating neurodegenerative diseases in humans. Dihydromyricetin (DHM) is one of the main flavonoids of some Asian medicinal plants that are used to treat diverse illness. The effects of DHM have been studied in different in vitro systems of oxidative damage and neuroinflammation, as well as in animal models of several neurodegenerative diseases, such as Alzheimer’s disease, Parkinson’s disease, and Huntington’s disease. Here we analyzed the most important effects of DHM, including its antioxidant, anti-inflammatory, and neuroprotective effects, as well as its ability to restore GABA neurotransmission and improve motor and cognitive behavior. We propose new areas of research that might contribute to a better understanding of the mechanism of action of this flavonoid, which could help develop a new therapy for aging and age-related brain diseases.

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Uptake and Transport Mechanism of Dihydromyricetin Across Human Intestinal Caco‐2 Cells

Cited by 29 publications

References 30 publications

Dihydromyricetin: A review on identification and quantification methods, biological activities, chemical stability, metabolism and approaches to enhance its bioavailability

Dihydromyricetin: A review on identification and quantification methods, biological activities, chemical stability, metabolism and approaches to enhance its bioavailability

Dihydromyricetin Acts as a Potential Redox Balance Mediator in Cancer Chemoprevention

Preclinical Research of Dihydromyricetin for Brain Aging and Neurodegenerative Diseases

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