Bioavailability of ellagic acid in human plasma after consumption of ellagitannins from pomegranate ( Punica granatum L.) juice (original) (raw)
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Journal of Natural Products, 1991
AssTuc".-This study was undertaken to measure the liberation in vitro of ellagic acid 121, a naturally occurring inhibitor of carcinogenesis, from precursor ellagitannins under conditions found in the gut tract. Enzymes, namely P-glucosidase, esterases, and a-amylase, were incubated with raspberry extract. In addition, raspberry extract and casuarictin 11) were treated at different pH's and with the contents of small intestine and cecum from rats fed AIN-76A diet. The esterase activity of the enzyme samples was measured spectrophotometrically using p-nitrophenol acetate as the substrate, and the amount of ellagic acid {2) released from all samples was analyzed by hplc. The hydrolysis of the ellagitannins was not catalyzed by any of the purified enzymes tested, and components of the raspberry extract were found to inhibit the purified esterases noncompetitively. Casuarictin {I) was hydrolyzed to yield high quantities ofellagic acid [2] when placed in buffer at pH 7 and 8, or when incubated with cecal contents for two hours. The release of ellagic acid [2] from the raspberry extract was optimal at p H 8, and maximal release in cecal contents occurred with 1 h. Small intestinal contents had no significant effect on ellagic acid liberation from either casuarictin 111 or raspberry extract.
The Journal of nutrition, 2006
Ellagitannins (ETs) from pomegranate juice (PJ) are reported to have numerous biological properties, but their absorption and metabolism in humans are poorly understood. To investigate the pharmacokinetics of pomegranate ETs, 18 healthy volunteers were given 180 mL of PJ concentrate, and blood samples were obtained for 6 h afterwards. Twenty-four-hour urine collections were obtained on the day before (-1), the day of (0), and the day after (+1) the study. Ellagic acid (EA) was detected in plasma of all subjects with a maximum concentration of 0.06 +/- 0.01 micromol/L, area under concentration time curve of 0.17 +/- 0.02 (micromol x h) x L(-1), time of maximum concentration of 0.98 +/- 0.06 h, and elimination half-life of 0.71 +/- 0.08 h. EA metabolites, including dimethylellagic acid glucuronide (DMEAG) and hydroxy-6H-benzopyran-6-one derivatives (urolithins), were also detected in plasma and urine in conjugated and free forms. DMEAG was found in the urine obtained from 15 of 18 sub...
Journal of Medicinal Food, 2008
Pomegranate juice (PJ), a rich source of polyphenols including ellagitannins, has attracted much attention due to its reported health benefits. This has resulted in the consumption of liquid and powder pomegranate extracts as alternatives to PJ. Therefore establishing the bioavailability of polyphenols from these extract preparations is necessary. Sixteen healthy volunteers sequentially consumed, with a 1-week washout period between treatments, PJ (8 ounces, Wonderful fruit variety), a pomegranate polyphenol liquid extract (POMxl, 8 ounces), and a pomegranate polyphenol powder extract (POMxp, 1,000 mg). The three interventions provided 857, 776, and 755 mg of polyphenols as gallic acid equivalents, respectively. Plasma bioavailability, judged based on ellagic acid levels over a 6-hour period, did not show statistical differences in area under the curve for the three interventions: 0.14 Ϯ 0.05, 0.11 Ϯ 0.03, and 0.11 Ϯ 0.04 mol и hour/L for PJ, POMxl, and POMxp, respectively. The time of maximum concentration was delayed for POMxp (2.58 Ϯ 0.42 hours) compared to PJ (0.65 Ϯ 0.23 hours) and POMxl (0.94 Ϯ 0.06 hours). Urolithin-A glucuronide, a urinary metabolite of ellagic acid, was not significantly different with the three interventions, reaching levels of approximately 1,000 ng/mL. This study demonstrates that ellagitannin metabolites, delivered from pomegranate fruits, as PJ, POMxl, and POMxp, reach equivalent levels with a delay in time of maximum concentration of POMxp compared to PJ and POMxl.
CRITICAL REVIEW IN PHARMACEUTICAL SCIENCES A review on Ellagic acid as a natural antioxidant
Ellagic acid(EA) is a naturally occurring polyphenolic compound. Recently there is growing interest in understanding the role and mechanism of the phytochemicals; such as polyphenolics, flavonoids and phenylpropanoids as inhibitors of oxidative stress. EA has wide array of biological properties, such as radical scavenging, chemopreventive, antiviral and antibacterial properties. EA is a naturally occurring dietary antimutagen and anticarcinogen with strong antioxidant and anti-inflammatory activities. EA is abundant in berries, walnuts pecans, pomegranate, cranberries and other plant foods in the form of hydrolysable tannins called ellagitannins. Ellagitannins are mostly found in the plants belonging to families Myrtaceae, Punicaceae and Combrataceae. While focusing on the multifunctional activities of such compounds, this review briefly points out increasing interest in polyphenolic derivatives as an antioxidant, which holds future promises.
Food Ellagitannins: Structure, Metabolomic Fate, and Biological Properties
Tannins - Structural Properties, Biological Properties and Current Knowledge [Working Title], 2019
Food sources of ellagitannins (ETs) are numerous, and dietary intake of these compounds is estimated up to 12 mg/day in some countries, even though ETs have been considered in the past as not bioavailable like other tannins and were mostly neglected by nutritionists. Nonetheless, new insights show that ETs are bioconverted by microbiota in the gut into metabolites called urolithins, which are bioavailable and can reach relatively high physiological concentration in the body up to 7 days after ingestion. According to the initial structure of ETs in the food source, the extent of bioconversion into urolithins may differ but all urolithins are susceptible to exert potential health benefits. Nonetheless, due to the intervention of microbiota, the production and excretion of urolithins are highly variable according to individuals, which have led to the classification of consumers into metabotype. According to metabotype, the potential health benefits of ellagitannins may differ among consumers. In in vitro, cellular and animal studies, numerous health benefits of ellagitannins and urolithins are reported mainly for the chemoprevention of hormone-dependent cancer and cardiovascular disease. Nonetheless, ellagitannins deserve closer attention from the scientific community to unravel more biological properties of this particular compound.
An update on ellagic acid as a natural powerful flavonoid
Ellagic acid is a polyphenol compound present in many fruits, nuts, and seeds, such as pomegranates, black raspberries, raspberries, strawberries, walnuts, and almonds. Some studies in the past indicated that ellagic acid showed powerful free radical scavenging action, and also has anti-diabetic, chemoprotective, anti-apoptotic, anti-inflammatory and anti-tumorigenic properties. While ellagic acid and its complex derivatives such as ellagitannins (ETs) play an important role in human nutrition and endowed with numerous biological properties, thus this substance may be suitable as a defensive factor against free radicals. Hence the aim of this paper is to review current research into the therapeutic potential of ellagic acid in prevention and treatment of some chronic conditions such as cancers or various chronic disease due to its main role as a potent scavenger of oxygen species.
Current Topics in Nutraceutical Research, 2020
A sensitive and specific liquid chromatography tandem mass spectrometric method was developed and validated for the simultaneous determination of rosuvastatin (ROS) and N-desmethyl rosuvastatin (NOR-ROS) in human plasma using deuterium-labeled internal standards. The plasma samples were prepared using liquid-liquid extraction with diethyl ether. Chromatographic separation was accomplished on an Xterra MS C 18 column. The mobile phase consisted of a gradient mixture of 15 mmol/L ammonium acetate in water and in methanol, maintained at a flow rate of 0.4 mL/min. Mass spectrometric detection was carried out in negative electrospray ionization mode and monitored by quantification and qualification transitions for each analyte. Using 300 mL plasma samples, the lower limits of quantification of ROS and NOR-ROS were 0.05 and 0.02 mg/L respectively. The linearity of ROS and NOR-ROS ranged from 0.05 to 42 and 0.02 to 14 mg/L respectively. The relative standard deviations of ROS and NOR-ROS were <13 and 9%, respectively, while the deviations from expected values were within À4.7-9.8 and À5.2-4.6%, respectively. The present method offered high sensitivity and was successfully applied to a 24 h pharmacokinetic study of ROS and NOR-ROS in healthy subjects receiving a single dose of 10 mg ROS.
The pharmacological use of ellagic acid-rich pomegranate fruit
International Journal of Food Sciences and Nutrition, 2013
In recent years, the therapeutic use of non-drug substances such as herbal and medicinal foods is increasing progressively. Of these substances, Punica granatum L., which is an ancient and highly distinctive fruit, has been proposed for treatment of several different illnesses. Ellagic acid (EA) is one of those biological molecules found in pomegranate and may have therapeutic potential in many diseases. EA has been detected not only in pomegranate but also in a wide variety of fruits and nuts such as raspberries, strawberries, walnuts, grapes and black currants, and is becoming an increasingly popular dietary supplement over recent years. Similar to other ellagitannins (ETs), EA is quite stable under physiological conditions in the stomach. EA and ETs as active agents induce vasorelaxation, oxygen free radical scavenging, hypolipidemic, antiinflammatory and anti-carcinogenic activities in various animal preparations call an attention to the need for designing adequate tests in humans to assess these potentially useful properties in diseased states.
Ellagic Acid: A Review on Its Natural Sources, Chemical Stability, and Therapeutic Potential
Oxidative Medicine and Cellular Longevity, 2022
Ellagic acid (EA) is a bioactive polyphenolic compound naturally occurring as secondary metabolite in many plant taxa. EA content is considerable in pomegranate (Punica granatum L.) and in wood and bark of some tree species. Structurally, EA is a dilactone of hexahydroxydiphenic acid (HHDP), a dimeric gallic acid derivative, produced mainly by hydrolysis of ellagitannins, a widely distributed group of secondary metabolites. EA is attracting attention due to its antioxidant, anti-inflammatory, antimutagenic, and antiproliferative properties. EA displayed pharmacological effects in various in vitro and in vivo model systems. Furthermore, EA has also been well documented for its antiallergic, antiatherosclerotic, cardioprotective, hepatoprotective, nephroprotective, and neuroprotective properties. This review reports on the health-promoting effects of EA, along with possible mechanisms of its action in maintaining the health status, by summarizing the literature related to the therapeu...
Journal of Agricultural and Food Chemistry, 2006
The intake of polyphenols has been demonstrated to have health-promoting and disease-preventive effects. The pomegranate (Punica granatum L.), which is rich in several polyphenols, has been used for centuries in ancient cultures for its medicinal purposes. The potential health benefits of pomegranate polyphenols have been demonstrated in numerous in vitro studies and in vivo experiments. This study investigated the absorption and antioxidant effects of a standardized extract from pomegranate in healthy human volunteers after the acute consumption of 800 mg of extract. Results indicate that ellagic acid (EA) from the extract is bioavailable, with an observed C max of 33 ng/mL at t max of 1 h. The plasma metabolites urolithin A, urolithin B, hydroxyl-urolithin A, urolithin A-glucuronide, and dimethyl ellagic acid-glucuronide were identified by HPLC-MS. The antioxidant capacity measured with the oxygen radical absorbance capacity (ORAC) assay was increased with a maximum effect of 32% after 0.5 h, whereas the generation of reactive oxygen species (ROS) was not affected. The inflammation marker interleukin-6 (IL-6) was not significantly affected after 4 h after the consumption of the extract. Overall, this study demonstrated the absorbability of EA from a pomegranate extract high in ellagitannin content and its ex vivo antioxidant effects.