T. Frank

Bioavailability and Biokinetics of Anthocyanins From Red Grape Juice and Red Wine

In a comparative study, 9 healthy volunteers ingested a single oral dose of 400u2009mL red grape juice or red wine with dose-adjusted anthocyanin content (283.5u2009mg or 279.6u2009mg, resp) in crossover. The content of anthocyanin glucosides was detected in plasma and urinary excretion. Additionally, the plasmatic antioxidant activity was assessed after intake. Based on the plasma content, biokinetic criteria of the single anthocyanins were calculated, such as AUC, cmax, tmax, and the elimination rate t1/2. The urinary excretion of total anthocyanins differed significantly and amounted to 0.18% (red wine) and 0.23% (red grape juice) of the administered dose. Additionally, the plasmatic antioxidant activity increased to higher levels after juice ingestion compared to wine. The intestinal absorption of the anthocyanins of red grape juice seemed to be improved compared to red wine, suggesting a possible synergistic effect of the glucose content of the juice. The improved absorption resulted in an enhanced plasmatic bioactivity.

Pharmacokinetics of Anthocyanidin-3-Glycosides Following Consumption of Hibiscus sabdariffa L. Extract

Pharmacokinetic parameters of several dietary anthocyanins following consumption of Hibiscus sabdariffa L. extract were determined in 6 healthy volunteers. Subjects were given a single oral dose of 150 mL of Hibiscus sabdariffa L. extract yielding 62.6 mg of cyanidin‐3‐sambubioside, 81.6 mg of delphindin‐3‐sambubioside, and 147.4 mg of total anthocyanins (calculated as cyanidin equivalents). Within 7 hours, the urinary excretion of cyanidin‐3‐sambubioside, delphinidin‐3‐sambubioside, and total anthocyanins (ie, the sum of all quantifiable anthocyanidin glycosides) was 0.016%, 0.021%, and 0.018% of the administered doses, respectively. Maximum excretion rates were determined at 1.5 to 2.0 hours after intake. The dose‐normalized plasma area under the curve estimates were 0.076, 0.032, and 0.050 ng•h/mL/mg for cyanidin‐3‐sambubioside, delphinidin‐3‐sambubioside, and total anthocyanins, respectively. The dose‐normalized Cmax estimates were 0.036, 0.015, and 0.023 ng/mL/mg in the same sequence. They were reached each at 1.5 hours (median) after intake. The geometric means of t1/2 were 2.18, 3.34, and 2.63 hours for cyanidin‐3‐sambubioside, delphinidin‐3‐sambubioside, and total anthocyanins, respectively. The urinary excretion of intact anthocyanins was fast and appeared to be monoexponential. To evaluate the contribution of anthocyanins to the health‐protecting effects of Hibiscus sabdariffa L. extract, it will be necessary to perform further studies on both the intact glycosides and their in vivo metabolites or conjugates in human plasma and urine.

Urinary Excretion of Cyanidin Glucosides and Glucuronides in Healthy Humans After Elderberry Juice Ingestion

In a pilot study with 6 females and 1 male, the metabolism of various cyanidin glucosides after oral administration of elderberry juice was investigated. The anthocyanin metabolites were detected in urinary excretion. After ingestion of a bolus quantity of 3.57u2009g total anthocyanins in a 150u2009mL elderberry juice concentrate, 0.053% of the administered dose was excreted in urine as glucosidically bound cyanidins within the first 5 hours. Only 0.003% of the ingested anthocyanin glucosides was excreted as cyanidin glucuronide, suggesting that this conversion step might be of minor importance in urinary excretion.

Application of stable isotope dilution assays based on liquid chromatography-tandem mass spectrometry for the assessment of folate bioavailability.

A pilot study was performed to prove the suitability of stable isotope dilution assays for assessing the bioavailability of endogenous folates in foods. By using [2H(4)]folic acid, [2H(4)]tetrahydrofolate, [2H(4)]5-methyltetrahydrofolate, [2H(4)]5-formyltetrahydrofolate and [2H(4)]10-formylfolic acid as internal standards, folates in spinach, apple juice and blood plasma were quantified by liquid chromatography coupled to tandem mass spectrometry. To liberate the pteroyl monoglutamates, sample extracts of foods were treated by rat plasma. Sample clean-up was achieved by solid-phase extraction on anion-exchange cartridges, which proved to be sufficient to obtain mass chromatograms devoid of matrix interferences. The bioavailability study was designed as a short-time protocol with three meals, the first consisting of 600 g spinach (meal A), the second consisting of 600 g apple sauce with additionally 400 microg synthetic folic acid (meal B) and the third consisting solely of 600 g apple sauce (meal C). Prior to the meals, the participating volunteers tissue was saturated with folates to achieve a significant response of plasma folate to the meals. After consumption of meals A and B a significant rise in folate plasma level compared to meal C (mean level at 28 microg/ml) was observed. The relative bioavailability of folate following meal A exceeded significantly the suggested value of 50% for food folates by taking the dose-normalized area under the curve (AUC) following ingestion of meal B as reference.

Consumption of Hibiscus sabdariffa L. aqueous extract and its impact on systemic antioxidant potential in healthy subjects

BACKGROUNDnTo evaluate health benefits attributed to Hibiscus sabdariffa L. a randomized, open-label, two-way crossover study was undertaken to compare the impact of an aqueous H. sabdariffa L. extract (HSE) on the systemic antioxidant potential (AOP; assayed by ferric reducing antioxidant power (FRAP)) with a reference treatment (water) in eight healthy volunteers. The biokinetic variables were the areas under the curve (AUC) of plasma FRAP, ascorbic acid and urate that are above the pre-dose concentration, and the amounts excreted into urine within 24 h (Ae(0-24) ) of antioxidants as assayed by FRAP, ascorbic acid, uric acid, malondialdehyde (biomarker for oxidative stress), and hippuric acid (metabolite and potential biomarker for total polyphenol intake).nnnRESULTSnHSE caused significantly higher plasma AUC of FRAP, an increase in Ae(0-24) of FRAP, ascorbic acid and hippuric acid, whereas malondialdehyde excretion was reduced. Furthermore, the main hibiscus anthocyanins as well as one glucuronide conjugate could be quantified in the volunteers urine (0.02% of the administered dose).nnnCONCLUSIONnThe aqueous HSE investigated in this study enhanced the systemic AOP and reduced the oxidative stress in humans. Furthermore, the increased urinary hippuric acid excretion after HSE consumption indicates a high biotransformation of the ingested HSE polyphenols, most likely caused by the colonic microbiota.

Assessment of thiamin status in chronic renal failure patients, transplant recipients and hemodialysis patients receiving a multivitamin supplementation.

The thiamin status of patients with chronic renal failure (CRF, n = 14), dialysis patients (DP, n = 24) and patients after renal transplantation (RT, n = 19) was assessed. Thiamin intake was calculated at mean levels of 1.26 mg/d (CRF), 0.83 mg/d (DP) and 1.42 mg/d (RT). Corresponding mean plasma concentrations were 64.2 nmol/l (CRF), 78.3 nmol/l (DP) and 55.1 nmol/l (RT). Thiamin supplements of 1.5 mg or 8.0 mg orally given to patients of the DP-group after each dialysis session showed slightly higher thiamin concentrations in plasma. Transketolase activity coefficients (ETK-AC) were in the same range (1.11...1.19) except for RT-patients who had a slightly but not significantly higher ETK-AC of 1.22. During dialysis treatment (DT), thiamin plasma concentrations dropped to 75 and/or 82% in patients supplemented with 1.5 and/or 8.0 mg. They both reached initial levels again 44 hours later. Despite large inter-individual differences, thiamin concentrations increased in the non-supplemented DP-group. ETK-AC did not change after a 14-day interruption of supplementation and did not deteriorate after a single dialysis session, both in supplemented and non-supplemented patients. A daily thiamin supplementation which complies with the RDA for healthy subjects is indicated in DP and is sufficient to keep thiamin status within the normal range.

Bioavailability of water- and lipid-soluble thiamin compounds in broiler chickens.

The bioavailability of thiamin mononitrate, thiamin chloride-hydrochloride and benfotiamin was compared in broiler chickens. A thiamin-deficient diet was supplemented with either 1.8 and 1.5 mg/kg thiamin equivalent as water-soluble salts, or with 1.5 and 1.2 mg/kg thiamin equivalent as benfotiamin, respectively, and fed to 3 replicate groups/treatment for 21 days. Weight gain, feed consumption and feed conversion rate were not significantly affected by solubility or dietary level of thiamin. Likewise, using biochemical indices of thiamin status (erythrocyte transketolase activation coefficient, and thiamin concentrations in blood and liver), no differences were found between the water-soluble thiamin salts, indicating that they have identical potency. In contrast, biochemical indices of thiamin status showed a significantly higher bioavailability for benfotiamin than for the water-soluble sources.

Does a 100-km walking affect indicators of vitamin status?

The status of thiamin (B1), riboflavin (B2), ascorbic acid (AA), and tocopherol was determined in 60 leisure athletes (age 46 +/- 10 y, BMI 23.7 +/- 2.0 kg.m-2, VO2max 39.4 +/- 6.5 ml.min-1.kg-1), who completed a 100-km walking race. Vitamin plasma levels and activities of erythrocyte transketolase (ETK) and glutathione reductase (EGR) were measured before start, immediately after finishing and 6 hours later. The participators finished the entire distance in 14.25 h (average speed 7 km.h-1). Before start, all participators showed an excellent vitamin status (prevalences of low vitamin status ranged between 1.7 and 1.8%). Plasma tocopherol concentrations correlated significantly with increased age (r = 0.35, p = 0.008). Compared to the values before start, plasma concentrations of B1 and B2 as well as ETK and/or EGR were increased significantly after finishing. The raised levels persisted 6 hours after finishing, whereas AA remained unaltered. The univariate analysis of variance revealed that the change in vitamin status after finish and 6 hours later was in part highly dependent on age, BMI and the level of physical fitness. Despite the long distance, the extensive character of the 100-km walking with its low intensity did not deteriorate the measured indicators of vitamin status.

Pilot Study on Folate Bioavailability from a Camembert Cheese Reveals Contradictory Findings to Recent Results from a Human Short-term Study

Different dietary sources of folate have differing bioavailabilities, which may affect their nutritional “value.” In order to examine if these differences also occur within the same food products, a short-term human pilot study was undertaken as a follow-up study to a previously published human trial to evaluate the relative native folate bioavailabilities from low-fat Camembert cheese compared to pteroylmonoglutamic acid as the reference dose. Two healthy human subjects received the test foods in a randomized cross-over design separated by a 14-day equilibrium phase. Folate body pools were saturated with a pteroylmonoglutamic acid supplement before the first testing and between the testings. Folates in test foods and blood plasma were analyzed by stable isotope dilution assays. The biokinetic parameters Cmax, tmax, and area under the curve (AUC) were determined in plasma within the interval of 0–12u2009h. When comparing the ratio estimates of AUC and Cmax for the different Camembert cheeses, a higher bioavailability was found for the low-fat Camembert assessed in the present study (≥64%) compared to a different brand in our previous investigation (8.8%). It is suggested that these differences may arise from the different folate distribution in the soft dough and firm rind as well as differing individual folate vitamer proportions. The results clearly underline the importance of the food matrix, even within the same type of food product, in terms of folate bioavailability. Moreover, our findings add to the increasing number of studies questioning the general assumption of 50% bioavailability as the rationale behind the definition of folate equivalents. However, more research is needed to better understand the interactions between individual folate vitamers and other food components and the potential impact on folate bioavailability and metabolism.