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With a yearly production of about 39 million tons, brewer’s spent grain (BSG) is the
most abundant brewing industry byproduct. Because it is rich in fiber and protein, it is commonly
used as cattle feed but could also be used within the human diet. Additionally, it contains many
bioactive substances such as hydroxycinnamic acids that are known to be antioxidants and potent
inhibitors of enzymes of glucose metabolism. Therefore, our study aim was to prepare different
extracts—A1-A7 (solid-liquid extraction with 60% acetone); HE1-HE6 (alkaline hydrolysis followed
by ethyl acetate extraction) and HA1-HA3 (60% acetone extraction of alkaline residue)—from various
BSGs which were characterized for their total phenolic (TPC) and total flavonoid (TFC) contents,
before conducting in vitro studies on their effects on the glucose metabolism enzymes α-amylase,
α-glucosidase, dipeptidyl peptidase IV (DPP IV), and glycogen phosphorylase α (GPα). Depending
on the extraction procedures, TPCs ranged from 20–350 μg gallic acid equivalents/mg extract
and TFCs were as high as 94 μg catechin equivalents/mg extract. Strong inhibition of glucose
metabolism enzymes was also observed: the IC50 values for α-glucosidase inhibition ranged from
67.4 ± 8.1 μg/mL to 268.1 ± 29.4 μg/mL, for DPP IV inhibition they ranged from 290.6 ± 97.4 to
778.4 ± 95.5 μg/mL and for GPα enzyme inhibition from 12.6 ± 1.1 to 261 ± 6 μg/mL. However, the
extracts did not strongly inhibit α-amylase. In general, the A extracts from solid-liquid extraction
with 60% acetone showed stronger inhibitory potential towards α-glucosidase and GPα than other
extracts whereby no correlation with TPC or TFC were observed. Additionally, DPP IV was mainly
inhibited by HE extracts but the effect was not of biological relevance. Our results show that BSG
is a potent source of α-glucosidase and GPα inhibitors, but further research is needed to identify
these bioactive compounds within BSG extracts focusing on extracts from solid-liquid extraction
with 60% acetone.
Winery by-products arise in high amounts during winemaking processes. Hence, recovery alternatives are of great interest. In this study, effects of extracts from winery by-products (Vitis vinifera L. cv. Riesling) on mitochondrial functions in human hepatocellular carcinoma (HepG2) cells were examined. Polyphenolic profiles of pomace (PE), stem (SE), vine leaf (VLE), and vine shoot extracts (VSE) were characterized by HPLC-UV/Vis-ESI-MS/MS. The extracts induced dose-dependent cytotoxic effects (PE > SE > VLE > VSE). VSE showed protective effects regarding modulation of tert-butyl hydroperoxide (TBH)-induced intracellular reactive oxygen species (ROS) levels. PE, SE and VLE increased the mitochondrial membrane potential (MMP), whereas VSE decreased it owing to mildly impaired mitochondrial respiration. Cells may try to compensate reduced respiration chain complex activities by increasing the mitochondrial mass, as indicated by enhanced citrate synthase activity and mRNA expression levels after VSE incubation. Thus, winery by-products represent interesting sources of bioactive compounds that exert positive or negative effects on mitochondrial functions.
We have investigated urine samples after coffee consumption using targeted and untargeted
approaches to identify furan and 2-methylfuran metabolites in urine samples by UPLC-qToF.
The aim was to establish a fast, robust, and time-saving method involving ultra-performance
liquid chromatography-quantitative time-of-flight tandem mass spectrometry (UPLC-qToF-MS/MS).
The developed method detected previously reported metabolites, such as Lys-BDA, and others that
had not been previously identified, or only detected in animal or in vitro studies. The developed
UPLC-qToF method detected previously reported metabolites, such as lysine-cis-2-butene-1,4-dial
(Lys-BDA) adducts, and others that had not been previously identified, or only detected in animal
and in vitro studies. In sum, the UPLC-qToF approach provides additional information that may be
valuable in future human or animal intervention studies.
Red fruits and their juices are rich sources of polyphenols, especially anthocyanins.
Some studies have shown that such polyphenols can inhibit enzymes of the carbohydrate metabolism,
such as α-amylase and α-glucosidase, that indirectly regulate blood sugar levels. The presented
study examined the in vitro inhibitory activity against α-amylase and α-glucosidase of various
phenolic extracts prepared from direct juices, concentrates, and purees of nine different berries which
differ in their anthocyanin and copigment profile. Generally, the extracts with the highest phenolic
content—aronia (67.7 ± 3.2 g GAE/100 g; cyanidin 3-galactoside; chlorogenic acid), pomegranate
(65.7 ± 7.9 g GAE/100 g; cyanidin 3,5-diglucoside; punicalin), and red grape (59.6 ± 2.5 g GAE/100 g;
malvidin 3-glucoside; quercetin 3-glucuronide)—showed also one of the highest inhibitory activities
against α-amylase (326.9 ± 75.8 µg/mL; 789.7 ± 220.9 µg/mL; 646.1 ± 81.8 µg/mL) and α-glucosidase
(115.6 ± 32.5 µg/mL; 127.8 ± 20.1 µg/mL; 160.6 ± 68.4 µg/mL) and, partially, were even more potent
inhibitors than acarbose (441 ± 30 µg/mL; 1439 ± 85 µg/mL). Additionally, the investigation of single
anthocyanins and glycosylated flavonoids demonstrated a structure- and size-dependent inhibitory
activity. In the future in vivo studies are envisaged.
Phosphodiesterases (PDEs) are essential enzymes for the regulation of pathways mediated
by cyclic adenosine monophosphate (cAMP). Secondary plant compounds like anthocyanins (ACs)
can inhibit PDE activity and, consequently, may be beneficial for lipid metabolism. This study
investigated 18 AC-rich juice extracts and pure reference compounds from red fruits for potential
inhibitory effects on PDE 3B activity. Extracts were obtained through adsorption on Amberlite® XAD
7 resin. Based on this screening, the chokeberry, blueberry, pomegranate, and cranberry extracts
were active, with half maximal inhibitory concentrations (IC50) ranging from 163 ± 3 µg/mL to
180 ± 3 µg/mL. The ACs in these extracts, peonidin-3-glucoside and cyanidin-3-arabinoside, were the
most active single compounds (IC50 = 56 ± 20 µg/mL, 108 ± 6 µg/mL). All extracts comprised high
amounts of phenolic compounds, as determined by the Folin–Ciocalteu assay, ranging from 39.8 ± 1.5
to 73.5 ± 4.8 g gallic acid equivalents (GAE)/100 g extract. Pomegranate and chokeberry extracts
exhibited the largest amounts of polyphenols (72.3 ± 0.7 g GAE/100 g, 70.6 ± 4.1 g GAE/100 g,
respectively). Overall, our results showed that fruit juice extracts and their ACs can inhibit PDE
activity. Any potential health benefits in vivo will be investigated in the future.