The aim of this study was to estimate the mode of thyroid peroxidase (TPO) inhibition by polyphenols: Chlorogenic acid, rosmarinic acid, quercetin, and rutin. All the tested polyphenols inhibited TPO; the IC50 values ranged from 0.004 mM to 1.44 mM (for rosmarinic acid and rutin, respectively). All these pure phytochemical substances exhibited different modes of TPO inhibition. Rutin and rosmarinic acid showed competitive, quercetin—uncompetitive and chlorogenic acid—noncompetitive inhibition effect on TPO. Homology modeling was used to gain insight into the 3D structure of TPO and molecular docking was applied to study the interactions of the inhibitors with their target at the molecular level. Moreover, the type and strength of mutual interactions between the inhibitors (expressed as the combination index, CI) were analyzed. Slight synergism, antagonism, and moderate antagonism were found in the case of the combined addition of the pure polyphenols. Rutin and quercetin as well as rutin and rosmarinic acid acted additively (CI = 0.096 and 1.06, respectively), while rutin and chlorogenic acid demonstrated slight synergism (CI = 0.88) and rosmarinic acid with quercetin and rosmarinic acid with chlorogenic acid showed moderate antagonism (CI = 1.45 and 1.25, respectively). The mixture of chlorogenic acid and quercetin demonstrated antagonism (CI = 1.79). All the polyphenols showed in vitro antiradical ability against 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid), ABTS. The highest ability (expressed as IC50) was exhibited by rosmarinic acid (0.12 mM) and the lowest value was ascribed to quercetin (0.45 mM).
This study investigated the activity, mode of inhibition, and interactions between lipoxygenase (LOX) inhibitors and compounds able to inhibit lipids oxidation (LPO) derived from green coffee beans (GCBs), wholemeal wheat flour (WF), and bread enriched with GCB, in comparison with pure chemical standards of the main active components—ferulic (FA) and chlorogenic acids (CGA). Both GCB and WF contain potentially bioaccessible and bioavailable LPO inhibitors acting synergistically. Both FA and CGA presented nearly additive interaction. Potentially bioaccessible LOX inhibitors from GCB and WF acted synergistically, whereas moderate antagonism was found for potentially bioavailable compounds. The activity of CGA and FA was quite similar (EC50 = 18.56 and 22.36 g DW/ml, respectively) and synergistic action between these components was found. The LPO activity of functional breads was positively correlated with the percentage of GCB (R2 = 0.98). Ferulic acid and CGA acted as competitive LOX inhibitors, whereas potentially bioaccessible compounds from bread enriched with GCB demonstrated an uncompetitive mode of action. Green coffee beans, WF, and the proposed functional product could be helpful in dietary therapy and prevention of so-called lifestyle disorders related with the lipid metabolism. Moreover, this paper highlights the need to study the interactions between the active ingredients of newly designed functional products.
This study focused on the effect of kaempferol, catechin, apigenin, sinapinic acid, and extracts from plants (i.e., parsley, cumin, mustard, green tea, and green coffee) on thyroid peroxidase (TPO) and lipoxygenase (LOX) activity, antiradical potential, as well as the result of interactions among them. Catechin, sinapinic acid, and kaempferol acted as a competitive TPO inhibitors, while apigenin demonstrated an uncompetitive mode of inhibitory action. Ethanol extracts from all plants acted as competitive TPO inhibitors, while, after in vitro digestion, TPO activation was found especially in the case of mustard (24%) and cumin (19.85%). Most importantly, TPO activators acted synergistically. The TPO effectors acted as LOX inhibitors. The most effective were potentially bioaccessible compounds from green tea and green coffee (IC50 = 29.73 mg DW/mL and 30.43 mg DW/mL, respectively). The highest free radical scavenging ability was determined for catechin and sinapinic acid (IC50 = 78.37 µg/mL and 84.33 µg/mL, respectively) and potentially bioaccessible compounds from mustard (0.42 mg DW/mL) and green coffee (0.87 mg DW/mL). Green coffee, green tea, cumin, and mustard contain potentially bioaccessible TPO activators that also act as effective LOX inhibitors, which indicate their potentially health-promoting effects for people suffering from Hashimoto’s disease.
In this study, we studied the drying process, grinding characteristics and physicochemical characteristics of broccoli sprouts (BS). The seeds of broccoli were germinated at 20 °C for 3 and 6 days. Then, the seeds were air- and freeze-dried, and the Page model was used for prediction of drying kinetics of broccoli sprouts. It was observed that the drying time of BS decreased about twofold as the air-drying temperature increased from 40 to 80 °C. An increasing the air-drying temperature from 40 to 80 °C decreased the drying time by approximately twofold. Freeze-drying of sprouts took the longest drying time. Germination of seeds significantly decreased the value of grinding energy requirements, and the ground sprouts exhibited a different grinding pattern in comparison to ground non-germinated seeds. In terms of color parameters, the highest lightness and yellowness were found for freeze-dried sprouts. Redness and yellowness of sprouts increased with an increase in the air-drying temperature. The lowest total color difference was obtained for the freeze-dried sprouts. Higher drying temperature resulted in lower total phenolics content (TPC) and decreased antioxidant activity (AA). The highest TPC and AA were observed in air-dried sprouts (40 °C) and freeze-dried sprouts after 6 days of germination.
The white beetroot cv. Śnieżna Kula is the first betanin-free beetroot registered in the European Union. The aim of this study was to compare the phenolic acids profile and antioxidant capacity of leaves of white (SK) and red (CC) beetroots and red (LC) and white (BL) Swiss chard growing in Poland. LC leaves were the richest source of total phenolics (16.55 mg GAE/g FW) and phenolic acids (1.81 mg/g FW), while the highest content of flavonoids was determined in CC leaves (1.6 mg QE/g FW). The highest antiradical activity was observed for LC, whereas CC extract exhibited the highest chelating power. BL and CC leaf extracts demonstrated high LOX inhibitory potential (EC50 = 53.23 and 56.97 mg FW/mL, respectively). An uncompetitive type of LOX inhibition was obtained for all extracts. SK extracts demonstrated the highest XO inhibitory activity (EC50 = 81.04 mg FW/mL). A noncompetitive type of XO inhibition was obtained in both extracts from red leaves (CC and LC), whereas an uncompetitive mode of inhibition was observed in the case of white leaf (SK and LC) extracts. Thus, it can be assumed that the presence of betanin influences the XO inhibition mechanism.
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