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Polyphenols have been used as natural medicaments for the management of hyperuricemia for a long history. They have been attracted many interests because of the little side effects in curing hyperuricemia, which is an important advantage over the antihyperuricemic drugs. In this review, the structure–activity relationships for polyphenols as xanthi...
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Hyperuricemia is the result of increased production and/or underexcretion of uric acid. Hyperuricemia has been epidemiologically associated with multiple comorbidities, including metabolic syndrome, gout with long-term systemic inflammation, chronic kidney disease, urolithiasis, cardiovascular disease, hypertension, rheumatoid arthritis, dyslipidem...
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... Flavonoid-enriched plant extracts are recognised as an important resource, exhibiting significant antimicrobial, antioxidant, antitumor effects (Patel et al., 2018;Zhao et al., 2019;Ullah et al., 2022), and are also promising agents for inflammation treatments (Al-Khayri et al., 2022). Moreover, flavonoid compounds have been reported to play a crucial role in the prevention of chronic ailments, such as diabetes, cardiovascular disease, and gouty arthritis-an inflammatory-mediated disorder that can diminish quality of life (Roddy & Doherty, 2010;Osman et al., 2016;Ullah & Munir, 2020;Liu et al., 2020a;Zhan et al., 2021;Das et al., 2022;He et al., 2023). Increased consumption of flavonoid-rich foods correlates with numerous health benefits (Bondonno et al., 2020), which has led to interest in isolating, identifying, and characterising these constituents from various botanical sources. ...
... Quercetin International Journal of Food Science and Technology 2024 has shown promise as an anti-inflammatory compound by enhancing the production of IL-10, a cytokine with anti-inflammatory properties, or by reducing heatinduced damage through the induction of heat shock protein HSP70 (Read, 1995;Serafini et al., 2010). Moreover, quercetin from plant extracts has been reported as an effective inhibitor of XO activity in vitro (Mehmood et al., 2020;Liu et al., 2020a). Other phytochemical constituents, including flavonoids, terpenoids, phenolics, alkaloids, and phytosterols, are likely contributors to the anti-inflammatory activities of both in vitro and in vivo of extracts (Ghasemian et al., 2016;Das et al., 2022). ...
Durian fruit rinds (Durio zibethinus) have increasingly attracted scientific interest due to their potent bioactive metabolites. In the present study, a comprehensive approach combining chromatographic techniques and bioassays was employed to elucidate the phytochemical constituents present in durian fruit rinds and their corresponding bioactivities. The crude ethanolic extract (CEE) and its fractions obtained through silica gel column chromatography (F1, F2, F3, and F4) were qualitatively and quantitatively analysed for their flavonoid profiles using thin‐layer chromatography, high‐performance liquid chromatography (HPLC), and liquid chromatography/mass spectrometry (LC/MS). Among the tested samples, fraction F2 exhibited the highest total flavonoid content (179.55 mg QE/g DW). TLC and HPLC analyses showed the presence of quercetin in all tested samples, with its content ranking in the order of F2 > F3 > F1 > F4 > CEE. The fractions exhibited inhibitory effects on albumin denaturation, protease activity, lipoxygenase (LOX), heat‐induced haemolysis, and xanthine oxidase (XO), surpassing those of the crude extract. These observed bioactivities correlated with the distribution of flavonoids and quercetin content in the samples. LC/MS analysis further showed the presence of flavonoids‐chalcone, flavonols, terpenoids, stilbene glycosides, anthocyanins, phenolics, and amino acids in fraction F2. These results determine the phytochemical profiles, anti‐inflammatory, and anti‐XO activities of bioactive fraction obtained from durian fruit rinds.
... Clinically reported, hyperuricemia not only increase the incidence rate of gout, arthritis and renal diseases, but also increase the neurological and cardiovascular diseases (Zhu et al., 2004). Due to XOD is the key enzyme of UA production, hence, inhibiting the activity of XOD is become the primary strategy to repress UA production (Hou et al., 2021;Liu et al., 2020;Mehmood et al., 2019). The febuxostat and allopurinol were approved mainly two XOD inhibitors to treatment of hyperuricemia (Gliozzi et al., 2016). ...
Hyperuricemia as one of the key factors for gout, and quercetin could reduce the uric acid (UA) content. However, the mechanism of quercetin reduces UA content is still uncovered. Herein, we found quercetin can reduce UA content, induce antioxidant enzyme activity, inhibit the enzyme activity of xanthine oxidase (XOD) in hyperuricemia mice. Moreover, the UA reabsorption was also significantly reduced in the kidney and the kidney inflammation was alleviated by quercetin in hyperuricemia mice. Meanwhile, the protein level of ATP‐binding cassette super‐family G member 2 (ABCG2) was markedly induced and the protein levels of urate transporter 1 (URAT1) and glucose transporter 9 (GLUT9) were significantly repressed by quercetin in hyperuricemia mice and HK‐2 cells and by quercetin‐3‐ O ‐glucuronide in HK‐2 cells. Additionally, the docking mode indicated that quercetin is stable bound to the active site of XOD. Overall, the data reveal that quercetin alleviates hyperuricemia by repressing the activity of XOD, reducing the UA absorption via enhancing ABCG2 expression, and repressing URAT1 and GLUT9 expression.
... Therefore, durian can be used for various health-related applications including neuroprotective, anticancer, anti-inflammatory, antibacterial and antioxidant agents (Isacson et al., 2002;Jayakumar & Kanthimathi, 2011;Evary & Nur, 2018;Doraiswamy & Saminathan, 2020;Charoenphun & Klangbud, 2022). The pharmaceutical properties of durian fruit extracts are related to their bioactive components, which include anthocyanins, carotenoids, polyphenols and flavonoids (Liu et al., 2020;Juarah et al., 2021;Zhan et al., 2021). ...
Durian (Durio zibethinus) fruit rinds are a promising source of bioactive phytochemicals, but they are currently wasted. This study optimised extraction conditions for flavonoids from durian fruit rinds and evaluated the biological activities of the flavonoid‐rich extracts. The highest flavonoid content of 82.17 mg QE g⁻¹ extract was achieved when performing the extraction at 60 °C using 75% ethanol and maceration time of 24 h. The crude ethanolic extract was then fractionated using liquid–liquid extraction to obtain three fractions (CHF, EAF and AQF). Among them, CHF demonstrated the highest amount of flavonoids (271.11 mg QE g⁻¹ extract) and quercetin (1006.19 μg g⁻¹ extract). This fraction also exhibited the highest ferric reducing power (IC50 of 307.88 μg vitamin C g⁻¹), DPPH radical scavenging activity (IC50 of 38.72 μg mL⁻¹), α‐amylase and α‐glucosidase inhibitory activity (IC50 of 685.76 μg mL⁻¹ and 441.10 μg mL⁻¹, respectively) and cytotoxicity against HepG‐2 and MCF‐7 cells with IC50 values of 490.30 μg mL⁻¹ and 343.38 μg mL⁻¹ respectively. The current work suggested that durian fruit rinds are a potential source of flavonoids and the CHF could be further used for pharmaceutical applications.
... The underlying mechanism for this inhibitory effect can be attributed to the polyphenolic composition within Moringa oleifera seed extracts, specifically the presence of flavonoids. Notably, flavonoids are recognized as potent XO inhibitors [24]. A parallel perspective was highlighted by [25], wherein it was emphasized that flavones contribute significantly to the inhibition of XO activity, provided they remain unaltered during the extraction process [25]. ...
... Conducting kinetic investigations to discern the inhibition mode exhibited by Moringa oleifera seed extracts on crude XO, crucial enzyme kinetic constants were unveiled: a Vmax (maximum velocity) of 0.05 U/mL and a Km (Michaelis-Menten constant) of 131.35 µM. Remarkably, these values mirrored those documented in [24]. Similar findings were observed in the works of Chioma et al. and Sakti et al., who reported congruent values of 0.05 U/mL and 131.35 µM for Km and Vmax, respectively, under extract-absent conditions [26,15]. ...
The quest for novel xanthine oxidase (XO) inhibitors, characterized by reduced side effects and heightened therapeutic efficacy, holds significant importance in addressing hyperuricemia and gout. This study was undertaken to assess the inhibitory properties of Moringa oleifera seed extracts on crude XO. The isolation of crude XO from bovine (cow) milk was achieved through ammonium sulfate precipitation techniques, and its activity was subsequently quantified using spectrophotometric measurements at a wavelength of 293 nm. The impact on xanthine oxidase inhibition was investigated utilizing varying concentrations of Moringa oleifera seed extracts in methanol, ethyl acetate, and aqueous solutions. Among these extracts, the ethyl acetate variant displayed the most robust inhibitory effect, with a notable inhibition rate of 89.16% ± 0.42, followed by the methanol extract at 65.59% ± 0.79 and the aqueous extract at 48.77% ± 0.85. For comparison, the positive control (allopurinol) exhibited an inhibition rate of 94.32% ± 0.66. The kinetic parameters of the enzyme were determined, revealing Vmax and km values of 0.05 U/ml and 131.35 µM, respectively. When the enzyme was exposed to the inhibitory extracts, the resulting Vmax and km values were as follows: ethyl acetate extract; 0.03 U/ml and 77.12 µM, methanol extract; 0.04 U/ml and 131.35 µM, and aqueous extract; 0.02 U/ml and 74.23 µM. This research work establishes a foundation for the potential utilization of Moringa oleifera seed extracts in addressing hyperuricemia and, consequently, gout.
... In this context, novel strategies with less side effects are being evaluated, such as the application of phytochemicals [13][14][15][16]. Dietary polyphenols, present in plants and also in plant-derived foods, have been reported to display several biological properties, including anti-oxidative and anti-inflammatory activities [17][18][19][20][21]. Thus, they have been proposed as possible agents for the prevention and relief of diabetes [22][23][24][25][26][27]. However, the mechanisms of antidiabetic activity still need to be investigated. ...
Dietary flavonoids are abundant in natural plants and possess multiple pharmacological and nutritional activities. In this study, apigenin, luteolin, and baicalein were chosen to evaluate their anti-diabetic effect in high-glucose and dexamethasone induced insulin-resistant (IR) HepG2 cells. All flavonoids improves the glucose consumption and glycogen synthesis abilities in IR-HepG2 cells via activating glucose transporter protein 4 (GLUT4) and phosphor-glycogen synthase kinase (GSK-3β). These fl avonoids signifi cantly inhibited the production of reactive oxygen species (ROS) and advanced glycation end-products (AGEs), which were closely related to the suppression of the phosphorylation form of NF-κB and P65. The expression levels of insulin receptor substrate-1 (IRS-1), insulin receptor substrate-2 (IRS-2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) pathway in IR-HepG2 cells were all partially activated by the fl avonoids, with variable effects. Furthermore, the intracellular metabolic conditions of the fl avonoids were also evaluated.
... The progression of asthma, cancer, chronic fatigue syndrome, and infertility was reported to be accelerated by inflammatory and oxidative stress [4]. When the body suffers harm from factors such as physical injury, toxins, and microorganisms [5,6], macrophage immune cells come into prominent play not only during the inflammatory response but also in the repair of tissue damage [7]. Hence, the inflammatory response is considered as a beneficial process to help the body defend against pathogens; however, excessive inflammation can induce fatal tissue damage [8]. ...
Although the honey produced by Lespedeza bicolor Turcz. is precious because of its medicinal value, its pharmacological mechanism is still unclear. Here, its anti-inflammatory and antioxidant functions on lipopolysaccharide (LPS)-treated murine RAW 264.7 macrophages were analyzed using targeted and non-targeted metabolomics. Results showed that twelve polyphenols were identified in L. bicolor honey using UHPLC-QQQ-MS/MS. L. bicolor honey extract could scavenge the free radicals DPPH• and ABTS+ and reduce Fe3+. Furthermore, pretreatment with L. bicolor honey extract significantly decreased NO production; suppressed the expression of COX-2, IL-10, TNF-α, and iNOS; and upregulated HO-1′s expression in the cells with LPS application. UHPLC-Q-TOF-MS/MS-based metabolomics results revealed that L. bicolor honey extract could protect against inflammatory damage caused by LPS through the reduced activation of sphingolipid metabolism and necroptosis pathways. These findings demonstrate that L. bicolor honey possesses excellent antioxidant and anti-inflammatory activities.
... They are also involved in the inhibition of oxidant enzymes, such as lipoxygenase (LO) [11], cyclooxygenase (COX) [12], myeloperoxidase (MPO) [13], Polyphenols also act as chelators of metals such as Fe, reducing the kinetics in the Fenton reaction [10]. They are also involved in the inhibition of oxidant enzymes, such as lipoxygenase (LO) [11], cyclooxygenase (COX) [12], myeloperoxidase (MPO) [13], NADPH oxidase (NOx) [14], and xanthine oxidase (XO) [15], thus preventing the generation of reactive oxygen species (ROS) [16], and stimulate others with antioxidant properties, such as catalase (CAT) [17] and superoxide dismutase (SOD) [18]. ...
... NADPH oxidase (NOx) [14], and xanthine oxidase (XO) [15], thus preventing the generation of reactive oxygen species (ROS) [16], and stimulate others with antioxidant properties, such as catalase (CAT) [17] and superoxide dismutase (SOD) [18]. ...
... The characteristic antioxidant potential of these three compounds is based on the phenolic OH group, which can donate H + and remove the unpaired electron through the resonant electron system [32]. The OH groups donate a proton to various radicals • X such NADPH oxidase (NOx) [14], and xanthine oxidase (XO) [15], thus preventing the generation of reactive oxygen species (ROS) [16], and stimulate others with antioxidant properties, such as catalase (CAT) [17] and superoxide dismutase (SOD) [18]. It is worth mentioning the importance of the efforts being made in the development of new synthetic antioxidants. ...
In this review, we have focused mainly on the study of their antioxidant and pro-oxidant capacity, and the analysis of the oxidation of the catechol group to o-quinone. The redox balance established between the different oxidase and reductase enzymes generates reducing species, H + and e − , and allows the oxidation of polyphenolic groups to quinones to be reversible. This continuous balance between these nucleophilic and electrophilic substances allows the activation of the NRF2/ARE axis, which regulates cellular antioxidant responses against oxidative stress, as well as cell proliferation. Understanding the ambivalent character of polyphenols, which can act simultaneously as antioxidants and pro-oxidants, will allow the design of specific therapies that can serve science and medicine in their tasks.
... The interest in these species is due to their high content of phenolic compounds, which are secondary plant metabolites. In addition, they are well-known for their health protection attributes as anti-inflammatory, antihypertensive, antimicrobial, and anticancer agents [3][4][5]. Furthermore, blueberries can inhibit colon, cervix, prostate, liver, and triple-negative breast cancer growth [3,[6][7][8][9][10][11][12][13][14][15][16][17]. ...
The blueberry fruit of the genus Vaccinium, including high blueberry, low blueberry, and wild bilberry, is consumed for its flavor and medicinal properties. The purpose of the experiments was to investigate the protective effect and mechanism of the interaction of blueberry fruit polyphenol extracts with the erythrocytes and their membranes. The content of polyphenolic compounds in the extracts was determined using the chromatographic UPLC–ESI–MS method. The effects of the extracts on red blood cell shape changes, hemolysis and osmotic resistance were examined. Changes in the order of packing and fluidity of the erythrocyte membrane and the lipid membrane model caused by the extracts were identified using fluorimetric methods. Erythrocyte membrane oxidation was induced by two agents: AAPH compound and UVC radiation. The results show that the tested extracts are a rich source of low molecular weight polyphenols that bind to the polar groups of the erythrocyte membrane, changing the properties of its hydrophilic area. However, they practically do not penetrate the hydrophobic part of the membrane and do not damage its structure. Research results suggest that the components of the extracts can defend the organism against oxidative stress if they are delivered to the organism in the form of dietary supplements.
... The pharmacological effects of these compounds not only reduce uric acid concentrations but also as anti-inflammatory and suppress the formation of free radicals such as superoxide anion and hydrogen peroxide. 57,58 affinity of the enzyme for the substrate. The ratio of the value of Km in the condition of adding the inhibitor and the Km in the condition without the inhibitor will reach the value of α. ...
Introduction: A medicinal plant from Central Kalimantan, Spatholobus littoralis Hassk., with a local name bajakah tampala, has long been used to treat gout or uric acid disease. This study aimed to develop the optimum conditions of xanthine oxidase (XO) activity, phytochemical screening, and to obtain the antigout activity of S. littoralis Hassk. Methods: Before performing the phytochemical screening, we performed a simplicia maceration with water and 70% ethanol solvents. The development of the optimum conditions for XO was carried out using the Response Surface Methodology (RSM) combined Box-Behnken Design (BBD). Toxicity assay (LC50) on both extracts was assessed by BSLT (Brine Shrimp Lethality Test). The two extracts were then evaluated for antigout activity. Results: The yield of 70% ethanol extract (11.24%) was higher than the aqueous extract (7.29%). The phytochemical screening on the simplicia and the two extracts positively contained steroids, flavonoids, saponins, and tannins. The optimum conditions of XO activity were temperature of 20 ℃, pH of 8.0, and xanthine concentration of 1.40 mM. The toxicity of the 70% ethanol extract (LC50 662.25 mg/L) was stronger than the aqueous extract (LC50 774.68 mg/L). Moreover, the 70% ethanol extract (IC50 224.14±8.62 mg/L) showed higher XO inhibition than the water extract (IC50 348.83±4.85 mg/L). Lineweaver-Burk plot analysis showed that 70% ethanol and water extracts inhibited XO competitively with the inhibition constant (KI) of 272.68 mg/L and 378.44 mg/L, respectively. Conclusion: This preliminary study can be a reference that S. littoralis Hassk. is potentially an antigout.
Keywords:Box-Behnken Design, Gout, Lineweaver-Burk plot, Spatholobus littoralis Hassk, Xanthine Oxidase.
... It appears that inhibition was higher when (7) has a methoxy group instead of a hydroxyl group at the 4 -position. These results are in agreement with those reported by Liu, in which some flavonoids have higher inhibitory activity when they are substituted with methoxy groups [26]. Acacetin glycosides (3)(4)(5)(6) showed significantly lower inhibitory activities, between 26.4 and >100 µM, compared with aglycone 7. ...
... It appears that inhibition was higher when (7) has a methoxy group instead of a hydroxyl group at the 4′-position. These results are in agreement with those reported by Liu, in which some flavonoids have higher inhibitory activity when they are substituted with methoxy groups [26]. Acacetin glycosides (3−6) showed significantly lower inhibitory activities, between 26.4 and >100 µ M, compared with aglycone 7. ...
The aerial parts of Agastache rugosa are used as a food material and traditional medicine in Asia. A 50% ethanol extract exhibited potent xanthine oxidase (XO) inhibitory activity (IC50 = 32.4 µg/mL). To investigate the major components responsible for this effect, seven known compounds were identified from A. rugosa; among these, salvianolic acid B (2) was isolated from this plant for the first time. Moreover, acacetin (7) exhibited the most potent inhibitory activity with an IC50 value of 0.58 µM, lower than that of allopurinol (IC50 = 4.2 µM), which is commonly used as a XO inhibitor. Comparative activity screening revealed that the C6-bonded monosaccharides (3) or sugars substituted with acetyl or malonyl groups (4–6) are critical for XO inhibition when converted to aglycone (7). The most potent inhibitor (7) in the A. rugosa extract (ARE) exhibited mixed-type inhibition kinetics and reversible inhibition toward XO. Furthermore, the hydrolysis of ARE almost converted to an inhibitor (7), which displayed the highest efficacy; UPLC-qTof MS revealed an increased content, up to five times more compared with that before treatment. This study will contribute to the enhancement in the industrial value of ARE hydrolysates as a functional ingredient and natural drug toward the management of hyperuricemia and treatment of gout.
