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The discovery of unspecific peroxygenases (UPOs) completely changed the paradigm of enzyme-based oxyfunctionalization reactions, as these enzymes can transform a wide variety of substrates with a relatively simple reaction mechanism. The fact that UPO can exert both peroxygenative and peroxidative activity in either aromatic or aliphatic carbons, represents a great potential in the production of high value-added products from natural antioxidants. In this work, the flavonoid rutin has been considered as possible substrate for UPO from Agrocybe aegerita , and its peroxygenation or its peroxidation and successive oligomerization have been studied. Different experiments were performed in order to reduce the range of process variables involved and gaining insight on the behavior of this enzyme, leading to a multivariable optimization of UPO-based rutin modification. While trying to preserve enzyme activity this optimization aimed for maximizing the production of more soluble antioxidants. Reusability of the enzyme was evaluated recovering UPO using an enzymatic membrane reactor, revealing challenges in enzyme stability due to inactivation during the filtration stages. The influence of the radical scavenger ascorbic acid on product formation was investigated, revealing its role in directing the reaction towards hydroxylated rutin derivatives, hence indicating a shift towards more soluble and bioactive products. [Display omitted] • UPO transforms rutin to more soluble products with enhanced antioxidant activity. • H 2 O 2 feeding rate, initial enzymatic activity and reaction time were optimized. • Peroxygenative and peroxidative activities are crucial to increase both bioactivity and solubility. • A poor stability of the enzyme limits its reuse in successive cycles. • Ascorbic acid concentration allows modulation of the characteristics of the products. [ABSTRACT FROM AUTHOR]

Aim: Rutin is a flavonoid glycoside obtained from the plant Ruta graveolens. It was known to have immunosuppressant activities. This study was focused on effect of rutin against immunoglobulin A (IgA) nephropathy. Methods: IgA nephropathy was induced in Sprague–Dawley rats with various inducing agents described in text. During the later part of the induction phase, rutin was administered. Control group rats did not receive any treatment or inducing agent, induced group rats received only the inducing agents, whereas treatment group received the inducing agents as well as rutin. Results: During the study, various biochemical parameters pertaining to kidney function were evaluated and also, the expression of proteins and cytokines responsible for inflammation and fibrosis were assessed. The effect of rutin in IgA nephropathy was promising as treatment with rutin reduced the deposition of IgA in the glomeruli of rats. Along with this we also tried to establish the probable mechanism of action of rutin and based on the summary of the results it was concluded that rutin reduced the inflammation and fibrosis related to IgA nephropathy by inhibiting the TGF‐β/SMAD pathways and ultimately reducing the expression of α‐smooth muscle actin (α‐SMA). Conclusion: Comprehending all the above consideration, it may be safely said that that rutin alleviated inflammation and also fibrosis mediated by IgA, by suppressing the transforming growth factor‐β (TGF‐β) activities through suppressor of mothers against decapentaplegic pathways and reduced the epithelial‐to‐mesenchymal transition by downregulating the α‐SMA which is a marker for fibrosis. [ABSTRACT FROM AUTHOR]

Vitrification of oocyte has become an important component of assisted reproductive technology and has important implications for animal reproduction and the preservation of biodiversity. However, vitrification adversely affects mitochondrial function and oocyte developmental potential, mainly because of oxidative damage. Rutin is a highly effective antioxidant, but no information is available to the effect of rutin on the mitochondrial function and development in vitrified oocytes. Therefore, we studied the effects of rutin supplementation of vitrification solution on mitochondrial function and developmental competence of ovine germinal vesicle (GV) stage oocytes post vitrification. The results showed that supplementation of vitrification solution with 0.6 mM rutin significantly increased the cleavage rate (71.6 % vs. 59.3 %) and blastocyst rate (18.9 % vs. 6.8 %) compared to GV-stage oocytes in the vitrified group. Then, we analyzed the reactive oxygen species (ROS), glutathione (GSH), mitochondrial activity and membrane potential (ΔΨm), endoplasmic reticulum (ER) Ca2+, and annexin V (AV) of vitrified sheep GV-stage oocytes. Vitrified sheep oocytes exhibited increased levels of ROS and Ca2+, higher rate of AV-positive oocytes, and decreased mitochondrial activity, GSH and ΔΨm levels. However, rutin supplementation in vitrification solution decreased the levels of ROS, Ca2+ and AV-positive oocytes rate, and increased the GSH and ΔΨm levels in vitrified oocytes. Results revealed that rutin restored mitochondrial function, regulated Ca2+ homeostasis and decreased apoptosis potentially caused by mitophagy in oocytes. To understand the mechanism of rutin functions in vitrified GV-stage oocytes in sheep, we analyzed the transcriptome and found that rutin mediated oocytes development and mitochondrial function, mainly by affecting oxidative phosphorylation and the mitophagy pathways. In conclusion, supplementing with 0.6 mM rutin in vitrification solution significantly enhanced developmental potential through improving mitochondrial function and decreased apoptosis potentially caused by mitophagy after vitrification of ovine GV-stage oocytes. • Rutin enhances the developmental capacity of vitrified ovine GV-stage oocytes. • Rutin ameliorates mitochondrial dysfunction in oocytes by reducing ROS levels. • Rutin reduces apoptotic events in vitrified ovine GV-stage oocytes. [ABSTRACT FROM AUTHOR]

Aminoglycoside antibiotics, including gentamicin (GM), induce delayed ototoxic effects such as hearing loss after prolonged use, which results from the death of hair cells. However, the mechanisms underlying the ototoxicity of aminoglycosides warrant further investigation, and there are currently no effective drugs in the clinical setting. Herein, the therapeutic effect of the flavonoid compound rutin against the ototoxic effects of GM in zebrafish hair cells was investigated. Animals incubated with rutin (100–400 µmol/L) were protected against the pernicious effects of GM (200 µmol/L). We found that rutin improves hearing behavior in zebrafish, and rutin was effective in reducing the number of Tunel-positive cells in the neuromasts of the zebrafish lateral line and promoting cell proliferation after exposure to GM. Subsequently, rutin exerted a protective effect against GM-induced cell death in HEI-OC1 cells and could limit the production of cytosolic reactive oxygen species (ROS) and diminish the percentage of apoptotic cells. Additionally, the results of the proteomic analysis revealed that rutin could effectively inhibit the expression of necroptosis and apoptosis related genes. Meanwhile, molecular docking analysis revealed a high linking activity between the molecular docking of rutin and STAT1 proteins. The protection of zebrafish hair cells or HEI-OC1 cells from GM-induced ototoxicity by rutin was attenuated by the introduction of STAT1 activator. Finally, we demonstrated that rutin significantly improves the bacteriostatic effect of GM by in vitro experiments, emphasising its clinical application value. In summary, these results collectively unravel a novel therapeutic role for rutin as an otoprotective drug against the adverse effects of GM. [ABSTRACT FROM AUTHOR]

Jujube leaves are by-products of jujube plants, which contain various flavonoid compounds. The identification and quantification of these flavonoids from 14 cultivars of jujube, cultivated in Cangzhou, Hebei, China was explored in this study. Altogether, nine flavonoids were obtained using ethanol as the extraction solvent and using preparative reversed phase liquid chromatography. The identified nine compounds were quercetin-3-O-robinobioside, rutin, 3′,5′-Di-C-β-D-glucosylphloretin, kaempferol-3-O-rutinoside, quercetin-3-O-rhamnoside, quercetin-3-O-α-L-arabinosyl- (1→2)-α-L-rhamnoside, quercetin-3-O-α-L-rhamnopyranosyl-2″-(6′′′-p-coumaroyl)-β-D-glucoside, 3′,5′-Di-C-β-D-glucosyl-4-O-p-coumaroyl- phloretin, and quercetin-3-O-β-D- glucoside. Among them, three compounds, namely quercetin-3-O-rhamnoside, quercetin-3-O-α-L-rhamnopyranosyl-2″-(6′′′-p-coumaroyl)-β-D-glucoside, and 5′-Di-C-β-D-glucosyl-4-O-p-coumaroyl-phloretin were detected as the novel compounds in jujube leaves from Cangzhou, Hebei, China. All the detected compounds were confirmed through HPLC, LC-MS, 1H-NMR, and 13C-NMR. The quantification analysis through HPLC chromatography revealed that young leaves contained much higher amounts of these compounds than the old counterpart. In terms of dominant major flavonoids, quercetin-3-O-robinobioside, rutin and 3′,5′-Di-C-β-D-glucosylphloretin in young leaves, while quercetin-3-O-robinobioside and rutin in old leaves took the accounts. It is concluded that jujube leaves can be utilized as the source of such flavonoids, which can be used by incorporating such leaves into mainstream food products for the valorization of these underutilized by-products. [ABSTRACT FROM AUTHOR]

Rutin, a flavone glycoside, has shown to have a significant beneficial kidney protection effect in drug-induced nephropathy. However, its poor solubility and low oral bioavailability have limited its pharmacological applications. This study aimed at formulating rutin-loaded bilosomes to enhance the renal protective effect of rutin for oral application. Rutin-loaded bilosomes were developed using thin-film hydration technique. The prepared formulations were characterized by entrapment efficiency percentage (EE%), vesicular size (VS) and zeta potential (ZP) measurement. The developed formula exhibited moderate EE%, ranging from 20.02 ± 2.85 to 48.57 ± 3.57%, suitable VS results that ranged from 502.1 ± 36 to 665.1 ± 45 nm and high ZP values (≤ -41.4 ± 7.27 mV). Transmission electron microscopy revealed the spherical shape of the developed bilosomes. The in-vitro release study revealed prolonged release of rutin from bilosomes, relative to free drug. F2, prepared using the molar ratio span 60: cholesterol: sodium cholate 1:1:0.5, was selected for further investigations as it showed the highest EE%, smallest VS, optimum ZP, and persistent release profile. In-vivo studies were performed on drug-induced nephropathy in rats. Acute renal failure was induced using a single dose of potassium dichromate (PDC; 15 mg/kg; i.p). The selected formulation, F2, alleviated kidney dysfunction, oxidative stress and inflammation via decreasing MDA, TNF-α and TGF-β and increasing GSH. In addition, F2 promoted Akt/PI3K activation against PDC-induced acute renal failure. Histopathology results came in accordance with in-vivo results. Thus, bilosomes could be considered a potential delivery system for enhancing the oral delivery and kidney protection activity of rutin. [ABSTRACT FROM AUTHOR]

Background: The research is aimed at exploring the potential of marigold petal tea (MPT), rich in polyphenol contents, against oxidative stress and obesity in a rat model following a high‐fat‐sugar diet (HFSD). Methods: The MPT was prepared through the customary method of decoction and was subjected to analysis for its polyphenol composition using reversed‐phase high‐performance liquid chromatography (RP‐HPLC). Two specific doses of MPT, namely, 250 and 500 mg/kg body weight (BW), were chosen for the study—referred to as MPT‐250 and MPT‐500, respectively. Result: The main phenolic acids and flavonoids identified in MPT, with concentrations exceeding 10 mg/100 mL of tea, included catechin, rutin, salicylic acid, gallic acid, sinapic acid, chlorogenic acid, cinnamic acid, and ellagic acid. The total phenolic (TP) and total flavonoid (TF) contents in MPT were measured to be 5.53 and 7.73 mg/g, respectively. Additionally, MPT demonstrated a 57.2% scavenging capacity with 2,2‐diphenyl‐1‐picrylhydrazyl radical. Notably, the administration of a higher dose (MPT‐500) showed a significant reduction in body mass index (BMI) and a 51.24% reduction in the rate of increase in BW compared to the HFSD group. The findings indicated that all the treatment groups, that is, orlistat treatment (OT), MPT‐250, and MPT‐500 groups, experienced reduced levels of serum total cholesterol (TC), triglyceride (TG), and markers of lipoproteins in contrast to the HFSD group. Moreover, MPT helped restore the levels of malondialdehyde (MDA), superoxide dismutase (SOD), and reduced glutathione (GSH), thereby demonstrating its potential in combating oxidative stress. The MPT‐500 group also displayed decreased liver and kidney weights and an improved atherogenic index when compared to the HFSD group. Conclusion: The results clearly indicate that a high dosage of MPT showed antiobesity activity which was comparable to the same effects produced by the conventional drug orlistat. [ABSTRACT FROM AUTHOR]

Hemerocallis citrina Borani is a traditional folk food used to promote the lactation of postpartum mothers in China; however, the active ingredients and corresponding mechanisms are still unknown. In this study, the lactogenic effect of alcoholic and aqueous extracts of H. citrina was primarily evaluated, and the aqueous extract (1,000 and 2,000 mg/kg) displayed significant lactationpromoting effects. Three eluates of the aqueous extract (0%, 30%, and 50%HCW) were further evaluated for their lactogenic effect, and 30% and 50%HCWshowed significant lactation-promoting activity. Nineteen ingredients, including those with a high content of rutin and isoquercetin, were then identified from 30% and 50%HCW using the ultra-performance liquid chromatography-quadrupole-time-of-flight-mass spectrometry (UPLC-Q-TOF-MS) method. Finally, the lactogenic effect of rutin and isoquercetin was evaluated, and both compounds displayed significant lactation-promoting activity. The mechanisms relative to the lactation-promoting active ingredients for H. citrina extracts and compounds are to stimulate the release of prolactin (PRL) and progesterone (P), as well as to induce the expression of prolactin receptor (PRLR) and improve the morphology of mammary tissue. This study first clarified the lactation-promoting active ingredients of H. citrina and the corresponding mechanisms, which provide a new insight into the new lactation-promoting drug and promote the high-value utilization of H. citrina resources. [ABSTRACT FROM AUTHOR]

Background/Objectives: An extract of calyces from Physalis peruviana with hypoglycemic activity is being considered as a potential herbal medicine. Preclinical pharmacokinetics (PK) studies of the extract in rats, focusing on plasma concentrations of its main compound, rutin, and its metabolites, revealed PK interactions in the extract matrix that improved the absorption of rutin metabolites compared to the pure compound, among other PK effects. This research aimed to study the PK of rutin alone and in the extract and assess potential PK interactions in the extract matrix on the flavonoid and its metabolites in rabbits, a nonrodent species; Methods: Animals received pure rutin or extract orally and intravenously. The PK analysis used noncompartmental and population pharmacokinetics (popPK) methods, and simple allometry was applied to predict human PK parameters; Results: The rutin concentration–time profile fit a two-compartment model with first-order elimination, while its metabolites fit a double first-order absorption model. The extract matrix led to increased absorption, distribution, and elimination of rutin as well as increased bioavailability of its metabolites in rabbits; Conclusions: The popPK model defined the equations for PK parameters describing these findings, and the increased volume of distribution and clearance of rutin was maintained in human predictions. These results will support the development of a new herbal medicine. [ABSTRACT FROM AUTHOR]

Amyotrophic lateral sclerosis (ALS) is a neurodegenerative disorder characterized by the progressive loss of motor neurons, with limited effective treatments. Recently, the exploration of natural products has unveiled their potential in exerting neuroprotective effects, offering a promising avenue for ALS therapy. In this study, the therapeutic effects of rutin, a natural flavonoid glycoside with neuroprotective properties, were evaluated in a superoxide dismutase 1 (SOD1)-G93A mouse model of ALS. We showed that rutin reduced the level of SOD1 aggregation and diminished glial cell activation in spinal cords and brainstems, resulting in significantly improved motor function and motor neuron restoration in SOD1-G93A mice. Our findings indicated that rutin's multi-targeted approach to SOD1-related pathology makes it a promising candidate for the treatment of ALS. [ABSTRACT FROM AUTHOR]

In this study, we focus on exploring the medicinal potential of Olea Europaea L., a commonly used plant with diverse indigenous medicinal applications. The main aim is to identify promising phytoconstituents from Olea Europaea L. leaves that can act as inhibitors for the PTP-1B target, utilizing an in silico approach. The phytoconstituents were sourced from the IMMPAT database, and molecular docking was employed to assess their binding affinities. The docking results revealed that rutin (−10.05 kcal/mol) and quercetin (−8.28 kcal/mol) displayed the highest binding scores against PTP-1B, outperforming reference compounds. Furthermore, MM-GBSA calculations indicated favorable free binding energy. To ensure stability, 200 ns Molecular Dynamics simulations were conducted on the 2QBS-Rutin complex. The results revealed that the 2QBS-Rutin complex showed stable conformation throughout the simulation, maintaining consistency with RMSD values below 1 Å. This study highlights rutin and quercetin as promising phytoconstituents from Olea Europaea L. leaves, demonstrating potent-binding affinities against PTP-1B inhibitors. In this current study, the phytoconstituents of Olea Europaea L, leaves were screened against PTP-1B inhibitory activity by in-silico approach. ADMET properties of the phytoconstituents were found to be acceptable and MM-GBSA calculations showed favourable free binding energy. The phytoconstituents Rutin and Quercetin were emerged as promising hit molecules from Olea Europaea L leaves, showing potential binding affinities against PTP-1B inhibitors. In silico analyses were predicted for all the phytoconstituents in order to assess safety and efficacy under the various models revealing promising results. Molecular Dynamics simulations were conducted for 200 ns on the ligand-protein complexes and found to be stable through out the simulation period. [ABSTRACT FROM AUTHOR]

Bain damage caused by Toxoplasma gondii (T. gondii) is associated with increased inflammatory response and oxidative stress. Rutin, a natural product extracted from tobacco leaves and tomatoes, has excellent anti-inflammatory and antioxidant properties in vivo, but its ameliorative effect on T. gondii infection-induced brain tissue damage remain unknown. In this study, mice were acutely infected with RH virulent strains of T. gondii, then treated with 0–50 mg/kg of Rutin. Results showed that Rutin significantly reduced the number of abnormal morphological neurons in the hippocampal region of brain tissue, decreased the concentration of Iba-1, the biomarker of microglia which indicates increased tissue damage and inflammation in the brain; decreased the level of inflammatory factors (TNF-α, IL-6 and IL-1β) in serum and increased the content of antioxidant enzymes (GSH and SOD) in brain tissue; and decreased the enrichment of oxidation products MDA. Results showed significant downregulation of key proteins in the two inflammation-related pathways, TLRs/NF-κB, P2X7R/NLRP3. While the proteins in the antioxidant-related pathways were noticeably upregulated in the T. gondii-infected brain tissue with Rutin treatment. These findings suggest that Rutin ameliorates T. gondii-induced brain tissue damage, may involving in inhibiting the TLRs/NF-κB and P2X7R/NLRP3 inflammatory signaling pathways, and activating the PI3K/AKT/Nrf2/HO-1 antioxidant pathway. The findings could provide some theoretical support for Rutin's potential therapeutic use in treating T. gondii-related brain damage in the future. [ABSTRACT FROM AUTHOR]

Buckwheat, a pseudo cereal, is a potent super-food crop known as a life support system in higher Himalayas. During field survey, it was reported by local people that long time consumption of buckwheat leaves and grains leads to digestive problems and numbness. Twelve buckwheat genotypes were collected from different regions of Himalayas and changes in phytoconstituents due to roasting of grains at 80 ℃ for 5 min., were analysed spectrophotometrically, to make it suitable for human consumption on daily basis. Roasting slightly decreased protein (2.98–18.52%), lysine (3.82–7.76%), arginine (1.61–6.03%), tryptophan (2.40–7.73%), phenols (6.18–14.17%), flavonoids (6.01–18.27%), antioxidants(3.38–9.23%), rutin (1.69–7.51%), whereas, anti-nutrients viz. phytic acid, tannin and oxalate were decreased significantly (p < 0.05) i.e. (17.50–44.15%), (2.27–6.25%) and (9.52–25.00%) respectively. Dodecyl Sulfate Polyacrylamide gel electrophoresis analysis of raw grain samples of buckwheat cultivars revealed distinct protein bands with molecular wt. ranging from 115.77 to 19.06 kDa. Allergenic protein of 100 kDa, 50 kDa and 24 kDa were found in the buckwheat grains of Indian Himalayan region. Sharp decrease of protein solubility and content of allergenic proteins was noticed in the buckwheat grains by raising the temperature beyond 60 °C. It may be concluded from the study that roasting make buckwheat grains more suitable from nutritional point of view and may be used for daily consumption, but reduction of nutrient loss by roasting and removal/reduction of 24-kDa allergenic protein is the thrust area for future research. [ABSTRACT FROM AUTHOR]

Rutin, a natural bioflavonoid compound, is one of the best-known antioxidants. This study aimed to investigate the protective effect of rutin-loaded chitosan alginate nanoparticles (RCA NPs) against lead (Pb)-induced oxidative stress in two different broiler breeds. A total number of 240 chicks from Cobb (CB) and Arbor Acres (AR) breeds were randomly allocated into 4 groups/breed. The 1st group received standard basal diet (SD) and drinking water (DW) while the 2nd group received SD and Pb-incorporated DW (350 mg/L). The 3rd group treated with both rutin-supplemented SD (50 mg/kg feed), and DW contain Pb (350 mg/L). Finally, the 4th group administered RCA NPs-supplemented SD (50 mg/kg feed) and Pb-incorporated DW (350 mg/L). On the 40th day of experiment, broilers weighed, and blood samples collected for biochemical and hematological analysis then slaughtered. Economic efficiency, growth performance, and oxidative stress biomarkers were evaluated. Gene expression level of growth-associated genes as insulin-like growth factor-I (IGF-1) and histopathological changes were assessed in liver and intestinal tissue of both breeds. Our results revealed that Pb-treated birds exhibited the lowest average body weight gain (BWG) and economic efficiency measures in both breeds while RCA NPs-treated groups revealed enhanced growth and economic performance. Furthermore, diet supplementation with RCA NPs considerably enhanced the antioxidant enzymes activity and expression of growth-associated genes than groups treated with rutin alone specifically in AR breed. In conclusion, RCA NPs supplementation could be a promising nanoformulation in poultry production through enhancing the antioxidant capacity and bioavailability of rutin. [ABSTRACT FROM AUTHOR]

AbstractThe nutraceutical and biological potential of Annona atemoya, a fruiting plant, has been reported. We and others have demonstrated that A. atemoya leaf extract (AAL) has various pharmacological properties, such as antioxidant, antimicrobial, and neuroprotective effects. However, knowledge about the safety and potential toxicity of AAL remains limited. We aimed to assess the potential toxicity of AAL using acute and repeated subacute oral toxicity tests in rats. In both acute and repeated subacute toxicity test, no AAL-related behavioral abnormalities or changes in mortality, food intake, body weight were observed up to a dosage of 2000 mg/kg, indicating that the median lethal dose of AAL is higher than 2000 mg/kg. In subacute toxicity tests, no significant changes in hematological and biochemical parameters, urinalysis results, and histopathological variables were observed. Therefore, the no-observed-adverse-effect level (NOAEL) of orally administered AAL was estimated to be 2000 mg/kg/day in male and female rats. We also examined the effect of AAL on the inflammatory reaction in lipopolysaccharide (LPS)-stimulated BV-2 cells. AAL treatment significantly inhibited the LPS-stimulated increases in the levels of nitric oxide (NO) and inflammatory cytokines, implying that AAL has an anti-inflammatory effect. Quality control analysis revealed that two marker compounds, rutin and isoquercitrin, were present at 27.570 and 4.322 mg/g, respectively, in a freeze-dried AAL sample and were completely eluted within 27 min. The extraction recovery was 99.47–103.80%, and the precision was ≤2.79%. Overall, these findings suggest the safety, anti-inflammatory activity, and standardization of AAL. [ABSTRACT FROM AUTHOR]

Herein, a micro‐solid‐phase extraction (μSPE) method was developed using a pipette tip for rutin extraction, employing activated hollow carbon nanospheres (HCNSs) as the sorbent. Characterization of the activated carbon nanospheres through TGA, FTIR, and SEM analysis confirmed the success of the activation process. The study demonstrated the efficacy of PT‐μSPE in rutin extraction under pH 2 conditions with a standard concentration of 2 mg·L−1. The optimal mass of HCNSs was found to be 2 mg, and a loading volume of 500 μL resulted in the maximum recovery of rutin. Propan‐2‐ol was the best elution solvent with 15 aspirating/dispensing cycles. The correlation of determination (R2) for the calibration curve was found to be 0.9991, and the LOD and LOQ values were 0.604 and 1.830 mg·L−1, respectively. The applicability of the method was demonstrated by extracting rutin from a complex Moringa oleifera leaf extract with the relative standard deviation (RSD) of 3.26%, thereby validating this method as feasible for the extraction of useful bioactive compounds from complex plant samples. [ABSTRACT FROM AUTHOR]

[Display omitted] • Rutin (Ru), an antioxidant flavonoid, is prevalent in plant-based human diets. • Ru/MnO 2 was synthesized using a straightforward, rapid one-step process. • Ru/MnO 2 exhibits significantly higher T 1 relaxivity than previously reported MnO 2. • Ru/MnO 2 can target glucose transporters (GLUTs) overexpressed in various tumors. • Ru/MnO 2 shows promise in MRI and photothermal therapy of malignant tumors. Manganese oxide nanoparticles (MONs)-based contrast agents have attracted increasing attention for magnetic resonance imaging (MRI), attributed to their good biocompatibility and advantageous paramagnetism. However, conventional MONs have poor imaging performance due to low T 1 relaxivity. Additionally, their lack of tumor-targeting theranostics capabilities and complex synthesis pathways have impeded clinical applications. Rutin (Ru) is an ideal tumor-targeted ligand that targets glucose transporters (GLUTs) overexpressed in various malignant tumors, and exhibits photothermal effects upon chelation with metal ions. Herein, a series of Ru-coated MONs (Ru/MnO 2) were synthesized using a straightforward, rapid one-step process. Specifically, Ru/MnO 2 -5, with the smallest crystal size of approximately 4 nm, exhibits the highest T 1 relaxivity (33.3 mM-1s−1 at 1.5 T, surpassing prior MONs) along with notable stability, photothermal efficacy, and tumor-targeting ability. Furthermore, Ru/MnO 2 -5 shows promise in MRI and photothermal therapy of H22 tumors owing to its superior GLUTs-mediated tumor-targeting capability. [ABSTRACT FROM AUTHOR]

Rutin is a natural flavonoid compound that is widely found in a variety of plants and has a variety of biological effects, including anti-inflammatory, antioxidant, and anti-tumor effects. Rutin has been shown to have anti-tumor effects in a variety of cancers, but its effects on gastric cancer need to be further explored. The aim of this study was to explore the effects of Rutin on gastric cancer cells and the potential molecular regulatory mechanisms. Gastric cancer cells (AGS and MGC803) were treated with different concentrations of Rutin. Cell proliferation, apoptosis, migration, and invasion were determined by MTT, flow cytometry, scratch assay, and Transwell analysis, respectively. Cell epithelial mesenchymal transition (EMT) markers and Wnt/β-catenin pathway were analyzed by RT-qPCR and western blot assay. The results showed that Rutin significantly inhibited the proliferation, migration and invasion ability of gastric cancer cells, induced apoptosis, and suppressed the EMT process. Further experiments revealed that Rutin achieved the effect of inhibiting the biological behavior of gastric cancer cells by suppressing the activation of the Wnt/β-catenin pathway. Therefore, Rutin may become a potential therapeutic candidate for gastric cancer. [ABSTRACT FROM AUTHOR]

Rutin, a flavonoid phytochemical compound, plays a vital role in human health. It is used in treating capillary fragility and has anti-Alzheimer, anti-inflammatory, and antioxidant effects. In this study, Ti-Mo-Ni-O nanotubes (NTs) were used, for the first time, in an unprecedented plant biotechnology application, wherein in vitro Philodendron shoots (Philodendron erubescens) known as "Imperial Red" were targeted for rutin accumulation. The antioxidant responses and the accumulation of rutin were evaluated in treated Philodendron erubescens (P. erubescens) shoots using 5.0 mg/L of Ti-Mo-Ni-O NTs. The total phenolic content and total flavonoid content were estimated, and an ABTS+ assay, FRAP assay, and iron metal chelation assay were performed. The application of Ti-Mo-Ni-O NTs enhanced the rutin content considerably from 0.02 mg/g to 2.96 mg/g for dry-weight shootlet extracts. Therefore, the use of Ti-Mo-Ni-O NTs is proposed to be a superior alternative to elevate the rutin content. The aim of the current study is to target P. erubescens shoots grown in vitro for the accumulation of rutin compounds using Ti-Mo-Ni-O NT powder, to determine the quantitative and qualitative accumulation of rutin via HPLC–DAD analysis, and to estimate the antioxidant activity of P. erubescens shoot extract. This study presents a novel methodology for utilizing nano-biotechnology in the synthesis of plant secondary metabolites. [ABSTRACT FROM AUTHOR]

Objective To develop a high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method for simultaneous determination of five flavonoids in Ganmao’an granules (GMA). Methods Chromatographic separation was achieved on a Kromasil C18 Column (150 mm× 4.6 mm,5 μm,100 Å), which was eluted with methanol (A) -0.1% formic acid (B) at the flow rate of 1.0 ml/min. The gradient condition was as follows: 0-20 min, 35% A, and 20-40 min, 45% A. The column temperature was 25 °C. Analytes were detected using a triple quadrupole tandem mass spectrometer equipped with an electrospray ionization source in the negative ion scanning. The multiple reaction monitoring mode was used for qualitative analysis. For each flavonoid, two precursor ion/product ion transitions were chosen: lutin m/z 609.1→300.1, hyperin and isoquercitrin m/z 463.0→300.1, quercetin m/z 301.0→151.0, luteolin m/z 285.0→132.9. Results Five flavonoids showed the good relationships within their own concentration ranges (correlation coefficient r>0.999 1), whose average recoveries were in the range of 100.63%-102.81% with RSDs of 0.67%-2.07%. The content results of rutin, hyperoside, isoquercetin, quercetin, and luteolin in 10 batches of GMA were 32.23-479.83, 0.291-1.825, 11.44-20.54, 6.32-18.41, 3.46-6.51 μg/g, respectively. Conclusion The results indicated that the developed method was sensitive, accurate and could provide excellent specificity for simultaneous determination of five flavonoids in GMA. [ABSTRACT FROM AUTHOR]

Buckwheat and other grains have become influential in sustainable agriculture and food security owing to climate change. However, subpar storage conditions can result in the deterioration of the nutritional value and active components of buckwheat, making storage quality a significant research subject. This study examined common buckwheat (CB) and Tartary buckwheat (TB) stored at 4 °C, 30 °C, and 55 °C from 0 to 6 months to assess storage quality and its relationship to the preservation of active components. The results of agglomerative hierarchical clustering (AHC) and principal component analysis (PCA) showed that as storage temperature and time increased, both CB and TB exhibited the following differences: significant alterations in color due to an increase in browning index (B.I.), higher acidity from accelerated acid production at high temperatures, and a decrease in total phenolics, flavonoid content, and antioxidant capacity due to thermal degradation of functional components. In the storage quality assessment, no alteration in microstructure or degradation in components was detected after exposure to all times and temperatures, and the content of the primary bioactive compound, rutin, was CB (16.57–27.81 mg/100 g d.w.) and TB (707.70–787.58 mg/100 g d.w.), demonstrating buckwheat's resistance to microbial contamination. Storage temperature significantly impacts buckwheat's quality and bioactive components, making it an important element in establishing a sustainable food supply chain. [ABSTRACT FROM AUTHOR]

Simple Summary: Phytochemicals are used against drug-resistant bacterial strains. In this work, diabetic mice with excision wounds infected with multidrug-resistant (MDR)-P. aeruginosa were used. The antibacterial, antibiofilm, and wound-healing properties of rutin and quercetin were studied. The broth dilution and crystal violet assay were used to investigate the antibacterial and antibiofilm activities in vitro, respectively. At higher concentrations, quercetin and rutin showed promise against MDR-P. aeruginosa. By inhibiting biofilm from the injured tissue, both phytochemicals aided in the healing of diabetic wounds by preventing the formation of biofilm in vitro. Compared to rutin, quercetin had an impact on accelerating wound healing and promoting epithelial layer regeneration. When combined with gentamicin, both phytochemicals were found to be more successful in regulating biofilm and wound-healing processes. The research validates the conventional application of phytochemicals possessing antibacterial, antibiofilm, and wound-healing properties for the treatment of diabetic infections. Phytochemicals are effective and are gaining attention in fighting against drug-resistant bacterial strains. In the present study, rutin and quercetin were tested for antibacterial, antibiofilm, and wound healing activities on excision wounds infected with MDR-P. aeruginosa in diabetic mice. Antibacterial and antibiofilm activities were studied in vitro using broth dilution assay and crystal violet assay, respectively. These phytochemicals were tested alone for wound-healing activities at different concentrations (0.5% and 1% in ointment base) and in combination with gentamicin to evaluate any additive effects. Rutin and quercetin demonstrated effectiveness against MDR-P. aeruginosa at higher concentrations. Both phytochemicals inhibited biofilm formation in vitro and contributed to the healing of diabetic wounds by eradicating biofilm in the wounded tissue. Rutin at a low concentration (0.5%) had a lesser effect on reducing the epithelization period and regeneration of the epithelial layer compared to quercetin. When combined with gentamicin, quercetin (1%) displayed the maximum effect on epithelium regeneration, followed by rutin (1%) in combination with gentamicin. Both phytochemicals were found to be more effective in controlling biofilm and wound-healing activities when used as an additive with gentamicin. The study supports the traditional use of phytochemicals with antibacterial, antibiofilm, and wound-healing activities in managing diabetic infections. [ABSTRACT FROM AUTHOR]

Background: The vulnerability of buffalo sperm to cryoinjury necessitates the improvement of sperm cryo‐resistance as a critical strategy for the widespread use of assisted reproductive technologies in buffalo. Objectives: The main aim of the present study was to evaluate the effects of different concentrations of rutin and chlorogenic acid (CGA) on buffalo semen quality, antioxidant activity and fertility during cryopreservation. Methods: The semen was collected and pooled from the 3 buffaloes using an artificial vagina (18 ejaculations). The pooled sperm were divided into nine different groups: control (Tris‐based extender); 0.4, 0.6, 0.8 and 1 mM rutin (rutin + Tris‐based extender); and 50, 100, 150 and 200 µM CGG (CGA + Tris‐based extender). Sperm kinematics, viability, hypo‐osmotic swelling test, mitochondrial activity, antioxidant activities and malondialdehyde (MDA) concentration of frozen and thawed buffalo sperm were evaluated. In addition, 48 buffalo were finally inseminated, and pregnancy was rectally determined 1 month after insemination. Results: Compared to the control group, adding R‐0.4, R‐0.6, CGA‐100 and CGA‐150 can improve total and progressive motility, motility characteristics, viability, PMF and DNA damage in buffalo sperm. In addition, the results showed that R‐0.4, R‐0.6, CGA‐50, CGA‐100 and CGA‐150 increased total antioxidant capacity, catalase, glutathione peroxidase and glutathione activities and decreased MDA levels compared to the control group. Furthermore, it has been shown that adding 150 µM CGA and 0.6 mM rutin to an extender can increase in vivo fertility compared to the control group. Conclusions: In conclusion, adding rutin and CGA to the extender improves membrane stability and in vivo fertility of buffalo sperm by reducing oxidative stress. [ABSTRACT FROM AUTHOR]

In this study, we developed a facile and low-cost method to prepare a modified electrode by coating the pencil graphite electrode (PGE) surface with 8-nitroquinoline (8-NQ). The surface modification process was carried out by electrochemical reduction of 8-NQ on the PGE surface in ethanol solution. The optimum conditions were determined for the experimental studies. The differential pulse voltammetry was used to determine rutin with the modified electrode (8-NQ/PGE). The developed electrode showed excellent performance for rutin oxidation in a pH 3.0 Britton Robinson buffer (BR). In this media, linearly increasing anodic peak currents were observed with the concentration of rutin in two wide concentration ranges (i.e., 0.016–0.96 μM and 0.96‒19.73 μM), the sensor showed a low detection limit (i.e., 4.14 nM) (3 s m−1). It displayed good stability and selectivity. Also, it was used successfully for the determination of rutin in orange juice samples. [ABSTRACT FROM AUTHOR]

The aim of this study was to evaluate the impact of ethanol extracts from sea buckthorn and Cornelian cherry fruits and leaves on physiology of gastrointestinal tract cells. We used three cell lines relevant to the types of cells, which are exposed to bioactive compounds after oral administration, namely intestinal absorptive cells (Caco-2/HT-29 MTX model), hepatocytes (HepG2 cells) and immunocompetent cells (RAW 264.7 and P388D1 monocytes). The contents of antioxidant and bioactive polyphenols, such as cinnamic, caffeic and p-coumaric acids, rutin, myricetin, resveratrol, quercetin, apigenin and kaempferol, were assessed in the extracts using HPLC chromatography. The application of the extracts to Caco-2/HT-29-MTX cultures increased enterocyte differentiation markers (alkaline phosphatase and villin1 level) and goblet cell markers (mucins) over a fortnight. The extracts reduced lipid droplet size in hepatocytes challenged with hyperglycaemic glucose concentration, insulin and palmitate. Sea buckthorn leaf, fruit and Cornelian cherry leaf extracts blocked oxidative burst in the PMA-stimulated monocytes, while the sea buckthorn leaf and Cornelian cherry fruit extracts downregulated lipopolysaccharide-induced NO and IL-1β, respectively. The results indicate that the tested extracts modulate the behaviour of cells in the gastrointestinal tract in a beneficial way, especially regarding lipid accumulation and innate immunity actions. [ABSTRACT FROM AUTHOR]

This paper concerns the evaluation of the antioxidant activity (AA) of extracts obtained from cistus herbs grown in Albania and Turkey. The extracts were prepared in a Soxhlet apparatus, as well as by the maceration and infusion methods, similar to the home method of preparing herbal teas. AA was determined using the DPPH (2,2′-diphenyl-1-picrylhydrazyl), ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), FRAP (ferric reducing antioxidant power) and β-carotene methods. It was proven that the AA of extracts depends not only on the extraction technique and AA assessment method but also on the place of plant cultivation. The smallest activity was determined using the β-carotene bleaching method, while the highest values were obtained using the FRAP method. On the other hand, the ABTS method showed a greater activity of the Albanian herb prepared using the Soxhlet technique. In addition, the antioxidant properties of extracts were compared with those of rutin standard solutions, showing that this characteristic component of cistus is not the only one that determines AA of extracts. As a result, the rutin content is not an indicator of the antioxidant properties of extracts. The other polyphenolic compounds, although occurring at lower concentration levels compared to rutin, modify the resultant AA of extracts. These studies confirmed the biological activity of cistus as a valuable source of polyphenolic compounds in the human diet. [ABSTRACT FROM AUTHOR]

Abstract Rutin, a flavone glycoside, has shown to have a significant beneficial kidney protection effect in drug-induced nephropathy. However, its poor solubility and low oral bioavailability have limited its pharmacological applications. This study aimed at formulating rutin-loaded bilosomes to enhance the renal protective effect of rutin for oral application. Rutin-loaded bilosomes were developed using thin-film hydration technique. The prepared formulations were characterized by entrapment efficiency percentage (EE%), vesicular size (VS) and zeta potential (ZP) measurement. The developed formula exhibited moderate EE%, ranging from 20.02 ± 2.85 to 48.57 ± 3.57%, suitable VS results that ranged from 502.1 ± 36 to 665.1 ± 45 nm and high ZP values (≤ -41.4 ± 7.27 mV). Transmission electron microscopy revealed the spherical shape of the developed bilosomes. The in-vitro release study revealed prolonged release of rutin from bilosomes, relative to free drug. F2, prepared using the molar ratio span 60: cholesterol: sodium cholate 1:1:0.5, was selected for further investigations as it showed the highest EE%, smallest VS, optimum ZP, and persistent release profile. In-vivo studies were performed on drug-induced nephropathy in rats. Acute renal failure was induced using a single dose of potassium dichromate (PDC; 15 mg/kg; i.p). The selected formulation, F2, alleviated kidney dysfunction, oxidative stress and inflammation via decreasing MDA, TNF-α and TGF-β and increasing GSH. In addition, F2 promoted Akt/PI3K activation against PDC-induced acute renal failure. Histopathology results came in accordance with in-vivo results. Thus, bilosomes could be considered a potential delivery system for enhancing the oral delivery and kidney protection activity of rutin.

Background and objectives: Rutin is a lipophilic natural flavonoid. It is found in vegetables, citrus fruits, and beverages. This study aims to evaluate rutin metabolic pathways in human senescent stromal cells. Methods: Data are extracted from the Gene Expression Omnibus (GEO) database and pre-evaluated via GEO2R to find the significant differentially expressed genes (DEGs). The significant DEGs were assessed via protein-protein interaction PPI network analysis to explore the hub genes. The hubs were screened via directed PPI to find the critical DEGs. Results: Data were assessed via volcano plot, Uniform Manifold Approximation and Projection (UMAP) plot, and Venn diagram. A total number of 9124 significant DEGs were analyzed to determine 33 upregulated and 61 downregulated hubs. The identified hubs were investigated via directed PPI and Il1B. ICAM1, CCL2, EGF, CXCL8, PTGS2, CAMK2B, CCN2, VCAM1, ELN, CXCL12, BGN, and TLR4 were pointed out as critical hub genes. Conclusion: Il1B, CCL2, GNAO1, ICAM1, EGF, and CXCL8 appeared as controller genes affected by rutin while PTGS2 and CAMK2B were the most controlled individuals. The finding refers to the significant advantages of the rutin effect on the function of treated cells. These advantages are corresponded to the usefulness of rutin as an herbal drug candidate. However, more investigations are required to decrease its side effects.

Buckwheat and other grains have become influential in sustainable agriculture and food security owing to climate change. However, subpar storage conditions can result in the deterioration of the nutritional value and active components of buckwheat, making storage quality a significant research subject. This study examined common buckwheat (CB) and Tartary buckwheat (TB) stored at 4 °C, 30 °C, and 55 °C from 0 to 6 months to assess storage quality and its relationship to the preservation of active components. The results of agglomerative hierarchical clustering (AHC) and principal component analysis (PCA) showed that as storage temperature and time increased, both CB and TB exhibited the following differences: significant alterations in color due to an increase in browning index (B.I.), higher acidity from accelerated acid production at high temperatures, and a decrease in total phenolics, flavonoid content, and antioxidant capacity due to thermal degradation of functional components. In the storage quality assessment, no alteration in microstructure or degradation in components was detected after exposure to all times and temperatures, and the content of the primary bioactive compound, rutin, was CB (16.57–27.81 mg/100 g d.w.) and TB (707.70–787.58 mg/100 g d.w.), demonstrating buckwheat’s resistance to microbial contamination. Storage temperature significantly impacts buckwheat’s quality and bioactive components, making it an important element in establishing a sustainable food supply chain.

Abstract Rutin is a natural flavonoid compound that is widely found in a variety of plants and has a variety of biological effects, including anti-inflammatory, antioxidant, and anti-tumor effects. Rutin has been shown to have anti-tumor effects in a variety of cancers, but its effects on gastric cancer need to be further explored. The aim of this study was to explore the effects of Rutin on gastric cancer cells and the potential molecular regulatory mechanisms. Gastric cancer cells (AGS and MGC803) were treated with different concentrations of Rutin. Cell proliferation, apoptosis, migration, and invasion were determined by MTT, flow cytometry, scratch assay, and Transwell analysis, respectively. Cell epithelial mesenchymal transition (EMT) markers and Wnt/β-catenin pathway were analyzed by RT-qPCR and western blot assay. The results showed that Rutin significantly inhibited the proliferation, migration and invasion ability of gastric cancer cells, induced apoptosis, and suppressed the EMT process. Further experiments revealed that Rutin achieved the effect of inhibiting the biological behavior of gastric cancer cells by suppressing the activation of the Wnt/β-catenin pathway. Therefore, Rutin may become a potential therapeutic candidate for gastric cancer.

Abstract Tyrosinase is a binuclear copper-containing enzyme that catalyzes the conversation of monophenols to diphenols via o-hydroxylation and then the oxidation of o-diphenols to o-quinones which is profoundly linked to eukaryotic melanin synthesis and fruits browning. The hyperpigmentation due to unusual tyrosinase activity has gained growing health concern. Plants and their metabolites are considered promising and effective sources for potent antityrosinase enzymes. Hence, searching for potent, specific tyrosinase inhibitor from different plant extracts is an alternative approach in regulating overproduction of tyrosinase. Among the tested extracts, the hydro-alcoholic extract of Moringa oleifera L. leaves displayed the potent anti-tyrosinase activity (IC50 = 98.93 µg/ml) in a dose-dependent manner using L-DOPA as substrate; however, the kojic acid showed IC50 of 88.92 µg/ml. The tyrosinase-diphenolase (TYR-Di) kinetic analysis revealed mixed inhibition type for the Ocimum basilicum L. and Artemisia annua L. extracts, while the Coriandrum sativum L. extract displayed a non-competitive type of inhibition. Interestingly, the extract of Moringa oleifera L. leaves exhibited a competitive inhibition, low inhibition constant of free enzyme ( $${\text{K}}_{\text{ii}}^{\text{app}}$$ K ii app ) value and no Pan-Assay Interfering Substances, hinting the presence of strong potent inhibitors. The major putative antityrosinase compound in the extract was resolved, and chemically identified as rutin based on various spectroscopic analyses using UV–Vis, FTIR, mass spectrometry, and 1H NMR. The in silico computational molecular docking has been performed using rutin and A. bisporus tyrosinase (PDB code: 2Y9X). The binding energy of the predicted interaction between tropolone native ligand, kojic acid, and rutin against 2Y9X was respectively − 5.28, − 4.69, and − 7.75 kcal/mol. The docking simulation results revealed the reliable binding of rutin to the amino acid residues (ASN260, HIS259, SER282) in the tyrosinase catalytic site. Based on the developed results, rutin extracted from M. oleifera L. leaves has the capability to be powerful anti-pigment agent with a potential application in cosmeceutical area. In vivo studies are required to unravel the safety and efficiency of rutin as antityrosinase compound.

Ehretia asperula Zoll. & Moritzi was a common medicinal herb found in several Asian nations. This herb was found in many provinces in northern Vietnam, especially Hoa Binh province. Leaves of E. asperula cultivated in Tay Ninh Province were used to isolate compounds and evaluate their potential as antioxidants by five methods, including TAC, RP, FRAP, DPPH, and ABTS•+. Seven compounds were isolated and elucidated from the ethyl acetate fraction, including kaempferol (1), astragalin (2), nicotiflorin (3), rutin (4), caffeic acid (5), (-)-loliolide (6), and daucosterol (7), where compounds 1, 4, 6, and 7 were found from this species for the first time. All isolated compounds from E. asperula leaves exhibited antioxidant activity, consisting of 5.70 ± 0.01 to 299.13 ± 10.19 μg/mL for EC50 values. Especially compound 5 had a very strong antioxidant effect based on five methods TAC (EC50 = 8.43 ± 0.15 μg/mL), RP (EC50 = 6.79 ± 003 μg/mL), FRAP (EC50 = 12.72 ± 006 μg/mL), DPPH (EC50 = 5.57 ± 0.02 µg/mL), and ABTS•+ (EC50 = 5.70 ± 0.01 μg/mL). From our results, Tay Ninh Province's E. asperula leaves are abundant in naturally occurring antioxidants, indicating their potential use as therapeutic materials.

Abstract This work examines the capacity of Naringin and Rutin to influence the DNA damage response (DDR) pathway by investigating their interactions with key DDR proteins, including PARP-1, ATM, ATR, CHK1, and WEE1. Through a combination of in silico molecular docking and in vitro evaluations, we investigated the cytotoxic and genotoxic effects of these compounds on MDA-MB-231 cells, comparing them to normal human fibroblast cells (2DD) and quiescent fibroblast cells (QFC). The research found that Naringin and Rutin had strong affinities for DDR pathway proteins, indicating their capacity to specifically regulate DDR pathways in cancer cells. Both compounds exhibited preferential cytotoxicity towards cancer cells while preserving the vitality of normal 2DD fibroblast cells, as demonstrated by cytotoxicity experiments conducted at a dose of 10 µM. The comet experiments performed particularly on QFC cells provide valuable information on the genotoxic impact of Naringin and Rutin, highlighting the targeted initiation of DNA damage in cancer cells. The need to use precise cell models to appropriately evaluate toxicity and genotoxicity is emphasized by this discrepancy. In addition, ADMET and drug-likeness investigations have emphasized the pharmacological potential of these compounds; however, they have also pointed out the necessity for optimization to improve their therapeutic profiles. The antioxidant capabilities of Naringin and Rutin were assessed using DPPH and free radical scavenging assays at a concentration of 10 µM. The results confirmed that both compounds have a role in reducing oxidative stress, hence enhancing their anticancer effects. Overall, Naringin and Rutin show potential as medicines for modulating the DDR in cancer treatment. They exhibit selective toxicity towards cancer cells while sparing normal cells and possess strong antioxidant properties. This analysis enhances our understanding of the therapeutic uses of natural chemicals in cancer treatment, supporting the need for more research on their mechanisms of action and clinical effectiveness.

Rutin has a variety of pharmacological activities, in order to solve the application defects caused by its poor water solubility. In this paper, rutin/hydroxypropyl-β-cyclodextrin (HPCD) inclusion complexes were prepared by solvent evaporation method and analysed for structure, solubility, antioxidant activity and stability. The analysis of the inclusion complex showed that HPCD could effectively encapsulate rutin in a molar ratio of 1:1, and its encapsulation efficiency and drug loading rate were 89.33% and 26.67%, respectively. The solubility of the inclusion complex in water was 51 times higher than that of rutin. After complexation, the crystal diffraction peaks of rutin disappeared and the temperature of the maximum weight loss increased from 266 ℃ to 318 ℃ and solid inclusion complex forms showed an irregular sheet-like structures indicating a successful complexation of rutin by HPCD. The IC50 of the inclusion complex for scavenging DPPH radicals and ABTS cationic radicals was significantly lower than that of rutin (P

Background. Salicylic acid is an important phytohormone in plants, influencing various functions such as senescence, respiration, and stress resistance. Despite extensive studies the role of salicylic acid in stress, its effects under normal conditions are less understood. This study explores the influence of salicylic acid on the biosynthesis of important biochemical compounds such as ascorbic acid, rutin, and other phenolic compounds in wheat (Triticum aestivum L.), aiming to elucidate potential applications in agriculture. Materials and Methods. Wheat variety 'Podolyanka' was treated with 0.05 mM salicylic acid and grown under controlled conditions. Biochemical analyses were studied on 7, 10 and 20 days of growth to using the spectrophotometric method for the determination of ascorbic acid, rutin, total phenolic compounds, anthocyanins, flavonoids, and xanthones. Methods included chromatography on the plate with silicagel for rutin. Results and Discussion. Salicylic acid treatment significantly increased the ascorbic acid content in wheat shoots at all studied stages. There was also a notable increase in rutin content in the early growth phase. However, the content of other phenolic compounds, such as xanthones, generally decreased under salicylic acid treatment. Intriguingly, anthocyanin content was increased, suggesting a complex interaction within the biosynthetic pathways influenced by salicylic acid. The study also revealed correlations among different phenolic compounds, indicating intertwined metabolic pathways. Conclusion. Salicylic acid enhances the biosynthesis of specific phenolic compounds like ascorbic acid and rutin in wheat, which can have implications for agricultural practices aiming at improving plant resilience and nutritional quality. The differential impact of SA on various phenolic compounds underscores the complexity of plant biochemical pathways and highlights the need for further research to fully understand these interactions and their practical applications.

Tyrosinase is a binuclear copper-containing enzyme that catalyzes the conversation of monophenols to diphenols via o-hydroxylation and then the oxidation of o-diphenols to o-quinones which is profoundly linked to eukaryotic melanin synthesis and fruits browning. The hyperpigmentation due to unusual tyrosinase activity has gained growing health concern. Plants and their metabolites are considered promising and effective sources for potent antityrosinase enzymes. Hence, searching for potent, specific tyrosinase inhibitor from different plant extracts is an alternative approach in regulating overproduction of tyrosinase. Among the tested extracts, the hydro-alcoholic extract of Moringa oleifera L. leaves displayed the potent anti-tyrosinase activity (IC50 = 98.93 µg/ml) in a dose-dependent manner using L-DOPA as substrate; however, the kojic acid showed IC50 of 88.92 µg/ml. The tyrosinase-diphenolase (TYR-Di) kinetic analysis revealed mixed inhibition type for the Ocimum basilicum L. and Artemisia annua L. extracts, while the Coriandrum sativum L. extract displayed a non-competitive type of inhibition. Interestingly, the extract of Moringa oleifera L. leaves exhibited a competitive inhibition, low inhibition constant of free enzyme ( K ii app ) value and no Pan-Assay Interfering Substances, hinting the presence of strong potent inhibitors. The major putative antityrosinase compound in the extract was resolved, and chemically identified as rutin based on various spectroscopic analyses using UV–Vis, FTIR, mass spectrometry, and 1H NMR. The in silico computational molecular docking has been performed using rutin and A. bisporus tyrosinase (PDB code: 2Y9X). The binding energy of the predicted interaction between tropolone native ligand, kojic acid, and rutin against 2Y9X was respectively − 5.28, − 4.69, and − 7.75 kcal/mol. The docking simulation results revealed the reliable binding of rutin to the amino acid residues (ASN260, HIS259, SER282) in the tyrosinase catalytic site. Based on the developed results, rutin extracted from M. oleifera L. leaves has the capability to be powerful anti-pigment agent with a potential application in cosmeceutical area. In vivo studies are required to unravel the safety and efficiency of rutin as antityrosinase compound. [ABSTRACT FROM AUTHOR]

Anthracycline-based therapies exert endothelial damages through peroxidation and the production of proinflammatory cytokines, resulting in a high risk of cardiovascular complications in cancer patients. Hyaluronic acid-based hybrid nanoparticles (LicpHA) are effective pharmacological tools that can target endothelial cells and deliver drugs or nutraceuticals. This study aimed to prepared and characterized a novel LicpHA loaded with Rutin (LicpHA Rutin), a flavonoid with high antioxidant and anti-inflammatory properties, to protect endothelial cells against epirubicin-mediated endothelial damages. LicpHA Rutin was prepared using phosphatidylcholine, cholesterol, poloxamers, and hyaluronic acid by a modified nanoprecipitation technique. The chemical-physical characterization of the nanoparticles was carried out (size, zeta potential, morphology, stability, thermal analysis, and encapsulation efficiency). Cytotoxicity studies were performed in human endothelial cells exposed to epirubicin alone or in combination with Free-Rutin or LicpHA Rutin. Anti-inflammatory studies were performed through the intracellular quantification of NLRP-3, MyD-88, IL-1β, IL-6, IL17-α, TNF-α, IL-10, and IL-4 using selective ELISA methods. Morphological studies via TEM and image analysis highlighted a heterogeneous population of LicpHA particles with non-spherical shapes (circularity equal to 0.78 ± 0.14), and the particle size was slightly affected by Rutin entrapment (the mean diameter varied from 179 ± 4 nm to 209 ± 4 nm). Thermal analysis and zeta potential analyses confirmed the influence of Rutin on the chemical-physical properties of LicpHA Rutin, mainly indicated by the decrease in the surface negative charge (from −35 ± 1 mV to −30 ± 0.5 mV). Cellular studies demonstrated that LicpHA Rutin significantly reduced cell death and inflammation when compared to epirubicin alone. The levels of intracellular NLRP3, Myd-88, and proinflammatory cytokines were significantly lower in epirubicin + LicpHA Rutin-exposed cells when compared to epirubicin groups (p < 0.001). Hyaluronic acid-based nanoparticles loaded with Rutin exerts significant vasculo-protective properties during exposure to anthracyclines. The overall picture of this study pushes towards preclinical and clinical studies in models of anthracycline-induced vascular damages. [ABSTRACT FROM AUTHOR]

Moringa oleifera Lam. (horseradish tree) leaves demonstrate high nutritional value, are rich in proteins, and are widely used in folk medicine and food. This study investigated the presence of secondary metabolites and antinutritional proteins in leaf extract (LE) and the protein-rich fraction (PRF) derived from M. oleifera leaves, as well as the cytotoxicity to human cells, hemolytic activity, and in vivo acute toxicity and genotoxicity in mice. The flavonoids rutin and vitexin as well as trypsin inhibitors and lectins were detected in LE and PRF. Neither sample demonstrated toxicity against human peripheral blood mononuclear cells and both showed low hemolytic action. In vivo, LE and PRF did not show antinutritional effects and caused no death. The hematological parameters of the animals in the treated group were similar to those of the control. A significant increase in the serum levels of alanine aminotransferase and a discrete leukocyte infiltration with cytoplasmic vacuolization of the hepatocytes in the liver were detected in LE-treated animals. The preparations were not genotoxic or mutagenic. This study shows that LE and PRF are not antinutritional agents and presented low acute toxicity and no genotoxicity or mutagenicity. The present study contributes to the determination of the safety of using M. oleifera leaf proteins. [ABSTRACT FROM AUTHOR]

BACKGROUND: Early weaning is prone to damage intestinal barrier function, resulting in diarrhea, whereas rutin, as a natural flavonoid with multiple biological functions, shows potential in piglets. Therefore, the effects of dietary rutin on growth, antidiarrheal, barrier function, antioxidant status and cecal microbiota of weaned piglets were investigated with the control group (CON) (basal diet) and Rutin (basal diet+500 mg kg−1 rutin) groups fed for 14 days. RESULTS: The results showed that dietary 500 mg kg−1 rutin significantly decreased diarrhea index, serum diamine oxidase activity and total aerobic bacterial population in mesenteric lymph nodes, whereas it significantly increased the gain‐to‐feed ratio (G:F) and serum growth hormone content, jejunal villus height and villus height to crypt depth ratio, and also enhanced jejunal claudin‐1 and zonula occludens‐1 mRNA and protein expression. Meanwhile, dietary rutin significantly decreased inflammation‐associated mRNA expression, malondialdehyde (MDA) content, swollen mitochondrial number and mitochondrial area in the jejunum, whereas it increased the total superoxide dismutase (T‐SOD) and glutathione peroxidase activities and activated the Nrf2 signaling pathway. Moreover, dietary rutin significantly increased Firmicutes abundance and decreased Campylobacterota abundance, which were closely associated with the decreased diarrhea index and MDA content or increased Claudin‐1 expression and T‐SOD activity. CONCLUSION: Dietary 500 mg kg−1 rutin increased G:F by improving intestinal morphology, and alleviated diarrhea by enhancing intestinal barrier, which might be associated with the enhanced antioxidant capacity via activating the Nrf2/Keap1 signaling pathway and the improved cecal microbial composition in weaned piglets. © 2024 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

α-L-Rhamnosidases with desirable activity and thermostability profiles could be used for the biocatalytic production of the flavonoid glucoside isoquercetin from natural rutin for functional food. Herein, to improve the catalytic activity of GH78 α-L-rhamnosidase BtRha78A from Bacteroides thetaiotaomicron VPI-5482, a list of residues located at the conserved general acid motif were selected for targeted mutagenesis by the sequence alignment of BtRha78A with homologous α-L-rhamnosidases. Ala-scanning mutagenesis and site-directed mutagenesis based on sequence alignment were performed, and the relative activity on rutin was evaluated. Furthermore, the reaction time curves and enzyme kinetics of better mutants were determined. The results indicate that the conversion rates of mutants V338A, V338I, S340A, and G341A were increased by 21.3%, 20.1%, 13.2%, and 1.6%, respectively, compared with the wild type when using whole-cell biotransformation. Moreover, the catalytic efficiency kcat/KM value of mutant V338A was 1.3-fold higher than that of the wild type. The best mutant, V338A, was employed for the enzymatic preparation of isoquercetin via the biotransformation of rutin at a concentration of 2 mM, and 1.80 g of isoquercetin was obtained. The identification of the best mutant V338A lays the foundation for the efficient preparation of isoquercetin via the biotransformation of rutin, which in turn provides theoretical guidance for its large-scale production. [ABSTRACT FROM AUTHOR]

A sensitive UPLC-HRMS method was developed and validated for simultaneous quantification of four active flavonoids from Chimonanthus nitens Leaf Granules (CNLG) in biological matrix. The method was utilized in pharmacokinetic study of the four flavonoids in rats as well as other evaluation assays in vitro. It was revealed that rutin, nicotiflorin, and astragalin had poor oral bioavailability in rats possibly due to low intestinal permeability and metabolism in intestinal flora. Kaempferol underwent rapid glucuronidation and sulphation in rat plasma with medium permeability coefficient. The results provided valuable data for future research and development of CNLG flavonoids. [ABSTRACT FROM AUTHOR]

Background: Psoriasis is a chronic inflammatory skin disease that can cause systemic inflammation in various organs. Rutin has been suggested to fight psoriasis, but the signaling pathways by which it works need to be explored. Materials and methods: HaCaT cells co‐stimulated with interleukin (IL)‐17, IL‐22, tumor necrosis factor‐alpha (TNF‐α), IL‐1α, and oncostatin M (M5) were used as an in vitro cell model of psoriasis. The proliferation and viability of HaCaT cells were determined by 5‐ethynyl‐2′‐deoxyuridine and cell counting assays. Relative mRNA levels of IL‐6, TNF‐α, chemokines (CXCL1 and CXCL2), and anti‐microbial peptides (S100A7 and S100A8) were detected by reverse transcriptase‐quantitative PCR. Release of IL‐6 and TNF‐α from HaCaT cells was measured by enzyme‐linked immunosorbent assay. Keratin1, Keratin5, p‐JAK2, and p‐STAT3 protein levels were estimated with western blotting. Molecular docking predicted binding sites for Rutin and STAT3. Results: Rutin treatment undercut M5‐urged viability increase and proliferation boost in HaCaT cells. Moreover, M5 stimulation mediated upregulation of IL‐6, TNF‐α, CXCL1, CXCL2, S100A7, and S100A8 was partially reversed after Rutin treatment. In addition, M5 stimulation induced downregulation of Keratin1 and Keratin5 proteins as well as upregulation of p‐JAK2 and p‐STAT3 proteins were attenuated in response to Rutin treatment, manifesting that Rutin treatment inhibited M5‐promoted aberrant differentiation and impaired M5‐mediated activation of the JAK2/STAT3 signaling in HaCaT cells. Molecular docking discovered that residues GLN326 and ASP334 in STAT3 might bind to Rutin. Conclusion: Rutin treatment blocked the JAK2/STAT3 signaling, thus attenuating psoriasis‐related inflammation and anomalous differentiation in keratinocytes. [ABSTRACT FROM AUTHOR]

As Ayurvedic herbal medicines have grown more commercialized, it has become crucial to standardize these products using modern techniques. Mansyadi Kwatha is an Ayurvedic formulation indicated for insomnia, epilepsy, hysteria and anxiety. It consists of three potent drugs, i.e., Nardostachys jatamansi rhizome, Withania somnifera L. root and Hyoscyamus niger L. seed. In this study, a novel instrumental thin-layer chromatography (TLC) method was developed for the simultaneous estimation of atropine, rutin and vanillin. It was then employed for marker-based standardization of Mansyadi Kwatha for detection of these constituents and quantifying the same in the formulation. A pre-coated silica gel TLC plate 60 F254 was used as the stationary phase with tetrahydrofuran‒toluene‒methanol‒formic acid (5:3.5:2:0.5, V/V) as the mobile phase for chromatographic separation with densitometric scanning at 206 nm. The developed method gave the desired separation with optimum RF values of 0.090 ± 0.0039, 0.290 ± 0.0099 and 0.679 ± 0.0056 for atropine, rutin and vanillin, respectively. The International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use (ICH) Q2(R1) guidelines were followed for method validation. The method was found to be specific with comparable RF and no interference of the mobile phase. It showed a good linear relation with correlation coefficient greater than 0.99. The method was also precise, robust with percentage relative standard deviation less than 2% and accurate with percent recovery between 95‒105%. [ABSTRACT FROM AUTHOR]

Acrylamide (AA) is a carcinogenic compound that affects people due to its frequent use in laboratories and industry as well as the high‐temperature cooking of foods with high hydrocarbon content. AA is known to cause severe reproductive abnormalities. The main aim of this study is to evaluate the protective effect of rutin (RU), a phytoactive compound, against AA‐induced reproductive toxicity in female rats. Initially, rats were exposed to AA (40 mg/kg for 10 days). Therapy of RU was given after AA intoxication consecutively for 3 days. After 24 h of the last treatment, all the animals were sacrificed. The study evaluated reproductive hormones, oxidative stress markers, membrane‐bound enzymes, DNA damage, histological findings, and an in silico approach to determine the protective efficacy of RU. The results indicated that RU significantly protected against inflammation, oxidative stress, and DNA damage induced by AA, likely due to its antioxidant properties. [ABSTRACT FROM AUTHOR]

Aluminium (Al) is one of the most abundant chemical elements in nature and metal in the earth’s crust. Accumulation of Aluminium ions (Al3+) in target tissues results into formation of oxygen radicals causing oxidative damage through inducing cytotoxicity. The aim of this study is to analyse the antioxidant effect of selected polyphenols (quercetin, rutin and a medicinal plant phagnalon rupestre) on rats intoxicated by aluminium with specific focus on the heart.This experiment was carried out on 6 groups of wistar albino rats,group 1; positive control, group 2; Al male intoxicated group treated with quercetin, group 3; Al male intoxicated group treated with rutin, group 4; Al female intoxicated, group 5; Al intoxicated treated with phagnalon rupestre, group 6; female control. Several Biochemical assays were carried out such as protein test, Thiobarbituric acid reactive substance (TBARS) assay, catalase assay (CAT), glutathione-s-transferase (GST) assay, superoxide dismutase (SOD) assay, Glutathione reduced and glutathione peroxidase (GSH & GPX) assay, lipids (cholesterol & triglycerides) assays. Aluminium intoxicated group showed decrease in the content of protein compared to the control and treated groups. Aluminium intoxicated group showed an increase in the activity of thiobarbituric reactive substances (TBARS) but a significant decrease in the activity of catalase (CAT), glutathione S transferase assays (GST) compared to the control group. Biomarkers of oxidative stress significantly reduced in heart Al-induced oxidative stress by administration of Quercetin. Therefore, Quercetin is an effective antioxidant against oxidative stress caused by free radicals produced because of aluminium exposure. [ABSTRACT FROM AUTHOR]

Background Ulcerative colitis, an inflammatory bowel disease, is characterized by a status of oxidative stress and inflammation. Rutin is a natural flavonoid with many pharmacological activities and its role in acetic acid-induced ulcerative colitis through the high mobility group B1 (HMGB1)/ toll-like receptor-4 (TLR4)/ myeloid differentiation primary response protein 88 (MYD88)/ nuclear factor-kB (NF-kB) signaling pathway needs to be explored. Methods Four experimental groups were divided into control group, rutin group: treated with 100 mg/kg/day rutin orally for 10 days, acetic acid (AA) group: given intracolonic instillation of AA to induce ulcerative colitis, and acetic acid with rutin treatment (AA/Rutin) group. Results Acetic acid caused a marked increase in the colon weight/length ratio and induced colonic histopathological changes, leading to a marked rise in the colonic histopathological scores. Acetic acid exhibited a significant rise in LDH and CRP serum levels as well as TOS colonic levels, accompanied by a marked decline in TAS colonic contents compared to the control group. Moreover, AA-induced activation of the HMGB1/TLR4/MYD88/NF-kB signaling pathway. Rutin demonstrated a significant decrease in the colon weight/length ratio, ameliorated the colonic histopathological changes induced by AA, and exhibited a marked decline in the colonic histopathological scores. Rutin showed a significant decrease in serum LDH, and CRP levels as well as colonic TOS contents when compared with the AA group. Rutin suppressed the colonic activation of the HMGB1/TLR4/MYD88/NF-kB signaling pathway. Conclusion Rutin could be a promising coloprotective agent against AA-induced ulcerative colitis by targeting the HMGB1/TLR4/MYD88/NF-kB signaling pathway. [ABSTRACT FROM AUTHOR]

Rutin, a flavonoid found in various plants, has gained attention for its potential applications in the cosmetic industry due to its antioxidant, anti-inflammatory, and potential photoprotective properties. Our review explored the use of rutin (rutoside, 3-O-rutinoside-quercetin) in cosmetics/dermocosmetics, focusing on its physicochemical properties and stability, cutaneous permeability, and efficacy in sunscreen systems, involving in vitro tests and the current state of clinical trials. Rutin's ability to scavenge free radicals, prevent peroxidation, and reduce vascular fragility makes this flavonoid a promising ingredient for photoprotection. Studies have shown that rutin can enhance the sun protection factor (SPF) of sunscreen formulations, especially when combined with organic UV filters. The encapsulation of rutin in nanostructures has also been investigated to improve its applicability. Overall, rutin shows potential as a safe and effective ingredient in cosmetics/dermocosmetics, offering protection against the harmful effects of UV radiation and oxidative stress on the skin, as well as being a feasible strategy for developing environmentally friendly multifunctional sunscreens. [ABSTRACT FROM AUTHOR]

This research delves into a systematic Analytical Quality by Design (AQbD) approach to develop and validate a stability-indicating robust RP-HPLC method for the simultaneous determination of Rutin and Curcumin, compounds known for their anti-inflammatory, antioxidant, and wound-healing properties. Utilizing QbD principles, critical method parameters (CMPs) were identified and screened using design of experiments (DoE) and optimized via response surface methodology (RSM) with Central Composite Design (CCD). The optimized chromatographic separation used a Phenomenex Luna C18 column with gradient elution, using methanol and 0.1% formic acid, a flow rate of 1 ml/min, and detection at 345 nm (isosbestic point). The retention times were 5.63 mins for Rutin and 17.01 mins for Curcumin. The stability indication of the developed HPLC method was performed, and validation parameters were meticulously conducted following the ICH Q2(R1) guidelines, demonstrating linearity over 2-10 μg/ml for Rutin and 5-25 μg/ml for Curcumin, with correlation coefficients of 0.9999 and 0.9998, respectively. Precision studies showed %RSD within acceptable limits, and accuracies ranged between 97-100%. This validated HPLC method offers a reliable, sensitive approach for simultaneous quantifying Rutin and Curcumin, suitable for routine analysis in pharmaceutical laboratories and quality control. [ABSTRACT FROM AUTHOR]

Pantothenate synthetase protein plays a pivotal role in the biosynthesis of coenzyme A (CoA), which is a crucial molecule involved in a number of cellular processes including the metabolism of fatty acid, energy production, and the synthesis of various biomolecules, which is necessary for the survival of Mycobacterium tuberculosis (Mtb). Therefore, inhibiting this protein could disrupt CoA synthesis, leading to the impairment of vital metabolic processes within the bacterium, ultimately inhibiting its growth and survival. This study employed molecular docking, structure-based virtual screening, and molecular dynamics (MD) simulation to identify promising phytochemical compounds targeting pantothenate synthetase for tuberculosis (TB) treatment. Among 239 compounds, the top three (rutin, sesamin, and catechin gallate) were selected, with binding energy values ranging from-11 to-10.3 kcal/mol, and the selected complexes showed RMSD (<3 Å) for 100 ns MD simulation time. Furthermore, molecular mechanics generalized Born surface area (MM/GBSA) binding free energy calculations affirmed the stability of these three selected phytochemicals with binding energy ranges from-82.24 ± 9.35 to-66.83 ± 4.5 kcal/mol. Hence, these identified natural plant-derived compounds as potential inhibitors of pantothenate synthetase could be used to inhibit TB infection in humans. [ABSTRACT FROM AUTHOR]

Renal aging, marked by the accumulation of senescent cells and chronic low‐grade inflammation, leads to renal interstitial fibrosis and impaired function. In this study, we investigate the role of macrophages, a key regulator of inflammation, in renal aging by analyzing kidney single‐cell RNA sequencing data of C57BL/6J mice from 8 weeks to 24 months. Our findings elucidate the dynamic changes in the proportion of kidney cell types during renal aging and reveal that increased macrophage infiltration contributes to chronic low‐grade inflammation, with these macrophages exhibiting senescence and activation of ferroptosis signaling. CellChat analysis indicates enhanced communications between macrophages and tubular cells during aging. Suppressing ferroptosis alleviates macrophage‐mediated tubular partial epithelial‐mesenchymal transition in vitro, thereby mitigating the expression of fibrosis‐related genes. Using SCENIC analysis, we infer Stat1 as a key age‐related transcription factor promoting iron dyshomeostasis and ferroptosis in macrophages by regulating the expression of Pcbp1, an iron chaperone protein that inhibits ferroptosis. Furthermore, through virtual screening and molecular docking from a library of anti‐aging compounds, we construct a docking model targeting Pcbp1, which indicates that the natural small molecule compound Rutin can suppress macrophage senescence and ferroptosis by preserving Pcbp1. In summary, our study underscores the crucial role of macrophage iron dyshomeostasis and ferroptosis in renal aging. Our results also suggest Pcbp1 as an intervention target in aging‐related renal fibrosis and highlight Rutin as a potential therapeutic agent in mitigating age‐related renal chronic low‐grade inflammation and fibrosis. [ABSTRACT FROM AUTHOR]