RESUMO
Advanced targeted nanoparticles (NPs) were designed to enhance the targeted delivery of resveratrol (RES) and quercetin (QUE) by utilizing carboxymethyl chitosan (CTS) and Jiuzao glutelin isolate (JGI) conjugates. Briefly, RES and QUE were encapsuled within CTS-JGI-2 (CTS/JGI, m/m, 2:1). The carrier's targeting properties were further improved through the incorporation of folic acid (FA) and polyethylenimine (PEI). Moreover, the stability against digestion was enhanced by incorporating baker yeast cell walls (BYCWs) to construct RES-QUE/FA-PEI/CTS-JGI-2/MAT/BYCW NPs. The results demonstrated that FA-PEI/CTS-JGI-2/MAT/BYCW NPs could improve cellular uptake and targeting property of RES and QUE through endocytosis of folic acid receptors (FOLRs). Additionally, RES-QUE successfully alleviated LPS- and DSS-induced inflammation by regulating NF-κB/IkBa/AP-1 and AMPK/SIRT1signaling pathways and reducing the secretion of inflammatory mediators and factors. These findings indicate FA-PEI/CTS-JGI-2/MAT/BYCW NPs hold promise as an oral drug delivery system with targeted delivery capacities for functional substances prone to instability in dietary supplements.
Assuntos
Quitosana , Ácido Fólico , Nanopartículas , Quercetina , Resveratrol , Quitosana/química , Quitosana/farmacologia , Quitosana/análogos & derivados , Ácido Fólico/química , Ácido Fólico/farmacologia , Quercetina/química , Quercetina/análogos & derivados , Quercetina/farmacologia , Quercetina/administração & dosagem , Nanopartículas/química , Resveratrol/química , Resveratrol/farmacologia , Resveratrol/administração & dosagem , Animais , Camundongos , Humanos , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Células RAW 264.7RESUMO
Quercetin (QUE) sufferred from poor processing adaptability and absorbability, hindering its application as a dietary supplement in the food industry. In this study, fatty acids (FAs)-sodium caseinate (NaCas) ligand complexes carriers were fabricated to improve the aqueous dispersibility, storage/thermal stability, and bioaccessibility of QUE using an ultrasound method. The results indicated that all six selected common dietary FAs formed stable hydrophilic complexes with NaCas and the FAs-NaCas complexes achieved an encapsulation efficiency greater than 90 % for QUE. Furthermore, the introduction of FAs enhanced the binding affinity between NaCas and QUE, but did not change the binding mode (static bursting) and types of intermolecular forces (mainly hydrogen bonding). In addition, a distinct improvement was discovered in the storage stability (>2.37-fold), thermal processing stability (>32.54 %), and bioaccessibility (>2.37-fold) of QUE. Therefore, the FAs-NaCas ligand complexes could effectively protect QUE to minimize degradation as fat-soluble polyphenol delivery vehicles.
Assuntos
Caseínas , Ácidos Graxos , Quercetina , Quercetina/química , Quercetina/metabolismo , Ácidos Graxos/química , Ácidos Graxos/metabolismo , Caseínas/química , Caseínas/metabolismo , Estabilidade de Medicamentos , Disponibilidade Biológica , Humanos , Interações Hidrofóbicas e Hidrofílicas , Água/química , Gorduras na Dieta/metabolismoRESUMO
Vachellia gummifera (Willd.) Kyal. & Boatwr. is a medicinal plant endemic to Morocco that has no documented studies on its chemical composition. In this study, the chemical composition of the water/methanol (4 : 1) extracts of air-dried leaf and stem samples of Moroccan V. gummifera was determined using UHPLC-MS and NMR. In total, over 100 metabolites were identified in our study. Pinitol was the major compound in both the leaf and stem extracts, being significantly more abundant in the former. Asparagine and 3-hydroxyheteroendrin were the second most abundant compounds in the stem and leaf extracts, respectively, though both compounds were present in each tissue. The other compounds included flavonoids based on quercetin, and phenolic derivatives. Eucomic acid, only identified in the stems and was the major aromatic compound distinguishing the leaf and stem profiles. Quercetin 3-O-(6''-O-malonyl)-ß-D-glucopyranoside was identified as the major flavonoid in the leaves but was also present in the stems. Other malonylated derivatives that were all flavonol glycosides based on myricetin, kaempferol, and isorhamnetin in addition to quercetin were also identified. This is the first report of eucomic acid and malonylated compounds in Vachellia species. This report provides valuable insights into the chemotaxonomic significance of the Vachellia genus.
Assuntos
Folhas de Planta , Plantas Medicinais , Cromatografia Líquida de Alta Pressão , Fabaceae/química , Flavonoides/química , Flavonoides/isolamento & purificação , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Folhas de Planta/química , Caules de Planta/química , Plantas Medicinais/química , Quercetina/química , Quercetina/isolamento & purificaçãoRESUMO
Traditional Chinese medicine (TCM) has been used to treat triple-negative breast cancer (TNBC), a breast cancer subtype with poor prognosis. Clinical studies have verified that the Sanyingfang formula (SYF), a TCM prescription, has obvious effects on inhibiting breast cancer recurrence and metastasis, prolonging patient survival, and reducing clinical symptoms. However, its active ingredients and molecular mechanisms are still unclear. In this study, the active ingredients of each herbal medicine composing SYF and their target proteins are obtained from the Traditional Chinese Medicine Systems Pharmacology database. Breast cancer-related genes are obtained from the GeneCards database. Major targets and pathways related to SYF treatment in breast cancer are identified by analyzing the above data. By conducting molecular docking analysis, we find that the active ingredients quercetin and luteolin bind well to the key targets KDR1, PPARG, SOD1, and VCAM1. In vitro experiments verify that SYF can reduce the proliferation, migration, and invasion ability of TNBC cells. Using a TNBC xenograft mouse model, we show that SYF could delay tumor growth and effectively inhibit the occurrence of breast cancer lung metastasis in vivo. PPARG, SOD1, KDR1, and VCAM1 are all regulated by SYF and may play important roles in SYF-mediated inhibition of TNBC recurrence and metastasis.
Assuntos
Proliferação de Células , Medicamentos de Ervas Chinesas , Simulação de Acoplamento Molecular , Neoplasias de Mama Triplo Negativas , Neoplasias de Mama Triplo Negativas/tratamento farmacológico , Neoplasias de Mama Triplo Negativas/patologia , Neoplasias de Mama Triplo Negativas/metabolismo , Neoplasias de Mama Triplo Negativas/genética , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Medicamentos de Ervas Chinesas/química , Humanos , Animais , Feminino , Camundongos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios Antitumorais Modelo de Xenoenxerto , Farmacologia em Rede , Movimento Celular/efeitos dos fármacos , Camundongos Nus , Luteolina/farmacologia , Luteolina/uso terapêutico , Camundongos Endogâmicos BALB C , Quercetina/farmacologia , Quercetina/química , Medicina Tradicional Chinesa , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacosRESUMO
Ruta chalepensis L. is a versatile herb used in culinary arts and traditional medicine. The study aimed to determine the chemical composition of an ethanolic extract from R. chalepensis and the total phenolic and flavonoid content. Additionally, the extracts' antimicrobial and antioxidant activities were tested. The disc diffusion method and minimum inhibitory concentration (MIC) were used to test the antibacterial properties on four types of bacteria: Escherichia coli, Proteus penneri, Bacillus cereus, and Staphylococcus aureus. A colorimetric assay was used to evaluate the total phenolic and flavonoid content, and the DPPH method was used to assess the antioxidant activity. The phytochemical constituents were determined using LC-MS/MS. The results indicated that R. chalepensis ethanolic extract had 34 compounds, and the predominant compounds were quercetin (9.2 %), myricetin (8.8 %), and camphene (8.0 %). Moreover, the extract had a good level of polyphenols and flavonoids, as demonstrated by inhibiting free radicals (DPPH) (IC50 was 41.2±0.1). Also, the extract exhibited robust antimicrobial activity against P. penneri and S. aureus with an MIC of 12.5 and 25.0â µg/mL, respectively. In conclusion, the results suggest that the R. chalepensis ethanolic extract has good antioxidant and antibacterial properties that could be utilized to develop new antibacterial agents.
Assuntos
Anti-Infecciosos , Ruta , Antibacterianos/farmacologia , Antibacterianos/química , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Antioxidantes/química , Cromatografia Líquida , Etanol , Flavonoides/química , Flavonoides/farmacologia , Fenóis/farmacologia , Fenóis/análise , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Ruta/química , Staphylococcus aureus , Espectrometria de Massas em Tandem , Polifenóis/química , Polifenóis/farmacologia , Quercetina/química , Quercetina/isolamento & purificação , Quercetina/farmacologiaRESUMO
The global prevalence of fungal infections is alarming in both the pre- and post- COVID period. Due to a limited number of antifungal drugs, there are hurdles in treatment strategies for fungal infections due to toxic potential, drug interactions, and the development of fungal resistance. All the antifungal targets (existing and newer) and pipeline molecules showing promise against these targets are reviewed. The objective was to predict or repurpose phyto-based antifungal compounds based on a dual target inhibition approach (Sterol-14-α- demethylase and HSP-90) using a case study. In pursuit of repurposing the phytochemicals as antifungal agents, a team of researchers visited Aravalli Biodiversity Park (ABP), Delhi, India, to collect information on available medicinal plants. From 45 plants, a total of 1149 ligands were collected, and virtual screening was performed using Schrodinger Suite 2016 software to get 83 hits against both the target proteins: Sterol-14-α-demethylase and HSP-90. After analysis of docking results, ligands were selected based on their interaction against both the target proteins and comparison with respective standard ligands (fluconazole and ganetespib). We have selected Isocarthamidin, Quercetin and Boeravinone B based on their docking score and binding interaction against the HSP-90 (Docking Score -9.65, -9.22 and -9.21, respectively) and 14-α-demethylase (Docking Score -9.19, -10.76 and -9.74 respectively). The docking protocol was validated and MM/GBSA studies depicted better stability of selected three ligands (Isocarthamidin, Quercetin, Boeravinone B) complex as compared to standard complex. Further, MD simulation studies were performed using the Desmond (67) software package version 2018-4. All the findings are presented as a case study for the prediction of dual targets for the repurposing of certain phytochemicals as antifungal agents.
Assuntos
Antifúngicos , Reposicionamento de Medicamentos , Simulação de Acoplamento Molecular , Compostos Fitoquímicos , Antifúngicos/farmacologia , Antifúngicos/química , Índia , Humanos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Proteínas de Choque Térmico HSP90/antagonistas & inibidores , Esterol 14-Desmetilase/metabolismo , Esterol 14-Desmetilase/química , Plantas Medicinais/química , Quercetina/farmacologia , Quercetina/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Micoses/tratamento farmacológico , Micoses/microbiologiaRESUMO
Some ingredients from herbal medicine can significantly affect the activity of CYP2D6, thus leading to serious interactions between herbs and drugs. Quercetin and hyperoside are active ingredients widely found in vegetables, fruits, and herbal medicines. Quercetin and hyperoside have many biological activities. In this work, the characteristic bindings of CYP2D6 with quercetin/hyperoside are revealed by multi-spectroscopy analysis, molecular docking, and molecular dynamics simulations. The fluorescence of CYP2D6 is statically quenched by quercetin and hyperoside. The binding constant (Ka ) values of CYP2D6-quercetin/hyperoside range from 104 L mol-1 , which indicates that these two flavonoids bind moderately to CYP2D6. Meanwhile, quercetin has a stronger quenching ability to CYP2D6 than that of hyperoside. The secondary structure of CYP2D6 is obviously changed by binding with quercetin/hyperoside. The docking results reveal that the quercetin/hyperoside enters the active site of CYP2D6 near heme and binds to CYP2D6 by hydrogen bonds and van der Waals forces. The molecular dynamics simulation results indicate that the binding of quercetin/hyperoside can stabilize the two complexes, enhance the flexibility of CYP2D6 backbone atoms, and make a more unfolded and looser structure of CYP2D6.
Assuntos
Simulação de Dinâmica Molecular , Quercetina , Quercetina/química , Citocromo P-450 CYP2D6/metabolismo , Simulação de Acoplamento MolecularRESUMO
Tartary buckwheat protein-rutin/quercetin covalent complex was synthesized in alkaline oxygen-containing environment, and its binding sites, conformational changes and functional properties were evaluated by multispectral technique and proteomics. The determination of total sulfhydryl and free amino groups showed that rutin/quercetin can form a covalent complex with BPI and could significantly reduce the group content. Ultraviolet-visible spectrum analysis showed that protein could form new characteristic peaks after binding with rutin/quercetin. Circular dichroism spectrum analysis showed that rutin and quercetin caused similar changes in the secondary structure of proteins, both promoting ß-sheet to α-helix, ß-ture and random coil transformation. The fluorescence spectrometry results showed that the combination of phenols can cause the fluorescence quenching, and the combination of rutin was stronger than the quercetin. Proteomics showed that there were multiple covalent binding sites between phenols and protein. Rutin had a high affinity for arginine, and quercetin and cysteine had high affinity. Meanwhile, the combination of rutin/quercetin and protein had reduced the surface hydrophobic ability of the protein, and improved the foaming, stability and antioxidant properties of the protein. This study expounded the mechanism of the combination of BPI and rutin/quercetin, and analysed the differences of the combination of protein and phenols in different structures. The findings can provide a theoretical basis for the development of complexes in the area of food.
Assuntos
Fagopyrum , Quercetina , Quercetina/química , Fenóis , Fenol , Fagopyrum/química , Rutina/química , Sítios de LigaçãoRESUMO
Novel biocompatible and effective hyperthermia (HT) treatment materials for breast cancer therapeutic have recently attracting researchers, because of their effective ablation of cancer cells and negligible damage to healthy cells. Magnetoliposome (MLs) have numerous possibilities for utilize in cancer treatment, including smart drug delivery (SDD) mediated through alternating magnetic fields (AMF). In this work, magnesium ferrite (MgFe2O4) encapsulated with liposomes lipid bilayer (MLs), Quercetin (Q)-loaded MgFe2O4@Liposomes (Q-MLs) nano-hybrid system were successfully synthesized for magnetic hyperthermia (MHT) and SDD applications. The hybrid system was well-investigated by different techniques using X-ray diffraction (XRD), Fourier transforms infrared spectroscopy (FT-IR), Energy dispersive X-ray (EDX), Vibrating sample magnetometer (VSM), Transmission electron microscope (TEM), and Zeta Potential (ZP). The characterization results confirmed the improving quercetin-loading on the MLs surface. TEM analysis indicated the synthesized MgFe2O4, MLs, and Q-MLs were spherical with an average size of 23.7, 35.5, and 329.5 nm, respectively. The VSM results revealed that the MgFe2O4 exhibit excellent and effective saturation magnetization (MS) (40.5 emu/g). Quercetin drug loading and entrapment efficiency were found to be equal to 2.1 ± 0.1% and 42.3 ± 2.2%, respectively. The in-vitro Q release from Q-loaded MLs was found 40.2% at pH 5.1 and 69.87% at pH 7.4, verifying the Q-loading pH sensitivity. The MLs and Q-MLs hybrid system as MHT agents exhibit specific absorption rate (SAR) values of 197 and 205 W/g, correspondingly. Furthermore, the Q-MLs cytotoxicity was studied on the MCF-7 breast cancer cell line, and the obtained data demonstrated that the Q-MLs have a high cytotoxicity effect compared to MLs and free Q.
Assuntos
Neoplasias da Mama , Hipertermia Induzida , Humanos , Feminino , Lipossomos/química , Quercetina/farmacologia , Quercetina/química , Neoplasias da Mama/tratamento farmacológico , Bicamadas Lipídicas , Células MCF-7 , Espectroscopia de Infravermelho com Transformada de Fourier , Hipertermia Induzida/métodos , Fenômenos MagnéticosRESUMO
This study examined the effects of methanol extract and its sub-extracts from Epilobium angustifolium on α-glucosidase and α-amylase activity. Secondary metabolites and amino acids were quantified using LC-MS/MS. Dichloromethane sub-extract displayed the highest activity and was chosen for further investigation. Despite the widespread use of E. angustifolium, genotoxicity studies were conducted to assess its safety. Dichloromethane significantly inhibited α-glucosidase (IC50 =17.340â µg/mL), making it approximately 293â times more effective than acarbose. Six known compounds, including gallic acid (1), a mixture of quercetin-3-O-α-galactoside (2a) and quercetin-3-O-α-glucoside (2b), quercetin-3-O-α-glucuronic acid (3), quercetin-3-O-α-rhamnoside (4), and kaempferol-3-O-α-rhamnoside (5) were identified. Quercetin-3-O-α-rhamnoside exhibited the highest inhibition of α-glucosidase (IC50 =1735±85â µM), making it 3.70â times more effective than acarbose. Dichloromethane also showed significant antigenotoxic activity against mutagenesis induced by NaN3, 9-AA, 4-NPD, and MNNG. Gallic acid was found in the highest abundance (13253.6931â ng/mL) in the methanolic extract. Furthermore, L-Aspartic acid was the most concentrated amino acid (363.5620â nmol/mL) in the methanolic extract.
Assuntos
Epilobium , Quercetina , Quercetina/química , Epilobium/química , Hipoglicemiantes/farmacologia , Acarbose , alfa-Glucosidases , Cromatografia Líquida , Cloreto de Metileno , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Espectrometria de Massas em Tandem , Ácido Gálico/farmacologia , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análiseRESUMO
Flavonoids have diverse beneficial roles that potentiate their application as nutraceutical agents in nutritional supplements and as natural antimicrobial agents in food preservation. To address poor solubility and bioactivity issues, we developed water-soluble micellar formulations loaded with single and multiple flavonoids using the biocompatible surface-active ionic liquid choline oleate. The food preservation performance was investigated using luteolin, naringenin, and quercetin as model bioactive compounds. The micellar formulations formed spherical micelles with particle sizes of <150 nm and exhibited high aqueous solubility (>5.15 mg/mL). Co-delivery of multiple flavonoids (luteolin, naringenin, and quercetin in LNQ-MF) resulted in 84.85% antioxidant activity at 100 µg/mL. The effects on Staphylococcus aureus and Salmonella enterica were synergistic with fractional inhibitory concentration indices of 0.87 and 0.71, respectively. LNQ-MF hindered the growth of S. aureus in milk (0.83-0.89 log scale) compared to the control. Co-delivered encapsulated flavonoids are a promising alternative to chemical preservatives.
Assuntos
Micelas , Quercetina , Quercetina/química , Ácido Oleico , Luteolina/farmacologia , Staphylococcus aureus , Flavonoides/químicaRESUMO
Leishmaniasis is an infectious disease that is often fatal in affected patients and represents a major public health problem. At present, no vaccine is available, and the drug treatments used are costly, long, and have numerous side effects, they also present variable effectiveness, frequent relapses, and a more and more marked resistance towards the parasites. Thus, new therapeutic strategies are urgently needed, and they are mainly based on the research of active natural products. The objective of our study is the chemical characterization and the quantification of the polyphenol contents contained in the EAF and EAT extracts of the Laperrine olive tree and the evaluation of their antileishmania effect against Leishmania infantum. The quantification of polyphenols, flavonoids and total tannins shows a higher content in the leaf extract. We find respectively 776.76±30.64 mg gallic acid equivalent/g DR; 114.35±14.12 mg quercetin equivalent/g DR and 214.89±.17 mg tannic acid equivalent/g DR.The chemical characterization of Olea europaea subsp. laperrinei extracts show the presence of numerous antileishmanial biomolecules such as oleuropein, hydroxytyrosol, rutin, gallic acid, cafeic acid, rosmarinic acid, and quercetin.In this context, we are testing the in vitro leishmanicidal effect of Laperrine olive tree extracts. The results obtained are promising and highlight the effectiveness of the tested extracts against the promastigote form of Leishmania infantum. Indeed, the LD50 is obtained with the leaf extract at a concentration of 7.52±2.71 µl/ml.
Assuntos
Leishmania infantum , Olea , Humanos , Quercetina/química , Olea/química , Extratos Vegetais/química , Antioxidantes , Polifenóis/farmacologia , Taninos , Ácido Gálico , Folhas de PlantaRESUMO
Colorectal cancer is among the frequently diagnosed cancers with high mortality rates around the world. Polyphenolic compounds such as flavonoids are secondary plant metabolites which exhibit anti-cancer activities along with anti-inflammatory effects. However, due to their hydrophobicity, sensitivity to degradation and low bioavailability, therapeutic effects have shown poor therapeutic effect. Nano delivery systems such as nanoliposomes, nanomicelles, silica nanoparticles have been investigated to overcome these difficulties. This review provides a summary of the efficiency of certain flavonoids and polyphenols (apigenin, genistein, resveratrol, quercetin, silymarin, catechins, luteolin, fisetin, gallic acid, rutin, and curcumin) on colorectal cancer models. It comprehensively discusses the influence of nano-formulation of flavonoids on their biological functions, including cellular uptake rate, bioavailability, solubility, and cytotoxicity, as well as their potential for reducing colorectal cancer tumor size under in vivo situations.
Assuntos
Neoplasias Colorretais , Nanopartículas , Humanos , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Flavonoides/química , Quercetina/química , Polifenóis/farmacologia , Polifenóis/uso terapêutico , Polifenóis/química , Nanopartículas/química , Neoplasias Colorretais/tratamento farmacológicoRESUMO
Edible electronics is a growing field that aims to produce digestible devices using only food ingredients and additives, thus addressing many of the shortcomings of ingestible electronic devices. Edible electronic devices will have major implications for gastrointestinal tract monitoring, therapeutics, as well as rapid food quality monitoring. Recent research has demonstrated the feasibility of edible circuits and sensors, but to realize fully edible electronic devices edible power sources are required, of which there have been very few examples. Drawing inspiration from living organisms, which use redox cofactors to power biochemical machines, a rechargeable edible battery formed from materials eaten in everyday life is developed. The battery is realized by immobilizing riboflavin and quercetin, common food ingredients and dietary supplements, on activated carbon, a widespread food additive. Riboflavin is used as the anode, while quercetin is used as the cathode. By encapsulating the electrodes in beeswax, a fully edible battery is fabricated capable of supplying power to small electronic devices. The proof-of-concept battery cell operated at 0.65 V, sustaining a current of 48 µA for 12 min. The presented proof-of-concept will open the doors to new edible electronic applications, enabling safer and easier medical diagnostics, treatments, and unexplored ways to monitor food quality.
Assuntos
Ingredientes de Alimentos , Quercetina/química , Eletrônica , Fontes de Energia ElétricaRESUMO
Okra pods have been utilized as a functional food due to their rich active ingredient composition, especially the high content of flavonoid compounds. This study conducted near-infrared spectroscopy (NIRS) modeling optimization and external validation based on the flavonoid components of 219 pod samples. Spectral correlation analyses identified two types of spectral response patterns classified as quercetin-3-O-xylose (1-2) glucoside (QOXG) and total flavonoid content (TFC), consisting of six different spectral regions. Different modeling effects were observed for QOXG and TFC with various spectral region combination analyses, where the lower wave-number region contributed more to both flavonoids calibration models. The combination of standard normal variate / "1, 9, 3" / partial least squares was found to be the most effective for developing calibration models for both flavonoids. The resulting models had small root mean square errors of prediction for external validation and high determination coefficients, indicating their usefulness for rapid prediction of flavonoid composition in okra pods.
Assuntos
Abelmoschus , Flavonoides , Flavonoides/análise , Abelmoschus/química , Quercetina/química , Antioxidantes/química , Extratos Vegetais/química , Análise dos Mínimos QuadradosRESUMO
Many of the medicinally active molecules in the flavonoid class of phytochemicals are being researched for their potential antiviral activity against various DNA and RNA viruses. Quercetin is a flavonoid that can be found in a variety of foods, including fruits and vegetables. It has been reported to be effective against a variety of viruses. This review, therefore, deciphered the mechanistic of how Quercetin works against some of the deadliest viruses, such as influenza A, Hepatitis C, Dengue type 2 and Ebola virus, which cause frequent outbreaks worldwide and result in significant morbidity and mortality in humans through epidemics or pandemics. All those have an alarming impact on both human health and the global and national economies. The review extended computing the Quercetin-contained natural recourse and its modes of action in different experimental approaches leading to antiviral actions. The gap in effective treatment emphasizes the necessity of a search for new effective antiviral compounds. Quercetin shows potential antiviral activity and inhibits it by targeting viral infections at multiple stages. The suppression of viral neuraminidase, proteases and DNA/RNA polymerases and the alteration of many viral proteins as well as their immunomodulation are the main molecular mechanisms of Quercetin's antiviral activities. Nonetheless, the huge potential of Quercetin and its extensive use is inadequately approached as a therapeutic for emerging and re-emerging viral infections. Therefore, this review enumerated the food-functioned Quercetin source, the modes of action of Quercetin for antiviral effects and made insights on the mechanism-based antiviral action of Quercetin.
Assuntos
Quercetina , Viroses , Humanos , Quercetina/farmacologia , Quercetina/uso terapêutico , Quercetina/química , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Alimento Funcional , Viroses/tratamento farmacológico , Antivirais/farmacologia , Antivirais/uso terapêutico , Antivirais/químicaRESUMO
Flavonoids are compounds abundantly found in nature and known as a polyphenolic group of compounds having flavancore and show the utmost abundant collection of complexes and are found in fiber-rich root vegetables, fruits, and their eatable items. Due to the presence of hydroxyl groups, flavonoids show various therapeutic activities like antioxidant, antibacterial, antiviral, and antiinflammatory. Substituent groups are responsible for the onset of biochemical actions of flavonoids, which affect the metabolism. The major example of flavonol is rutin, which is constituted of rutinose and quercetin. It is a glycosidic type of flavonoid, similarly identified as purple quercitrin and Vitamin P with over 70 plant species and plant-derived foods, exclusively grapefruit, buckwheat seeds, cherries, apricots, grapes, onions, plums, and oranges. Another name forrutin is a citrus flavonoid known as rutoside, and sophorin. Rutin is a polyphenolic compound having a low molecular weight.
Assuntos
Vias Biossintéticas , Rutina , Antioxidantes/metabolismo , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Quercetina/química , Rutina/química , Sementes/químicaRESUMO
To investigate the effects of structure, multiple binding sites and antioxidant property of Tartary buckwheat protein-phenols covalent complex, protein was combined with different concentrations of phenolic extract. Four kinds of phenols were identified by UPLC-Q/TOF-MS, which were rutin, quercetin, kaempferol and myricetin. UV-vis absorption spectroscopy and X-ray diffraction showed that the phenols can successfully bind to BPI. Fourier-transform infrared, circular dichroism and fluorescence emission spectroscopy showed that the binding of phenol can change the secondary/tertiary structure of protein. The particle distribution indicated that the binding of phenols could reduce the particle size (from 304.70 to 205.55 nm), but cross-linking occurred (435.35 nm) when the bound phenol content was too high. Proteomics showed that only rutin, quercetin and myricetin can covalently bind to BPI. Meanwhile, 4 peptides covalently bound to phenols were identified. The DPPH· scavenging capacity of complexes were from 8.38 to 33.76 %, and the ABTS·+ binding activity of complexes were from 19.35 to 63.99 %. The antioxidant activity of the complex was significantly higher than that of the pure protein. These results indicated that protein-phenol covalent complexes had great potential as functional components in the food field.
Assuntos
Antioxidantes , Fagopyrum , Antioxidantes/química , Quercetina/química , Fenóis/química , Fagopyrum/química , Fenol/metabolismo , Rutina/química , Sítios de LigaçãoRESUMO
Tartary buckwheat is rich in rutin, quercetin, and other flavonoids, which exert prominent effects by inhibiting non-enzymatic glycosylation. In this study, an in vitro non-enzymatic glycosylation model was established, and the inhibitory effects of rutin and quercetin on the early, middle, and late products of non-enzymatic glycosylation were determined. Furthermore, their effects on the formation of advanced glycation end products (AGEs) and on protein functional groups and secondary structure were analyzed. These findings provided a theoretical basis for further investigation of the mechanism via which Tartary buckwheat's rutin and quercetin inhibited non-enzymatic glycosylation. The results showed that rutin and quercetin inhibited the formation of fructosamine, dicarbonyl compounds, and fluorescent AGE in a concentration-dependent manner. Rutin and quercetin exhibited antioxidant activity and could reduce the formation of protein oxidation products. The highest clearance rates for DPPH and ABTS+ were 62.74 % and 71.14 %, respectively.
Assuntos
Fagopyrum , Rutina , Rutina/química , Quercetina/farmacologia , Quercetina/química , Fagopyrum/química , Reação de Maillard , Flavonoides/químicaRESUMO
In Tartary buckwheat (Fagopyrum tataricum), the edible parts are mainly grain and sprouts. Tartary buckwheat contains protecting substances, which make it possible for plants to survive on high altitudes and under strong natural ultraviolet radiation. The diversity and high content of phenolic substances are important for Tartary buckwheat to grow and reproduce under unfriendly environmental effects, diseases, and grazing. These substances are mainly flavonoids (rutin, quercetin, quercitrin, vitexin, catechin, epicatechin and epicatechin gallate), phenolic acids, fagopyrins, and emodin. Synthesis of protecting substances depends on genetic layout and on the environmental conditions, mainly UV radiation and temperature. Flavonoids and their glycosides are among Tartary buckwheat plants bioactive metabolites. Flavonoids are compounds of special interest due to their antioxidant properties and potential in preventing tiredness, diabetes mellitus, oxidative stress, and neurodegenerative disorders such as Parkinson's disease. During the processing and production of food items, Tartary buckwheat metabolites are subjected to molecular transformations. The main Tartary buckwheat traditional food products are bread, groats, and sprouts.