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1.
Physiol Rep ; 11(2): e15413, 2023 01.
Artigo em Inglês | MEDLINE | ID: mdl-36708512

RESUMO

Recently, the use of ergogenic aids in sports by both athletes and fans has increased. Moreover, the overall demand for new ergogenic aids has increased. Hesperidin is a polyphenol that is useful for improving exercise performance by activating energy generation through ß-oxidation and oxidative phosphorylation in skeletal muscles. However, it is difficult to use this compound as an ergogenic aid because of its poor water solubility and low bioavailability. Glucosyl hesperidin is formed when one molecule of glucose is transferred to hesperidin via glycosyl-transferase. It is 10,000× more soluble and has 3.7× higher bioavailability than hesperidin. In this study, we assessed whether continuous (14 days) intake of glucosyl hesperidin improves the aerobic exercise capacity of rats during long-term acute exercise. Although glucosyl hesperidin intake did not improve the performance of high-intensity running (30 m/min), we did observe improvement in low-intensity running (15 m/min) (p < 0.05). We demonstrate that in sedentary rats, glucosyl hesperidin intake increased ß-oxidation and oxidative phosphorylation in the skeletal muscle (p < 0.05 and p < 0.01, respectively). Glucosyl hesperidin intake may have created a metabolic state useful for long-term exercise. In conclusion, the continuous intake of glucosyl hesperidin improved the aerobic exercise capacity of rats during long-term acute exercise.


Assuntos
Hesperidina , Corrida , Ratos , Animais , Hesperidina/farmacologia , Glucosídeos , Fosforilação Oxidativa
2.
Molecules ; 28(2)2023 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-36677930

RESUMO

Hesperidin and narirutin are a class of flavanone glycosides, which are the main active constituents in Citrus reticulata Blanco. In the present study, a chiral HPLC-UV method with amylose tris(3,5-dimethylphenylcarbamate) as a stationary phase under a normal-phase mode was used to achieve the stereoselective separation of the C-2 diastereomers of hesperidin and narirutin simultaneously. The single epimer was then successfully prepared by applying semi-preparative chromatography, whose absolute configuration (R/S) was characterized by combining the experimental electronic circular dichroism (ECD) detection with time-dependent density functional theory (TDDFT) calculations. The epimer composition of these two chiral flavanone glycosides in Citrus reticulata Blanco was then determined, which was found to be slightly different in the herbs from different production regions. The anti-inflammatory activity of each prepared single epimer was further evaluated, and some differences between one pair of epimers of hesperidin and narirutin were observed, which suggested that the presence of different epimers should be considered in the quality evaluation and control of natural medicine.


Assuntos
Citrus , Flavanonas , Hesperidina , Hesperidina/química , Citrus/química , Estereoisomerismo , Flavanonas/química , Glicosídeos/química , Cromatografia Líquida de Alta Pressão
3.
Sci Rep ; 13(1): 158, 2023 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-36599902

RESUMO

Cyclophosphamide (CYP) is an alkylating agent that is used on a wide range as a treatment of malignancies and autoimmune diseases. Previous studies have shown the promising role of hesperidin (HSP) as an antioxidant agent against various models of toxic agents. The protective effect of the HSP against CYP-induced parotid damage was evaluated in this study. Forty rats (180-200 g) were divided into four equal groups: Group I (received normal saline), Group II (HSP-treated at a dose of 100 mg/kg/day for 7 consecutive days), Group III (CYP-treated at a dose of 200 mg/kg single intraperitoneal injection on the 7th day of the experiment), Group IV (CYP + HSP); HSP-treated at a dose of 100 mg/kg/day for 7 consecutive days and CYP (200 mg/kg) single intraperitoneal injection on the 7th day of the experiment. Afterwards, the oxidative stress and inflammatory markers, the histopathological and immunohistochemical alterations of the parotid tissues in the studied groups were evaluated. CYP intoxication induced a significant parotid tissue injury represented by the elevation in the values of malondialdehyde (MDA), tumor necrosis factor-α (TNF-α) and interleukin-1ß (IL-1ß) and decrease in the catalase activity and glutathione peroxidase (GPx). Histologically, extensive histopathological alterations e.g., widely spaced serous acini with irregular shapes and congested blood vessels as well as downregulated ki-67 and alpha-smooth muscle actin (α-SMA) immunoexpression were induced by CYP. HSP administration markedly improved the biochemical and the histopathological studies. We can conclude that HSP elicited protective effects against the CYP-induced parotid toxicity.


Assuntos
Hesperidina , Glândula Parótida , Animais , Ratos , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Ciclofosfamida/toxicidade , Hesperidina/farmacologia , Hesperidina/uso terapêutico , Estresse Oxidativo , Ratos Wistar , Glândula Parótida/lesões , Glândula Parótida/patologia
4.
Bioorg Chem ; 131: 106333, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36587504

RESUMO

Hesperidin (C28H34O15), a flavanone glycoside abundantly present in citrus fruits, has proven therapeutic effects including anti-inflammatory activities. Herein, we report a novel formulation of HESP loaded solid lipid nanoparticles (SLNs) using hot homogenization and ultrasound to improve the poor solubility and bioavailability. In the present study, the formulation was developed and optimized by response surface method and then characterized by scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy (FT-IR), and dynamic light scattering (DLS). Encapsulation efficiency was determined and the anti-inflammatory effect was assessed through in vivo ear edema inflammation model. According to the electron microscopy results, the product has a spherical shape. The optimized parameters produced small size (179.8 ± 3.6 nm) HESP-SLNs with high encapsulation efficiency (93.0 ± 3.8 %). The outcomes exhibited that encapsulation in SLNs carriers improves the anti-inflammatory potential of HESP.


Assuntos
Hesperidina , Nanopartículas , Hesperidina/farmacologia , Hesperidina/uso terapêutico , Lipídeos/química , Espectroscopia de Infravermelho com Transformada de Fourier , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Nanopartículas/química , Portadores de Fármacos/química
5.
Molecules ; 28(2)2023 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-36677929

RESUMO

Arthroplasty is an orthopedic surgical procedure that replaces a dysfunctional joint by an orthopedic prosthesis, thereby restoring joint function. Upon the use of the joint prosthesis, a wearing process begins, which releases components such as titanium dioxide (TiO2) that trigger an immune response in the periprosthetic tissue, leading to arthritis, arthroplasty failure, and the need for revision. Flavonoids belong to a class of natural polyphenolic compounds that possess antioxidant and anti-inflammatory activities. Hesperidin methyl chalcone's (HMC) analgesic, anti-inflammatory, and antioxidant effects have been investigated in some models, but its activity against the arthritis caused by prosthesis-wearing molecules, such as TiO2, has not been investigated. Mice were treated with HMC (100 mg/kg, intraperitoneally (i.p.)) 24 h after intra-articular injection of 3 mg/joint of TiO2, which was used to induce chronic arthritis. HMC inhibited mechanical hyperalgesia, thermal hyperalgesia, joint edema, leukocyte recruitment, and oxidative stress in the knee joint (alterations in gp91phox, GSH, superoxide anion, and lipid peroxidation) and in recruited leukocytes (total reactive oxygen species and GSH); reduced patellar proteoglycan degradation; and decreased pro-inflammatory cytokine production. HMC also reduced the activation of nociceptor-sensory TRPV1+ and TRPA1+ neurons. These effects occurred without renal, hepatic, or gastric damage. Thus, HMC reduces arthritis triggered by TiO2, a component released upon wearing of prosthesis.


Assuntos
Artrite , Chalconas , Hesperidina , Camundongos , Animais , Nociceptores/metabolismo , Chalconas/uso terapêutico , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Artrite/tratamento farmacológico , Estresse Oxidativo , Antioxidantes/farmacologia , Anti-Inflamatórios/farmacologia , Hiperalgesia/tratamento farmacológico , Citocinas/metabolismo
6.
Biochim Biophys Acta Mol Basis Dis ; 1869(2): 166620, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36494040

RESUMO

Obesity has become an increasingly serious health issue with the continuous improvement in living standards. Its prevalence has become an economic burden on health care systems worldwide. Flavonoids have been shown to be beneficial in the prevention and treatment of obesity. Here, we evaluated the therapeutic potential of the flavonoid hesperidin methyl chalcone (HMC) on mice with high-fat diet (HFD)-induced hepatic steatosis in vivo and in vitro. Treatment with HMC reduced oleic and palmitic acid-induced increases in intracellular triglyceride accumulation in HepG2, AML12 and LMH cells. HMC also enhanced energy metabolism and lowered oxidative stress. We used Discovery studio to dock key proteins associated with lipid metabolism disorders to HMC, and found that HMC interacted with lipase. Furthermore, we demonstrated that HMC improved lipase activity and lipolysis. In addition, we found that HMC promoted glucose absorption, alleviated lipid metabolic disorders, improved HFD-induced liver injury, and regulated HFD-induced changes in energy metabolism. In conclusion, our study demonstrated that HMC ameliorated HFD-induced obesity and its complications by promoting lipase activity, and provides a novel approach for the prevention and treatment of obesity and related diseases.


Assuntos
Chalconas , Hesperidina , Transtornos do Metabolismo dos Lipídeos , Camundongos , Animais , Hesperidina/farmacologia , Hesperidina/uso terapêutico , Chalconas/farmacologia , Obesidade/metabolismo , Flavonoides/uso terapêutico , Metabolismo Energético , Lipase/metabolismo , Lipídeos
7.
Life Sci ; 313: 121280, 2023 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-36526046

RESUMO

Hepatic encephalopathy (HE) is a serious neurological disorder which might occur in both acute and chronic liver injury. AIMS: This study was carried out to explore the protective effects of hesperidin against experimentally induced HE. MAIN METHODS: Rats were sorted into four groups each of six; Normal group, TAA group: rats were administered 350 mg/kg of TAA i.p. from day 5 to day 7. TAA+ Hesp 100 group: rats were administered hesperidin 100 mg/kg/day orally for 7 days along with i.p TAA injection 350 mg/kg from day 5 to 7. TAA+ Hesp 200 group: rats were administered hesperidin 200 mg/kg/day orally for 7 days along with i.p TAA injection 350 mg/kg from day 5 to 7. Liver function, oxidative stress biomarkers, behavioral tests in addition to histopathological examination were assessed. KEY FINDINGS: Hesperidin efficiently mitigated TAA-induced HE as evidenced by significant reduction in liver enzymes, bile and ammonia levels in serum. Moreover, hesperidin restored oxidant/antioxidant balance as manifested by reduction in MDA content in both cerebral and hepatic tissues. Additionally, hesperidin improved motor and cognitive abilities besides tissues' architecture as demonstrated by behavioral tests and histopathology results, respectively. Hesperidin also decreased levels of NLRP3 and increased levels of Sirt1 and FOXO in both cerebral and hepatic tissues. Finally, hesperidin markedly decreased the expression of IL-1ß and caspase-1 as shown by immunohistochemical results. SIGNIFICANCE: Taken together, the hepatoprotective impact of hesperidin and its ameliorative effect on the progression of HE appear to be mediated by its modulatory influence on NLRP3/Sirt1/FOXO signaling.


Assuntos
Encefalopatia Hepática , Hesperidina , Ratos , Animais , Encefalopatia Hepática/induzido quimicamente , Encefalopatia Hepática/tratamento farmacológico , Encefalopatia Hepática/prevenção & controle , Hesperidina/farmacologia , Hesperidina/uso terapêutico , Tioacetamida/toxicidade , Sirtuína 1/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Ratos Wistar , Fígado/metabolismo , Estresse Oxidativo , Cognição
8.
Comput Biol Med ; 152: 106392, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36502697

RESUMO

COVID-19 caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) emerged first around December 2019 in the city of Wuhan, China. Since then, several variants of the virus have emerged with different biological properties. This pandemic has so far led to widespread infection cycles with millions of fatalities and infections globally. In the recent cycle, a new variant omicron and its three sub-variants BA.1, BA.2 and BA.3 have emerged which seems to evade host immune defences and have brisk infection rate. Particularly, BA.2 variant has shown high transmission rate over BA.1 strain in different countries including India. In the present study, we have evaluated a set of eighty drugs/compounds using in silico docking calculations in omicron and its variants. These molecules were reported previously against SARS-CoV-2. Our docking and simulation analyses suggest differences in affinity of these compounds in omicron and BA.2 compared to SARS-CoV-2. These studies show that neohesperidin, a natural flavonoid found in Citrus aurantium makes a stable interaction with spike receptor domain of omicron and BA.2 compared to other variants. Free energy binding analyses further validates that neohesperidin forms a stable complex with spike RBD in omicron and BA.2 with a binding energy of -237.9 ± 18.7 kJ/mol and -164.1 ± 17.5 kJ/mol respectively. Key residual differences in the RBD interface of these variants form the basis for differential interaction affinities with neohesperidin as drug binding site overlaps with RBD-human ACE2 interface. These data might be useful for the design and development of novel scaffolds and pharmacophores to develop specific therapeutic strategies against these novel variants.


Assuntos
COVID-19 , Hesperidina , Humanos , SARS-CoV-2 , Simulação por Computador
9.
Exp Gerontol ; 172: 112064, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36528304

RESUMO

Hesperidin possesses myriads of pharmacological benefits, including anti-inflammatory and antioxidant properties. Herein, we speculated that the described pharmacological benefits of hesperidin might be due to its potentiating action on SIRT1; thereby, inhibition of NOX4. We developed diabetic neuropathy in Sprague-Dawley rats by feeding them a high-fat diet (HFD) for 12 weeks. We checked the effect of hesperidin on the level of oxidative stress, inflammatory markers, NOX4, and SIRT1 by biochemical analysis, histopathology, immunoblotting, immunocytochemistry, and real-time qPCR in HFD-fed rats and Palmitate encountered rat glial C6 cells. Hesperidin administration improved mechanical, thermal allodynia, and glucose homeostasis. There was a decrease in oxidative stress and inflammation and an enhanced level of antioxidant enzymes. Besides, the expression of NOX4 was down-regulated, while SIRT1 was upregulated. Interestingly, hesperidin treatment protected them from oxidative and inflammatory damage by upregulating SIRT1 and inhibiting NOX4 expression.


Assuntos
Diabetes Mellitus , Neuropatias Diabéticas , Hesperidina , Ratos , Animais , Antioxidantes/metabolismo , Hesperidina/farmacologia , Sirtuína 1/metabolismo , Neuropatias Diabéticas/tratamento farmacológico , Ratos Sprague-Dawley , Estresse Oxidativo , Inflamação/tratamento farmacológico , Dieta Hiperlipídica/efeitos adversos , NADPH Oxidase 4/genética
10.
Food Res Int ; 162(Pt A): 111983, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36461226

RESUMO

Effects of sweetener neomethyl hesperidin dihydrochalcone (NHDC) on the gelation properties of myofibrillar protein (MP) at 0.2 M and 0.6 M NaCl were investigated. The results showed that addition of NHDC did not obviously change the cooking loss and strength of MP gels at 0.2 M NaCl. Whilst at 0.6 M NaCl, addition of high doses of NHDC (50-100 µM/g) remarkably increased cooking loss and decreased strength of MP gels. The expanded MP enhanced the interactions between NHDC and MP, leading to aggregation of MP as evidenced by the increasing particle size and the reducing solubility. The MP aggregates impeded hydrophobic interactions and disulfide bonds crosslinking in the gelation process, thereby damaged the gelation properties of MP at 0.6 M NaCl. This was supported by the poor network of MP gels observed by SEM. In the end, molecular docking elucidated the main types of interaction at molecular level, including hydrogen bonding and hydrophobicity. The results would provide guidance for NHDC as a potential sweetener in meat products.


Assuntos
Hesperidina , Carne de Porco , Carne Vermelha , Suínos , Animais , Cloreto de Sódio , Simulação de Acoplamento Molecular , Excipientes , Edulcorantes
11.
Food Res Int ; 162(Pt B): 112059, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36461387

RESUMO

The present study examined the relationship between the anti-diabetic effect of hesperidin (HES) and the differential gene expression in HES treated high fat diet (HFD)-induced obese mice. Based on the glucose uptake assay, the treatment of HES restored the glucose uptake to control level in an insulin-independent manner in PA-treated HepG2 cells. Western blot analysis confirmed that the treatment of HES increased the insulin-stimulated phosphorylation of Akt and GSK3ß in insulin-resistant PA-treated HepG2 cells. HFD-induced obese mice treated with HES significantly reduced serum insulin, blood glucose, and homeostatic model assessment for insulin resistance (HOMA-IR) values. In addition, both glucose tolerance and insulin tolerance were significantly improved to normal level by HES in HFD-induced obese mice. RNA sequencing analysis disclosed that the expression levels of up-regulated 12 genes and down-regulated 6 genes related to insulin signaling and glucose metabolism were restored to normal level by HES in the liver of HFD-induced obese mice. A protein-protein interaction (PPI) network was constructed via search tool for the retrieval of interacting genes/proteins (STRING) analysis, and Eno1, Pik3cd, Hk2, Trib3, Myc, Nos3, Ppargc1a, and Igf2 were located in the functional hubs of the PPI network of glucose metabolism. Furthermore, Western blot analysis confirmed that HES improved insulin sensitivity and glucose homeostasis by normalizing the expression levels of hexokinase-II, enolase-1, and PI3 kinase p110δ to normal level. The overall results suggest that HES possess a potential anti-diabetic effect by normalizing the expression levels of the insulin signaling and glucose metabolism related genes which were perturbed in the liver of HFD-induced obese mice.


Assuntos
Hesperidina , Resistência à Insulina , Animais , Camundongos , Humanos , Camundongos Obesos , Dieta Hiperlipídica/efeitos adversos , Células Hep G2 , Palmitatos , Hesperidina/farmacologia , Insulina , Glicemia
12.
Medicine (Baltimore) ; 101(48): e32127, 2022 Dec 02.
Artigo em Inglês | MEDLINE | ID: mdl-36482520

RESUMO

INTRODUCTION: Globally, the number of patients with primary biliary cholangitis (PBC) is increasing. Growing evidence suggests that oxidative stress plays a significant role in the pathogenesis of chronic liver disease regardless of its etiology. Hesperidin, a natural antioxidative substance derived from citrus peel, has been shown to have an anti-inflammatory effect in a rat arthritis model and may be a potential substance to attenuate intrahepatic inflammation in patients with PBC. In this study, the potential of glucosyl hesperidin as a therapeutic agent for PBC will be investigated through antioxidative stress mechanisms. METHODS: Patients with PBC who are 20 years or older will be eligible to participate. Patients will be assigned to 1 of 2 groups and given either 500 or 1000 mg of glucosyl hesperidin per day. The primary endpoint is the ratio of changes in serum gamma-glutamyl transferase levels before and after 24 weeks of glucosyl hesperidin administration. The secondary endpoints are serum hepatobiliary enzyme levels (alkaline phosphatase, transaminase, and total bilirubin levels) and the protein expression levels of nuclear factor erythroid 2-related factor 2 and its target molecule 8, 16, and 24 weeks after administration compared to before administration. DISCUSSION: The prospective clinical interventional study was designed to assess the supportive effect of glucosyl hesperidin on hepatic function in patients with PBC receiving basic ursodeoxycholic acid treatment.


Assuntos
Hesperidina , Cirrose Hepática Biliar , Adulto , Humanos , Cirrose Hepática Biliar/tratamento farmacológico , Estudos Prospectivos , Transaminases , Ensaios Clínicos Controlados Aleatórios como Assunto , Estudos Multicêntricos como Assunto , Hesperidina/uso terapêutico
13.
Biomolecules ; 12(12)2022 12 17.
Artigo em Inglês | MEDLINE | ID: mdl-36551321

RESUMO

The aim of this study was to establish the influence of flavonoid-enriched diets on the immune alterations induced by an intensive training and a final exhaustion test in rats. A flavanol-enriched diet (with 10% cocoa, C10 diet) and a flavanol and flavanone-enriched diet (C10 plus 0.5% hesperidin, CH diet) were used. Lewis rats were fed either a standard diet, C10 diet or CH diet while they were submitted to an intensive running training on a treadmill. After 6 weeks, samples were obtained 24 h after performing a regular training (T groups) and after carrying out a final exhaustion test (TE groups). The C10 diet attenuated the increase in plasma cortisol induced by exhaustion, while both the C10 and the CH diets prevented the alterations in the spleen Th cell proportion. The experimental diets also induced an increase in serum immunoglobulin concentration and an enhancement of spleen natural killer cytotoxicity, which may be beneficial in situations with a weakened immunity. Most of the effects observed in the CH groups seem to be due to the cocoa content. Overall, a dietary intervention with flavonoids enhances immune function, partially attenuating the alterations in systemic immunity induced by intensive training or exhausting exercise.


Assuntos
Cacau , Hesperidina , Ratos , Animais , Flavonoides/farmacologia , Hesperidina/farmacologia , Ratos Endogâmicos Lew , Dieta
14.
Nutrients ; 14(24)2022 Dec 11.
Artigo em Inglês | MEDLINE | ID: mdl-36558440

RESUMO

Gastric cancer is a common malignant tumor worldwide. N-methyl-N-nitro-N-nitroguanidine (MNNG) is one of the most important inducing factors of gastric cancer. Autophagy can affect the occurrence and development of gastric cancer, but the mechanism is not clear. Chemoprevention has been shown to be a rational and very promising approach to the prevention of gastric cancer. Hesperidin is a citrus flavone, an abundant polyphenol in citrus fruits and traditional Chinese medicine. It has an excellent phytochemistry that plays an intervention role in gastric cancer. However, it is unclear whether long-term exposure to MNNG will affect the occurrence of gastric cancer by regulating autophagy and whether hesperidin can play an intervention role in this process. In the present study, we demonstrated that long-term MNNG exposure inhibits autophagy in stomach tissues of rats, promotes the epithelial-mesenchymal transition (EMT) process and cell proliferation and suppresses the activity of the PI3K/AKT pathway. We further found that after rapamycin-activated autophagy, long-term MNNG exposure promoted cell proliferation and EMT were inhibited. In addition, hesperidin promotes autophagy and the activity of the PI3K/AKT pathway, as well as the suppression of proliferation and EMT in the stomach tissues of rats. Our findings indicate that hesperidin reverses MNNG-induced gastric cancer by activating autophagy and the PI3K/AKT pathway, which may provide a new basis for the early prevention and treatment of MNNG-induced gastric cancer.


Assuntos
Hesperidina , Neoplasias Gástricas , Animais , Ratos , Autofagia , Proliferação de Células , Transição Epitelial-Mesenquimal , Hesperidina/farmacologia , Metilnitronitrosoguanidina/toxicidade , Fosfatidilinositol 3-Quinases , Proteínas Proto-Oncogênicas c-akt/metabolismo , Neoplasias Gástricas/induzido quimicamente , Neoplasias Gástricas/tratamento farmacológico , Neoplasias Gástricas/prevenção & controle
15.
J Agric Food Chem ; 70(47): 14831-14840, 2022 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-36383360

RESUMO

Hesperetin-7-O-glucoside (Hes-7-G) is a typical flavonoid monoglucoside, which can be generated from hesperidin with the removal of rhamnose by hydrolysis. Untargeted and targeted metabolomics together with 16S rRNA gene sequencing were employed to explore the exact absorption site of Hes-7-G and its beneficial effect in mice. Intestinal 1H nuclear magnetic resonance (NMR)-based metabolomics screening showed that Hes-7-G is mainly metabolized in the small intestine of mice, especially the ileum segment. Quantification analysis of bile acids (BAs) in the liver, intestinal tract, feces, and serum of mice suggests that Hes-7-G intake accelerates the processes of biosynthesis and excretion of BAs, thus promoting digestion and lowing hepatic cholesterol and triglyceride. 16S rRNA gene sequencing reveals that Hes-7-G significantly elevates the diversity of the gut microbiota in mice, especially those bacteria associated with BA secondary metabolism. These results demonstrated that long-term dietary Hes-7-G plays beneficial roles in health by modulating the gut bacteria and BA metabolism in mice.


Assuntos
Microbioma Gastrointestinal , Hesperidina , Camundongos , Animais , Microbioma Gastrointestinal/genética , Hesperidina/metabolismo , RNA Ribossômico 16S/genética , Ácidos e Sais Biliares/metabolismo , Fígado/metabolismo , Bactérias/genética , Bactérias/metabolismo , Glucosídeos/metabolismo , Camundongos Endogâmicos C57BL
16.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao ; 44(5): 777-784, 2022 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-36325774

RESUMO

Objective To explore the effect and mechanism of hesperidin in treating the lung injury in the mouse model of respiratory syncytial virus (RSV)-induced bronchiolitis. Methods A mouse model of RSV-induced bronchiolitis was established,and 60 BALB/c mice were assigned into a control group,a model group,a low-dose hesperidin (18 mg/kg) group,a high-dose hesperidin (36 mg/kg) group,and a high-dose hesperidin (36 mg/kg)+Jagged1(1 mg/kg) group by random number table method,with 12 mice in each group. Corresponding doses of drugs were administrated for intervention,and the control group and model group were administrated with the same amount of saline.The bronchoalveolar lavage fluid (BALF) samples were collected and alveolar macrophages were isolated.ELISA was employed to detect the levels of interleukin (IL)-4,IL-6,tumor necrosis factor-α (TNF-α),and IL-10 in BALF,and flow cytometry to detect the M1/M2 polarization of macrophages.qRT-PCR and Western blotting were respectively conducted to detect the mRNA and protein levels of inducible nitric oxide synthase (iNOS),arginase 1 (Arg-1),Jagged1,and Notch1 in the lung tissue. Results Compared with the control group,the modeling of RSV-induced bronchiolitis elevated the IL-4,IL-6,and TNF-α levels,increased the proportion of M1-type macrophages and the lung inflammation and mucus secretion scores,and up-regulated the mRNA and protein levels of iNOS,Jagged1,and Notch1 in BALF (all P<0.001).Meanwhile,the modeling lowered the IL-10 level,decreased the proportion of M2-type macrophages,and down-regulated the mRNA and protein levels of Arg-1 (all P<0.001).Compared with the model group,low- and high-dose hesperidin lowered the IL-4,IL-6,TNF-α levels,decreased the proportion of M1-type macrophages and the lung inflammation and mucus secretion scores,and down-regulated the mRNA and protein levels of iNOS,Jagged1,and Notch1 in BALF (all P<0.05).Moreover,hesperidin elevated the IL-10 level,increased the proportion of M2-type macrophages,and up-regulated the mRNA and protein levels of Arg-1 (all P<0.001).Using recombinant Jagged1 protein to activate Notch1 signaling pathway can significantly attenuate the promotion of high-dose hesperidin on M2 macrophage polarization and amelioration of lung inflammation damage (all P<0.01). Conclusion Hesperidin may alleviate the lung inflammation damage in mice with RSV-induced bronchiolitis by inhibiting the Jagged1/Notch1 signaling pathway and promoting the M2-type polarization of macrophages.


Assuntos
Bronquiolite , Hesperidina , Lesão Pulmonar , Animais , Camundongos , Bronquiolite/metabolismo , Hesperidina/farmacologia , Hesperidina/uso terapêutico , Hesperidina/metabolismo , Interleucina-10/metabolismo , Interleucina-10/farmacologia , Interleucina-4/metabolismo , Interleucina-4/farmacologia , Interleucina-6/metabolismo , Proteína Jagged-1/metabolismo , Proteína Jagged-1/farmacologia , Lesão Pulmonar/metabolismo , Macrófagos , Camundongos Endogâmicos BALB C , RNA Mensageiro/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
17.
Nutrients ; 14(20)2022 Oct 16.
Artigo em Inglês | MEDLINE | ID: mdl-36297009

RESUMO

Obesity is an established risk factor for metabolic disease. This study explores the functional complementation of anti-adipogenic phytonutrients for obesity prevention and management. Nine phytonutrients were selected based on their ability to affect the expression of one or more selected adipogenic biomarker proteins. The phytonutrients include berberine, luteolin, resveratrol, fisetin, quercetin, fucoidan, epigallocatechin gallate, hesperidin, and curcumin. The selected adipogenic biomarker proteins include PPARÉ£, SREBP1c, FASN, PLIN1, FABP4, and ß-catenin. Individually, phytonutrients had variable effects on the expression level of selected adipogenic biomarker proteins. Collectively, the functional complementation of nine phytonutrients suppressed de novo fatty acid biosynthesis via the negative regulation of PPARÉ£, FASN, PLIN1, and FABP4 expression; activated glycolysis via the positive regulation of SREBP1c expression; and preserved cell-cell adhesion via the inhibition of ß-catenin degradation. In primary human subcutaneous preadipocytes, the composition of nine phytonutrients had more potent and longer lasting anti-adipogenic effects compared to individual phytonutrients. In a diet-induced obesity murine model, the composition of nine phytonutrients improved glucose tolerance and reduced weight gain, liver steatosis, visceral adiposity, circulating triglycerides, low-density lipoprotein cholesterol, and inflammatory cytokines and chemokines. The functional complementation of anti-adipogenic phytonutrients provides an effective approach toward engineering novel therapeutics for the prevention and management of obesity and metabolic syndrome.


Assuntos
Obesidade , Compostos Fitoquímicos , Animais , Humanos , Camundongos , Adipócitos , Adipogenia , Berberina/farmacologia , beta Catenina/metabolismo , Colesterol/metabolismo , Curcumina/farmacologia , Citocinas/metabolismo , Ácidos Graxos/metabolismo , Glucose/metabolismo , Hesperidina/farmacologia , Lipoproteínas LDL/metabolismo , Luteolina/farmacologia , Obesidade/prevenção & controle , Obesidade/metabolismo , Compostos Fitoquímicos/farmacologia , PPAR gama/metabolismo , Quercetina/farmacologia , Resveratrol/farmacologia , Proteína de Ligação a Elemento Regulador de Esterol 1/metabolismo , Triglicerídeos/metabolismo
18.
Ceska Slov Farm ; 71(4): 137-141, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36208917

RESUMO

Metabolic syndrome is diagnosed mainly in people of economically developed parts of the world and it affects 20-25% of the adult population worldwide. Nowadays, it is also more frequently diagnosed in children and adolescents. In addition to standard treatment that often involves polypharmacotherapy, and thus increases risk of side effects caused by drugdrug interactions, it is appropriate to look for alternative tools to support the treatment of metabolic syndrome components. Natural polyphenolic compounds, usually present in the so-called functional foods, are suitable candidates for that matter, due to the bioactivity and beneficial effects on the human body. Quercetin, troxerutin, diosmin, hesperidin or silybin are among the currently studied and used natural polyphenolic compounds with a positive effect on aspects of the metabolic syndrome. In addition to their antioxidant and anti-inflammatory effects, these compounds have other positive properties that very often outweigh their side effects whilst their usage in the pharmacotherapy.


Assuntos
Diosmina , Hesperidina , Síndrome Metabólica , Adolescente , Adulto , Anti-Inflamatórios , Antioxidantes/efeitos adversos , Criança , Diosmina/uso terapêutico , Hesperidina/uso terapêutico , Humanos , Síndrome Metabólica/tratamento farmacológico , Quercetina , Silibina/uso terapêutico
19.
Artigo em Russo | MEDLINE | ID: mdl-36279373

RESUMO

Postthrombophlebitic syndrome (PTPS) develops in 20-50% of patients who have had deep vein thrombosis (DVT). Patients with chronic venous insufficiency (CVI) of class C4-C5 according to the CEAP clinical classification, which developed as a result of DVT of the lower extremities, including those who underwent endovascular treatment (iliac vein stenting), are subject to staged medical rehabilitation. In this regard, the development of personalized complex technologies for the sanatorium treatment of patients with PTPS is an important medical and social problem. PURPOSE OF THE STUDY: Study of clinical efficacy and identification of the mechanisms of action of a new complex of spa treatment of patients with PTPS of the lower extremities using supravenous laser radiation, low-frequency magnetotherapy, dry-air carbon dioxide baths and structured therapeutic exercises in the gym. MATERIAL AND METHODS: 60 patients with PTPS of the lower extremities (CVI C4-C5 according to CEAP) were under observation. All patients were randomly divided into 2 groups: first group (main group) included 30 patients who received a treatment, including procedures for supravascular laser blood irradiation, pulsed magnetotherapy and dry-air carbon dioxide baths, as well as structured therapeutic exercises in gym under the supervision of an exercise therapy instructor; second group (control group) included 30 patients who received standard elastic compression (compression class 2-3) while taking lymphovenotonics (a combination of diosmin and hesperidin) and therapeutic exercises in the gym. RESULTS: Against the background of the course of treatment in patients of the main group, to a greater extent than in the control group, a decrease in the clinical symptoms of the disease was noted: a more pronounced regression of edema, a decrease in heaviness in the legs, as evidenced by the data of anthropometric studies and questionnaires on the CIVIQ-2 scale. Positive dynamics in the microcirculation system (MC) was established, which was confirmed by the data of laser Doppler flowmetry. In patients with spastic-congestive type of MC, a decrease in the initially increased myogenic and neurogenic tone of arterioles was registered. There was a decreasing of stagnation in the venular link. In patients with hyperemic-congestive type of MC, the initially reduced tone of arterioles increased, which contributed to the improvement of blood flow in the capillaries. There was also a decrease in congestion in the venular link of the microvasculature. CONCLUSION: A new effective complex method for the rehabilitation of patients with PTPS has been developed, including laser exposure according to the general method, pulsed magnetotherapy and dry-air carbon dioxide baths, which have a multifocal effect on different links in the pathogenesis of PTPS.


Assuntos
Diosmina , Hesperidina , Insuficiência Venosa , Humanos , Diosmina/uso terapêutico , Hesperidina/uso terapêutico , Dióxido de Carbono/uso terapêutico , Insuficiência Venosa/terapia , Fluxometria por Laser-Doppler , Síndrome
20.
J Mol Model ; 28(11): 365, 2022 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-36274116

RESUMO

Dengue fever has been a global health concern. Mitigation is a challenging problem due to non-availability of workable treatments. The most difficult objective is to design a perfect anti-dengue agent capable of inhibiting infections caused by all four serotypes. Various tactics have been employed in the past to discover dengue antivirals, including screening of chemical compounds against dengue virus enzymes. The objective of the current study is to investigate phytocompounds as anti-dengue remedies that target the non-structural 2B and non-structural 3 protease (NS2B-NS3pro), a possible therapeutic target for dengue fever. Initially, 300 + antiviral phytocompounds were collected from Duke's phytochemical and ethnobotanical database and 30 phytocompounds with anti-dengue properties were identified from previously reported studies, which were virtually screened against NS2B-NS3pro using molecular docking and toxicity evaluation. The top five most screened ligands were naringin, hesperidin, gossypol, maslinic acid and rhodiolin with binding affinities of - 8.7 kcal/mol, - 8.5 kcal/mol, - 8.5 kcal/mol, - 8.5 kcal/mol and - 8.1 kcal/mol, respectively. The finest docked compounds complexed with NS2B-NS3pro were subjected for molecular dynamics (MD) simulations and binding free energy estimations through molecular mechanics generalized born surface area-based calculations. The results of the study are intriguing in the context of computer-aided screening and the binding affinities of the phytocompounds, proposing maslinic acid (MAS) as a potent bioactive antiviral for the development of phytocompound-based anti-dengue agent.


Assuntos
Vírus da Dengue , Dengue , Gossipol , Hesperidina , Humanos , Simulação de Acoplamento Molecular , Antivirais/farmacologia , Antivirais/química , Simulação de Dinâmica Molecular , Proteínas não Estruturais Virais/química , Vírus da Dengue/metabolismo , Peptídeo Hidrolases/metabolismo , Compostos Fitoquímicos , Dengue/tratamento farmacológico , Inibidores de Proteases/farmacologia , Inibidores de Proteases/química
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