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https://www.readbyqxmd.com/read/29346059/fermented-extraction-of-citrus-unshiu-peel-inhibits-viability-and-migration-of-human-pancreatic-cancers
#1
Jungwhoi Lee, Jungsul Lee, Myungseung Kim, Jae Hoon Kim
Pancreatic cancer is one of the most dangerous cancers with high mortality rates. Despite continuous efforts, there has been limited improvement in its prognosis. In this study, we prepared fermented extract of Citrus unshiu peel (fCUP) from the by-product after juice processing and then examined the anticancer effects of fCUP on human pancreatic cancer cells. Treatment with fCUP inhibited the growth of human pancreatic cancer cells through induction of caspase-3 cleavage both in vitro and in vivo. Treatment with fCUP also blocked the migration of human pancreatic cancer cells through activation of intracellular signaling pathways such as MKK3/6 and P38...
January 2018: Journal of Medicinal Food
https://www.readbyqxmd.com/read/29337219/citrus-bioflavonoid-hesperetin-as-inhibitor-of-two-thrombin-like-snake-venom-serine-proteases-isolated-from-crotalus-simus
#2
Roney Vander Dos Santos, Fabian Villalta-Romero, Danijela Stanisic, Luiz Borro, Goran Neshich, Ljubica Tasic
Around 5.5 million people suffer from snakebites per year, with about 400,000 cases with some type of sequelae, such as amputation, and 20,000 to 125,000 cases with the fatal end. Usually, the victim outcome depends on correct, agile and many times in situ intervention based on the proper identification of the snake venom type and its potential effects, among other factors. Therefore, knowledge on the snake venom composition and a research on inhibitors of snake venom target components might ameliorate envenoming dangerous outcome...
January 11, 2018: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/29334238/chemical-constituents-from-the-flowers-of-satsuma-mandarin-and-their-free-radical-scavenging-and-%C3%AE-glucosidase-inhibitory-activities
#3
Anjana Adhikari-Devkota, Sara Mustafa Idris Elbashir, Takashi Watanabe, Hari Prasad Devkota
Flowers of Citrus plants are used as mild sedatives and for the treatment of insomnia in traditional medicines. In Japan, tea made from the flowers of Satsuma mandarin is consumed as healthy drink. Hesperidin (1), hesperetin (2), rutin (3), quercetin (4), nicotiflorin (5), eriocitrin (6), narirutin (7), phenylethyl glucoside (8) and unshuoside A (9) were isolated from the MeOH extract of fresh flowers. Structure elucidation of these compounds was performed on the basis of NMR spectroscopic data. Among them, rutin (3), quercetin (4) and eriocitrin (6) showed potent free radical scavenging activity, whereas hesperetin (2) and quercetin (4) showed potent α-glucosidase inhibitory activity...
January 15, 2018: Natural Product Research
https://www.readbyqxmd.com/read/29224841/metal-ion-improved-complexation-countercurrent-chromatography-for-enantioseparation-of-dihydroflavone-enantiomers
#4
Chao Han, Wenli Wang, Guimin Xue, Dingqiao Xu, Tianyu Zhu, Shanshan Wang, Pei Cai, Jianguang Luo, Lingyi Kong
Cu(II) ion was selected as an additive to improve the enantioseparation efficiency of three dihydroflavone enantiomers in high-speed counter-current chromatography (HSCCC), using hydroxypropyl-β-cyclodextrin (HP-β-CyD) as the chiral selector. The influences of important parameters, including the metal ion, the concentrations of HP-β-CyD and the Cu(II) ion, and the sample size were investigated. Under optimal conditions, three dihydroflavone enantiomers, including (±)-hesperetin, (±)-naringenin, and (±)-farrerol, were successfully enantioseparated...
December 6, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29211032/bioavailability-of-bergamot-citrus-bergamia-flavanones-and-biological-activity-of-their-circulating-metabolites-in-human-pro-angiogenic-cells
#5
Valentina Spigoni, Pedro Mena, Federica Fantuzzi, Michele Tassotti, Furio Brighenti, Riccardo C Bonadonna, Daniele Del Rio, Alessandra Dei Cas
Myeloid angiogenic cells (MACs) play a key role in endothelial repairing processes and functionality but their activity may be impaired by the lipotoxic effects of some molecules like stearic acid (SA). Among the dietary components potentially able to modulate endothelial function in vivo, (poly)phenolic compounds represent serious candidates. Here, we apply a comprehensive multidisciplinary approach to shed light on the prospects of Bergamot (Citrus bergamia), a citrus fruit rich in flavanones and other phenolic compounds, in the framework of lipotoxicity-induced MACs impairment...
December 6, 2017: Nutrients
https://www.readbyqxmd.com/read/29160087/glyoxalase-1-modulation-in-obesity-and-diabetes
#6
Naila Rabbani, Paul J Thornalley
SIGNIFICANCE: Obesity and type 2 diabetes mellitus are increasing globally. There is also increasing associated complications, such as non-alcoholic fatty liver disease (NAFLD) and vascular complications of diabetes. There is currently no licensed treatment for NAFLD and no recent treatments for diabetic complications. New approaches are required, particularly those addressing mechanism-based risk factors for health decline and disease progression. Recent Advances: Dicarbonyl stress is the abnormal accumulation of reactive dicarbonyl metabolites such as methylglyoxal (MG) leading to cell and tissue dysfunction...
January 2, 2018: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/29138782/vasorelaxant-activity-of-twenty-one-physiologically-relevant-poly-phenolic-metabolites-on-isolated-mouse-arteries
#7
E Van Rymenant, C Grootaert, K Beerens, P W Needs, P A Kroon, A Kerimi, G Williamson, R García-Villalba, A González-Sarrías, F Tomas-Barberan, J Van Camp, J Van de Voorde
Polyphenols are beneficial for health, but are metabolised after consumption. We compared the vasorelaxant capacity of twenty-one physiologically relevant polyphenol metabolites in isolated mouse arteries. Hesperetin, urolithins and ferulic acid-4-O-sulfate - not their glucuronidated forms or ferulic acid - caused vasorelaxation. Therefore, we advise the use of relevant conjugates in future mechanistic research.
November 15, 2017: Food & Function
https://www.readbyqxmd.com/read/29136946/neuroprotective-effect-of-hesperetin-and-nano-hesperetin-on-recognition-memory-impairment-and-the-elevated-oxygen-stress-in-rat-model-of-alzheimer-s-disease
#8
Elham Kheradmand, Akbar Hajizadeh Moghaddam, Mahboobeh Zare
Alzheimer disease (AD) is a progressive dementia affecting a large proportion of the aging population. There is evidence that brain tissue in patients with AD is exposed to oxidative stress during the course of the disease. Hesperetin (Hst) is a natural flavonoid, which has been reported to exert various biological activities such as antioxidant and anti-inflammatory effect. The present study aimed to investigate the effects of hesperetin and nano-hesperetin on neurobehavioral activity and superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GRx) and catalase (CAT) enzymes activity, malondialdehyde (MDA) and glutathione (GSH) levels in hippocampal area of rats in an experimental model of AD...
November 9, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29115547/preventive-effect-of-hesperidin-modulates-inflammatory-responses-and-antioxidant-status-following-acute-myocardial-infarction-through-the-expression-of-ppar%C3%A2-%C3%AE-and-bcl%C3%A2-2-in-model-mice
#9
Chunying Meng, Zeheng Guo, Dagang Li, Hanwei Li, Jianbin He, Dingguo Wen, Bin Luo
Hesperetin is the main pharmacological ingredient of fruit of the citrus family, rutaceae. It is a flavanone, which has potent antioxidation and anti‑inflammatory activities. The present study investigated the preventive effect of hesperidin in the modulation of acute myocardial infarction (AMI)‑induced inflammatory responses and antioxidant status in a mouse model. The levels of creatine kinase‑MB, tumor necrosis factor (TNF‑α), interleukin (IL)‑1β, IL‑6, monocyte chemoattractant protein 1 (MCP‑1), intercellular adhesion molecule 1 (ICAM‑1), malondialdehyde (MDA), catalase (CAT), superoxide dismutase (SOD) and caspase‑3/9 were measured using ELISA kits...
November 6, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29080465/antihyperglycemic-effect-of-hesperetin-a-citrus-flavonoid-extenuates-hyperglycemia-and-exploring-the-potential-role-in-antioxidant-and-antihyperlipidemic-in-streptozotocin-induced-diabetic-rats
#10
Revathy Jayaraman, Srinivasan Subramani, Shahul Hameed Sheik Abdullah, Muruganathan Udaiyar
Diabetes is the major health problem in modern civilization which occurs due to inadequate metabolism of carbohydrate and lipid could cause tremendous changes in the metabolic activities of liver. In this study, we investigated the antihyperglycemic, antioxidant and antihyperlipidemic effects of hesperetin, a citrus flavonoid against streptozotocin (STZ)-induced experimental rats. To stimulate diabetes mellitus, rats were injected with STZ intraperitoneally at a single dose of 45mg/kg. STZ induced rats showed marked increase in the level of plasma glucose and significant reduction in the level of plasma insulin...
October 31, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29042968/hesperetin-alleviates-renal-interstitial-fibrosis-by-inhibiting-tubular-epithelial-mesenchymal-transition-in-vivo-and-in-vitro
#11
Hong-Wei Wang, Lei Shi, Yan-Ping Xu, Xing-Ya Qin, Qi-Zhi Wang
Hesperetin (HES) is a flavonoid that has been reported to exert protective effects against cardiac remodeling, lung fibrosis and hepatic fibrosis. However, reports on the effects and potential mechanisms of HES in renal fibrosis are limited. In the present study, a unilateral ureteric obstruction (UUO) mouse model and a transforming growth factor (TGF)-β1-activated normal rat kidney (NRK)-52E cell model were established. HES was subsequently administered to these models to evaluate its anti-fibrotic effects and potential underlying mechanisms of action...
October 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29042280/biochemical-and-biophysical-characterization-of-a-mycoredoxin-protein-glutaredoxin-a1-from-corynebacterium-pseudotuberculosis
#12
Raphael J Eberle, Liege A Kawai, Fabio R de Moraes, Ljubica Tasic, Raghuvir K Arni, Monika A Coronado
Glutaredoxin A1 from Corynebacterium pseudotuberculosis was shown to be a mycoredoxin protein. In this study, we established a process to overexpress and purify glutaredoxin A1. The aim of this study was the investigation of the Glutaredoxin A1 from C. pseudotuberculosis behavior under different redox environments and the identification of lead molecules, which can be used for specific inhibitor development for this protein family. A quantitative assay was performed measuring the rate of insulin reduction spectrophotometrically at 640nm through turbidity formation from the precipitation of the free insulin...
October 16, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29032208/chitosan-based-nano-formulation-enhanced-the-anticancer-efficacy-of-hesperetin
#13
Lizha Mary, Balaji Sadhasivam, Kanagaraj Palaniyandi, Thangavel Muthuswamy, Ilangovan Ramachandran, Anandhan Balakrishnan, Surajit Pathak, Shoba Narayan, Satish Ramalingam
Cancer is one of the major causes of increased morbidity and mortality in modern society. Colorectal cancer is the third leading cause for cancer related death worldwide. Current chemotherapeutics are not very effective and have severe side effects. Hesperetin is a bioflavonoid from citrus fruits and its clinical use is restricted because of the poor water solubility. Folate receptor is over expressed in various cancer cells. In this regard, we have synthesized the Chitosan Folate Hesperetin nanoparticle (CFH) by covalently conjugating folic acid with chitosan molecules...
October 12, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29029741/enantioseparation-of-single-layer-native-cyclodextrin-chiral-stationary-phases-effect-of-cyclodextrin-orientation-and-a-modeling-study
#14
Xiaoxuan Li, Xiaobin Yao, Yin Xiao, Yong Wang
A novel native cyclodextrin (CD) chiral stationary phase (CSP) with single triazole-bridge at CD C2 position (CSP1) was prepared by anchoring mono(2(A)-azido-2(A)-deoxy)-β-CD onto alkynyl silica via click chemistry. The effect of CD orientation on single layer CD-CSP's enantioseparation was comprehensively investigated using CSP1 (reversed orientation) and our previously reported CSP2 (C6 single triazole-bridge, normal orientation) as well as a commercial CD-CSP (Cyclobond I 2000, hybrid orientation) by separating several groups of analytes in chiral high performance liquid chromatography...
October 16, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/29023372/parp-inhibition-by-flavonoids-induced-selective-cell-killing-to-brca2-deficient-cells
#15
Cathy Su, Alexis H Haskins, Chisato Omata, Yasushi Aizawa, Takamitsu A Kato
High consumption of dietary flavonoids might contribute to a reduction of cancer risks. Quercetin and its glycosides have PARP inhibitory effects and can induce selective cytotoxicity in BRCA2-deficient cells by synthetic lethality. We hypothesized that common flavonoids in diet naringenin, hesperetin and their glycosides have a similar structure to quercetin, which might have comparable PARP inhibitory effects, and can induce selective cytotoxicity in BRCA2-deficient cells. We utilized Chinese hamster V79 wild type, V-C8 BRCA2-deficient and its gene-complemented cells...
October 12, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28962151/hesperetin-protects-against-inflammatory-response-and-cardiac-fibrosis-in-postmyocardial-infarction-mice-by-inhibiting-nuclear-factor-%C3%AE%C2%BAb-signaling-pathway
#16
Bing Wang, Lianghai Li, Ping Jin, Mengqiu Li, Jianguo Li
Cardiac inflammation and cardiac fibrosis are important parts of cardiac remodeling following myocardial infarction (MI), which may be the basic mechanisms of the development of chronic heart failure. The nuclear factor (NF)-κB signaling pathway promotes cardiac inflammation and fibrosis. It has reported that hesperetin inhibits cardiac remodeling induced by pressure overload in mice. However, it has remained elusive whether and how hesperetin has a role in cardiac fibrosis post-MI. Therefore, a mouse model of MI was established by left anterior descending coronary artery ligation...
September 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28956456/production-of-drug-nanosuspensions-effect-of-drug-physical-properties-on-nanosizing-efficiency
#17
Tao Liu, Rainer H Müller, Jan P Möschwitzer
Objective Drug nanosuspension is one of the established methods to improve the bioavailability of poorly soluble drugs. Drug physical properties aspect (morphology, solid state, starting size et al) is a critical parameter determining the production efficiency. Some drug modification approaches such as spray-drying were proved to improve the millability of drug powders. However, the mechanism behind those improved performances is unclear. This study is to systematically investigate the influence of those physical properties...
September 28, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28954539/gontscharovia-popovii-a-new-source-of-carvacrol-its-polyphenolic-constituents-essential-oil-analysis-total-phenolic-content-and-antioxidant-activity
#18
Faraneh Zareiyan, Vahid Rowshan, Atefeh Bahmanzadegan, Ahmad Hatami
The experiment was carried out using the shadow-dried aerial parts including leaves and shoots of Gontscharovia popovii collected in Fars province in order to investigate the polyphenolic compositions, antioxidant activity, total phenolic content and essential oil constituents. The result showed IC50 of 395.77 μg mL(-1) and total phenolic content of about 20.01 mg g(-1) gallic acid equivalent dry weight. It also showed a wild range of polyphenols such as; Gallic acid, catechin, chloregenic acid, rutin, vanillin, trans-Ferulic acid, sinapic acid, coumarin, hesperedin, quercetin, hesperetin, eugenol and carvacrol as the main detected polyphenols...
September 28, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28942652/polyphenols-from-blossoms-of-citrus-aurantium-l-var-amara-engl-show-significant-anti-complement-and-anti-inflammatory-effects
#19
Chun-Yan Shen, Jian-Guo Jiang, Chun-Ling Huang, Wei Zhu, Chao-Yang Zheng
Citrus aurantium L. var. amara Engl. (CAVA) was traditionally used as a digestant or expectorant in China. Crude polyphenols (CAVAP-W) extracted from blossoms of CAVA were mainly composed of eriocitrin/neoeriocitrin, eriocitrin/neoeriocitrin, rhoifolin, hesperidin, naringin, rutin, veronicastroside, neohesperidin, and hesperetin by LC-MS analysis. CAVAP-W showed significant anticomplement and anti-inflammatory effects. Due to the close relationship between anticomplement and anti-inflammatory activity, the anti-inflammatory effect was further investigated and the results showed that CAVAP-W significantly suppressed production of interleukin-6 (IL-6), tumor necrosis factor-alpha (TNF-α), interleukin-1beta (IL-1β), and mRNA expression of inducible nitric oxide synthase (iNOS), IL-6, TNF-α, IL-1β, and cyclooxygenase-2 (COX-2) in lipopolysaccharides-stimulated RAW264...
October 9, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28923363/anti-inflammatory-effects-of-flavonoids-in-neurodegenerative-disorders
#20
Carmela Spagnuolo, Stefania Moccia, Gian Luigi Russo
Neuroinflammation is one of the main mechanisms involved in the progression of several neurodegenerative diseases, such as Parkinson, Alzheimer, multiple sclerosis, amyotrophic lateral sclerosis and others. The activation of microglia is the main feature of neuroinflammation, promoting the release of pro-inflammatory cytokines and resulting in the progressive neuronal cell death. Natural compounds, such as flavonoids, possess neuroprotective potential probably related to their ability to modulate the inflammatory responses involved in neurodegenerative diseases...
September 7, 2017: European Journal of Medicinal Chemistry
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