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Tendinopathy is a common disease in elite and recreational athletes, and Eriocitrin is a flavonoid compound, which has antioxidant properties. The present study was undertaken to investigate the effect of Eriocitrin on tendon stem cells in vitro. Different concentrations of Eriocitrin (0, 25, 50, 75 µM) were used to treat tendon stem cells, cell proliferation was determined by CCK8 assay, apoptosis was detected by propidium iodide (PI) staining assays and caspase-3 activity assessment, wound-healing assaywas selected to detect the migration, and RT-PCR was chosen to detect the expression levels of scar formation-related gene markers (COMP, Fibronectin, and Biglycan). Eriocitrin treatment promoted cell proliferation of tendon stem cells in dose-dependent manner, and it reduced the apoptotic activities and improved the migration of tendon stem cells. It inhibited COMP, Biglycan, and Fibronectin expression. In summary, eriocitrin promoted cell proliferation of tendon stem cells, improved the migration of tendon stem cells, and inhibited the expression levels of some scar formation-related gene markers.

Background Cisplatin, a common anti-neoplastic drug used in the medical industry for cancer treatment has shown adverse nephrotoxic effects. This research targets to demonstrate the protective measure of eriocitrin, a bioactive flavonoid, against cisplatin-induced renal toxicity in rats. Materials and methods Rats of normal control and model groups were treated with saline whereas experimental groups received oral administration of eriocitrin (25 and 50 mg/kg b.w.) for 10 days and a single intraperitoneal (i.p.) injection of cisplatin (8 mg/kg b.w.) was given on the 7th day for all except normal control group. Blood serum, urine, and kidney tissue samples were collected for analysis. Results Cisplatin-induced rats demonstrated significant renal toxicity and damage. Eriocitrin dose-dependently reversed the effects by decreasing the proteinuria in urine, and urea, creatinine, lipid peroxidation, nitric oxide (NO) and pro-inflammatory cytokine levels (TNF-α, IL-1β) in serum. The tissue levels of reduced glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT) were increased, whereas the levels of tissue DNA fragmentation and serum PARP-1 and Caspase-3 were reduced against model group. Histopathological modulations were supporting the protective effect of eriocitrin. Conclusion Eriocitrin has significant nephroprotective effects against cisplatin-induced renal toxicity by alleviating oxidative stress, preventing apoptosis and DNA damage.

Background Postoperative pain remains a major clinical problem as there are limited analgesic strategies that have been proven to be effective in preventing and relieving this type of pain. Natural products, including flavonoids, have distinct pharmacological properties and play an important role in the discovery of analgesic drugs. Materials and Methods In this study, the flavonoid eriocitrin (eriodictyol 7-O-rutinoside), which is the main flavonoid in lemon fruit (Citrus limon), was mechanistically investigated for its prospective antinociceptive effect in a mouse model of postoperative pain. The antinociceptive property was evaluated by utilizing both tonic (acetic acid-induced writhing behavior) and phasic (hot-plate) nociception modalities. The hindpaw incisional surgery was performed and hyperalgesia was assessed using von Frey filaments. Results The tested doses of eriocitrin significantly attenuated (P

Atherosclerosis is a multifactorial disease that develops and progresses in the arterial wall in response to a variety of stimuli. Among various other stimuli, hyperlipidemia is an extremely important factor that is correlated with the development of atherosclerosis. Lemon and citrus fruits contain various bioactive flavonoids, such as eriocitrin, that prevent obesity and related metabolic diseases. Therefore we concentrated on eriocitrin, a potent flavonoid with numerous therapeutic properties, particularly its beneficial lipid-lowering action in rats subjected to high fat diet. The anti-atherosclerotic efficacy of eriocitrin was assessed in rats administered a diet rich in fat. Wistar rats were divided into five groups consisting of six animals in all groups. Group I served the control, Group II was fed a high-fat diet (HFD), and the third and fourth groups were fed an HFD supplemented with varying doses of eriocitrin, and the last group was administered simvastatin for the last 30 days. Body weight, organ weight, lipid and lipoprotein parameters, cardiac and inflammatory markers, and histological examination were evaluated in animals induced with an HFD. Eriocitrin displayed a significant anti-atherosclerotic action by lowering the body weight, organ weight, reduction in lipid content, cardiac and inflammatory markers, myocardial changes confirmed by histopathology, malondialdehyde and increased antioxidant enzyme activities, nitric oxide, as well as 6-keto-PGF1α and high-density lipoprotein levels in rats fed an HFD. The findings of the experiment suggest that the anti-atherosclerotic action of eriocitrin was due to its modulatory activity in lipid metabolism. Considering the overall results of the study it can be validated that a use of flavonoid eriocitrin might be beneficial in altering HFD-induced alterations in atherosclerotic rats.

Lung carcinogenesis is one of the main sources of cancer-related mortality globally and it is estimated that nearly 1 million people die from it every year. The 5-year survival rate of lung carcinogenesis is reported at just 15%. The aim of the current research was to investigate the immunomodulatory effect of eriocitrin against benzo(a)pyrene [B(a) P]-induced lung tumorigenesis in Swiss albino mice. The lung sarcoma was provoked through oral gavage of B(a)P (50 mg/kg body weight) two times/week for four weeks. CEA, lung weight, lipid peroxidation (LPO), body weight, immuno-globulin (IgG, IgA, and IgM), tumor incidence, serum marker enzymes (LDH, AHH, λ-GT, and 5'-NTs), hematological counts (leucocytes, lymphocytes, neutrophils, absolute numbers of lymphocytes and neutrophils), antioxidants (SOD and CAT), inflammatory modulators (IL-1β, IL-6, and TNF-α), immune complexes (avidity index, phagocyte index, NBT reduction, and SIC) and histopathological changes were analyzed. Moreover, the status of apoptosis proteins (Bax, caspase-9, and caspase-3) and cell proliferative protein (cyclin D1 and cyclin A) expression was determined by Western blot and PCNA by immunohistochemical analysis. B(a)P-challenged cancer-bearing mice exhibited augmented levels of lipid peroxidation, tumor incidence, lung weight, CEA, serum marker enzymes, IgA, SIC, cell proliferative markers, and inflammatory cytokines with concurrent decrease in body weight, antioxidant levels, hematological counts, immunoglobulins, immune complexes, and apoptotic protein expression. The eriocitrin treatments caused significant reversion of all these marker to previous levels. Overall, the results propose the immunomodulatory prospective of eriocitrin against B(a) P-induced lung carcinogenesis on Swiss albino mice.

Juices from nine new late-season triploid mandarins (Tania-46 (1), Tania-47 (2), Omet (3), Albir (4), Tania-48 (5), Tania-43 (6), Tania-44 (7), Coral (8), and Matiz (9), and from their parents were analyzed for mainly internal quality attributes, vitamin C, total phenolics, flavonoids, phenolic, and organic acids. Antioxidant activity was measured by three methods, the DPPH free radical-scavenging assay, ferric reducing antioxidant power (FRAP) test, and ABTS analysis. All the new hybrids exhibited high internal and nutritional quality which may be considerate rich sources of phytochemicals. Among the nine varieties, Tania-48 hybrid was shown to be the richest in vitamin C, flavanones (hesperidin, eriocitrin, and neoeriocitrin), polymethoxyflavones, and malic and succinic acids. Furthermore, the juice of this new triploid hybrid displayed high antioxidant capacity which may make it important for human diet as a source of health-promoting components. On the other hand, Tania-44, Tania-48, and Tania-43 fruit juices exhibited greater content of eriocitrin and neoeriocitrin than the others.

Peppermint leaf, sage leaf, thyme herb, and their preparations are common components of herbal medicinal products (HMPs). According to the European Pharmacopoeia guidelines, the above-mentioned plant substances are standardized for the content of essential oils, omitting polyphenols, which also have a significant impact on their activities. The aim of this study was to evaluate the stability of the predominant polyphenols—rosmarinic acid, luteolin-7-O-β-glucuronide, and eriocitrin—in selected commercial liquid HMPs containing thyme, sage, and peppermint under long-term, intermediate, and accelerated testing conditions. Qualitative and quantitative analyses of these polyphenols were performed by the previously optimized and validated HPLC-DAD method. Rosmarinic acid stability was better in hydroethanolic than in an aqueous solution. The effect of the solvent on the stability of luteolin-7-O-β-glucuronide and eriocitrin could not be determined and requires further investigation. The present study is the first to analyze the stability of these compounds in commercial herbal medicinal products. The expiration dates proposed by the manufacturers of the tested HMPs did not guarantee stable levels of all analyzed polyphenols throughout the stated period. However, this study is preliminary and requires continuation on a larger number of medicinal products.

Unloading stress enhances oxidative stress, which in turn induces disuse muscle atrophy. This study evaluated the suppressive effect of lemon peel extract containing eriocitrin on muscle atrophy. Both lemon peel extract and eriocitrin suppressed weight loss in the gastrocnemius muscle under denervation in C57BL/6 mice. The mRNA level of ubiquitin ligases and their transcription factor were downregulated by eriocitrin. Eriocitrin inhibited the increase in lipid peroxidation and the ratio of glutathione disulfide/glutathione. These data suggest that eriocitrin ameliorated disuse muscle atrophy by suppressing the expression of ubiquitin ligase genes by its antioxidative effect.

Eriocitrin is a flavonoid that is isolated from orange peel. Resveratrol is a polyphenol compound, which is present in various fruits, such as grapes. The aim of the present study was to investigate both in vitro and in vivo anti-inflammatory effects of eriocitrin combined with resveratrol using lipopolysaccharide (LPS)-induced RAW264.7 cells and a mouse model of ear edema. The results showed that eriocitrin combined with resveratrol strongly inhibited LPS-induced secretion of nitric oxide (NO), tumor necrosis factor-α (TNF-α), and Interleukin-1β (IL-1β). Moreover, Eriocitrin combined with resveratrol potently inhibited nuclear factor-κB (NF-κB), phosphor-STAT3, and phosphor-AKT, which was accompanied by inhibition of phosphorylation in mitogen-activated protein kinase (MAPK) signaling pathways. Treatment with eriocitrin combined with resveratrol alleviated edema and subcutaneous tissue inflammation caused by 12-O-tetradecanoylphorbol-13-acetate (TPA) in vivo. This study also demonstrated that treatment with eriocitrin and resveratrol decreased the levels of the pro-inflammatory cytokines TNF-α and IL-1β. The results of the present study indicate that eriocitrin combined with resveratrol effectively inhibits inflammatory responses both in vitro and in vivo.

Lemon fruits are well-known for their economic, nutrition and health values. In this study, the maturity degree, phenolic compounds and antioxidant capacity of Eureka lemon [Citrus limon (L.) Burm. f.] fruits harvested at different months of the year were investigated. We found that the fruits harvested in November outperformed others in terms of weight, total sugar and soluble solid content (SSC). The ρ-coumaric acid, ferulic acid, eriocitrin and hesperidin were the predominant phenolic compounds in lemon fruits. The highest total phenolic content (TPC, 3.49 ± 0.05 mg GAE g−1 FW), total flavonoid content (TFC, 1.46 ± 0.05 mg RE g−1 FW), sum of individual phenolic acids content (269.36 μg g−1 FW) and their antioxidant potency composite (APC) index (100.00%) were found in the pulps of April fruits. The maximum of sum of individual flavonoids content (3098.42 μg g−1 FW) exhibited in August. For the peels, the highest TFC (6.35 ± 0.24 mg RE g−1 FW) and APC (95.14%) appeared in April fruits, while the highest TPC (7.96 ± 0.17 mg GAE g−1 FW) and sum of individual flavonoids content (9003.91 μg g−1 FW) occurred in the August. However, the maximum of sum of individual phenolic acids content (769.28 μg g−1 FW) was detected in June fruits. We also found that soluble solid content (SSC) of the pulps of lemon fruits were negatively correlated with their TPC and APC. TPC also decreased with the increase in SSC of peels. Most importantly, our study indicated that the contents of phenolic compounds and antioxidant activity of lemon fruits varied significantly with their maturity degrees depending on different harvest time, and this information is essential for a better use of different lemons fruits resources.

Eriocitrin, a main flavonoid in lemons, possesses strong antioxidant, lipid-lowering and anticancer activities and has long been used in food, beverages and wine. However, its metabolism in vivo and in vitro is still unclear. In this study, an efficient strategy was developed to detect and identify metabolites of eriocitrin by using ultra-high-performance liquid chromatography coupled with hybrid triple quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS) based on online data acquisition and multiple data processing techniques. A total of 32 metabolites in vivo and 27 metabolites in vitro were obtained based on the above method. Furthermore, the main metabolic pathways of eriocitrin included reduction, hydrogenation, N-acetylation, ketone formation, oxidation, methylation, sulfate conjugation, glutamine conjugation, glycine conjugation, desaturation and demethylation to carboxylic acid. This study will lay a foundation for further studies on the metabolic mechanisms of eriocitrin.

Made available in DSpace on 2021-06-25T10:52:18Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-02-17 Eriocitrin plays a role in the reduction of oxidative stress and inflammation linked to the development of diabetes mellitus and atherosclerosis. We investigated the pharmacokinetics and distribution of eriocitrin metabolites in rats orally administered with eriocitrin. Plasma, urine, and organs were collected at 12 different time points from 0 to 24 h and analyzed by HPLC-PDA-MS. For the first time, the metabolism and distribution of orally administered eriocitrin were shown. Nine metabolites of eriocitrin were identified in rat urine, and seven in various tissues (eriodictyol, homoeriodictyol, hesperetin, and glucuronidated metabolites), and preliminary identifications of these metabolites are suggested. Overall, eriocitrin metabolites were widely distributed in the rat tissues, where homoeriodictyol and homoeriodictyol-7-O-glucuronide were the major metabolites. The half-lives of the metabolites in plasma were between 3 and 3.2 h, and the total bioavailability of eriocitrin was less than 1%. Universidade Estadual Paulista (UNESP) Faculdade de Ciências Farmacêuticas Araraquara Departamento de Alimentos e Nutrição, Rodovia Araraquara - Jau, km 1 U.S. Horticultural Research Laboratory Agricultural Research Service USDA, 2001 South Rock Road Universidade Estadual Paulista (UNESP) Faculdade de Ciências Farmacêuticas Araraquara Departamento de Alimentos e Nutrição, Rodovia Araraquara - Jau, km 1

Recently, several studies have highlighted the role of Citrus flavanones in counteracting oxidative stress and inflammatory response in bowel diseases. The aim of study was to identify the most promising Citrus flavanones by a preliminary antioxidant and anti-inflammatory screening by in vitro cell-free assays, and then to mix the most powerful ones in equimolar ratio in order to investigate a potential synergistic activity. The obtained flavanones mix (FM) was then subjected to in vitro simulated digestion to evaluate the availability of the parent compounds at the intestinal level. Finally, the anti-inflammatory activity was investigated on a Caco-2 cell-based model stimulated with interleukin (IL)-1&beta, FM showed stronger antioxidant and anti-inflammatory activity with respect to the single flavanones, demonstrating the occurrence of synergistic activity. The LC-DAD-ESI-MS/MS analysis of gastric and duodenal digested FM (DFM) showed that all compounds remained unchanged at the end of digestion. As proof, a superimposable behavior was observed between FM and DFM in the anti-inflammatory assay carried out on Caco-2 cells. Indeed, it was observed that both FM and DFM decreased the IL-6, IL-8, and nitric oxide (NO) release similarly to the reference anti-inflammatory drug dexamethasone.

Background Cerebral ischemia (CI) can lead to ischemic stroke. The most effective therapy for cerebral ischemic stroke is the early restoration of blood reperfusion. However, reperfusion after CI can result in cerebral ischemia reperfusion (CI/R) injury. This study aimed to detect the effect of eriocitrin on cerebral I/R injury and investigate the underlying mechanism. Methods Seventy male Sprague-Dawley (SD) rats were randomly divided into 5 groups: the control group, the cerebral I/R group, the I/R + eriocitrin 8 mg/kg group, the I/R + eriocitrin 16 mg/kg group, and the I/R + eriocitrin 32 mg/kg group. Different doses of eriocitrin or 0.5% carboxymethyl cellulose sodium were administrated to the rats once daily for 7 days before middle cerebral artery occlusion (MCAO). PCR staining was performed to observe cerebral infarction. Hematoxylin and eosin (H&E) staining was carried out to observe the damage to the brain tissue. Terminal-deoxynucleotidyl transferase mediated nick end labeling (TUNEL) was used to detect apoptosis. Quantitative real-time polymerase chain reaction (qRT-PCR) was used to detect the relative mRNA levels of related molecules. Western blot was used to detect the expression of related proteins. The detection kits were used to detect superoxide dismutase (SOD) and lactic dehydrogenase (LDH) activity, and malondialdehyde (MDA) content respectively. Enzyme-linked immunosorbent assay (ELISA) was used to detect TNF-radiation, interleukin-6 (IL-6), and interleukin-10 (IL-10). Results The results showed that Eriocitrin significantly reduced the cerebral infarct volume, cerebral water content, and cerebral indexes. Eriocitrin treatment alleviated pathological injury, promoted cell proliferation, and inhibited cell apoptosis. Eriocitrin upregulated SOD activity and downregulated MDA and LDH content. Eriocitrin also effectively decreased the levels of IL-6 and tumor necrosis factor-α (TNF-α), but increased the content of IL-10 in serum and brain tissues. Furthermore, Eriocitrin increased the phosphorylation of nuclear factor erythroid 2-related factor (Nrf2), as well as the expressions of heme-oxygenase-1 (HO-1) and quinine oxidoreductase 1 (NQO1). Moreover, Eriocitrin decreased the phosphorylation of nuclear factor-κB (NF-κB) p65. Conclusions Our results indicated that Eriocitrin attenuated oxidative injury and inflammatory response in rats with CI/R via the Nrf2/HO-1/NQO1/NF-κB signaling pathway.

The effects of preharvest treatments with 0.1 mM methyl jasmonate (MeJA) and 0.5 mM salicylic acid (SA) on quality parameters of lemon fruit and their relationship with antioxidant systems, gene expression and bioactive compounds at harvest and during cold storage were evaluated. Results showed that total antioxidant activity, total phenolic content and the major individual phenolics (hesperidin and eriocitrin) were always higher in treated fruit than in controls. The activity of the antioxidant enzymes catalase, peroxidase and ascorbate peroxidase was also increased at harvest by SA and MeJA treatments, especially the last enzyme, for which the expression of its codifying gene was also enhanced. In addition, treated fruit had lower weight and firmness losses, respiration rate and production of ethylene than controls. Moreover, sugars and organic acids were maintained at higher concentration in flavedo and juice as a consequence of preharvest SA and MeJA treatments, showing an effect on maintaining fruit quality properties.

Made available in DSpace on 2021-06-25T10:18:11Z (GMT). No. of bitstreams: 0 Previous issue date: 2020-01-01 Eriocitrin is a citrus flavonoid with a high capacity to reduce the oxidative stress related to metabolic disorders and obesity. We assessed the effects of low doses of eriocitrin on the oxidative stress, inflammation, and metabolism of glucose and lipids of high-fat diet (HFD)-fed obese mice. Fifty male C57BL/6J mice were randomly assigned into five groups (n 10). The mice were fed an HFD (45 % kcal from fat, i.e. lard) for 4 weeks for obesity induction. After this period, the mice continued receiving the same HFD, but supplemented with eriocitrin at 10, 25 or 100 mg/kg body weight (bw) for an additional 4 weeks. Control groups were fed with standard diet (10 % kcal of fat, i.e. soy oil) or with HFD without eriocitrin, for eight consecutive weeks. At the end of the study, mice supplemented with eriocitrin showed lower levels of blood serum glucose and blood and liver triacylglycerols (P < 0â.05). There was also improved levels of insulin, HOMA-IR, total-cholesterol, resistin and lipid peroxidation in the supplemented mice. It was concluded that the 25 mg dose of eriocitrin improved all the parameters studied and had positive effects on oxidative stress, systemic inflammation and metabolism of lipids and glucose in general. Laboratory of Nutrition School of Pharmaceutical Sciences Sao Paulo State University-UNESP U.S. Horticultural Research Laboratory Agricultural Research Service Usda, 1401 South Rock Road/Port Fierce Laboratory of Pathology School of Dentistry Unesp Sao Paulo State University Laboratory of Nutrition School of Pharmaceutical Sciences Sao Paulo State University-UNESP Laboratory of Pathology School of Dentistry Unesp Sao Paulo State University

Natural plant extracts contain a variety of phenolic compounds which are assigned various biological activities. Our work aims to make a quantitative and qualitative characterization of the Zest (ZL) and the Flesh (FL) of lemon (Citrus limon), to valorize the pharmacological uses of lemon, by evaluating in vitro activities (DPPH, free radical scavenging and reducing power). The antibacterial, antifungal, and antiproliferative activities were sought in the ability of Citrus limon extracts to protect DNA and protein. We found that the ZL contains high amounts of phenolics responsible for the important antioxidant properties of the extract. However, the FL is richer in flavonoids than the ZL. The FL extract was also found to be more effective than the ZL in protecting plasmid DNA against the strand breakage induced by hydroxyl radicals. We also concluded that the FL extract exhibited potent antibacterial activity unlike ZL. Analysis by LC/MS-MS identified 6 compounds (Caffeoyl N-Tryptophan, Hydroxycinnamoyl-Oglucoside acid, Vicenin 2, Eriocitrin, Kaempferol-3-O- rutinoside, and Quercetin-3-rutinoside). These preliminary results showed that Citrus limon has antibacterial and antioxidant activity in vitro. It would be interesting to conduct further studies to evaluate the in vivo potential in an animal model.

Changes in contents of sugars, organic acids, limonoids, phenolics contents, and antioxidant capacities of lemon slices dried at different temperatures were evaluated. Air drying (AD) promoted losses of sugars, citric acid, ascorbic acid, extractable phenolics (EPs), and non-extractable phenolics (NEPs), while it introduced an increase in limonoids. Phenolics of lemon were mainly presented in their extractable form. Hesperidin and eriocitrin were the main EPs; protocatechuic acid and poncirin were the predominant NEPs. The decrease in extractable phenolic acid, EP, and NEP content in lemon is lower at low drying temperatures, while the increase in non-extractable phenolic acid content is higher at high drying temperatures. The antioxidant capacity of EP was higher than that of NEP. Phenolics contributed to antioxidant capacities of lemon slices, and flavonoids were the main contributors among phenolics. Considering limonoids contents and the high levels of EP, NEP, and antioxidant capacities, AD at 60 °C could be an appreciate treatment for dehydrating lemon slices.

In this contribution, the influence of Pulsed Electric Fields (PEF) of different intensities (3–9 kV/cm and 0–300 μs) on the extraction of Total Phenols from lemon peel residues by pressing was investigated. According to the cellular disintegration index, the optimum treatment time for the increase in permeability was determined as 30 pulses of 30 μs. It was determined that the effect of PEF was independent of lemon residue size. The effectiveness of pressing-assisted extraction was evaluated by measuring the Total Phenol Content (TPC), the real antioxidant capacity and the concentrations of the main lemon polyphenols, the flavonones hesperidin and eriocitrin. The variables studied in the extraction were time, pressure applied and intensity of the electric fields. This study concludes that electric field intensity of 7 kV/cm increased the efficiency of polyphenol extraction by 300%, giving maximum values of 84 mg of hesperidin in 100 g FW and 176 mg of eriocitrin in 100 g FW. Thus, it was concluded that PEF provides a new methodology to improve polyphenol extraction with a non-thermal, environment-friendly technology, and this represents a method for increasing economic benefits of industrial processes.

The aim of this study was to evaluate the antidegenerative effect in osteoarthritis damage of eriocitrin alone and eriocitrin formulated as innovative “dietary flavonoid supplement.” A complexation between eriocitrin and hydroxypropylβ-cyclodextrin by solubilization/freeze-drying method was performed. The complex in solution was evaluated by phase solubility studies and the optimal 1 : 2 flavanone/cyclodextrin molar ratio was selected. Hydroxypropylβ-cyclodextrin was able to complex eriocitrin as confirmed by UV-Vis absorption, DSC, and FTIR studies. The complex formed increased the eriocitrin water solubility (from4.1±0.2 g·L−1to11.0±0.1 g·L−1) and dissolution rate (from 37.0% to 100%) in 30 min. The in vitro studies exhibit the notion that eriocitrin and its complex inhibit AGEs in a similar manner because hydroxypropylβ-cyclodextrin does not interfere with the flavanone intrinsic property. Instead, the presence of cyclodextrin improves eriocitrin antioxidant stability maintaining a high fluorescence value until 8 hours with respect to the pure materials. Moreover, hydroxypropylβ-cyclodextrin showed moderate GAGs restoration acting synergistically with the complexed compound to maintain the structural chondrocytes integrity. The results point out that ERT/HP-betaCD complex possesses technological and biological characteristics able to obtain an easily soluble nutraceutical product, which reduces the degenerative and oxidative damage which occurs in osteoarthritis, and improve the patient compliance.

Inflammatory bowel disease (IBD) is a continual ailment condition which engrosses the entire alimentary canal. The IBD can be primarily distinguished into two forms, ulcerative colitis, and Crohn's disease. The major symptoms of IBD include pustules or abscesses, severe abdominal pain, diarrhea, fistula, and stenosis, which may directly affect the patient's quality of life. A variety of mediators can stimulate the circumstances of IBD, some examples include infections by microbes such as bacteria, perturbation of the immune system and the surrounding environment of the intestines. Severe colitis was stimulated in the experimental animals through administering 4% dextran sulfate sodium (DSS) which is mixed in water ad libitum for 6 days. Eriocitrin (30 mg/kg) was then administered to the experimental animals followed by the induction of severe colitis to evaluate the therapeutic prospective of eriocitrin against the colon inflammation stimulated by DSS. In this study, eriocitrin (30 mg/kg) demonstrated significant (P < .05) attenuation activity against the DSS-stimulated severe colitis in experimental animals. Eriocitrin counteracted all of the clinical deleterious effects induced by DSS, such as body-weight loss, colon shortening, histopathological injury, accretion of infiltrated inflammatory cells at the inflamed region and the secretion of inflammatory cytokines. The results clearly showed that eriocitrin effectively attenuated DSS-induced acute colitis in experimental animals.

So far, there is no report on the quality evaluation of lemonade available in the market. In this study, a sample preparation method was developed for the determination of flavonoid glycosides by ultra-performance liquid chromatography&ndash, mass spectrometry (UPLC-MS) based on vortex-assisted dispersive liquid-liquid microextraction. First, potential flavonoids in lemonade were scanned and identified by ultra-performance liquid chromatography&ndash, time of flight mass spectrometry (UPLC-TOF/MS). Five flavonoid glycosides were identified as eriocitrin, narirutin, hesperidin, rutin, and diosmin according to the molecular formula provided by TOF/MS and subsequent confirmation of the authentic standard. Then, an ultra-performance liquid chromatography&ndash, triple quadrupole mass spectrometry (UPLC-QqQ/MS) method was developed to determine these five flavonoid glycosides in lemonade. The results showed that the content of rutin in some lemonade was unreasonably high. We suspected that many illegal manufacturers achieved the goal of low-cost counterfeiting lemonade by adding rutin. This suggested that it was necessary for relevant departments of the state to make stricter regulations on the quality standards of lemonade beverages.

Citrus fruits are a rich source of bio-functional compounds with various and well-proven health properties. We focused our attention on an ancient Mediterranean species, Citrus lumia Risso. The aim of this work was to investigate the polyphenol content and biological activities of C. lumia albedo extract by cell-free and cell-based assays. Fifteen polyphenols were quantified by LC-DAD-FLD analysis (flavonoids 89.34% and phenolic acids 10.66%) with eriocitrin and hesperidin as major components (52.81% and 31.31%, respectively). These results were corroborated also by micromorphological observations, which showed clusters of needle-shaped crystals of hesperidin highlighted by TBO staining. C. lumia albedo extract revealed marked antioxidant and free radical scavenging properties, and a significant cytoprotective activity on t-BOOH-treated lymphocytes. Results indicate that C. lumia albedo extract could be exploited as an antioxidant source, suggesting the use of albedo, currently considered a by-product, as a valuable raw material for nutraceutical employments.

Obesity and oxidative damage are two important risk factors associated closely with metabolic syndrome. Utilization of functional food ingredients is considered as a feasible way to tackle these challenges. In the present study, eight representative species of citrus peel extracts (CPEs) were evaluated and compared for their flavonoid profiles, antioxidant activities, and pancreatic lipase (PL) inhibitory capacities and mechanisms. Results indicated that hesperidin, naringin, neohesperidin, narirutin and eriocitrin were the five major flavonoids in CPEs, among which hesperidin was the main active PL inhibitor. Moreover, hesperidin could interact with PL by hydrogen bonds and van der Waals forces, and the interaction would not obviously change the secondary structure of PL. Overall, ponkan peel extract, having the strongest overall antioxidant activity, the highest content of hesperidin and total phenolic compounds among all tested CPEs, is a promising natural ingredient to scavenge free radicals and manage obesity.

Background Ischemia reperfusion (IR)-induced acute kidney injury (AKI) is accompanied by increased inflammatory response and oxidative stress. Eriocitrin is a flavonoid that is mainly derived from lemon or citrate juice. It exhibits various pharmacological effects and is known to have antioxidant and anti-steatotic benefits. However, research on the effect of eriocitrin against IR-induced oxidative stress and inflammation in AKI is limited. Methods In this study, an OGD/R of HK-2 cell in vitro and rat model of AKI in vivo were constructed. Then the cell or rats were treated with eriocitrin at different doses (60, 30, 10 mg/kg). The levels of apoptotic were detected by flow cytometry. Inflammatory and oxidative stress factors in supernatant in vitro and tissue in vivo. Meanwhile, Western blot was used to detect the change of dual-specificity phosphatase 14 (DUSP14), Nrf2 and nuclear factor-κB (NF-κB). Results Eriocitrin attenuated apoptosis of the human renal tubular epithelial cell line HK-2 mediated by oxygen glucose deprivation/reperfusion via the repression of inflammation and oxidative stress in a dose-dependent manner. Eriocitrin also enhanced the levels of dual-specificity phosphatase 14 (DUSP14) and Nrf2, and decreased NF-κB phosphorylation. Furthermore, the in vivo experiments indicated that eriocitrin dose-dependently alleviated IR-induced AKI and apoptosis in rats. By elevating DUSP14, eriocitrin promoted the expression of Nrf2 and inactivated NF-κB, thereby downregulating inflammation and oxidative stress. Moreover, inhibiting DUSP14 expression with protein tyrosine phosphatase (PTP) inhibitor IV reversed the kidney-protective effects of Eriocitrin. Conclusions Eriocitrin protected IR-induced AKI by attenuating oxidative stress and inflammation via elevating DUSP14, thereby providing a theoretical basis for the treatment of IR-induced AKI.

Background: Stroke is ranked on top of the persistent ailments associated with the brain. The incidence of ischemic stroke is rapidly rising along with intensified mortality as well as permanent disability conditions. However, tissue plasminogen activator (tissue-type plasminogen activator) is the only FDA-approved treatment for the treatment of stroke with decreased success rate. Eriocitrin, a flavonoid compound of Citrus limon with incredible therapeutic values, was active in the current investigation to explore the neuroprotective capability in arterial occlusion-provoked cerebral ischemic reperfusion injury (CIRI) in mouse replica. Materials and Methods: The neurological defects were considered through the standard scoring method and the expression status of apoptotic proteins, i.e., nuclear factor kappa B (NF-ƙB), caspase-3, and caspase-9, was examined via western blotting test. The expression of neuronal nitric oxide synthase (nNOS) was scrutinized through real-time polymerase chain reaction and standard ELISA kits were employed to examine the status of the proinflammatory markers. Results: The arterial occlusion provoked cerebral ischemic animals displayed the severely elevated status of inflammatory markers namely interleukin-6 (IL-6), IL-1β and tumor necrosis factor α, and the expression statuses of apoptotic proteins, as well as nNOS, were also uplifted while comparing to the sham subjected animals. Amazingly, eriocitrin (100 mg/kg) treatment revealed the declined inflammatory markers level, besides, the expression patterns of apoptotic proteins and nNOS were also reduced noticeably in the cerebral ischemic-reperfusion-operated animals. Conclusion: The novel findings of this investigation were demonstrated that the Eriocitrin delivered an astounding neuroprotection in the arterial occlusion-mediated CIRI in mouse replica, which possibly a promising neuroprotectant in cerebral ischemia.

The lime industry is generating more waste due to the increasing demand of juice. In this study, extractable and non-extractable phenolics in the Gallega lime waste, dried at different temperatures were determined and their antioxidant capacities were evaluated using DPPH (2,2-diphenyl-picrylhydrazyl), ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6/sulphonic acid) and, ORAC (oxygen radical absorbance capacity) methods. The amount of non-extractable phenolics measured in lime waste dried at 60, 90, and 120 °C were 38.4%, 39.2%, and 33.5%, respectively higher, compared to the amount of extractable phenolics. Dried lime waste is rich in extractable and non-extractable hesperidin (213.87 and 181.32 mg/g, respectively), and eriocitrin (55.22 and 97.24 mg/g, respectively) and non-extractable gallic acid (42.45 μg/g,). The antioxidant capacities of extractable and non-extractable phenolics were from highest to lowest: ABTS > ORAC > DPPH and ABTS > DPPH > ORAC, respectively. The information reported here may encourage lime industry operators to re-evaluate their by-products, extending the application of lime fruits and reducing waste.

The flavanones hesperidin, eriocitrin and eriodictyol were investigated for their prevention of the oxidative stress and systemic inflammation caused by high-fat diet in C57BL/6J mice. The mice received a standard diet (9.5% kcal from fat), high-fat diet (45% kcal from fat) or high-fat diet supplemented with hesperidin, eriocitrin or eriodictyol for a period of four weeks. Hesperidin, eriocitrin and eriodictyol increased the serum total antioxidant capacity, and restrained the elevation of interleukin-6 (IL-6), macrophage chemoattractant protein-1 (MCP-1), and C-reactive protein (hs-CRP). In addition, the liver TBARS levels and spleen mass (g per kg body weight) were lower for the flavanone-treated mice than in the unsupplemented mice. Eriocitrin and eriodictyol reduced TBARS levels in the blood serum, and hesperidin and eriodictyol also reduced fat accumulation and liver damage. The results showed that hesperidin, eriocitrin and eriodictyol had protective effects against inflammation and oxidative stress caused by high-fat diet in mice, and may therefore prevent metabolic alterations associated with the development of cardiovascular diseases in other animals.

Peppermint and spearmint, both members of the Lamiaceae family, have been used in the form of extracts, infusions, and decoctions, because of their health benefits. Consumers are looking for functional food products which not only provide health benefits but also necessitate less preparation time. Therefore, this study aimed to investigate the bioactive properties of powdered peppermint and spearmint extracts. Peppermint and spearmint extracts obtained using pressurized water extraction were made into powder forms with a spray dryer using the air inlet temperature of 140 degrees C. Powdered peppermint extract (PPE) and powdered spearmint extract (PSE) showed significant inhibition against key enzymes of type 2 diabetes (alpha-glucosidase) and hypertension (angiotensin 1-converting enzyme, ACE). Alpha glucosidase inhibition degree of PPE and PSE as IC50 values was 0.6 and 1.2 mg/mL, respectively, while IC50 values for the ACE inhibition test were 4.5 mg for PPE and 5.8 mg for PSE. The HPLC-DAD method for ACE inhibition activity showed the suitability of this method for plant extracts high in phenolics which had no interference effects on the results. There were no differences between PPE and PSE in the DPPH test. However, PPE had higher Trolox equivalent antioxidant capacity (190 mg/g) with the ABTS test than PSE (170 mg/g). The predominant phenolics of PPE and PSE were found to be eriocitrin (47 mg/g) and rosmarinic acid (27 mg/g), respectively.

Lemon processing generates thousands of tons of residues that can be preserved as flours by thermal treatment to obtain phenolic compounds with beneficial bioactivities. In this study, the effect of different drying temperatures (40, 50, 60, 70, 80, 90, 100 and 110 &deg, C) on the Total Phenolic Content (TPC), antioxidant and antimicrobial activities of phenolic compounds present in Citrus. lemon (L.) Burn f waste was determined. Identification and quantification of phenolic compounds were also performed by UPLC-PDA and UPLC-ESI-MS analysis. Eriocitrin (19.79&ndash, 27.29 mg g&minus, 1 DW) and hesperidin (7.63&ndash, 9.10 mg g&minus, 1 DW) were detected as the major phenolic compounds in the flours by UPLC-PDA and confirmed by UPLC-ESI-MS. Antimicrobial activity determined by Minimum Inhibitory Concentration (MIC) against Salmonella typhimurium, Escherichia coli and Staphylococcus aureus was observed. Accordingly, a stable functional flour as a source of bioactive phenolic compounds obtained from lemon residues at 50 &deg, C may be produced as a value-added product useful in various industrial sectors.

Cyclopia subternata plants are traditionally used for the production of the South African herbal tea, honeybush, and recently as aqueous extracts for the food industry. A C. subternata aqueous extract and mangiferin (a major constituent) are known to have anti-diabetic properties. Variation in phenolic composition and antioxidant capacity is expected due to cultivation largely from seedlings, having implications for extract standardization and quality control. Aqueous extracts from 64 seedlings of the same age, cultivated under the same environmental conditions, were analyzed for individual compound content, total polyphenol (TP) content and total antioxidant capacity (TAC) in a number of assays. An HPLC method was developed and validated to allow quantification of xanthones (mangiferin, isomangiferin), flavanones (hesperidin, eriocitrin), a flavone (scolymoside), a benzophenone (iriflophenone-3-C-β-glucoside) and dihydrochalcones (phloretin-3',5'-di-C-β-glucoside, 3-hydroxyphloretin-3',5'-di-C-hexoside). Additional compounds were tentatively identified using mass spectrometric detection, with the presence of the 3-hydroxyphloretin-glycoside, an iriflophenone-di-O,C-hexoside, an eriodictyol-di-C-hexoside and vicenin-2 being demonstrated for the first time. Variability of the individual phenolic compound contents was generally higher than that of the TP content and TAC values. Among the phenolic compounds, scolymoside, hesperidin and iriflophenone-3-C-β-glucoside contents were the most variable. A combination of the measured parameters could be useful in product standardization by providing a basis for specifying minimum levels.

The diet polyphenols are a secondary metabolites of plants able to act on inflammation process. Their anti-inflammatory activity is articulated through several mechanisms that are related to their antioxidative and radical scavengers properties. Our work is focused on a novel approach to inflammatory disease management, based on anti-glycative and matrix metalloproteinases (MMPs) inhibition effects, as a connected phenomena. To better understand these correlation, polyphenols Structure-Activity Relationship (SAR) studies were also reported. The antioxidant polyphenols inhibit the AGEs at different levels of the glycation process in the following ways: (1) prevention of Amadori adduct oxidation; (2) trapping reactive dycarbonyl compounds; (3) attenuation of receptor for AGEs (RAGE) expression. Moreover, several flavonoids with radical scavenging property showed also MMPs inhibition interact directly with MMPs or indirectly via radical scavengers and AGEs reduction. The essential polyphenols features involved in these mechanisms are C2-C3 double bond and number and position of hydroxyl, glycosyl and O-methyl groups. These factors induce a change in molecular planarity interfering with the hydrogen bond formation, electron delocalization and metal ion chelation. In particular, C2-C3 double bond improve the antioxidant and MMPs inhibition, while the hydroxylation, glycosylation and methylation induce a positive and negative correlation, respectively.

Naturally occurring flavonoids display a plethora of different biological activities, but emerging evidence suggests that this class of compounds may also act as antidepressant agents endowed with multiple mechanisms of action in the central nervous system, increasing central neurotransmission, limiting the reabsorption of bioamines by synaptosomes, and modulating the neuroendocrine and GABAA systems. Due to their presence in foods, food-derived products, and nutraceuticals, we established their role and structure-activity relationships as reversible and competitive human monoamine oxidase (MAO) inhibitors. In addition, molecular modeling studies, which evaluated their modes of MAO inhibition, are presented. These findings could provide pivotal implications in the quest of novel drug-like compounds and for the establishment of harmful drug-dietary supplement interactions commonly reported in the therapy with antidepressant agents.

This study aimed to investigate the immunomodulatory and antiallergic properties of preparations from lemon, Citrus medica L. (citrus), and quince, Cydonia oblonga Mill. (Cydonia), which are used in pharmaceutical products to treat patients suffering from allergic disorders. Preparations were analyzed with respect to their impact on the degranulation capacity from basophilic cells as well as mediator release from activated human mast cells in vitro, including IL-8 and TNF- α secretion. The results show that the degranulation of basophilic cells was diminished only in the presence of Citrus, and this effect was compared to the synthetic drug azelastine. Furthermore, Citrus and Cydonia both inhibited the production of IL-8 and TNF- α from human mast cells, and at low concentrations additive effects were observed. As a positive inhibition control, dexamethasone was used. LC-MS analyses showed that the major phenolic components in extracts from Citrus and Cydonia are eriocitrin and neochlorogenic acid, respectively. Nevertheless, these compounds do not show biological effects at concentration levels detected in their corresponding extracts. In conclusion, the present data provide a rational base for the use of the single pharmaceutical preparations from Citrus and Cydonia in a differentiated treatment of allergic disorders in part by the regulation of soluble allergic mediators from basophilic cells and mast cells.

Analysis of phenolic compounds in Cyclopia spp. (honeybush) is very important because of commercial interest in the plant material as an herbal tea and in extracts for the nutraceutical and cosmeceutical markets. An existing HPLC-DAD method was adapted and proved reproducible as evidenced by good intra- and inter-day precision. The method allows the quantification of several well-known as well as unidentified phenolic compounds. Its suitability for quantification of the major phenolic compounds present in the water extracts of unfermented and fermented Cyclopia subternata, Cyclopia intermedia, Cyclopia genistoides and Cyclopia sessiliflora was evaluated. Known compounds that were identified and quantified include mangiferin (0.1–11.8 g/100 g), isomangiferin (0.1–3.2 g/100 g), eriocitrin (not detected–0.4 g/100 g), hesperidin (0.2–1.2 g/100 g) and scolymoside (not detected–1.8 g/100 g), while narirutin and luteolin were detected in most samples, but could not be quantified due to low concentrations and co-elution. An unidentified compound (traces–4.8 g hesperidin equivalents/100 g), unidentified hydroxycinnamic acid derivative (not detected–0.3 g mangiferin equivalents/100 g), unidentified flavanone (not detected–2.0 g hesperidin equivalents/100 g) and an eriodictyol-glycoside (not detected–0.5 g hesperidin equivalents/100 g) could also be quantified. Large variation was observed within a sample series of the same extract type due to the nature of the plant material. Qualitative and quantitative differences were observed between species, while “fermentation”, a high-temperature process involving non-enzymatic oxidation, decreased the content of most phenolic compounds. Results using DAD as the only detection method should be handled with care, as the tentative identification of compounds 9 and 10, based on retention time and UV–Vis spectrum, could not be confirmed using liquid chromatography–electrospray ionisation-mass spectrometry.

Eriocitrin (eriodictyol 7-O-β-rutinoside) is the main flavonoid in lemon fruit. In this study, eriocitrin was investigated for its lowering effect on serum and hepatic lipids in high-fat and high-cholesterol fed rats. Rats in the control group (N= 6) were fed a 20% lard and 1% cholesterol diet for 21 d, and rats in the 0.35% eriocitrin group (N= 6) and 0.70% eriocitrin group (N= 6) were fed a diet supplemented with eriocitrin 0.35% and 0.70%, respectively. The content of hepatic total cholesterol and triglyceride in the eriocitrin group was no different from that of the control group. The total cholesterol, VLDL+LDL, triglyceride, and phospholipid in the serum of the 0.35% eriocitrin group showed significantly lower concentrations than the control group (P < 0.05), although there was no difference in the HDL concentrations among the groups. The lowering effect of eriocitrin for serum total cholesterol was thought to be caused by a decrease in VLDL+LDL. The 0.35% eriocitrin group was shown to have a significant increase in excretion of fecal bile acid (P < 0.05) and a tendency for enhanced hepatic m-RNA levels of LDL receptor in comparison with the control group.

Polyphenolic compounds such as eriocitrin, luteolin-7-O-rutinoside, diosmin, hesperidin, narirutin, isorhoifolin, rosmarinic and caffeic acids were identified in an aqueous extract (Ex) obtained from peppermint leaves (Menthae × piperitae folium). The content of polyphenols in Ex was as follows: eriocitrin 38%, luteolin-7-O-rutinoside 3.5%, hesperidin 2.9%, diosmin 0.8%, isorhoifolin 0.6%, narirutin 0.3%, rosmarinic acid 3.7% and caffeic acid 0.05%. The strongest antiradical activity (determined as DPPH• scavenging features) was observed for luteolin-7-O-rutinoside, eriocitrin and rosmarinic acid. Caffeic acid and hesperidin revealed a lower antiradical activity while isorhoifolin, narirutin and diosmin showed the lowest activity. The strongest anti-H2O2 activity was observed for eriocitrin, a little lower for rosmarinic acid. The rate of hydrogen peroxide scavenging activity displayed by luteolin-7-O-rutinoside and caffeic acid was lower than that of rosmarinic acids. Hesperidin appeared to be a very weak scavenger of hydrogen peroxide. Almost no anti-H2O2 activity was demonstrated for diosmin, narirutin and isorhoifolin. Among examined flavonoids, the strongest antiradical and anti-H2O2 activity was shown for compounds with two hydroxy groups bound to the Bring in ortho position in relation to each other. Replacement of one hydroxy group in the Bring with a methoxy group or removing one hydroxy group leads to decrease of antiradical and anti-H2O2 activity of flavonoids. Our results suggest that eriocitrin is a powerful peppermint antioxidant and a free radical scavenger.

Some of the medicinal properties of lemons are due to the flavonoids they contain since they are involved in many biological activities and have many health-related functions. The levels of the principal flavanones and flavone found in different cultivars of Citrus limon, are analysed in an attempt to identify the most interesting as regards the content of such secondary compounds. The results show that the immature fruits from cultivars Lisbon and Fino-49 are ideal for obtaining the flavanone hesperidin, while the mature fruits of cultivar Fino-49 and the leaves of cultivar Eureka are the most interesting for obtaining the flavone diosmin and the flavanone eriocitrin.

This review discusses the relationship between the chemical composition and antioxidant property of peppermint tisane and essential oil. Phenolic acids (e.g. rosmarinic and caffeic acids), flavones (e.g. luteolin derivatives) and flavanones (e.g. eriocitrin derivatives) are possibly the major infusion antioxidants. Vitamin antioxidants (e.g. ascorbic acid and carotenoids) are minor contributors to the overall antioxidant potential. Unsaturated terpenes having a cyclohexadiene structure (e.g. terpinene) and minor cyclic oxygenated terpenes (e.g. thymol), may contribute to antioxidant potential whilst acyclic unsaturated oxygenated monoterpenes (e.g. linalool) may act as pro-oxidants in essential oil. Findings on the antioxidant potential of major cyclic oxygenated terpenes (menthol and menthone) are conflicting. Antioxidant behaviour of aqueous/organic solvent extracts and essential oil as well as the effect of environmental stresses on essential oil and phenolic composition are briefly discussed.

Purpose: To investigate 38 natural and 62 branded lemon juices for their total antioxidant activities and flavonoid content. Methods : The ferric reducing antioxidant power was applied to evaluation of antioxidant. Additionally quercetin, eriocitrin, diosmin and hesperidin contents were evaluated by high performance liquid chromatography (HPLC). Results : Total antioxidant activity of the juices ranged from 91.38 ± 0.01 to 526.93 ± 0.12 μg/ml. The maximum contents of quercetin, hesperidin and eriocitrin 14.83 ± 2.83, 104.84 ± 12.58 and 10.68 ± 2.41 μg/mL, respectively. The natural juices had diosmin levels as high as 236.18 mL. The limit of detection (LOD) ranged from 0.15 μg mg-1 for hesperidine to 0.53 μg ml-1 for diosmin while the limit of quantification (LOQ) ranged from 0.27 μg mg-1 for hesperidine to 0.93 μg ml-1 for quercetin. Conclusion: The developed method can also be applied to the determination of related extracts of orange cultivars as well as various extracts of medicinal plants. Keywords : Antioxidant, Flavonoid, Hesperidin, Diosmin, Eriocitrin, Quercetin, Lemon juice

Lemon (Citrus limon) contains various bioactive flavonoids, and prevents obesity and obesity-associated metabolic diseases. We focused on eriocitrin (eriodictyol 7-rutinoside), a powerful antioxidative flavonoid in lemon with lipid-lowering effects in a rat model of high-fat diet. To investigate the mechanism of action of eriocitrin, we conducted feeding experiments on zebrafish with diet-induced obesity. Oral administration of eriocitrin (32 mg/kg/day for 28 days) improved dyslipidaemia and decreased lipid droplets in the liver. DNA microarray analysis revealed that eriocitrin increased mRNA of mitochondrial biogenesis genes, such as mitochondria transcription factor, nuclear respiratory factor 1, cytochrome c oxidase subunit 4, and ATP synthase. In HepG2 cells, eriocitrin also induced the corresponding orthologues, and reduced lipid accumulation under conditions of lipid loading. Eriocitrin increased mitochondrial size and mtDNA content, which resulted in ATP production in HepG2 cells and zebrafish. In summary, dietary eriocitrin ameliorates diet-induced hepatic steatosis with activation of mitochondrial biogenesis.

Objective: To assess the fruit of Feijoa sellowiana Berg var. coolidge and gorgiona, cultured in Sicily, for its gastroprotective effect, in association with performing phytochemical evaluation. Methods: By means of HPLC, vitamin E complex and polyphenol compounds were determined. The gastroprotective effect was investigated on ethanol-induced ulcers in rats, with sucralfate as reference drug. Samples of gastric mucosae, stained by periodic acid-Shiff and haematoxylin/ eosin, were observed by light microscopy. Results: In pulp and peel samples of both varieties of fruit α, β and γ tocopherols were identified, while δ was only in var. coolidge. In whole fruit of two varieties, catechin, eriodictyol, eriocitrin, pyrocatechol, quercetin, rutin, ellagic, gallic and syringic acid were determined. The fruit showed gastroprotective effect (ulcer index: var. coolidge=1.07, var. gorgiona=1.02). The efficacy was comparable to that of sucralfate (ulcer index 1.10). Histological examination confirmed the inhibition of ulcerogenic activity of the ethanol. Conclusions: Active principles of Feijoa sellowiana can play an important role in human diet and show beneficial effects on various diseases, particularly those caused by oxidative processes resulting in cell damage. The amount of polyphenols and vitamin E complex confirms the nutritional value of this fruit, grown in pedoclimatic condition very different from the origin area.

We could proposed that Ne-(hexanoy)lysine, HEL, become a useful biomarker for detection of oxidative stress damage occurred by exhaustive exercise. We examined the preventive effect of flavonoid compound, eriocitrin, against exercise-induced oxidative damage in rat liver. Eriocitrin administration prior to exercise significantly suppressed the increases in thiobarbituric acid-reactive substance caused by lipid peroxidation during exhaustive exercise. The increase in the contents of HEL in rat liver was also abolished by eriocitrin administration. The concentration of oxidized glutathione was significantly increased by exercise, but the eriocitrin administration suppressed this increase. These results suggested that eriocitrin administration prior to exercise prevented oxidative damages caused by exhaustive exercise-induced oxidative stress. Therefore, it was suggested that HEL could be a good biomarker for oxidative stress, especially at earlier stage when oxidative damage was occurred by lipid peroxidation than a stage of harmful aldehyde formation. Moreover, it was suggested that eriocitrin metabolites, eriodictyol and 3, 4 – dihydroxyhydrocinnamic, might scavenge free radicals and reactive oxygen species, resulting in suppression of lipid peroxidation and reactive proteins with radicals to form HEL. These findings implied that eriocitrin might be useful as an anti-oxidative compound to protect oxidative stress damages.

The monoclonal antibody to N(epsilon)-(hexanonyl)lysine (HEL), a novel adduct formed by the reaction of linoleic acid hydroperoxide and lysine, has been prepared and characterized. The obtained antibody specifically recognized the HEL moiety. Using the monoclonal antibody, we evaluated the protective effects of feeding eriocitrin, which is one of flavonoids in lemon fruit, on oxidative modification induced by exercise in rats. The supplementation of eriocitrin significantly suppressed the increase in HEL in the skeletal muscle by exercise. The result suggests that the determination of HEL may be a good method for evaluation of the protective effect of beneficial food factors against oxidative stress.

The effects of lemon flavonoids, as crude flavonoids prepared from lemon juice, were investigated in diabetic rats. The oxidative stress of eriocitrin (eriodictyol 7-O-beta-rutinoside) and hesperidin (hesperetin 7-O-beta-rutinoside) on streptozotocin-induced diabetic rats was investigated. Diabetic rats were given a diet which contained 0.2% crude flavonoids, 0.2% eriocitrin, and 0.2% hesperidin. After the 28-d feeding period, the concentration of the thiobarbituric acid-reactive substance in the serum, liver, and kidney of diabetic rats administered crude flavonoids, eriocitrin, and hesperidin significantly decreased as compared with that of the diabetic group. The levels of 8-hydroxydeoxyguanosine, which is exchanged from deoxyguanosine owing to oxidative stress, in the urine of diabetic rats administered eriocitrin and hesperidin significantly decreased as compared with that of the diabetic rat group. Crude flavonoids, eriocitrin, and hesperidin suppressed the oxidative stress in the diabetic rats. These results demonstrated that dietary lemon flavonoids of eriocitrin and hesperidin play a role as antioxidant in vivo.

We investigated the antioxidative flavonoid glycosides in the peel extract of lemon fruit (Citrus limon). Six flavanon glycosides: eriocitrin, neoeriocitrin, narirutin, naringin, hesperidin, and neohesperidin, and three flavone glycosides: diosmin, 6,8-di-C-β-glucosyldiosmin (DGD), and 6-C-β-glucosyldiosmin (GD) were identified by high-performance liquid chromatography (HPLC) analysis. Their antioxidative activity was examined using a linoleic acid autoxidation system. The antioxidative activity of eriocitrin, neoeriocitrin and DGD was stronger than that of the others. Flavonoid glycosides were present primarily in the peel of lemon fruit. There was only a small difference in the content of the flavonoid glycosides of the lemon fruit juice from various sources and varieties. Lemon fruit contained abundant amounts of eriocitrin and hesperidin and also contained narirutin, diosmin, and DGD, but GD, neoeriocitrin, naringin, and neohesperidin were present only in trace amounts. The content of DGD, GD, and eriocitrin was especially abundant in lemons and limes; however, they were scarcely found in other citrus fruits. The content of flavonoid compounds in lemon juice obtained by an in-line extractor at a juice factory was more abundant than that obtained by hand-squeezing. These compounds were found to be stable even under heat treatment conditions (121°C, 15 min) in acidic solution.

An antioxidant was isolated from the peel and juice of lemon fruit (Citrus limon BURM. f.). It was identified as eriocitrin (eriodictyol 7-rutinoside) of the flavanone glycoside by HPLC, 1H-NMR and 13C-NMR analyses. The purified eriocitrin was readily soluble in water, methanol, and ethanol. A water solution of 0.05% eriocitrin was weakly acidic (pH 4.2). Eriocitrin was found to be stable even at high temperature (121°C, 15 min) in acidic solution (pH 3.5). The distribution of eriocitrin in citrus fruits was found to be especially abundant in lemons and limes, however, it was scarcely found in other citrus fruits. In the case of lemon fruit, eriocitrin was primarily distributed in the peel (about 1,500 ppm) composed of the albedo (mesocarp), flavedo (epicarp), and pulp vesicles. It was also significantly present in the juice (about 200 ppm) but was not detected in the seed. Two varieties of lemon fruits, eureka and lisbon, almost had the same eriocitrin content. The antioxidative activity of eriocitrin in the linoleic acid autoxidation system was equal to that of α-tocopherol, and it was enhanced when used together with citric acid. The eriocitrin had a synergistic effect on α-tocopherol.

Objective To evaluate the chemopreventive potential of phenolic compounds – potassium apigenin, cocoa, catechins, eriocitrin and rosmarinic acid in oral carcinogenesis induced in hamsters by means of the topical application of 7,12-dimethylbenz(a)anthracene(DMBA). Study design An experimental study at the University of Murcia. Methods 50 male Syrian hamsters (Mesocricetus auratus) were divided into five groups of ten: Group I (control group): 0.5% DMBA; Group II: 0.5% DMBA + 1.1 mg/15 ml potassium apigenin; Group III: 05% DMBA + 2.5 mg/15 ml cocoa catechins; Group IV: 0.5% DMBA + 6 mg/15 ml eriocitrin; Group V: 0.5% DMBA + 1.3 mg/15 ml rosmarinic acid. The flavonoids were administered orally. All the animals were sacrificed after 12 weeks. Macroscopic, microscopic and immunohistochemical (PCNA and p53) analyses of the lesions were performed. Results All the groups treated with phenolic compounds showed lower incidences of tumour, greater differentiation and lower scores in the tumour invasion front grading system in comparison with the control group. Potassium apigenin and rosmarinic acid achieved the best results, the former considerably reduced the carcinoma tumour volumes developed and both significantly reduced the intensity and aggression of the tumours. Immunoexpression of PCNA and p53 were significantly altered during DMBA-induced oral carcinogenesis. Conclusions Animals treated with phenolic compounds, particularly potassium apigenin and rosmarinic acid, showed a lower incidence of tumours.