Evaluation of the Mutagenicity Potential of Trace-Rutinosidase Variety of Tartary Buckwheat (Fagopyrum tataricum Gaertn.) Using the Ames Test

To ensure the safety of “Manten-Kirari”, a non-bitter and trace-rutinosidase variety of Tartary buckwheat, we evaluated its mutagenic activity in a bacterial reverse mutagenicity assay, the Ames test. Salmonella typhimurium TA100, TA1535, TA98, TA153, and Escherichia coli WP2 uvrA were employed as test bacteria. The flour of “Manten-Kirari” was dissolved at 12 - 50,000 μg/mL in DMSO and investigated. The number of revertants did not differ compared to the negative control for all concentrations tested, whereas that in the positive control, the number of revertants was increased with or without metabolic activation for each bacterial strain tested. These results suggested that the flour of the Tartary buckwheat “Manten-Kirari” was not genotoxic.

Neuroprotective mechanisms of rutin for spinal cord injury through anti-oxidation and anti-inflammation and inhibition of p38 mitogen activated protein kinase pathway

Rutin has anti-inflammatory, antioxidant, anti-viral, anti-tumor and immune regulatory effects. However, the neuroprotective effects of rutin in spinal cord injury are unknown. The p38 mitogen activated protein kinase （p38 MAPK） pathway is the most important member of the MAPK family that controls inflammation. We assumed that the mechanism of rutin in the repair of spinal cord injury is associated with the inhibition of p38 MAPK pathway. Allen’s method was used to establish a rat model of spinal cord injury. The rat model was intraperitoneally injected with rutin （30 mg/kg） for 3 days. After treatment with rutin, Basso, Beattie and Bresnahan locomotor function scores increased. Water content, tumor necrosis factor alpha, interleukin 1 beta, and interleukin 6 levels, p38 MAPK protein expression and caspase-3 and -9 activities in T8–9 spinal cord decreased. Oxidative stress related markers superoxide dismutase and glutathione peroxidase levels increased in peripheral blood. Rutin exerts neuroprotective effect through anti-oxidation, anti-inflammation, anti-apoptosis and inhibition of p38 MAPK pathway.

Microwave-assisted Extraction of Rutin and Quercetin from Flos Sophorae

Three microwave-assisted extraction(MAE) procedures were studied. The first procedure was household microwave oven dynamic extraction(HMODE). The second procedure was special microwave oven bath extraction(SMOBE). The third procedure was microwave resonant cavity dynamic extraction(MRCDE). The results obtained by the three microwave-assisted extraction procedures were compared with those obtained by using traditional Soxhlet extraction. The results indicate that the MAE not only took a shorter time, but also simplified the procedure, and made the extraction a higher yield. At the same time the results obtained by the three MAE procedures were also compared with each other.

The Effect of Administration of Rutin on Plasma Levels of Estrogen, Prolactin, Growth Hormone and Gene Expression of Their Receptors in Mammary Glands in Ovariectomized Rats

The development of mammary glands, endocrine hormone concentrations and the gene expression of related receptors were measured in ovariectomized virgin rats after adminstration of an estrogen-like plant extract, rutin. Thirty-two ovariectomized virgin Wistar rats were randomly assigned to 4 treatments with 8 animals each： gastric infusion of 2 mL normal saline per unovariectomized rat per day （Sham）, gastric infusion of 2 mL normal saline per ovariectomized rat per day （Ova）, gastric infusion of 60 mg rutin kg-1 body weight （BW） per ovariectomized rat per day （Ova＋Rut）, or intramuscular injection of 60 ug estradiol kg-1 BW per ovariectomized rat weekly （Ova＋Est）. Samples of blood and mammary glands were harvested to determine the levels of estrogen （E2）, prolactin （PRL） and growth hormone （GH）, and the gene expression of estrogen receptors （ER）, prolactin receptors （PRLR） and growth hormone receptors （GHR） with radioimmunoassy （RIA） and RT-PCR technology, respectively. The E2 concentration in plasma and gland tissues from the rats of Ovx＋Rut or Ovx＋Est was higher than that of Ovx （P〈0.05）, but the plasma E2 concentration from the rats of Ovx＋Rut was lower than that of Sham （P〈0.05）. The order of the PRL concentration in plasma and gland tissues was Ovx〈Ovx＋Rut〈Ovx＋Est 〈Sham, and the difference in each treatment （P〈0.05）. The plasma GH concentration was lower in Ovx than in Ovx＋Rut or Ovx＋Est, and lower in Ovx＋Rut than in Sham （P〈0.05）. The GH concentration in gland tissues was lower in Ovx than in Ovx＋Rut or Ovx＋Est （P〈0.05）, and lower in Ovx＋Rut than in Sham （P〈0.05）. The gene expression of ER in gland tissues was increased in an order as Ovx〈Ovx＋Rut〈Ovx＋Est〈Sham （P〈0.05）, and PRLR, GHR showed the same trend. In conclusion, adminstration of rutin increased the E2 concentration in plasma and mammary glands, promoted pituitary PRL and GH release, up-regulated the gene expression of ER, PRLR and GHR, and stimulated mammary development in ovariectomized virgin rats.

Highly sensitive simultaneous electrochemical determination of myricetin and rutin via solid phase extraction on a ternary Pt@r-GO@MWCNTs nanocomposite

The simultaneous electrochemical determination of myricetin and rutin remains a challenge due to their indistinguishable potentials.To solve this problem,we constructed a ternary platinum nanoparticle,reduced graphene oxide,multi-walled carbon nanotubes (Pt@r-GO@MWCNTs) nanocomposite via a facile one-pot synthetic method.Under the optimized conditions,the ternary Pt@r-GO@MWCNTs nanocomposite exhibited good electrocatalytic activity toward myricetin and rutin via solid phase extraction and excellent performance for the simultaneous determination of myricetin and rutin.The oxidation peak current of myricetin was proportional to its concentrations in the range of 0.05-50μM with a detection limit of 0.01μM (S/N=3).The linear range for rutin was 0.05-50μM with a detection limit of 0.005μM(S/N=3).The ternary nanocomposite sensor also exhibited good reproducibility and stability,and was successfully used for the simultaneous determination of myricetin and rutin in real orange juice samples with recoveries ranging between 100.57% and 108.46%.

The leaf extract of Mallotus japonicus and its major active constituent, rutin,suppressed on melanin production in murine B16F1 melanoma

Objective: To find anti-melanogenesis materials used in whitening cosmetics.Methods: The ethanolic leaf extract of Mallotus japonicus(M. japonicus) having an anti-melanogenesis activity was separated by a sephadex LH-20 chromatography. Each fraction was measured for its tyrosinase inhibitory activity together with its polyphenol content using the Folin–Ciocalteu method. The anti-melanogenesis activity of the active fractions was determined by the melanin content in the murine B16F1 melanoma. The active fractions were put together due to similar constituents, and then separated by high performance liquid chromatography using a C-18 ODS column. The major antimelanogenesis compound was identified using1 H and13C-NMR and liquid chromatography-mass spectrometry.Results: The ethanolic leaf extract of M. japonicus showed an anti-tyrosinase activity with a high polyphenol content, resulting in suppression of melanin production in the B16F1 melanoma. The extract was separated and the active compound was identical as rutin based on the1 H,13C-NMR and liquid chromatography-mass spectrometry analysis data. In addition, the rutin treatment with cells reduced the melanin content in a concentration dependent manner without any cell toxicity. The leaf extract of M. japonicus containing rutin would be useful in whitening cosmetics for protection from UV-light exposure to be limiting the accumulation of melanin in skin.Conclusions: The leaf extract of M. japonicus and/or rutin isolated from the extract as a key whitening agent would be useful as a whitening cosmetic material for protecting against disorder skin due to melanin accumulation.

Rutin pretreatment promotes microglial M1 to M2 phenotype polarization

Microglial cells are important resident innate immune components in the central nervous system that are often activated during neuroinflammation.Activated microglia can display one of two phenotypes,M1 or M2,which each play distinct roles in neuroinflammation.Rutin,a dietary flavonoid,exhibits protective effects against neuroinflammation.However,whether rutin is able to influence the M1/M2 polarization of microglia remains unclear.In this study,in vitro BV-2 cell models of neuroinflammation were established using 100 ng/mL lipopolysaccharide to investigate the effects of 1-hour rutin pretreatment on microglial polarization.The results revealed that rutin pretreatment reduced the expression of the proinflammatory cytokines tumor necrosis factor-α,interleukin-1β,and interleukin-6 and increased the secretion of interleukin-10.Rutin pretreatment also downregulated the expression of the M1 microglial markers CD86 and inducible nitric oxide synthase and upregulated the expression of the M2 microglial markers arginase 1 and CD206.Rutin pretreatment inhibited the expression of Toll-like receptor 4 and myeloid differentiation factor 88 and blocked the phosphorylation of I kappa B kinase and nuclear factor-kappa B.These results showed that rutin pretreatment may promote the phenotypic switch of microglia M1 to M2 by inhibiting the Toll-like receptor 4/nuclear factor-kappa B signaling pathway to alleviate lipopolysaccharide-induced neuroinflammation.

UPLC-DAD法同时测定刺五加叶中Chlorogenic acid,Rutin,Hyperoside及Isoquercitrin四种成分的含量

目的：建立UPLC同时定量刺五加叶药材中Chlorogenic acid,Rutin,Hyperoside及Isoquercitrin等4种有效成分的方法。方法：色谱柱：HSS T3（100 mm×2.1 mm,1.8μm,Waters）;柱温：40℃;流速：0.4m L/min;进样量：5μL;流动相A：0.1%甲酸水溶液,流动相B：乙腈;梯度洗脱,洗脱条件：0-8 min,88%-75%A;8-9 min,75%-88%A;9-10 min,88%-88%A;紫外检测波长：360 nm。结果：对9批产地的刺五加叶药材进行测定,绿原酸最高的是虎林（1.287 mg/g）;芦丁含量最高的是鸡东（0.122mg/g）;金丝桃苷含量最高的是宾县（0.528 mg/g）;异槲皮苷含量最高的是五常（0.337 mg/g）。结论：该方法可用于刺五加叶中四种成分的含量测定,本研究所建立的方法稳定性、精密度、重复性良好,适用于刺五加叶的含量测定;不同来源的药材成分含量差异显著,对刺五加实施多指标的含量控制是保证其临床药用安全可控的必要途径。

The protective effect of rutin and quercetin on 5-FU-induced hepatotoxicity in rats

Objective: To investigate the effects of quercetin(Q) and rutin on 5-fluorouracil(5-FU)-induced hepatotoxicity.Methods: The control group was corn oil. The 5-FU group rats were corn oil and injected intraperitoneal 5-FU 50 mg/kg. Groups rutin 50 + 5-FU and rutin 100 + 5-FU were respectively 50 mg/kg and 100 mg/kg rutin. These groups were given 5-FU(50 mg/kg) in the 18th day. The group rutin 100 was rutin(100 mg/kg i.g.). Groups Q50 + 5-FU and Q100 + 5-FU were respectively 50 mg/kg and 100 mg/kg quercetin. These groups were given 5-FU(50 mg/kg) in the 18th day of quercetin application. The group Q100 was quercetin(100 mg/kg i.g.). In the end of experimental applications, blood was collected from anesthetized rats.Results: The MDA level was significantly higher in the 5-FU group compared with control group, and determined to be decreased in other groups. GPx and GSH levels were significantly decreased in the 5-FU group compared to the control, rutin 100 + 5-FU and Q100 + 5-FU groups. AST, ALT, LDH and ALP levels in the serum were significantly increased in the 5-FU group compared with the other groups. The results from this analysis show that while the caspase-3 level increases in the 5-FU group, it decreases in the Q50 + 5-FU, Q100 + 5-FU, rutin 50 + 5-FU and rutin 100 + 5-FU groups. Bcl-2 level decreased in the 5-FU group compared to the control group, but increased in the rutin 100 + 5-FU, Q50 + 5-FU and Q100 + 5-FU groups.Conclusions: In this study it was determined that the rutin and Q have protective effects on 5-FU-induced hepatotoxicity.

Protective Effects of Combined Therapy of Rutin with Silymarin on Experimentally-Induced Diabetic Neuropathy in Rats

The management of diabetic neuropathy (DN) is still a challenge for physicians. Hyperglycemia induced oxidative stress involves in the development of diabetic neuropathy, which could be reversed by supplementation of antioxidants. In the present study, it has targeted the oxidative stress mediated nerve damage in DN by using combined therapy of rutin (RT) and silymarin (SM). Diabetes was induced by single streptozotocin (STZ, 65 mg/kg i.p.) injection. The diabetic rats were treated daily with RT (100 mg/kg), SM (60 mg/kg) and RT (50 mg/kg) + SM (30 mg/kg) for 6 consecutive weeks. Pain-related behavior tests were performed including tail flick, paw-pressure analgesia and Rota-rod treadmill performance. Serum glucose, insulin, tumor necrosis factor-α (TNF-α), interleukine-6 (IL-6) and interleukine-1β (IL-β) levels were estimated. Thiobarbituric acid reactive substances (TBARS), reduced glutathione (GSH) levels and enzymatic activities of superoxide dismutase (SOD), catalase (CAT), glutathione-S-transferase (GST), glutathione reductase (GR) and glutathione peroxidase (GPx) were measured. Diabetic rats that developed neuropathy were revealed by decreased tail-flick latency, paw-withdrawal latency and motor coordination. RT (100 mg/kg/day) and SM (60 mg/kg/day) dosed to diabetic rats, ameliorated hyperalgesia, analgesia and led to improved motor coordination. However, the combined therapy of RT (50 mg/kg/day) with SM (30 mg/kg/day) showed more significant effects in these parameters. STZ significantly increased TBARS and decreased GSH levels in sciatic nerve whereas combined therapy of RT and SM produced higher significant protection compared to individual. Similarly, combined therapy showed more significant amelioration in decreased levels of SOD, CAT, GST, GS and GPx activities in sciatic nerve of diabetic rats. Present results concluded that the combined therapy of phenolic compounds such as RT and SM had higher protective effects than their individual supplementations against DM.

Effects of rutin on oxidative stress in mice with kainic acid-induced seizure

Flavonoids are present in foods such as fruits and vegetables. Several studies have demonstrated a relationship between the consumption of flavonoid-rich foods and prevention of human disease, including neurodegenerative disorders. We assessed the effect of rutin （quercetin-3-O-rutinoside） on oxidative stress in kainic acid （KA）-induced seizure. METHODS： Thirty-six BALB/c mice were randomly divided into three groups. In the control group, saline （intra-peritoneal, i.p.） was administered for 7 d, and on the last day, KA （10 mg/kg, i.p.） was injected 30 min after administration of saline. In rutin groups, mice were pretreated with rutin （100 and 200 mg/kg, i.p.） for 7 d, and on the last day, KA （10 mg/kg, i.p.） was injected 30 min after administration of rutin. Subsequently, behavioural changes were observed in mice. Lipid peroxidation and oxidative stress were measured respectively in the early and late phases after KA-induced seizures. RESULTS： Seizure scores in the rutin groups were significantly lower than those in the control group （P 〈 0.01）. Furthermore, rutin dose-dependently inhibited the number of wet-dog shakes （WDS） （P 〈 0.05）. Malondialdehyde level in the hippocampus of the rutin groups was significantly lower than that in the hippocampus of the control group on days 1 and 21 after KA administration. In the rutin groups, the thiol levels observed on day 1 after KA administration were higher than that in the control group （P 〈 0.01）. CONCLUSION： These results indicate that rutin has potential anticonvulsant and antioxidative activities against oxidative stress in KA-induced seizure in mice.

The pharmacokinetic study of rutin in rat plasma based on an electrochemically reduced graphene oxide modified sensor

An electrochemical method based on a directly electrochemically reduced graphene oxide （ERGO） film coated on a glassy carbon electrode （GCE） was developed for the rapid and convenient determination of rutin in plasma. ERGO was modified on the surface of GCE by one-step electro-deposition method. Electrochemical behavior of rutin on ERGO/GCE indicated that rutin underwent a surface-controlled quasi-reversible process and the electrochemical parameters such as charge transfer coefficient （α）, electron transfer number （n） and electrode reaction standard rate constant （ks） were 0.53, 2 and 3.4 s -1, respectively. The electrochemical sensor for rutin in plasma provided a wide linear response range of 4.70 × 10 ^-7 1.25 × 10^-5 M with the detection limit （s/n=3） of 1.84 × 10^-8 M. The assay was success- fully used to the pharmacokinetic study of rutin. The pharmacokinetic parameters such as elimination rate half-life （t1/2）, area under curve （AUC）, and plasma clearance （CL） were calculated to be 3.345 ± 0.647 rain, 5750 ±656.0 μg min/mL, and 5.891± 0.458 mL/min/kg, respectively. The proposed method utilized a small sample volume of 10 μL and had no complicated sample pretreatment （without deproteinization）, which was simple, eco-friendly, and time- and cost-efficient for rutin pharmacokinetic studies.

Anti-Nociceptive Effect in Mice of Thillai Flavonoid Rutin

We investigated the anti-nociceptive effect of Excoecorio ogollocho （E.ogollocho） against chemically and thermally induced nociception, Albino mice received a dose of 10, 15, 20, or 25 mg/kg of alkaline chloroform fraction （Alk-CF） of E.ogollocho by oral administration. Compared with controls, AIk-CF decreased the writhing numbers （P〈0.01） in a dose dependent manner. Further we determined that, AIk-CF contained, a potent compared to control, also potent anti-nociceptive agent that acted via opioid receptors and using HPLC, identified this compound as Rutin. Docking simulation demonstrated that Rutin interacted strongly with cyclooxygenase, forming a number of specific hydrogen bonds. In conclusion we have identified peripheral and central anti-nociceptive activities of E.ogollocho that involve opioid receptor, and in which the active compound is Rutin.

Highly sensitive electrochemical determination of rutin based on the synergistic effect of 3D porous carbon and cobalt tungstate nanosheets

Rutin,a flavonoid found in fruits and vegetables,is a potential anticancer compound with strong anticancer activity.Therefore,electrochemical sensor was developed for the detection of rutin.In this study,CoWO_(4) nanosheets were synthesized via a hydrothermal method,and porous carbon(PC)was prepared via high-temperature pyrolysis.Successful preparation of the materials was confirmed,and characterization was performed by transmission electron microscopy,scanning electron microscopy,and X-ray photoelectron spectroscopy.A mixture of PC and CoWO_(4) nanosheets was used as an electrode modifier to fabricate the electrochemical sensor for the electrochemical determination of rutin.The 3D CoWO_(4) nanosheets exhibited high electrocatalytic activity and good stability.PC has a high surface-to-volume ratio and superior conductivity.Moreover,the hydrophobicity of PC allows large amounts of rutin to be adsorbed,thereby increasing the concentration of rutin at the electrode surface.Owing to the synergistic effect of the 3D CoWO_(4) nanosheets and PC,the developed electrochemical sensor was employed to quantitively determine rutin with high stability and sensitivity.The sensor showed a good linear range(5-5000 ng/mL)with a detection limit of 0.45 ng/mL.The developed sensor was successfully applied to the determination of rutin in crushed tablets and human serum samples.

Electrochemical study and application on rutin at chitosan/graphene films modified glassy carbon electrode

Graphene（G） was dispersed into 0.5% chitosan（Chit） solution,then the composite films were coated on glassy carbon electrode（GCE）,the electrochemical behavior of rutin on a Chit/G modified GCE was investigated and the electrochemical parameters of rutin were calculated.Rutin effectively accumulated on the Chit/G/GCE and caused a pair of redox peaks at around 408 mV and 482 mV（vs.SCE） in 0.1M phosphate buffer solution（pH 4.0）.Under optimized conditions,the anodic peak current was linear to the rutin concentration in the range of 5×107-1.04×105M.The regression equation was：y 9.9219x-0.0025,r=0.9958.The proposed method was successfully used for the determination of rutin content in tablet samples with satisfactory results.

Determination of Ascorbic Acid, Rutin and Antioxidant Capacities of Wild <i/>Allium roseum</i>from Italy

This study is designed to investigate the antioxidant status and the presence of biologically-active compounds in Allium roseum L. and to compare the results with those of Allium sativum L. The content of thiosulfinates (Thio) and the levels of flavonols (quercetin and rutin), ascorbic acid (AA), glutathione reduced (GSH), glutathione oxidized (GSSG) and the antioxidant enzymes activities of glutathione peroxidase (GPx), glutathione reductase (GR) and catalase (CAT), were evaluated in bulbs, bulblets, flowers bulblets, leaves and flowers. Our study shows that bulbs of Allium roseum contain levels significantly higher of GSH, GSSG, AA, Thio, rutin and the activity of GPx and GR significantly higher than bulbs of Allium sativum. Moreover, the bulbs of Allium roseum show a significantly higher content of GPx, GR, CAT, GSH and GSSG than bulblets, flowers bulblets, leaves and flowers of Allium roseum. In Allium roseum, the greatest content of Thio is present in the flowers bulblets, while the levels of AA, quercetin and rutin are greater in the flowers. In conclusion, our result shows how Allium roseum exhibits antioxidant capabilities in all its fresh organs. The bulbs, bulblets, flowers bulblets, leaves and flowers are a good source of important bioactive compounds. Allium roseum possesses properties comparable to garlic indicating its possible nutritional and medicinal value.

Relaxant Effects of Quercetin and Rutin on Human Isolated Bronchus

Increasing epidemiological evidence supports the view, that quercetin has protective roles in a multitude of disease states in human who have a high intake of polyphenols. To investigate the ability of quercetin and its rutinoside, rutin, to modulate the relaxation of human airways smooth muscle and to determine the mechanism (s) of such relaxation, isolated human bronchus rings were suspended in individual organ baths, precontracted with acetylcholine or with histamine and the relaxing effects of quercetin and rutin were determined by measurement of isometric tension. Quercetin induced concentration-dependent relaxant responses on acetylcholine or histamine precontracted human bronchial rings and with almost equal effectiveness. In terms of potency (pD2) and efficacy (Emax), quercetin is more potent than rutin on relaxant responses of human bronchus. K+ and Ca2+ concentration-dependent contraction curves were inhibited after incubation with increasing concentrations of quercetin. Quercetin potentiated in a concentration-dependent manner the relaxant effects of isoprenaline or sodium nitroprusside. Rutin had no effect on K+-induced contraction and on relaxant activity of isoprenaline or sodium nitroprusside. Our results suggest that the bronchodilator effects of quercetin are modulated by an increase in cyclic nucleotide levels as well as an alteration in availability of Ca2+ to the contractile machinery.

分光光度法研究镧(Ⅲ)与芦丁(Rutin)的配合物(Ⅰ)

本文报导了用分光光度法研究镧(Ⅲ)与芦丁形成配合物的条件和配合物的组成,以及测定出的配合物稳定常数。

Study of inducibility and mechanism of phase 2 enzymes by quercetin and rutin

Objective The increasing recognition of the role for oxidative stress in hepatic disorders has led to extensive investigation on the protection by exogenous antioxidants against hepatic injury.In this study,we choose two typical polyphenol,quercetin and rutin,to investigate the mechanism of induction of cellular antioxidants and phase 2 enzymes in human HepG2 cells.Methods The HepG2 cells were treated with various concentrations of quercetin and rutin for 6 h and 24 h.The activities of NAD(P)H:quinone oxidoreductase(NQO1)in HepG2 cells were measured by 2,6-dichloroindophenol reduction method.The content of superoxide dismutase(SOD)was determined with the method of chemical colorimetry.The protein expressions of NQO1 and NF-E2-related factor 2(Nrf2)in HepG2 cells were detected by Western blotting.Results Incubation of HepG2 cells with quercetin and rutin resulted in a marked concentration-and time-dependent induction of a number of cellular antioxidants and phase 2 enzymes,including NQO1,SOD.Quercetin and rutin treatment of HepG2 cells also caused increase in protein expressions of NQO1 and Nrf2.Conclusions This study demonstrates that a series of phase 2 enzymes in HepG2 cells can be induced by quercetin and rutin in a concentration-and time-dependent fashion by upregulation the protein expression of nrf2.

Tris(2,2'-bipyridyl)ruthenium(Ⅱ) electrochemiluminescence (ECL) enhanced by rutin on platinum electrode

Ru（bpy）3^2＋ electrochemiluminescence （ECL） was applied to determination of rutin. ECL intensity of Ru（bpy）3^2＋ could be enhanced in the presence of rufin in basic solution on platinum electrode. At pH 9.9, light emission intensity was found to be linear with rutin in the range of 1-50μmol/L.