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PubMed2005

[Investigation on interactions of rutin and chloramphenicol with beta-cyclodextrin using capillary electrophoresis].

The interactions of two medicines of rutin and chloramphenicol with beta-cyclodextrin were investigated using mobility shift method by capillary electrophoresis. The size of the capillary column was 37 cm x 50 microm i.d. with an effective length of 30 cm. The running buffer was a mixture of 25 mmol/L sodium borate and 100 mmol/L boric acid (pH 8.6). Effective mobilities of the two medicines changed with altering the concentration of beta-cyclodextrin. By nonlinear least square fitting curve, the inclusion constants of 98.5 and 1 204 L/mol for rutin and chloramphenicol were obtained at 25 degrees C, respectively. The inclusion constants at different temperatures were determined, from which a series of thermodynamic parameters were derived. Experimental results show that an obvious relationship of mutual compensation between enthalpy and entropy existed in these inclusion reactions. The most stable configurations of the inclusions were calculated using MM2 force field, and the results were well in agreement with the experimental results.

Chloramphenicol↗
PubMed1980

Flavonoids with antioxidant action (naringin and rutin) and the release of mastocytic and nonmastocytic histamine.

In view of the data about the antioxidant mechanism of the membrane-stabilizing action of the bioflavonoids, the participation of this mechanism in the release of histamine as well is assumed to be possible. Experiments are carried out on 35 male albino rats. The effect of the flavonoids naringin and rutin on the level of mastocytic and nonmastocytic histamine is studied, as well as on its release induced by compound 48/80 (2 mg/kg i. p.). The substances are applied intraperitonealy in doses of 200 mg/kg; corresponding to 10% DL50. The histamine content is determined fluorimetrically by the method of Schore et al. (1959). The results show that naringin and rutin have no effect on the levels of mastocytic and nonmastocytic histamine. They prevent the release of mastocytic histamine, induced by compound 48/80.

Animals↗
PubMed1983

[Effect of rutin on the cholesterol content of the lymph, blood and tissues of the dog].

It has been discovered in experiments on mongrel dogs anesthetized with morphine and hexenal that intravenous injection of rutin (3 mg/kg bw) reduced the concentration of total, esterified and free cholesterol in blood serum, with the exception of free cholesterol level in arterial blood, which increased. Under the same conditions, the concentration of free and esterified cholesterol in thoracic duct lymph ascended. In the popliteal lymph node, gastrocnemius muscle and liver, the content of total cholesterol appreciably dropped as compared to control. Rutin has been found to accelerate the lymph flow and to raise cholesterol resorption from the interstitial space. It is inferred that lymph plays an important part in cholesterol transport in the body.

Animals↗
PubMedDate not supplied

[The effect of the combined use of mineral water and rutin on the function of the adrenal cortex and pancreatic islet apparatus (an experimental study)].

Before modelling of experimental ulcer according to I. S. Zavodskaia the animals (157 male Wistar rats) were given for 24 days mineral water Essentuki N 17 and rutin in a dose 20 or 40 mg. Those given 20 mg of rutin in combination with mineral water demonstrated a higher rise in blood concentrations of hydrocortisone, insulin and thyroxine. Gastric mucosa and levels of serum alpha-1, alpha-2, beta-globulins and albumins were less damaged.

Adrenal Cortex↗
PubMed1996

Comparison of the Inhibitory Effects of Quercetin and Rutin on the Oxidative Modification of LDL induced By Fe(2+)Cu(2+).

Using the oxidative modification of low density lipoprotein (LDL) as a model and the content of thiobabituric acid reactive substances (TBARS) s an index, the inhibitory effects of quercetin and rutin on oxidative modification of LDL induced by Fe(2+) and Cu(2+) were compared. The results showed that the rates of oxidative modification of LDL induced by Fe(2+) and Cu(2+) were similar in 0.15 mM NaCl (pH 7.4). The inhibitory action of quercetin on the oxidative modification of LDL induced by Cu(2+) was slightly more effective than in the case of induction by Fe(2+), and the action of rutin on the oxidation modification induced by Fe(2+) was significantly more effective than in the case of induction by Cu(2+).

Journal Article↗
PubMed1994

Pharmacodynamics and pharmacokinetics of Veliten (rutine, alpha-tocopherol and ascorbic acid) in patients with chronic venous insufficiency.

The aim of this study was to evaluate the pharmacodynamics and pharmacokinetics of a single oral dose of Veliten in 12 patients affected by chronic venous insufficiency. In particular, the pharmacokinetics of two components of Veliten, namely rutine and alpha-tocopherol, were considered, while with respect to pharmacodynamics, studies were made of venous function, haemocoagulative and fibrinolytic balance, and haemorheological parameters. Correlation between such changes and plasma drug levels was also evaluated. We found a significant increase of venous tone, venous capacity and venous distension after drug intake, as well as a significant activation of fibrinolysis (globally evaluated with euglobulin lysis time), related to a slight increase of plasminogen tissue activator. These changes appeared concomitantly with maximal plasma levels of rutine. We did not find any modifications of coagulative and haemorheological parameters.

Administration, Oral↗
PubMed2006

Metabolism of quercetin and rutin by the pig caecal microflora prepared by freeze-preservation.

Several studies confirm a protection of cardiovascular diseases and certain forms of cancer by dietary flavonoid intake. The bioavailability of flavonoids is influenced by the metabolism of the microflora in the intestine. Using a new in vitro model system the deglycosylation of the flavonol rutin and the degradation of its aglycone quercetin were investigated by using fresh pig caecal inocula in comparison to inocula prepared before by freeze-preservation between 6 wk and 5 months. The incubation experiments led to the same pattern of phenolic degradation products in comparable amounts in both preparations using HPLC-DAD and GC-flame ionization detection (GC-FID) or GC-MS detection within 24-48 h of incubation. With the preservation of the microbial vitality and the metabolic efficiency by freeze-preparation over several months the experimental design of microbial metabolism studies will be independent in time and locality.

Animals↗
PubMed2006

Effect of thermal processing on the flavonols rutin and quercetin.

The current research involves the study of the thermal treatment of quercetin and rutin in an aqueous model system (cooking). These substances were heated and their degradation was followed by high-performance liquid chromatography/diode-array detection (HPLC/DAD). The influence of pH and the involvement of oxygen in the degradation were studied. HPLC/electrospray ionization multi-stage mass spectrometry (ESI-MS(n)) was used for the structural characterization of the compounds produced. The influence of the degradation of the phenolic compounds on their antioxidant properties was elucidated by a electron spin resonance (ESR) spectrometry study of the reaction samples mixed with the stabilized radical, Fremy's salt. Strong degradation of the model substances took place under weak basic and oxidative conditions. Quercetin showed the most intense degradation. Protocatechuic acid could be identified as a cleavage reaction product by analyzing its retention time and molar mass during the degradation of quercetin. The structure of a second cleavage product could be identified on the basis of ESI-MS(n) fragmentation data. Also, several structures for reaction products of oxidized quercetin are suggested. The ESR analysis showed a decrease in the antioxidant activity of the reaction samples after heat treatment in aqueous solution.

Chromatography, High Pressure Liquid↗
PubMed1991

The synthesis and characterization of uridine 5'-(beta-L-rhamnopyranosyl diphosphate) and its role in the enzymic synthesis of rutin.

Uridine 5'-(beta-L-rhamnopyranosyl diphosphate) was synthesized by the condensation of uridine 5'-diphenylpyrophosphate and beta-L-rhamnopyranosyl phosphate. That sugar 1-phosphate was made via the phosphitylation of the hemiacetal hydroxyl group of 2,3,4-tetra-O-acetyl-beta-L-rhamnopyranose. An enzyme preparation from the primary leaves of mung bean (Phaseolus aureus) was shown to catalyze the transfer of L-rhamnose from UDP-beta-L-rhamnose to the flavonol D-glucoside isoquercitrin to form rutin.

Plants↗
PubMed1986

Isolation and identification of rutin as the major mutagen of red wine.

The polyphenolics of a red wine were concentrated by salt-induced phase separation into acetone-alcohol and fractionated by Sephadex LH-20 and multi-layer counter-current chromatography. The mutagenicity of each fraction was evaluated by the Salmonella mutagenesis assay. The mutagen of red wine required activation by both rat-liver microsomal enzymes and human-fecal enzymes (fecalase). The mutagenic component of red wine was purified to homogeneity by reverse-phase high-performance liquid chromatography (RPHPLC) on Lichrosorb C18 and was identified as rutin by UV spectrometry, co-chromatography with authentic standard on RPHPLC and gas-liquid chromatography/mass spectrometry.

Adult↗
PubMed1987

Urinary and faecal mutagenicity in Sprague-Dawley rats dosed with the food mutagens quercetin and rutin.

The natural flavonoid quercetin was administered to Sprague-Dawley rats by ip injection or gastric intubation of a single dose of 500, 1000 or 2000 mg/kg body weight. Mutagenicity assays with Salmonella typhimurium strain TA98 showed moderate mutagenic activity in the urines and faecal extracts but not in plasma samples from the treated animals. The mutagenic activity detected in the urines accounted for about 0.5% of the administered dose, irrespective of the route of administration and the dose level. Higher mutagenicity was demonstrated in faecal extracts. Rutin (quercetin-3-O-rutinoside) was administered by gavage and ip injection at 2000 mg/kg. Although the chemical was inactive as a mutagen in vitro, significant mutagenicity was detected in the urines and faecal extracts of the treated rats. Such activity was similar to that detected after administration of free quercetin in a dose some four times lower (by weight).

Animals↗
PubMed1993

Simultaneous isolation of Rutin and Esculin from plant material and drugs using solid-phase extraction.

Simultaneous isolation of Rutin and Esculin from pharmaceutical materials (plant--Flos hippocastani and drugs--Venescin, Venacorn) using solid-phase extraction (SPE) have been made. For this investigation the Bakerbond SPE columns with different unpolar and polar chemically bonded phases were used. On the basis of isolation investigation the influence of SPE packing materials on the selectivity change and recovery of both extracted substances were studied.

Chemistry, Pharmaceutical↗
PubMed2005

Quercetin, but not rutin and quercitrin, prevention of H2O2-induced apoptosis via anti-oxidant activity and heme oxygenase 1 gene expression in macrophages.

In the present study, we examine the protective mechanism of quercetin (QE) on oxidative stress-induced cytotoxic effect in RAW264.7 macrophages. Results of Western blotting show that QE but not its glycoside rutin (RUT) and quicitrin-induced HO-1 protein expression in a time- and dose-dependent manner, and HO-1 protein induced by QE was blocked by an addition of cycloheximide or actinomycin D. Induction of HO-1 gene expression by QE was accompanied by inducing ERKs, but not JNKs or p38, proteins phosphorylation. Addition of PD98059, but not SB203580 or SP600125, significantly attenuates QE-induced HO-1 protein and mRNA expression associated with blocking the expression of phosphorylated ERKs proteins. H(2)O(2) addition reduces the viability of cells by MTT assay, and appearance of DNA ladders, hypodiploid cells, and an increase in intracellular peroxide level was detected. Addition of QE, but not QI or RUT, significantly reduced the cytotoxic effect induced by H(2)O(2) associated with blocking the production of intracellular peroxide, DNA ladders, and hypodiploid cells. QE protection of cells from H(2)O(2)-induced apoptosis was significantly suppressed by adding HO inhibitor SnPP or ERKs inhibitor PD98059. Additionally, QE protects cells from H(2)O(2)-induced a decrease in the mitochondrial membrane potential and a release of cytochrome c from mitochondria to cytosol by DiOC6 and Western blotting assay, respectively. Activation of apoptotic proteins including the caspase 3, caspase 9, PARP, D4-GDI proteins was identified in H(2)O(2)-treated cells by Western blotting and enzyme activity assay, and that was significantly blocked by an addition of QE, but not RUT and QI. Furthermore, HO-1 catalytic metabolites carbon monoxide (CO), but not Fe(2+), Fe(3+), biliverdin or bilirubin, performed protective effect on cells from H(2)O(2)-induced cell death with an increase in HO-1 protein expression and ERKs protein phosphorylation. These data suggest that induction of HO-1 protein may participate in the protective mechanism of QE on oxidative stress (H(2)O(2))-induced apoptosis, and reduction of intracellular ROS production and mitochondria dysfunction with blocking apoptotic events were involved. Differential anti-apoptotic effect between QE and its glycosides RUT and QI via distinct HO-1 protein induction was also delineated.

Animals↗
PubMed2004

Evaluation of the toxicity of enzymatically decomposed rutin with 13-weeks dietary administration to Wistar rats.

The subchronic toxicity of enzymatically decomposed rutin, which consists mainly of isoquercitrin, was investigated in male and female Wistar rats with dietary administration at concentrations of 0, 0.2, 1 and 5% for 13 weeks. No mortality or abnormal clinical signs were observed throughout the experimental period in any groups. Body weight gain was reduced from week 10 to the end of the experiment in the 5% dosed males as compared to the 0% controls. Decreased erythrocytic parameters, i.e. red blood cell count, hemoglobin concentration and hematocrit, and significantly lowered serum triglyceride levels were also detected in the 5% males. Organ weight measurement, macro and microscopic observation revealed no test substance-related toxicological changes. Based on the above findings, no-observed-adverse-effect levels (NOAELs) for male and female rats were estimated to be 1 and 5%, respectively, translating into 539 and 3227 mg/kg b.w./day.

Animals↗
PubMed2006

Determination of rutin deca(H-) sulfate sodium in rat plasma using ion-pairing liquid chromatography after ion-pairing solid-phase extraction.

Rutin deca(H-) sulfate sodium (RDS) is one of the most important drug candidates, which possesses very good activity as inhibitor of the complement system of warm-blooded animals and human immunodeficiency virus (HIV). In order to understand RDS metabolism and disposition, an ion-pairing coupled with solid-phase extraction technique (IP-SPE) was developed to extract RDS from rat plasma sample. Tetrabutyl ammonium bromide (TBAB) buffer (0.2 M, pH 8.0) was used as the ion-pairing extraction reagent and LC-18 was used as SPE sorbent. In addition, an ion-pairing HPLC method was established for the specific determination of RDS. A reversed phase C8 column was used for the separation of RDS and nitrendipine (internal standard). The mobile phase was composed of 10 mM phosphate buffer solution containing 25 mM TBAB-acetonitrile (52:48, v/v, pH 7.5). The calibration curve was linear from 0.3 to 30 nmol/mL. The analytical recovery from rat plasma was found to be 97.9+/-4.1% (n = 15). LOD and LOQ for RDS in plasma were calculated to be 0.12 nmol/mL and 0.30+/-0.024 nmol/mL (R.S.D. = 8.2%, n = 5), respectively. The intra- and inter-day precision was less than 9.2%. The assay was applied to a preliminary pharmacokinetic study in three male rats after those received a single intravenous bolus via caudal vein of 12 micromol/kg RDS.

Animals↗
PubMed2005

Resonance light scattering technique for the determination of protein with rutin and cetylpyridine bromide system.

A new resonance light scattering (RLS) assay of protein is presented. In Tris-NaOH (pH = 10.93) buffer, the RLS of rutin-cetylpyridine bromide (CPB) system can be greatly enhanced by protein, including bovine serum albumin (BSA) and human serum albumin (HSA). The enhanced RLS intensities are in proportion to the concentration of proteins in the range of 5 x 10(-9) to 2.5 x 10(-6) g ml(-1) for BSA and 2.5 x 10(-8) to 3.5 x 10(-6) g ml(-1) for HSA. The detection limits (S/N = 3) are 3.0 ng ml(-1) for BSA and 10.0 ng ml(-1) for HSA. Samples are determined satisfactorily.

Animals↗
PubMed2006

Fluorescence enhancement of yttrium(III)-rutin by nucleic acids in the presence of cetyltrimethylammonium bromide.

It is found that nucleic acids can enhance the fluorescence intensity of yttrium(III) (Y(3+))-rutin in presence of cetyltrimethylammonium bromide (CTMAB) system. In hexamethylenetetramine (HMTA)-HCl buffer, the maximum enhanced fluorescence is produced, with maximum excitation and emission wavelengths at 452 and 520 nm, respectively. Based on this, a new fluorimetric method of determination of nucleic acids is proposed. Under optimum conditions, the enhanced fluorescence intensity is proportion to the concentration of nucleic acids in the range of 1.0 x 10(-7) to 1.0 x 10(-5)g/ml for fish sperm DNA (fsDNA), 1.0 x 10(-7) to 4.6 x 10(-6)g/ml for yeast RNA (yRNA), their detection limits (S/N=3) are 7.5 x 10(-8), 8.0 x 10(-8)g/ml, respectively. The interaction mechanism is also studied.

Animals↗