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Determination of hydrochlorothiazide and rutin in Chinese herb medicines and human urine by capillary zone electrophoresis with amperometric detection.

In this paper, capillary zone electrophoresis with amperometric detection (CZE-AD) was firstly applied to the simultaneous determination of rutin (RT) and hydrochlorothiazide (HCT) in compound Chinese herb medicines and human urine samples. The two analytes could be perfectly analyzed within 12 min and showed significant current responses at carbon electrode under the optimum conditions. It was found that the linear range of HCT was from 2.0 x 10(-6) to 1.0 x 10(-4) mol l(-1) and that of RT was from 1.0 x 10(-6) to 1.0 x 10(-4) mol l(-1). Their sensitivity was determined by linear regression and calculated as 7.02 x 10(4) and 2.17 x 10(5) nA l mol(-1), respectively, and their detection limits were 5.0 x 10(-7) and 2.0 x 10(-7) mol l(-1), respectively (S/N=3). Above results demonstrated that this method was of high sensitivity, good repeatability, high selectivity and could be used in metabolic kinetics studies of medicines. Satisfactory results were obtained when this method was used to simultaneously analyze the amounts of RT and HCT in one general compound Chinese herb medicine-Zhen Ju jiang Ya Pian and human urine samples.

Drugs, Chinese Herbal↗

Simultaneous spectrophotometric determination of rutin, quercetin and ascorbic acid in drugs using a Kalman Filter approach.

A UV-spectrophotometric analysis of severely overlapped spectra yielded by anti-capillary fragility pharmaceutical materials, viz. rutin, quercetin and ascorbic acid, in authentic mixtures and in tablets or soft elastic capsules was proposed. The method was based on Kalman Filter calibration of either orthogonal experimental design, i.e. standard solutions containing only one component at a time, or non-orthogonal experimental design, i.e. standard solutions containing more than one component. This calibration was followed by quantitative determinations of two- and three-component mixtures in synthetic mixtures or in oral dosages within the concentration range 2-10 microg ml(-1). A statistical analysis of the results was reported.

Ascorbic Acid↗

Repair of amino acid radicals of apolipoprotein B100 of low-density lipoproteins by flavonoids. A pulse radiolysis study with quercetin and rutin.

Selective oxidative damage to apolipoprotein B in LDL can be effected radiolytically by (*)Br(2)(-) radicals. Twenty-seven Trp residues constitute major primary sites of oxidation, but two-thirds of oxidized Trps ((*)Trp) that are formed are repaired by intramolecular electron transfer from Tyr residues with formation of phenoxyl radicals (TyrO(*)). Analysis of (*)Trp and TyrO(*) transient absorbance changes suggests that other apolipoprotein B residues, probably Cys, are oxidized. LDL-bound quercetin can efficiently repair this damage. Absorption studies show that a LDL particle has the capacity to bind approximately 10 quercetin molecules through interaction with apolipoprotein B. The repair occurs by intramolecular electron transfer characterized by a rate constant of 2 x 10(3) s(-)(1). In contrast, rutin, a related flavonoid which does not bind to LDL, cannot repair oxidized apolipoprotein B. Urate is a hydrophilic plasma antioxidant which displays synergistic antioxidant properties with flavonoids. Urate radicals produced by (*)Br(2)(-) can also be repaired by LDL-bound quercetin. This repair occurs with a reaction rate constant of 6.8 x 10(7) M(-)(1) s(-)(1). Comparison with previous studies conducted with human serum albumin-bound quercetin suggests that quercetin analogues tailored to be carried preferentially by lipoproteins might be more powerful plasma antioxidants than natural quercetin carried by serum albumin.

Amino Acids↗

Heat-induced, metal-catalyzed oxidative degradation of quercetin and rutin (Quercetin 3-O-rhamnosylglucoside) in aqueous model systems.

The oxidative degradation of quercetin and rutin in phosphate buffer solutions, pH 8.0, at 97 degrees C, was studied by means of UV-vis spectroscopy and reversed-phase high-performance liquid chromatography (HPLC). The effect of the transition metal ions Fe(2+) and Cu(2+) on degradation rate and browning development was also assessed. It was shown that both flavonols are very labile to thermally induced degradation under oxidative conditions. Fe(2+) and Cu(2+) caused an increase in the degradation rate, as well as an increase in browning (A(420)). Significant differences were observed in the degradation mechanisms, as implied by HPLC analyses. It is postulated that metal ions promote flavonol oxidation through reactive oxygen species formation, whereas increases in browning could be ascribed to oxidation and metal-polyphenol interactions.

Catalysis↗

The effect of dietary quercetin and rutin on AOM-induced acute colonic epithelial abnormalities in mice fed a high-fat diet.

Dietary quercetin (QU) and rutin (RU), phenolic flavonoids found in many fruits and vegetables, when fed to mice on a low-fat diet successfully modified the response to azoxymethanol (AOM) by initially inhibiting hyperproliferation and the formation of foci of dysplasia (FADs) and ultimately reducing tumor incidence (Carcinogenesis 12, 1193-1196, 1991). In this study, we tested the efficacy of QU and RU when a high-fat diet was presented. An AIN 76A diet made with 20% corn oil (CO) was supplemented with QU (0.5%, 2.0%, or 5.0%) and RU (2.0% or 4.0%). These five diets, as well as a 5.0% and a 20.0% CO diet, were fed to a group of CF1 female mice for nine weeks. Both QU and RU showed nonsignificant dose-related trends toward normalization of the AOM-induced upward extension of S phase cells. Examination of 500 microns of serially sectioned distal colon revealed that 29% of mice fed the 20% CO control diet were free of FADs. Among the mice fed QU, regardless of dose, > 80% were free of FADs. When the three groups fed QU were pooled and compared with the control 20% CO-fed mice, the degree of protection was significant (p < 0.01). Mice fed RU expressed a level of protection that bordered on the significant (p < 0.08). These data suggest that, regardless of the fat content of the diet, QU and RU are capable of modifying or inhibiting events in the development of chemically induced colonic neoplasia.

Animals↗

The effects of dietary bioflavonoid (rutin, quercetin, and naringin) supplementation on physiological changes in molar crestal alveolar bone-cemento-enamel junction distance in young rats.

The objective of this study was to evaluate the influence of dietary bioflavonoid (rutin [R], quercetin [Q], and naringin [N]) supplementation on physiological molar crestal alveolar bone(CAB)-cemento-enamel junction (CEJ) distances in young male albino rats. The effects of diets supplemented with 0.57% R, Q, or N, at the expense of dextrose, were tested on 40 young rats, divided into four groups, for a period of 42 days. Rat skulls were defleshed, and CAB-CEJ distance was scored according to the modified method of Keyes and Gold (Oral Surg Oral Med Oral Pathol 1955;8:492). Data were analyzed using one-way analysis of variance, post hoc Tukey's test, and Spearman's (R(2)) correlation. P <.05 was used to reject the null hypothesis. The N group demonstrated the lowest CAB-CEJ distance, followed by the R and Q groups (P <.001-.05), except in the mandibular lingual region, where the Q group had a lower CAB-CEJ distance than the N and R groups (P <.05). The control group showed the largest CAB-CEJ distances. Dietary bioflavonoid supplementation was shown to significantly reduce molar CAB-CEJ distance (P <.001-.05) during alveolar development in male young rats.

Animals↗

Quercetin and rutin as inhibitors of azoxymethanol-induced colonic neoplasia.

Dietary quercetin (QU) and rutin (RU), phenolic flavonoids commonly found in many fruits and vegetables, were provided to CF1 female mice for 50 weeks to assess the ability of these compounds to inhibit azoxymethanol (AOM)-induced colonic neoplasia. In addition to a control group fed an AIN 76A diet, five other groups received that diet to which was added either 0.1, 0.5 or 2.0% QU and 1.0 or 4.0% RU. Acute studies revealed that, among saline controls, no alteration of any proliferative parameters of colonic epithelial cells was observed among those groups receiving any dose of QU or RU. However, among the AOM-treated mice, both 2% QU and 4% RU significantly reduced hyperproliferation and inhibited the shift of S-phase cells to the middle and upper portion of crypts. Moreover, mice fed these concentrations of QU and RU had significantly fewer AOM-induced focal areas of dysplasia (FADs) than those fed the control diet (0.2 +/- 0.4 and 0.4 +/- 0.5 versus 3.6 +/- 2.3 respectively). Tumors occurred more frequently in the distal half of the colon, regardless of treatment. Compared with controls, mice fed 2% QU had a significantly reduced tumor incidence (25.0% versus 5.9%, P = 0.03). Those fed 4% RU showed only a trend toward inhibition (25% versus 9.7%, P = 0.11). Nevertheless, both 2% QU and 4% RU suppressed tumor multiplicity, i.e. fewer tumors/animal arose in these groups than in the AOM-treated control mice (1.2 versus 2.3, P = 0.005; 1.1 versus 2.3, P = 0.003 respectively). Clearly, QU and RU exhibit significant activity in reducing AOM-induced hyperproliferation of colonic epithelial cells and FAD incidence. This behavior successfully forecast the ability of both flavonoids to suppress tumor multiplicity and ultimately tumor development.

Animals↗

Interaction between riboflavin and rutin.

Riboflavin-5'-phosphate forms a charge transfer complex with rutin at neutral pH in the same manner as it forms one with tryptophan or serotonin, when the system is observed by quantitative spectrophotometry.

Flavin Mononucleotide↗

Transport characteristics of rutin deca (H-) sulfonate sodium across Caco-2 cell monolayers.

The aim of this study was to explore potential transport mechanisms of rutin deca (H-) sulfonate sodium (RDS) across Caco-2 cell monolayers. As an in-vitro model of human intestinal epithelial membrane, Caco-2 cells were utilized to evaluate the transepithelial transport characteristics of this hydrophilic macromolecular compound. Bi-directional transport study of RDS demonstrated that the apparent permeability (P(app)) in the secretory direction was 1.4 approximately 4.5-fold greater than the corresponding absorptive P(app) at concentrations in the range 50.0 approximately 2,000 microM. The transport of RDS was shown to be concentration, temperature and pH dependent. In the presence of ciclosporin and verapamil, potent inhibitors of P-glycoprotein (P-gp)/MRP2, the absorptive transport was enhanced and secretory efflux was diminished. RDS significantly reduced the efflux ratio of the P-gp substrate rhodamine-123 in a fashion indicative of P-gp activity suppression, while rhodamine-123 competitively inhibited the polarized transport of the compound. In conclusion, the results indicated that RDS was likely a substrate of P-gp. Several efflux transporters, including P-gp, participated in the absorption and efflux of RDS and they might play significant roles in limiting the oral absorption of the compound. These observations offered important information for the pharmacokinetics of RDS.

Biological Transport↗

Effects of combined administration of quercetin, rutin, and extract of white radish sprout rich in kaempferol glycosides on the metabolism in rats.

Quercetin, rutin, the extract of white radish sprout rich in kaempferol glycosides, and their combination were intragastrically administered to Wistar rats to investigate the interactive metabolism of these flavonoids. The combined administration of these flavonoids changed the concentrations of the metabolites in plasma as compared with the concentrations after the administration of a single compound.

Animals↗

[The effects of the combined use of mineral water with ascorbic acid and rutin experimentally and clinically].

Effects of a single and course intake of glucose, ascorbic acid and rutin in combination with mineral water Essentuki N17 on blood levels of glucose, hydrocortisone, ACTH, insulin were studied in 336 Wistar male rats. 80 patients with diabetes mellitus type I and II received a course of ascorutin and mineral water. Mineral water proved able to reduce a hyperglycemic effect of vitamins. A course of mineral water and ascorutin promotes improvement of carbohydrate, lipid metabolism, elevates plasma content of ascorbic acid, diminishes the need in sugar-reducing drugs.

Animals↗

[Effectiveness of the combination of alpha tocopherol, rutin, melilotus, and centella asiatica in the treatment of patients with chronic venous insufficiency].

BACKGROUND: The aim of this comparative clinical study was to evaluate the efficacy of the association of alphatocopherol, rutin, melilotus officinalis, and centella asiatica with oral administration in patients with chronic venous insufficiency. METHODS: Thirty patients with chronic venous insufficiency have been randomized in two groups of fifteen subjects (control and treatment group). During the period of treatment the patients didn't wear elastocompressive stockings. The therapeutic efficacy and the clinical tolerability of this association have been valued with clinical-instrumental evaluations and by a control after 15 and 30 days. Functional bothers, cramps and the edema have been valued in function presence and of their gravity with a clinical-score between 0 and 4. RESULTS: At the end of the observation period, a significant improvement of the clinical simptomatology was obtained, characterised by a diminution of the sovrafascial edema. CONCLUSIONS: The present study confirms previous clinical experiences regarding the described treatment and suggests its application in chronic venous insufficiency.

Antioxidants↗

[Oxidative determination of rutin in tablets using flow injection analysis and chemiluminescence].

A simple, rapid and fully automated flow injection method (FIA) with chemiluminescence detection after oxidation with KMnO4 in acid medium at room temperature has been developed for the determination of routine in pharmaceutical formulation. Hexamethaphosphate sodium was utilized as enhancer of chemiluminescence. The calibration curve was linear in the range 0.01-0.26 mmol.l-1 with detection limit 0.005 mmol.l-1, RSD 0.46% (n = 10) and a sample throughput of 75.h-1 using a 200 microliters sample volume. The method was used for the determination of routine in mass-produced dosage form: Rutin 250 tablets á 50 mg, (firm Nature's Bounty, USA). The FIA method was statistically compared with the official German Pharmacopoeia method and showed comparable accuracy, but with the advantages of simplicity, speed and amounts of reagents consumed.

Flow Injection Analysis↗

The use of rutin in a cat with idiopathic chylothorax.

A 9-year-old, male castrated cat was presented with labored breathing and lethargy of 5 d duration. Idiopathic chylothorax was diagnosed based on clinical signs, thoracic radiographs, and thoracentesis. Partial resolution of the pleural effusion followed treatment with rutin, a benzopyrone extracted from plants. The etiology, diagnosis, and treatment of this disease are discussed.

Animals↗

[Lipid peroxidation in aged patients. Influence of an antioxidant combination (vitamin C-vitamin E-rutin)].

Lipoperoxidation has an important role in the normal processes of the cell-life. The induction is produced by oxygen-derived free radicals which attack the membrane phospholipids. Such an attack is modulated by an enzymatic protection system (superoxide dismutase, catalase, glutathione peroxidase, glutathione transferase) and by a non-enzymatic one (vitamin C, vitamin E...). In various pathologic conditions, a dispoise takes place between radical attack and antiradical protection. The place taken by lipoperoxidation in the ageing process seems to be fundamental. We report here the results of a study carried out in aged and sick patients who were given an antioxidant medicamentous combination made from Vitamin C, Vitamin E and Rutin. Our results evidence that such a synergistic combination does modify both enzymatic protection system and lipoperoxidation, this latter showing a decrease under treatment.

Aged↗

[Effect of rutin and esculamine on models of aseptic inflammation].

It was shown in experiments on rats that intraabdominal administration of silver nitrate solution induces peritonitis and the subplantar administration of histamine, serotonin and prostaglandin E2 leads to an acute paw edema. Preliminary subcutaneous administration of esculamine or rutin inhibited the development of the inflammation. Esculamine proved more active here.

Animals↗