Reduction of enantioselectivity in the kinetic disposition and metabolism of verapamil in rats exposed to toluene

2008 ◽  
Vol 86 (5) ◽  
pp. 232-239 ◽  
Author(s):  
F.H. Mateus ◽  
J.S. Lepera ◽  
M.P. Marques ◽  
V.B. Boralli ◽  
V.L. Lanchote
Keyword(s):  
Single Dose ◽  
Oxidative Metabolism ◽  
Wistar Rats ◽  
Plasma Concentrations ◽  
Wilcoxon Test ◽  
Control Group ◽  
Chiral Drugs ◽  
Blood Samples ◽  
Male Wistar Rats ◽  
Air Control

Toluene and verapamil are subject to extensive oxidative metabolism mediated by CYP enzymes, and their interaction can be stereoselective. In the present study we investigated the influence of toluene inhalation on the enantioselective kinetic disposition of verapamil and its metabolite, norverapamil, in rats. Male Wistar rats (n = 6 per group) received a single dose of racemic verapamil (10 mg/kg) orally at the fifth day of nose-only toluene or air (control group) inhalation for 6 h/day (25, 50, and 100 ppm). Serial blood samples were collected from the tail up to 6 h after verapamil administration. The plasma concentrations of verapamil and norverapamil enantiomers were analyzed by LC-MS/MS by using a Chiralpak AD column. Toluene inhalation did not influence the kinetic disposition of verapamil or norverapamil enantiomers (p > 0.05, Kruskal–Wallis test) in rats. The pharmacokinetics of verapamil was enantioselective in the control group, with a higher plasma proportion of the S-verapamil (AUC 250.8 versus 120.4 ng·h·mL–1; p ≤ 0.05, Wilcoxon test) and S-norverapamil (AUC 72.3 versus 52.3 ng·h·mL–1; p ≤ 0.05, Wilcoxon test). Nose-only exposure to toluene at 25, 50, or 100 ppm resulted in a lack of enantioselectivity for both verapamil and norverapamil. The study demonstrates the importance of the application of enantioselective methods in studies on the interaction between solvents and chiral drugs.

scholarly journals PENGARUH PEMBERIAN SAGU DIBANDING NASI TERHADAP BERAT BADAN TIKUS WISTAR

e-CliniC ◽  
2013 ◽  
Vol 3 (2) ◽  
Author(s):  
Eny A. Watumlawar ◽  
Sarah M. Warouw ◽  
Stefanus Gunawan
Keyword(s):  
Body Weight ◽  
Wistar Rats ◽  
Wilcoxon Test ◽  
Control Group ◽  
Increase Body Weight ◽  
Control Group Design ◽  
Tissue Mass ◽  
Group Design ◽  
Post Test ◽  
Male Wistar Rats

Abstract: Weight is one measure that gives description of the tissue mass including body fluids. Weight change is nfluenced by nutriment consumption. Sago contains high carbohydrates that can increase body weight. This study aimed to obtain the effect of sago compared to rice to body weight of wistar rats. This was a random laboratory experimental pre-post test with control group design. Subjects were male wistar rats, aged 5-6 months. The rats were divided in two groups: rice group as control and sago group. Sago was cooked in papeda form as much as 75 g of dried sago and 300 mL water. The rats were fed for 2 weeks. Data were analyzed by using the Wilcoxon test. The results showed that the sago group showed an increase of body weight significantly (p=0,001) meanwhile the rice group lose body weight significantly (p=0,001). Conclusion: Sago can increase body weight of wistar rats significantly.Keywords: body weight, sago, riceAbstrak: Berat badan merupakan salah satu ukuran yang memberikan gambaran massa jaringan termasuk cairan tubuh. Salah satu yang memengaruhi berat badan yaitu dengan mengonsumsi makanan bergizi. Sagu memiliki kandungan karbohidrat (pati) yang besar dan dapat meningkatkan berat badan. Penelitian ini bertujuan untuk mengetahui pengaruh pemberian sagu terhadap berat badan dibanding nasi pada tikus wistar. Desain penelitian ini ialah eksperimental laboratorium acak pre-post test with control group design. Subjek penelitian ialah tikus wistar jantan berusia 5-6 bulan dibagi atas 2 kelompok: kelompok nasi (kontrol) dan kelompok sagu. Sagu dimasak dalam bentuk papeda sebanyak 75 g sagu kering dan 300 mL air. Tikus diperlihara selama 2 minggu. Berat badan diukur dengan menggunakan timbangan. Data dianalisis dengan uji Wilcoxon. Hasil penelitian menunjukkan bahwa pemberian sagu sebanyak 2 cc setiap hari selama seminggu mampu meningkatkan berat badan secara bermakna (p = 0,001) sedangkan pemberian nasi menurunkan berat badan (p=0,001). Simpulan: Pemberian sagu dapat meningkatkan berat badan tikus wistar secara bermakna.Kata kunci: berat badan, sagu, nasi

Influence of quinidine, fluvoxamine, and ketoconazole on the enantioselective pharmacokinetics of citalopram in rats

2008 ◽  
Vol 86 (11) ◽  
pp. 770-776 ◽  
Author(s):  
Adriana Rocha ◽  
Eduardo B. Coelho ◽  
Vera L. Lanchote
Keyword(s):  
Single Dose ◽  
Wistar Rats ◽  
Vehicle Control ◽  
Racemic Mixture ◽  
Blood Samples ◽  
Chiralcel Od ◽  
Male Wistar Rats ◽  
Enantioselective Pharmacokinetics ◽  
Enantioselective Metabolism ◽  
Cyp Inhibitors

Citalopram (CITA) is available as a racemic mixture or as (+)-(S)-CITA. In humans, CITA is metabolized to demethylcitalopram (DCITA) by CYP2C19, CYP2D6, and CYP3A and to didemethylcitalopram by CYP2D6. There are no data regarding the enzymes involved in CITA and DCITA metabolism in rats. The present study investigated the influence of CYP inhibitors on the enantioselective metabolism of CITA in rats. Male Wistar rats (n = 6) received a single dose of 20 mg·kg–1 CITA after pretreatment with 80 mg·kg–1 quinidine, 10 mg·kg–1 fluvoxamine, 50 mg·kg–1 ketoconazole, or vehicle (control). Blood samples were collected up to 20 h after CITA administration. The CITA and DCITA enantiomers were analyzed by LC-MS/MS using a Chiralcel OD-R column. The kinetic disposition of CITA was enantioselective in rats (AUCS/R ratio = 0.4). Coadministration with quinidine resulted in non-enantioselective inhibition of the metabolism of CITA. Coadministration with fluvoxamine or ketoconazole, however, inhibited only the metabolism of (+)-(S)-CITA, but not of (–)-(R)-CITA when the racemic drug was administered to rats.

Differences in the Composition of Inflammatory Cell Infiltrate in Lens-Induced Uveitis under Therapy with Allopurinol or Steroids

2001 ◽  
Vol 11 (3) ◽  
pp. 264-268 ◽  
Author(s):  
W. Sekundo ◽  
A.J. Augustin
Keyword(s):  
Single Dose ◽  
Wistar Rats ◽  
Inflammatory Cell ◽  
Control Group ◽  
Inflammatory Cell Infiltrate ◽  
Polymorphonuclear Leucocytes ◽  
Cell Infiltrate ◽  
Anterior Capsule ◽  
Male Wistar Rats ◽  
Qualitative Changes

Purpose The aim of this study was to compare the qualitative changes in the composition of inflammatory cell infiltrate in lens-induced uveitis (LIU) under treatment with allopurinol (Allo), methylprednisolone (Pred) or the two drugs combined (Allo/Pred). Methods Twenty male Wistar rats were sensitized with lens proteins for eight weeks. Intravenous (IV) therapy was started after anterior capsule disruption in one eye of each animal. Five rats were randomly assigned to each of the four groups: controls, Allo (50 mg/kg bw), Pred (7.5 mg/kg bw) and Allo/Pred (50 mg/7.5 mg per kg bw). Eyes were enucleated 24 hours later and fixed in paraformaldehyde/glutaraldehyde. Sections at three levels were stained with Giemsa and examined using a 0 to 4+ score for each type of inflammatory cell. Granulocytes were seen as neutrophils and eosinophils. Neutrophils were divided into polymorphs and “others”, and graded with lymphocytes. Results In all therapy groups there was a significant reduction of polymorphs (p<0.05) in comparison to the control group. There was also a significant reduction in lymphocytes (p<0.05) in the Pred and Allo/Pred groups as compared to the control group and the Allo group. Conclusions Single-dose IV allopurinol significantly reduced the overall number of polymorphonuclear leucocytes in LIU. Unlike methylprednisolone, allopurinol did not have any significant impact on lymphocytes.

Role of thioredoxin nitration in bleomycin-induced pulmonary fibrosis in rats

2016 ◽  
Vol 94 (1) ◽  
pp. 59-64 ◽  
Author(s):  
Lei Wang ◽  
Yimin Song ◽  
Xiankui Li ◽  
Haizhou Guo ◽  
Guojun Zhang
Keyword(s):  
Single Dose ◽  
Pulmonary Fibrosis ◽  
Wistar Rats ◽  
Intratracheal Instillation ◽  
Treated Group ◽  
Control Group ◽  
Tyrosine Nitration ◽  
Male Wistar Rats ◽  
Phosphate Buffered Saline

Oxidant stimulation has been suggested to play an important role in the pathogenesis of idiopathic pulmonary fibrosis (IPF). Our study aimed to investigate the role and mechanisms of thioredoxin (Trx) nitration during the development of IPF. A rat model of IPF was established by intratracheal instillation of bleomycin (BLM). Male Wistar rats were randomly distributed among the control group and BLM-treated group, in which rats were intratracheally instilled with a single dose of BLM (5.0 mg/kg body mass in 1.0 mL phosphate-buffered saline). At 7 or 28 days after instillation the rats were euthanized. Histopathological and biochemical examinations were performed. The activity and protein level of thioredoxin were assessed. The thioredoxin nitration level was determined using immunoprecipitation and immunoblotting techniques. Our results demonstrated that protein tyrosine nitration increased in the BLM-treated group compared with the control group. Trx activity decreased in the BLM group compared with control group, whereas Trx expression and nitration level increased dramatically in the BLM group compared with the control group. Our results indicated that Trx nitration might be involved in the pathogenesis of IPF.

Pulsatile secretion of growth hormone and insulin in relation to feeding in rats

1987 ◽  
Vol 253 (5) ◽  
pp. R772-R778
Author(s):  
P. Even ◽  
J. Danguir ◽  
S. Nicolaidis ◽  
C. Rougeot ◽  
F. Dray
Keyword(s):  
Growth Hormone ◽  
Insulin Secretion ◽  
Food Intake ◽  
Wistar Rats ◽  
Plasma Concentrations ◽  
Endocrine Activity ◽  
Blood Samples ◽  
Gh Secretion ◽  
Male Wistar Rats ◽  
Intracardiac Catheters

In unrestrained male Wistar rats chronically implanted with intracardiac catheters, blood samples were taken every 20 min throughout the 24 h of the diurnal cycle. Plasma concentrations of growth hormone (GH), insulin, and glucose were measured. The pattern of food intake was continuously monitored. The existence of 3-h pulsatile cycles of GH secretion was confirmed. In addition, short bursts of insulin secretion were observed in the middle of every second GH peak-to-peak interval. Food intake appeared to be enhanced during short periods that corresponded with GH release into the blood and was reduced during the GH peak-to-peak periods in which the bursts of insulin secretion were observed. From these observations this study draws a schematic relationship between the rhythmicity of the secretion of GH and insulin and the probability of occurrence of feeding. We speculate that the rhythmic endocrine activity may be causally related to feeding.

scholarly journals Roselle (Hibiscus sabdariffa L.) calyx water extract ameliorates isoniazid and rifampicin induced liver and renal injuries in rats

2021 ◽  
Vol 10 (3) ◽  
pp. 296-303
Author(s):  
Yulia Yusrini Djabir ◽  
Jumasni Adnan ◽  
Nurul Amalia ◽  
Nurfadillah Ramli ◽  
Sartini Sartini ◽  
...  
Keyword(s):  
Wistar Rats ◽  
Water Extract ◽  
Natural Antioxidants ◽  
Control Group ◽  
Hibiscus Sabdariffa ◽  
Protective Effects ◽  
Blood Samples ◽  
Therapeutic Benefits ◽  
Male Wistar Rats ◽  
Pre Treatment

Introduction: Roselle (Hibiscus sabdariffa L.) calyces possess natural antioxidants that may provide therapeutic benefits. This study aimed to investigate the protective effects of Roselle calyx water extract against isoniazid (INH) and rifampicin (RIF) induced liver and renal toxicities.Methods: Male Wistar rats (150-250 g) were designated into five groups: control group, INH-RIF group that was treated with INH-RIF at the toxic doses (50-100 mg/kg for 4 weeks, followed by 100-200 mg/kg for 2 weeks), and Roselle groups that were treated daily with Roselle extract at the doses 62.5, 125, and 250 mg/kg, respectively prior to INH-RIF administration. Blood samples were withdrawn weekly for 6 weeks before removing rats’ livers and kidneys for tissue malondialdehyde (MDA) and histopathological analysis.Results: The results showed all rats in the INH-RIF group experienced marked elevations of serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), urea, creatinine, and tissue MDA levels compared to the controls (P<0.05). In contrast, these biomarkers were maintained at near-normal levels in Roselle extract groups. Significant inflammation and cellular degeneration were found in the liver and renal tissues of the INH-RIF group, which were noticeably reduced with Roselle extract pre-treatment at the dose of 250 mg/kg.Conclusion: It is concluded that Roselle calyx extract can provide protection against liver and renal toxicities induced by INH-RIF administration in rats.

Pengaruh Profilaksis Ekstrak Ubi Jalar Ungu (Ipomoea batatas L.) terhadap Kadar Malondialdehida Hepar Tikus Putih (Rattus norvegicus) Jantan Galur Wistar yang Diinduksi Karagenan

2018 ◽  
Vol 15 (2) ◽  
pp. 146
Author(s):  
BRILIAN DINANTI ◽  
FITRI HANDAJANI
Keyword(s):  
Sweet Potato ◽  
Ipomoea Batatas ◽  
Wistar Rats ◽  
Group Method ◽  
Control Group ◽  
Intraplantar Injection ◽  
Significant Difference ◽  
Male Wistar Rats ◽  
Potato Extract ◽  
Purple Sweet Potato

<p>Liver is an organ with complex metabolism. When the liver is inflamed, cellular immunity will defend against inflammatory agents by stimulating immune cells to produce reactive oxygen species (ROS). Excessive ROS accumulation cause oxydative stress with increased  liver malondialdehyde (MDA) level. Some researches showed that purple sweet potato contain flavonoids (anthocyanins) that functioned as antioxydants. This study aimed to show the prophylactic effect of purple sweet potato extract to the liver MDA level of male Wistar rats induced by carrageenan.</p><p>This study used post-only control group method using 18 male Wistar rats divided into 3 groups: group of rats without treatment, group of rats induced by 0,1 ml of 1% carrageenan by intraplantar injection on day-8, and group of rats given with 872 mg/kgBW of purple sweet potato extract for 7 days and induced by 0,1 ml of 1% carrageenan. In the end of the study, the liver MDA levels were measured by Thio-Barbituric Acid method on each groups.</p><p>The results of One-Way ANOVA test showed there was no significant difference (p = 0,290) between group of rats without treatment (<em>x̅</em>= 207,50) and group of rats induced by carrageenan (<em>x̅</em>=233,17). Then, there is no significant difference (p = 0.978) between group of rats induced by carrageenan and group of rats given with prophylactic purple sweet potato extract and induced by carrageenan (<em>x̅</em>= 232,50).</p><p>The conclusion of this study is giving intraplantar injection of carrageenan can increase liver MDA level insignificantly and giving prophylactic purple sweet potato extract has an effect to decrease the liver MDA level of rats induced by carragenan insignificantly because it contains anthocyanins as antioxidants.</p><p> </p><strong>Keywords: </strong>Liver, <em>Ipomoea batatas</em> L., Malondialdehyde, Anthocyanins

scholarly journals Impact of Vanadium Complexes Treatment on the Oxidative Stress Factors in Wistar Rats Plasma

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
R. Francik ◽  
M. Krośniak ◽  
M. Barlik ◽  
A. Kudła ◽  
R. Gryboś ◽  
...  
Keyword(s):  
Wistar Rats ◽  
Reduced Glutathione ◽  
The Body ◽  
Stress Factors ◽  
Control Group ◽  
Vanadium Complexes ◽  
Healthy Male ◽  
Reducing Ability ◽  
Male Wistar Rats ◽  
Antioxidant Parameters

The aim of this study was to investigate the clinical efficacy of vanadium complexes on triglycerides (TG), total cholesterol (Chol), uric acid (UA), urea (U), and antioxidant parameters: nonenzymatic (FRAP—ferric reducing ability of plasma, and reduced glutathione—GSH) and enzymatic (glutathione peroxidase—GPx, catalase—CAT, and GPx/CAT ratio) activity in the plasma of healthy male Wistar rats. Three vanadium complexes: [VO(bpy)2]SO4⋅2H2O, [VO(4,4′Me2bpy)2]SO4⋅2H2O, and Na[VO(O2)2(bpy)]⋅8H2O are administered by gavage during 5 weeks in two different diets such as control (C) and high fatty (F) diets. Changes of biochemical and antioxidants parameters are measured in plasma. All three vanadium complexes statistically decrease the body mass growth in comparison to the control and fatty diet. In plasma GSH was statistically increased in all vanadium complexes-treated rats from control and fatty group in comparison to only control group. Calculated GPX/CAT ratio was the highest in the control group in comparison to others.

scholarly journals Anticarcinogenic effect of probiotic fermented milk and chlorophyllin on aflatoxin-B1-induced liver carcinogenesis in rats

2011 ◽  
Vol 107 (7) ◽  
pp. 1006-1016 ◽  
Author(s):  
M. Kumar ◽  
V. Verma ◽  
R. Nagpal ◽  
A. Kumar ◽  
P. V. Behare ◽  
...  
Keyword(s):  
Wistar Rats ◽  
Lactobacillus Rhamnosus ◽  
Thiobarbituric Acid ◽  
Fermented Milk ◽  
Hepatoprotective Effect ◽  
Control Group ◽  
Time Interval ◽  
Group I ◽  
Male Wistar Rats ◽  
Aflatoxin B

The present investigation was carried out to evaluate the hepatoprotective effect of probiotic fermented milk (FM) containing Lactobacillus rhamnosus GG and Lactobacillus casei strain Shirota, alone as well as in combination with chlorophyllin (CHL) as an antioxidant agent in male Wistar rats administered aflatoxin-B1 (AFB1). AFB1 was injected intraperitoneally at the rate of 450 μg/kg body weight per animal twice a week for 6 weeks, maintaining an equal time interval between the two consecutive AFB1 administrations. A total of 125 male Wistar rats were randomly allocated to five groups, each group having twenty-five animals. Group I was offered FM containing L. rhamnosus GG and L. casei strain Shirota. Group II was administered AFB1 and served as the control group; group III was administered FM-AFB1, in which besides administering AFB1, FM was also offered. Group IV was offered CHL and AFB1, and group V was offered both FM and CHL along with AFB1. The rats were euthanised at the 15th and 25th week of the experiment and examined for the biochemical and hepatopathological profile. A significant reduction in thiobarbituric acid-reactive substances (TBARS) was observed in the FM–CHL–AFB1 group compared with the AFB1 control group. FM alone or in combination with CHL was found to show a significant (P < 0·05) hepatoprotective effect by lowering the levels of TBARS and by enhancing the activities of antioxidant enzymes such as glutathione peroxidase, superoxide dismutase, catalase and glutathione-S-transferase, indicating that probiotic FM alone or in combination with CHL possesses a potent protective effect against AFB1-induced hepatic damage.

Potential Antiseptic of Rhodomyrtus tomentosa leaves extract on Healing wound in Male Wistar rats

2021 ◽  
pp. 3143-3149
Author(s):  
Endang Sri Purwanti Ningsih ◽  
Noorlaila Noorlaila ◽  
Ikhwan Rizki Muhammad ◽  
Windy Yuliana Budianto
Keyword(s):  
Wound Healing ◽  
Wistar Rats ◽  
Leaf Extract ◽  
Wound Care ◽  
Positive Control ◽  
Negative Control ◽  
Control Group ◽  
Significant Difference ◽  
Male Wistar Rats ◽  
Rhodomyrtus Tomentosa

Background: The process of wound healing is influenced by various factors such as age, hormones, and wound care. Wound care is done to accelerate wound healing which can be done by various methods, one of them is traditional care. Traditional wound care can use medicinal plants. Rhodomyrtus tomentosa is a medicinal plant that has an antioxidant, anti-inflammatory, antitumor and antibacterial content. Thus this study aims to evaluate the effectiveness of the antiseptic solution of the Rodhomyrtus tomentosa leaf extract on wound healing in male Wistar rats. Method: this research is pure experimental research with post test only control group design. Thirty male white rats were divided into five groups, namely negative control, positive control, Rhodomyrtus tomentosa leaf extract 15%, 30%, and 60%. Rhodomyrtus tomentosa leaf extraction was carried out by maceration method with 70% ethano solvent. The extraction results are divided into 3 concentrations (15%, 30% and 60%). The wound healing process was evaluated by measuring the length of the wound manually from 0 to 10 days in each group. Meanwhile, the number of fibroblast cells was calculated through hematoxylin eosin (HE) staining and observed using an Olympus CX41 microscope with a 10x magnification and objective lens magnification in 3 fields. Result: There was a significant difference in the reduction in wound length (p =< 0,000) between the five experimental groups (Rhodomyrtus tomentosa leaf extract solution 15%, 30% and 60%, negative control and positive control. Solution of rhodomyrtus tomentosa leaf extract accelerated the increase in the number of fibroblasts compared to the negative control group (p = 0.003), but did not make a difference (p = 0.403) with the positive control group. Rhodomyrtus tomentosa leaf extraction solution had the same microscopic effect on the number of fibroblasts with a positive control group given 0.9% NaCl solution. Conclusion: There was a significant difference in the number of fibroblasts between all groups, but no difference in wound healing length.

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