Oral Administration (oral + administration)

Distribution by Scientific Domains
Distribution within Medical Sciences

Kinds of Oral Administration

  • acute oral administration
  • daily oral administration
  • long-term oral administration
  • single oral administration

  • Selected Abstracts

    Identification of Major Alkaloids in Rat Urine by HPLC/DAD/ESI-MS/MS Method Following Oral Administration of Cortex Phellodendri Decoction

    Chun-Hui Ma
    Abstract A rapid, sensitive, and specific high-performance liquid chromatography (HPLC), diode-array detection, and mass-spectrometry techniques were developed for an identification of the constituents of Cortex Phellodendri and their metabolites in rat urine. The dose of 10,ml/kg of Cortex Phellodendri decoction was used for rats' oral administration. 0,24-h Urine was purified using a C18 solid-phase extraction cartridge, and then analyzed by an on-line MS detector. A total of 13,characteristic HPLC peaks were detected in the urine samples. Nine of them, including five alkaloids and four of their metabolites, were tentatively elucidated as magnoflorine (1), the glucuronide conjugate of demethyleneberberine (2), menisperine (3), jatrorrhizine 3- O -glucuronide (4), berberubine 9- O -glucuronide (5), jatrorrhizine (6), the monomethyl and monohydroxy catabolite of berberubine (7), palmatine (8), and berberine (9). Identification and structural elucidation of the metabolites were performed by comparing their MSn spectra data with those reported. [source]

    Body Distribution of Poly- DL -lactide-poly(ethylene glycol) Microspheres with Entrapped Leptospira interrogans Antigens Following Intravenous and Oral Administration to Guinea-pigs

    Poly- DL -lactide-poly(ethylene glycol) (PELA) microspheres with entrapped antigens were administered intravenously and orally into guinea-pigs to quantitatively determine the in-vivo distribution and release profiles. PELA microspheres containing 125I-labelled outer-membrane protein Leptospira interrogans antigens (125I-OMP) were prepared by double-emulsion solvent extraction procedure, and characterized with respect to size, morphology and in-vitro release profiles. The fractured sections of liver and spleen were inspected by scanning electron microscopy, which indicated that microspheres had successfully been entrapped within the above tissues after intravenous injection and oral administration. At predetermined intervals, the blood and such tissues as the liver, spleen, kidney, thyroid, small intestine and mesentery were collected, and the radioactivity was measured by gamma scintillation counting. Following intravenous administration, 56.7% of administered microspheres were accumulated in immunization-related tissues, and 40.1% of microspheres were located in the liver and spleen. However, there was limited uptake efficiency (8.33%) following oral administration, and 49.5% of the absorbed microspheres were located in the intestinal mucosa. Compared with in-vitro release, the in-vivo release profiles of 125I-OMP from PELA microspheres, determined from the decreasing radioactivity in the above tissues, were much faster and the burst effect was higher. Antigen-loaded PELA microspheres were efficiently entrapped within immunization-related tissues after intravenous administration, but orally administered PELA microspheres showed limited uptake efficiency. Further investigation is needed to improve intestinal absorption. [source]

    Effects of Oral Administration of Specific Antibodies to Rainbow Trout Oncorhynchus mykiss

    Michael Engelbrecht Nielsen
    A new product called oralized fish serum concentrate (OFSC) was evaluated for a possible effect against various bacterial pathogens in rainbow trout. The OFSC produced from immune trout sera was found to contain fully functional antibodies and complement component C3. The antibodies detected in the serum concentrate were specific to Vibrio anguillarum (O1 and O2) and Aeromonas salmonicida, which had been used for vaccination of the fish prior to serum collection. The functionality of the specific antibodies in OFSC was not reduced after 6 wk storage at -20 C, 5 C, and 20 C. The serum was mixed with commercial trout feed and used for feeding rainbow trout fry (first feed period). After oral delivery of OFSC to rainbow trout for 1 mo, samples of gut content and gut tissue contained functional antibodies. In gutted fish no functional antibodies were found. This suggests that antibodies from OFSC are unable to be transferred across the gut wall in a functional state. Oral administration of OFSC did not increase survival of rainbow trout in an immersion challenge with Vibrio anguillarum. [source]

    The Effects of Oral Administration of D-Modafinil on Male Rat Ejaculatory Behavior

    Lesley Marson PhD
    ABSTRACT Introduction., Premature ejaculation (PE) is one of the most common forms of male sexual dysfunction. Examination of various classes of drugs on ejaculation latency would provide further opportunities for drug development in this field. Aim., This study was conducted to examine the effects of the d-isomer of modafinil (d-modafinil) on ejaculatory behavior in a rat model. Methods., Male sexual behavior in the rat was examined after acute oral administration of d-modafinil (10 mg/kg, 30 mg/kg, and 100 mg/kg) in copulation studies with receptive females. Main Outcome Measures., The latency to ejaculation, post-ejaculatory interval, and the frequency of mounting behavior were measured. Results d-modafinil (30 mg/kg and 100 mg/kg) produced a significant delay in ejaculation. The delay in ejaculation was accompanied by an increase in the number of intromissions without any change in the mount or intromission latency. The possible mechanisms of action of d-modafinil to produce this delay in ejaculation are discussed. Conclusions., These results demonstrate that acute oral administration of d-modafinil can lengthen the latency to ejaculation in rats without suppressing sexual behavior. The greatest delay in ejaculation was observed in animals with shorter baseline ejaculatory latencies. Investigation into new classes of drugs that modulate ejaculation may provide new therapeutic options for treating PE. Marson L, Yu G, and Farber NM. The effects of oral administration of d-modafinil on male rat ejaculatory behavior. J Sex Med 2010;7:70,78. [source]

    Sinus Tissue Pharmacokinetics After Oral Administration of Amoxicillin/Clavulanic Acid

    THE LARYNGOSCOPE, Issue 6 2000
    Paulo Borges Dinis MD
    Abstract Objectives The in vitro synergy of the amoxicillin/clavulanic acid combination has not always translated in vivo into clinical superiority compared with amoxicillin alone. Specifically, conflicting reports have disputed the superiority of the combination in the treatment of both acute otitis media and acute sinusitis. One possible reason for this may have to do with inadequate target tissue pharmacokinetics. To explore this possibility in the sinuses, we undertook the present investigation. Study Design A randomized, open, single-dose, sinus tissue pharmacokinetic study with oral amoxicillin/clavulanic acid. Methods Twenty-three adult patients with chronic rhinosinusitis who had been selected for surgery were randomly allocated to receive a tablet of 875/125 mg amo-icillin/clavulanate 2 to 4 hours before surgery began. During the operation tissue samples were collected at specific sinonasal sites for determination of both amo-icillin and clavulanic acid concentration levels. Results Amoxicillin displayed adequate tissue levels throughout the sinuses, high enough to cover common susceptible pathogens. However, the presence of clavulanate was detected in only half of the sinonasal tissue samples. Conclusions The kinetics of oral clavulanic acid apparently fails to provide a widespread anti,,-lactamase activity capable of enhancing the activity of amoxicillin in all parts of the sinuses. Despite this, amoxicillin/clavulanic acid maintains a central role in the treatment of acute rhinosinusitis, because amoxicillin is still the most effective oral ,-lactam against Streptococcus pneumoniae, a particularly virulent and increasingly resistant upper respiratory tract pathogen. Also, as our data show, a concomitant anti,,-lactamase activity can be expected to occur, although in an unpredictable fashion. [source]

    Concentration Of Egg White Lysozyme In The Serum Of Healthy Subjects After Oral Administration

    Seiichi Hashida
    SUMMARY 1. While the egg white lysozyme preparation ER0068 (Neuzym®; Eisai, Tokyo, Japan) is widely used clinically, no studies have been performed on its pharmacokinetic properties at clinically relevant doses. In the present study, we used a highly sensitive two-site enzyme immunoassay in order to determine the pharmacokinetic properties of egg white lysozyme after oral administration of two doses within the clinical range, paying particular attention to the effects of food intake. 2. A total of 22 healthy male subjects aged 20,45 years participated in the study. All subjects had been screened for egg white allergy and non-specific lysozyme inhibitors in their serum. Subjects who received 90 mg ER0068 after an overnight fast reached a maximum serum concentration of 1700 pg/mL within 1 h, compared with non-detectable levels in untreated controls. In a second experiment, subjects received 30 and 90 mg ER0068 after an overnight fast and 90 mg in the non-fasted state and exhibited maximum serum levels of 37, 360 and 49 pg/mL, respectively. Egg white lysozyme concentrations in serum returned to undetectable levels after a maximum of 48 h. 3. We conclude that clinically relevant concentrations of egg white lysozyme are absorbed in significant amounts, despite its high molecular weight. However, food intake considerably reduces the amount of enzyme absorbed. [source]

    Effect of Cogent db, a herbal drug, on serum and tissue lipid metabolism in experimental hyperglycaemic rats

    G. Saravanan
    Aims:, We have previously reported the antidiabetic effect of Cogent db. The present study with alloxan-induced hyperglycaemic rats is focused on the mechanism of action, specifically on the activity of hepatic lipogenic enzymes, serum and tissue lipids. Methods:, Male Wistar rats body weight of 180,200 g (six normal and 18 diabetic rats) were used in this study. The rats were divided into four groups after the induction of alloxan diabetes: normal rats; diabetic control; diabetic rats given Cogent db (0.45 g/kg body weight); diabetic rats given glibenclamide (600 µg/kg body weight). After 40 days treatment, fasting blood glucose, plasma insulin, activities of hepatic lipogenic enzymes, serum and tissue lipids were determined in normal and experimental animals. Results:, Oral administration of Cogent db for 40 days resulted in significant reduction in blood glucose, serum and tissue (liver and kidney) lipids, whereas the level of plasma insulin and the activity of hepatic lipogenic enzymes were significantly increased in alloxan diabetic rats. Similar studies using glibenclamide have been conducted to compare the mode of action of these two drugs. Conclusions:, Thus our study shows that Cogent db exhibits a strong antihyperlipidaemic effect, which could exert a beneficial action against macrovascular complications (cardiovascular disease) associated with diabetes mellitus. [source]

    Theophylline does not potentiate the effects of a low dose of dexamethasone in horses with recurrent airway obstruction

    Summary Reasons for performing study: Theophylline has been shown to have corticosteroid-sparing effects for the treatment of human asthma. A similar effect, if present in horses, would allow diminishing the dose of corticosteroids administered to equine patients with inflammatory airway diseases. Objectives: To evaluate whether theophylline potentiates the effects of a low dose of dexamethasone when treating horses with recurrent airway obstruction (RAO). Hypothesis: Theophylline has steroid-sparing effects in horses with RAO. Methods: Ten mature mixed breed horses in clinical exacerbation of RAO were studied. Using an incomplete crossover design and 3 experimental periods of 7 days duration, horses were distributed randomly in 5 treatment groups; and administered dexamethasone s.i.d., at either 0.05 mg/kg bwt i.v. or per os, or 0.02 mg/kg bwt alone or combined with theophylline at 5 mg/kg bwt per os b.i.d. A fifth group was treated with theophylline alone at the above dosage. Lung function was evaluated prior to drug administration and then 3 and 7 days later. Results: Oral administration of dexamethasone alone or combined with theophylline failed to improve lung function significantly in RAO affected horses. Theophylline alone also failed to improve lung function in all treated horses. Conversely, dexamethasone administration at 0.05 mg/kg bwt i.v. resulted in a significant improvement in lung function starting on Day 3. Conclusions and potential relevance: Oral theophylline for 7 days did not improve the effects of a low dose of dexamethasone for the treatment of horses with RAO. [source]

    Withanoside IV and its active metabolite, sominone, attenuate A,(25,35)-induced neurodegeneration

    Tomoharu Kuboyama
    Abstract At the present, medication of dementia is limited to symptomatic treatments such as the use of cholinesterase inhibitors. To cure dementia completely, that is regaining neuronal function, reconstruction of neuronal networks is necessary. Therefore, we have been exploring antidementia drugs based on reconstructing neuronal networks in the damaged brain and found that withanoside IV (a constituent of Ashwagandha; the root of Withania somnifera) induced neurite outgrowth in cultured rat cortical neurons. Oral administration of withanoside IV (10 µmol/kg/day) significantly improved memory deficits in A,(25,35)-injected (25 nmol, i.c.v.) mice and prevented loss of axons, dendrites, and synapses. Sominone, an aglycone of withanoside IV, was identified as the main metabolite after oral administration of withanoside IV. Sominone (1 µm) induced axonal and dendritic regeneration and synaptic reconstruction significantly in cultured rat cortical neurons damaged by 10 µm A,(25,35). These data suggest that orally administrated withanoside IV may ameliorate neuronal dysfunction in Alzheimer's disease and that the active principle after metabolism is sominone. [source]

    Quercitrin, a bioflavonoid improves glucose homeostasis in streptozotocin-induced diabetic tissues by altering glycolytic and gluconeogenic enzymes

    Ranganathan Babujanarthanam
    Abstract The present study is an investigation into the role of quercitrin on carbohydrate metabolism in normal and streptozotocin (STZ)-induced diabetic rats. Administration of STZ leads to a significant increase (P < 0.05) in fasting plasma glucose and a decrease in insulin levels. The content of glycogen is significantly decreased (P < 0.05) in liver and muscle, but increased in the kidney. The activity of hexokinase decreased whereas the activities of glucose 6-phosphatase and fructose 1,6-bisphosphatase significantly increased (P < 0.05) in the tissues. Oral administration of quercitrin (30 mg/kg) to diabetic rats for a period of 30 days resulted in significant (P < 0.05) alterations in the parameters studied but not in normal rats. A decrease of plasma glucose and increase in insulin levels were observed along with the restoration of glycogen content and the activities of carbohydrate metabolic enzymes in quercitrin-treated diabetic rats. The histopathological study of the pancreas revealed the protective role of quercitrin. There was an expansion of the islets and decreased fatty infiltrate of the islets in quercitrin treated diabetic rats. In normal rats treated with quercitrin, we could not observe any significant change in all the parameters studied. Combined, these results show that quercitrin plays a positive role in carbohydrate metabolism and antioxidant status in diabetic rats. [source]

    99mTc-MIBI imaging for prediction of therapeutic effects of second-generation MDR1 inhibitors in malignant brain tumors

    Toshio Sasajima
    Abstract The aim of this study was to explore whether 99mTc-methoxyisobutylisonitrile (99mTc-MIBI) is suitable to elucidate multidrug resistance and prediction of potentiation of antitumor agents by second-generation MDR1 inhibitors (PSC833, MS-209) in malignant brain tumors in rat. Malignant tumor cells (RG2 and C6 gliomas, Walker 256 carcinoma) were incubated with low dose vincristine (VCR) to induce multidrug resistance. MTT assay demonstrated a significant increase of surviving fractions in VCR-resistant sublines compared to those of drug-naive cells. Reverse transcriptase polymerase chain reaction revealed higher expression of MDR1 mRNA in VCR-resistant cells than drug-naive cells in each line. Volume distribution (Vd) of 99mTc-MIBI was negatively correlated with MDR1 mRNA expression among drug-naive and VCR-resistant cells. MDR1 inhibitors decreased surviving fractions and increased Vd of 99mTc-MIBI significantly in VCR-resistant sublines, whereas MDR1 mRNA expression was unchanged. These findings indicate that 99mTc-MIBI efflux was functionally suppressed by MDR1 inhibitors. Autoradiographic images of 99mTc-MIBI revealed higher uptake in drug-naive cells at basal ganglia compared with VCR-resistant cells at the opposite basal ganglia of rats. Oral administration of the second-generation MDR1 inhibitors significantly increased 99mTc-MIBI accumulation of both tumors. Therapeutic effects of VCR with or without the MDR1 inhibitors were also evaluated autoradiographically using 14C-methyl- L -methionine (14C-Met) and MIB-5 index. 14C-Met uptake and MIB-5 index of both tumors treated with VCR following the MDR1 inhibitor treatment significantly decreased compared with tumors treated with VCR alone. Analysis of 99mTc-MIBI accumulation is considered informative for detecting MDR1-mediated drug resistance and for monitoring the therapeutic effects of MDR1 inhibitors in malignant brain tumors. © 2007 Wiley-Liss, Inc. [source]

    Selective cyclooxygenase-2 inhibitor downregulates the paracrine epithelial,mesenchymal interactions of growth in scirrhous gastric carcinoma

    Masakazu Yashiro
    Abstract The importance of cancer-mesenchymal interactions in the aggressive behavior of scirrhous gastric cancer is supported by experimental and clinical evidences. We have previously reported that gastric fibroblasts secretion of keratinocyte growth factor (KGF) underline the remarkable proliferation of scirrhous gastric cancer cells. Cyclooxygenase-2 (COX-2) is not only expressed in cancer cells, but also in interstitial fibroblasts in gastric carcinoma. To clarify the mechanisms responsible for the antiproliferation effect of COX-2 inhibitors, effect of COX-2 inhibitor on the paracrine epithelial,mesenchymal interactions of growth was examined. Scirrhous gastric cancer cell line, OCUM-2M, gastric fibroblasts, NF-21, and COX-2 inhibitor, JTE-522, were used. Growth-interaction was examined by calculating the number of cancer cells or by measuring [3H] thymidine incorporation of cancer cells. Effect of JTE-522 on KGF expression from NF-21 cells and OCUM-2M cells was analyzed by ELISA and RT-PCR. The conditioned medium from gastric fibroblasts significantly stimulated the growth of scirrhous gastric cancer cells. JTE-522 at the concentrations of 10,5 and 10,6 M significantly decreased the growth-stimulating activity of gastric fibroblasts. JTE-522 reduced the expression of KGF mRNA and the production of KGF from gastric fibroblasts. Oral administration of JTE-522 significantly decreased the size of xenografted tumor coinoculated with OCUM-2M cells and NF-21 cells in nude mice. JTE-522 decreased COX-2 expression and Ki67 labeling index within the coinoculated tumor. These findings suggested that a selective COX-2 inhibitor, JTE-522, downregulates KGF production from gastric fibroblasts, resulting in the inhibition of paracrine epithelial,mesenchymal interactions of proliferation between scirrhous gastric cancer cells and gastric fibroblasts. © 2006 Wiley-Liss, Inc. [source]

    Cyclooxygenase-2 inhibitor celecoxib augments chemotherapeutic drug-induced apoptosis by enhancing activation of caspase-3 and -9 in prostate cancer cells

    Devendra S. Dandekar
    Abstract Many tumors constitutively express high levels of the inducible form of proinflammatory enzyme, cyclooxygenase-2 (COX-2). Increased COX-2 expression is associated with tumor cell resistance to many cytotoxic chemotherapy drugs. Furthermore, increased resistance to cytotoxic antitumor drugs is also known to be dependent on associated stromal cells in many tumors. We investigated whether prostate tumor-associated stromal cells, marrow-derived osteoblasts, affect cytotoxicity of 2 antitumor drugs, COL-3 and docetaxel (TXTR), and whether it is dependent on COX-2 activity. We further examined whether inhibiting the activity of COX-2 negate the stroma-induced decrease in drug sensitivity in tumor cells. COX-2-specific inhibitor celecoxib (CXB) was used to inhibit COX-2 activity and associated alteration in cell death signaling was investigated. Coculturing PC-3ML cells with osteoblasts decreased the cytotoxicity of the tested antitumor drugs and was associated with increased COX-2 activity in PC-3ML cells. A significant decrease in drug-induced PGE2 increase and an increase in cytotoxicity were observed when cells were treated with COL-3 or TXTR combined with CXB. Cytotoxicity of single or combination treatment increased apoptosis, which was associated with caspase-3 and -9 activation, PARP cleavage, increased BAD protein, but decreased protein levels of XIAP and BCL- xL. Oral administration of CXB (40 mg/kg) to mice with PC-3ML tumors for 42 days increased tumor latency, decreased tumor growth and enhanced tumor control with COL-3 or TXTR. Overall, a synergistic enhancement of antitumor activity in combination treatment was observed in vitro and an additive effect in vivo. These observations suggest a potential clinical use of combined dosing of COX-2 inhibitors and cytotoxic drugs at lower, nontoxic dose than currently used to treat advanced prostate cancer. © 2005 Wiley-Liss, Inc. [source]

    Oral administration of diphenyl diselenide potentiates hepatotoxicity induced by carbon tetrachloride in rats

    Cristina W. Nogueira
    Abstract Carbon tetrachloride (CCl4) is a model for studying free radical-induced liver injury and screening hepato-protective drugs. Numerous studies have reported the involvement of oxidative stress in CCl4 -induced liver damage and the hepato-protective effects mediated by different antioxidants. The present study examined the effects of diphenyl diselenide, (PhSe)2, on hepatotoxicity induced by CCl4 in rats. To this end, male Wistar rats received (PhSe)2 by oral route at the dosage of 31.2 mg/kg for one or two days. After the second day of treatment, rats received CCl4 orally in a single dose. The liver and kidney were utilized for determination of histopathology, biochemical [aspartate (ALT) and alanine (AST) aminotransferases, alkaline phosphatase (ALP), total bilirrubin (TB) and gamaglutamyl transferase (GGT)] and toxicological parameters [thiobarbituric reactive species (TBARS) levels, catalase activity, ascorbic acid, nonprotein thiols (NPSH) and aminolevulinate dehydratase (, -ALA-D) activity]. Repeated administration of (PhSe)2 caused a marked potentiation of hepatotoxicity induced by CCl4 exposure, as manifested by an increase in biochemical parameters (AST, ALT, ALP, GGT and BT) and severe alteration in histopathology. This study also demonstrated a potentiation of TBARS levels and a consequent depletion of important antioxidant defenses including catalase and ascorbic acid. Pre-treatment with a single dose of (PhSe)2 prevented the effect of strychnine, a substrate for CYPs, abolishing lethality in mice. This result indicates that (PhSe)2 prevented animal death, suggesting an activator action of (PhSe)2 in CYPs. This study clearly indicates that (PhSe)2 potentiated acute hepatic damage induced by CCl4. Copyright © 2008 John Wiley & Sons, Ltd. [source]

    Effect of textile waste water on the spermatogenesis of male albino rats

    R. S. Gupta
    Abstract Textile waste water released from dyeing and printing industries situated in Sanganer, Jaipur (India), brought about inhibition of spermatogenesis in male rats. Water analysis showed the presence of heavy metals at more than permissible limits. Oral administration of waste water to the rats at the dose level of 26.6 ml kg,1 body wt. significantly reduced the weights of testes, epididymides and seminal vesicle. Treated animals showed a notable depression of various stages of spermatogenesis. The production of spermatids was inhibited by 70.8% in waste-water-treated rats. The populations of spermatogonia, preleptotene spermatocytes and secondary spermatocytes were decreased by 67.2, 71.1 and 73.2%, respectively. The total number of Sertoli cells was affected after waste water treatment. Reduced sperm count and motility resulted in treated groups. A significant fall in the content of various biochemical parameters of reproductive tissues was observed after water treatment. Copyright © 2003 John Wiley & Sons, Ltd. [source]

    Protective effect of arjunolic acid against arsenic-induced oxidative stress in mouse brain,

    Mahua Sinha
    Abstract Arsenic, a notoriously poisonous metalloid, is ubiquitous in the environment, and it affects nearly all organ systems of animals including humans. The present study was designed to investigate the preventive role of a triterpenoid saponin, arjunolic acid against arsenic-induced oxidative damage in murine brain. Sodium arsenite was selected as a source of arsenic for this study. The free-radical-scavenging activity and the in vivo antioxidant power of arjunolic acid were determined from its 2,2-diphenyl-1-picryl hydrazyl radical scavenging ability and ferric reducing/antioxidant power assay, respectively. Oral administration of sodium arsenite at a dose of 10 mg/kg body weight for 2 days significantly decreased the activities of antioxidant enzymes, superoxide dismutase, catalase, glutathione- S -transferase, glutathione reductase and glutathione peroxidase, the level of cellular metabolites, reduced glutathione, total thiols and increased the level of oxidized glutathione. In addition, it enhanced the levels of lipid peroxidation end products and protein carbonyl content. Treatment with arjunolic acid at a dose of 20 mg/kg body weight for 4 days prior to arsenic administration almost normalized above indices. Histological findings due to arsenic intoxication and arjunolic acid treatment supported the other biochemical changes in murine brains. Results of 2,2-diphenyl-1-picryl hydrazyl radical scavenging and ferric reducing/antioxidant power assays clearly showed the in vitro radical scavenging as well as the in vivo antioxidant power of arjunolic acid, respectively. The effect of a well-established antioxidant, vitamin C, has been included in the study as a positive control. Combining all, results suggest that arjunolic acid possessed the ability to ameliorate arsenic-induced oxidative insult in murine brain and is probably due to its antioxidant activity. © 2008 Wiley Periodicals, Inc. J Biochem Mol Toxicol 22:15,26, 2008; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/jbt.20209 [source]

    Antilipoperoxidative and antioxidant effects of S-allyl cysteine sulfoxide on isoproterenol-induced myocardial infarction in wistar rats

    T. Sangeetha
    Abstract Our study evaluates the preventive effect of S-allyl cysteine sulfoxide (SACS) on lipid peroxidative products and enzymic and nonenzymic antioxidants in isoproterenol (ISO) induced myocardial infarction in rats. The male Wistar rats were rendered myocardial infarction by ISO (150 mg kg,1, once a day for two days). The concentrations of thiobarbituric acid reactive substances and lipid hydroperoxides were increased in hearts from ISO-treated rats, whereas the content of enzymic and nonenzymic antioxidants were declined in rats administered ISO. Oral pretreatment with SACS (40 mg kg,1 and 80 mg kg,1 daily for a period of 35 days) significantly (p < 0.05) decreased the lipid peroxidative products and significantly (p < 0.05) increased antioxidants in ISO-induced rats. Oral administration of SACS (40 mg kg,1 and 80 mg kg,1) did not show any significant effect in normal rats. Thus, the present study shows that SACS exhibits antilipoperoxidative and antioxidant effects in experimental myocardial infarction. © 2006 Wiley Periodicals, Inc. J Biochem Mol Toxicol 20:167,173, 2006; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/jbt.20132 [source]

    Ameliorative potential of resveratrol on proinflammatory cytokines, hyperglycemia mediated oxidative stress, and pancreatic ,-cell dysfunction in streptozotocin-nicotinamide-induced diabetic rats

    P. Palsamy
    Chronic exposure of pancreatic ,-cells to supraphysiologic glucose causes adverse ,-cell dysfunction. Thus, the present study was aimed to investigate the hypothesis that oral administration of resveratrol attenuates hyperglycemia, proinflammatory cytokines and antioxidant competence and protects ,-cell ultrastructure in streptozotocin-nicotinamide-induced diabetic rats. Oral administration of resveratrol (5,mg/kg body weight) to diabetic rats for 30 days showed a significant decline in the levels of blood glucose, glycosylated hemoglobin (HbA1c), TNF-,, IL-1,, IL-6, NF-,B p65 unit and nitric oxide (NO) with concomitant elevation in plasma insulin. Further, resveratrol treated diabetic rats elicited a notable attenuation in the levels of lipid peroxides, hydroperoxides and protein carbonyls in both plasma and pancreatic tissues. The diminished activities of pancreatic superoxide dismutase (SOD), catalase, glutathione peroxidase (GPx) and glutathione-S-transferase (GST) as well as the decreased levels of plasma ceruloplasmin, vitamin C, vitamin E and reduced glutathione (GSH) in diabetic rats were reverted to near normalcy by resveratrol administration. Based on histological and ultrastructural observations, it is first-time reported that the oral administration of resveratrol may effectively rescue ,-cells from oxidative damage without affecting their function and structural integrity. The results of the present investigation demonstrated that resveratrol exhibits significant antidiabetic potential by attenuating hyperglycemia, enhancing insulin secretion and antioxidant competence in pancreatic ,-cells of diabetic rats. J. Cell. Physiol. 224: 423,432, 2010. © 2010 Wiley-Liss, Inc. [source]

    Effect of dietary administration of Porphyridium cruentum on the respiratory burst activity of sole, Solea senegalensis (Kaup), phagocytes

    P Díaz-Rosales
    Abstract The stimulatory effect of the red microalga Porphyridium cruentum on respiratory burst activity of sole phagocytes was evaluated in vivo. Oral administration of a diet supplemented with lyophilized P. cruentum cells (10 g kg,1) stimulated respiratory burst activity after 4 weeks feeding in sole vaccinated with Photobacterium damselae subsp. piscicida bacterin. [source]


    ABSTRACT The antioxidant activities and hypolipidemic effects of aqueous extract from Cleistocalyx operculatus flower buds (COB) (Roxb.) Merr. and Perry, a commonly used material for drink preparation in Vietnam, were investigated in vitro and in diabetic rats. In vitro, the aqueous extract of COB which has highest phenolic and flavonoid contents showed a strong antioxidant effect and highest pancreatic lipase inhibitory activity when compared with green tea and guava leaf extracts. Oral administration of aqueous extract from COB (500 mg/kg body weight/day) on streptozotocin-induced diabetic rats for 8 weeks resulted in significant reduction in the levels of glucose, total cholesterol and triglyceride in plasma as well as the concentration of glucose and sorbitol in the lens. In addition, COB showed significant recovery in the activities of antioxidant enzymes (superoxide dismutase, glutathione S-transferase) and glutathione level in liver with markedly decrease in the lipid peroxide level in liver and lens of the COB-treated diabetic rats. These results indicated that COB showed antioxidant activities, prevention of sorbitol accumulation in lens and hypolipidemic effects in addition to its antidiabetic effects and may be considered as a promising material for the prevention of diabetic complications and metabolic syndrome. PRACTICAL APPLICATIONS In recent years, research on traditional medicinal plants for the management of diabetes has attracted the interest of medical scientists. A suitable plant material for antidiabetes and prevention of diabetic complications should possess various biological components, such as antihyperglycemia, antioxidant activities and antihyperlipidemia, without side effects. In this study, the aqueous extract from Cleistocalyx operculatus flower buds (COB) with high polyphenolic and flavonoid content has shown beneficial biological functions in vitro and in diabetic rats, including antioxidant activity, hypolipidemic and hypoglycemic effects. The results of our study suggest that COB might have a potential role in the management of the prediabetic state and the prevention of diabetic complications. Therefore, there is the possibility for the development of C. operculatus as a beverage for the prevention of diabetes, as well as the prevention of the metabolic syndrome. [source]

    Amelioration of Cadmium-Induced Oxidative Stress, Impairment in Lipids and Plasma Lipoproteins by the Combined Treatment with Quercetin and ,-Tocopherol in Rats

    S. Milton Prabu
    Abstract:, Cadmium (Cd) exposure results in numerous pathological consequences including oxidative stress and dyslipidemia. The present study was designed to investigate the efficacy of combined treatment with quercetin (QE) and ,-tocopherol (AT) against Cd-induced oxidative stress and alterations in lipids and lipoproteins in the plasma and liver of rats. Oral administration of Cd (5 mg/kg bw/d) for 4 wk has shown a significant (P < 0.05) increase in thiobarbituric acid reactive substances (TBARS), lipid hydro peroxides (LOOH), total cholesterol, low density lipoprotein cholesterol (LDL-C), very low density lipoprotein cholesterol (VLDL-C), free fatty acids (FFA), phospholipids (PL), triglycerides (TGs), and the activity of hydroxyl-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) in plasma with a significant (P > 0.05) reduction in the levels of reduced glutathione (GSH), high density lipoprotein cholesterol (HDL-C), and the activity of lecithin cholesterol acyl transferase (LCAT) in plasma. In addition, the levels of hepatic thiobarbituric acid reactive substances (TBARS), LOOH, conjugated dienes (CD), protein carbonyls (PC), and the activity of HMG-CoA reductase, levels of cholesterol, FFA, and TGs were significantly (P > 0.05) increased and the level of PL is significantly (P > 0.05) decreased along with the decreased activity of LCAT in the liver of Cd-treated rats. Oral supplementation with QE (50 mg/kg bw/d) and AT (50 mg/kg bw/d) for 4 wk in Cd intoxicated rats significantly (P > 0.05) has reduced the plasma levels of TBARS, LOOH, GSH, cholesterol, FFA, TGs, VLDL-C, LDL-C, and the activity of HMG-CoA and significantly (P > 0.05) has increased the activity of LCAT and the plasma levels of HDL-C. The oral supplementation also significantly (P > 0.05) has reduced the hepatic oxidative stress markers, cholesterol, TGs, FFA, and significantly (P > 0.05) has increased the LCAT activity and the PL in liver. Our results indicate that the combined treatment with QE and AT has normalized all the previously mentioned biochemical parameters in Cd-intoxicated rats than the individual treatments. The combined treatment has provided remarkable protection against Cd-induced oxidative stress and alterations in lipid metabolism and, thereby, reduced the Cd-mediated cardiovascular diseases. [source]

    A Lipoprotein-derived Antimicrobial Factor from Hen-egg Yolk is Active Against Streptococcus Species

    D. Brady
    ABSTRACT: Oral administration of hen-egg yolk provides protection against specific pathogens. We examined the antibacterial activity of fractionated egg yolk against 2 pathogenic Streptococcus strains, using an in vitro assay. A water-soluble protein fraction (WSPF) of egg yolk consistently inhibited the growth of S. mutans by 25%. The WSPF treated with pancreatin demonstrated > 80% inhibition of bacterial growth. Growth of S. sanguis was completely inhibited. Gel filtration and ion exchange chromatography established that anti-Streptococcal activity resided with lipoproteins. Antibacterial activity was released by crude lipase or a combination of lipase and protease treatment of egg lipoproteins. Thus, hen-egg yolk lipoproteins are important molecules for lipid-mediated antimicrobial activity. [source]

    Protective effect of glucosamine against ibuprofen-induced peptic ulcer in rats

    Sethumadhavan Santhosh
    Abstract Background:,Helicobacter pylori is the major causative factor of ulcer but the use of ibuprofen and other non-steroidal anti-inflammatory drugs have also been implicated in development of ulcer. The purpose of the present study was to determine the anti-ulcer effect of glucosamine. Methods:, The protective effect of glucosamine on ibuprofen-induced peptic ulcer in male albino rats was studied with respect to changes in the volume of gastric juice, acid output, pepsin activity, activities of membrane bound ATPases, protein content, glycoprotein components and histopathology. Results:, Oral administration of ibuprofen caused significant increase in the number of lesions in the gastric mucosa, increases in the volume of gastric juice and acidity, and decreased activity of pepsin. The levels of protein content and glycoprotein components (hexose, hexosamine and sialic acid) and ATPase activities were also observed. Oral pretreatment with glucosamine resulted in significant reduction in the number of lesions in the gastric mucosa and decreases in the volume of gastric juice and acidity. The pepsin activity was also maintained at near normalcy. Prior oral administration of glucosamine significantly prevented the ibuprofen-induced depletion of protein and glycoprotein components and maintained the activities of membrane bound ATPases as compared to untreated ulcer induced group of rats. Conclusion:, The anti-ulcerogenic activity of glucosamine might be ascribable to its ability to neutralize the hydrochloric acid secreted into the stomach and to its capability to strengthen the mucosal barrier by increasing mucosal glycoprotein synthesis and to its free radical scavenging property. Histopathological investigations of the mucosal tissue also support the anti-ulcerogenic effect of glucosamine. [source]

    Increased survival and neuroprotective effects of BN82451 in a transgenic mouse model of Huntington's disease

    Peter Klivenyi
    Abstract There is substantial evidence that excitotoxicity and oxidative damage may contribute to Huntington's disease (HD) pathogenesis. We examined whether the novel anti-oxidant compound BN82451 exerts neuroprotective effects in the R6/2 transgenic mouse model of HD. Oral administration of BN82451 significantly improved motor performance and improved survival by 15%. Oral administration of BN82451 significantly reduced gross brain atrophy, neuronal atrophy and the number of neuronal intranuclear inclusions at 90 days of age. These findings provide evidence that novel anti-oxidants such as BN82451 may be useful for treating HD. [source]

    Bacopa monniera protects rat heart against ischaemia,reperfusion injury: role of key apoptotic regulatory proteins and enzymes

    Ipseeta Ray Mohanty
    Abstract Objectives, Rat isolated hearts were perfused in a Langendorff model to study the cardioprotective effects of Bacopa monniera, a medicinal herb used in the Indian system of medicine, on cardiomyocyte apoptosis and antioxidant status following ischaemia,reperfusion (I-R) injury. Methods, Forty-eight rats were randomly divided into four groups (12 in each group): sham group (no ischaemia,reperfusion injury), B. monniera control group (orally fed B. monniera at a dose of 75 mg/kg, for three weeks); ischaemia,reperfusion control group(subjected to ischaemia,reperfusion-induced myocardial injury) and B. monniera -treated group (same protocol as ischaemia,reperfusion control group except that rats also fed B. monniera). Key findings, Post-ischaemic reperfusion injury resulted in significant cardiac necrosis, apoptosis, depression of heart rate, decline in antioxidant status and elevation in lipid peroxidation. Oral administration of B. monniera per se for three weeks to healthy rats caused augmentation of myocardial antioxidants, superoxide dismutase, catalase and glutathione, along with induction of heat shock protein 72 (HSP72). Ischaemia,reperfusion-induced biochemical and histopathological perturbations were significantly prevented by B. monniera (75 mg/kg) pre-treatment. Interestingly, B. monniera also restored the antioxidant network of the myocardium and reduced myocardial apoptosis, caspase 3 and Bax protein expression. Conclusions, Histopathological studies and myocardial creatine phosphokinase content further confirmed the cardioprotective effects of B. monniera (75 mg/kg) in the experimental model of ischaemia,reperfusion injury. The study provides scientific basis for the putative therapeutic effect of B. monniera in ischaemic heart disease. [source]

    Antidiabetic properties of the alcoholic extract of Sphaeranthus indicus in streptozotocin-nicotinamide diabetic rats

    Kirti S. Prabhu
    We have investigated the possible antihyperglycaemic effects of Sphaeranthus indicus extract in rats rendered diabetic by nicotinamide (120 mgkg,1 i.p.) and streptozotocin (STZ) (60 mgkg,1 i.p). Fasting plasma glucose levels, serum insulin levels, serum lipid profiles, magnesium levels, glycosylated haemoglobin, changes in body weight and liver glycogen levels were evaluated in normal and diabetic rats. Oral administration of S. indicus for 15 days resulted in significant decrease in blood glucose levels and increases in hepatic glycogen and plasma insulin levels. Fasting normal rats treated with the alcoholic extract of S. indicus showed significant improvement in oral glucose tolerance test. Glibenclamide was used as a reference standard. The findings demonstrate that the alcoholic S. indicus extract may be useful in the treatment of diabetes. [source]

    Protective effect of total flavonoids from Bidens bipinnata L. against carbon tetrachloride-induced liver injury in mice

    Ming-mei Zhong
    Bidens bipinnata L. is well known in China as a traditional Chinese medicine. This study was designed to evaluate the hepatoprotective activity of the total flavonoids of B. bipinnata L. (TFB) against carbon tetrachloride (CCI4)-induced acute liver injury in mice and to determine its mechanism of action. Oral administration of TFB at doses of 50, 100 and 200 mg kg,1 for 7 days significantly reduced the elevated relative values of liver weight, serum transaminases (alanine aminotransferase and aspartate aminotransferase) and the hepatic morphologic changes induced by CCl4 in mice. In addition, TFB markedly inhibited CCl4 -induced lipid peroxidation and enhanced the activity of the antioxidant enzymes superoxide dismutase and glutathione peroxidase. Moreover, pretreatment with TFB suppressed nitric oxide production and nuclear factor- kB activation in CCl4 -treated mice. The results suggest that TFB has significant hepatoprotective activity and its mechanism is related, at least in part, to its antioxidant properties. Further research is required to investigate the detailed mechanism of the protective effect of TFB on acute liver injury. [source]

    D- chiro -Inositol found in Cucurbita ficifolia (Cucurbitaceae) fruit extracts plays the hypoglycaemic role in streptozocin-diabetic rats

    Tao Xia
    Cucurbita ficifolia is commonly used as an antihyperglycaemic agent in Asia. However, the mechanism of its action is unknown. Chemically synthesized D- chiro -inositol (D-CI), a component of an insulin mediator, has been demonstrated to have antihyperglycaemic effects in rats. In this study, we found that C. ficifolia contained fairly high levels of D-CI, thus, C. ficifolia may be a natural source of D-CI for reducing blood glucose concentrations in diabetics. We evaluated C. ficifolia fruit extract, containing D-CI, for its antihyperglycaemic effect in streptozotocin-induced diabetic rats. Oral administration of C. ficifolia fruit extract containing 10 or 20 mg D-CI kg,1 body weight for 30 days resulted in significantly lowered levels of blood glucose, and increased levels of hepatic glycogen, total haemoglobin and plasma insulin. An oral glucose tolerance test was performed in fasted diabetic and normal rats, in which there was a significant improvement in blood glucose tolerance in the diabetic rats treated with C. ficifolia fruit extract. The effects were compared with 20 mg kg,1 body weight chemically synthesized D-CI. Findings from this study demonstrated that C. ficifolia fruit extract was an effective source of D-CI for its hypoglycaemic effects in rats, and therefore may be useful in the treatment of diabetes. [source]

    Modulatory effects of Aloe vera leaf gel extract on oxidative stress in rats treated with streptozotocin

    S. Rajasekaran
    Oxidative stress is currently suggested as a mechanism underlying diabetes and diabetic-related complications. Oxidative stress results from an imbalance between radical-generating and radical-scavenging systems. Many secondary plant metabolites have been reported to possess antioxidant activity. This study was designed to evaluate the potential antioxidative activity of the ethanolic extract from Aloe vera leaf gel in the plasma and pancreas of streptozotocin (STZ)-induced diabetic rats. Glibenclamide was used as a standard reference drug. Oral administration of ethanolic extract at a concentration of 300 mg kg,1 body weight for 21 days resulted in a significant reduction in fasting blood glucose, thiobarbituric acid reactive substances, hydroperoxides and alpha-tocopherol and significant improvement in ascorbic acid, reduced glutathione and insulin in the plasma of diabetic rats. Similarly, the treatment also resulted in a significant reduction in thiobarbituric acid reactive substances, hydroperoxides, superoxide dismutase, catalase and glutathione peroxidase and significant improvement in reduced glutathione in the pancreas of STZ-induced diabetic rats when compared with untreated diabetic rats. The ethanolic extract appeared to be more effective than glibenclamide in controlling oxidative stress. Thus, this study confirms the ethnopharmacological use of Aloe vera in ameliorating the oxidative stress found in diabetes. [source]

    Effects of oral administration of extracts of Hypericum perforatum (St John's wort) on brain serotonin transporter, serotonin uptake and behaviour in mice

    Kazufumi Hirano
    The pharmacological effects of extracts of Hypericum perforatum (St John's wort) were characterized in-vitro and ex-vivo, in relation to its behavioural effects. In in-vitro experiments, St John's wort inhibited brain synaptosomal [3H]serotonin uptake in mice with little effect on specific [3H]paroxetine binding. For selective serotonin-reuptake inhibitors (SSRIs), the IC50 value for [3H]serotonin uptake (molar concentration of unlabelled drug necessary to displace 50% of specific uptake) correlated well with the inhibition constant Ki value for [3H]paroxetine binding in mouse brain. Oral administration of St John's wort (900 mg kg,1), paroxetine (1 mg kg,1) and sertraline (10 mg kg,1) brought about significant increases in the Km value for [3H]serotonin uptake into brain synaptosomes 4 h later, and only SSRIs suppressed specific [3H]paroxetine binding in mouse brain. St John's wort and SSRIs significantly inhibited marble-burying behaviour in mice and the time-course of attenuation of this behaviour by St John's wort was similar to that of [3H]serotonin uptake inhibition. In the forced swimming test, St John's wort, but not SSRIs, suppressed the immobility time of mice after oral administration. These results provide the first in-vivo evidence to suggest that the mode of antidepressant action of St John's wort differs from that of SSRIs. Thus, this study may have a significant impact on phytotherapy with St John's wort. [source]