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1.
Rev. bras. parasitol. vet ; 26(3): 323-330, July-Sept. 2017. tab, graf
Article in English | LILACS | ID: biblio-899288

ABSTRACT

Abstract Thymol is a monoterpene and acetylation form of this compound can reduce the toxicity and enhance its biological effects. The objective of this study was to evaluate the effect of thymol and thymol acetate (TA) on egg, larva and adult Haemonchus contortus and the cuticular changes, acute toxicity in mice and the efficacy on sheep gastrointestinal nematodes. In vitro tests results were analyzed by analysis of variance (ANOVA) and followed by comparison with Tukey test or Bonferroni. The efficacy of in vivo test was calculated by the BootStreet program. In the egg hatch test (EHT), thymol (0.5 mg/mL) and TA (4 mg/mL) inhibited larval hatching by 98% and 67.1%, respectively. Thymol and TA (8 mg/mL) inhibited 100% of larval development. Thymol and TA (800 µg/mL) reduced the motility of adult worms, by 100% and 83.4%, respectively. Thymol caused cuticular changes in adult worm teguments. In the acute toxicity test, the LD50 of thymol and TA were 1,350.9 mg/kg and 4,144.4 mg/kg, respectively. Thymol and TA reduced sheep egg count per gram of faeces (epg) by 59.8% and 76.2%, respectively. In in vitro tests thymol presented better anthelmintic activity than TA. However TA was less toxic and in in vivo test efficacy was similar.


Resumo Timol é um monoterpeno e a acetilação deste composto pode reduzir a toxicidade e potencializar os seus efeitos biológicos. O objetivo deste trabalho foi avaliar o efeito do timol e acetato de timolila (AT) sobre ovos, larvas e adultos de Haemonchus contortus e suas alterações cuticulares, toxicidade aguda em camundongos e a eficácia sobre nematoides gastrintestinais de ovinos. Os resultados dos testes in vitro foram analisados por análise de variância (ANOVA) e comparados pelo testes de Tukey ou Bonferroni. A eficácia do teste de redução da contagem de ovos nas fezes (RCOF) foi calculada pelo programa BootStreet. No teste de inibição da eclosão de ovos (TEO), timol (0,5 mg/mL) e AT (4 mg/mL) inibiram a eclosão das larvas em 98% e 67,1%, respectivamente. Timol e AT (8 mg/mL) inibiram 100% do desenvolvimento larval. Timol e AT (800 μg/mL) reduziram a motilidade dos nematoides adultos, em 100% e 83,4%, respectivamente. O timol provocou alterações cuticulares nos nematoides adultos. No teste de toxicidade aguda, a DL50 do timol e AT foi de 1.350,9 mg/kg e 4.144,4 mg/kg, respectivamente. Timol e AT reduziram a contagem de ovos por gramas de fezes (OPG) dos ovinos em 59,8% e 76,2%, respectivamente. Nos testes in vitro timol apresentou atividade melhor anti-helmíntica do que AT. Entretanto, AT foi menos tóxico do que o timol e no teste in vivo apresentaram eficácia semelhante.


Subject(s)
Animals , Female , Mice , Sheep Diseases/parasitology , Sheep Diseases/drug therapy , Thymol/toxicity , Thymol/therapeutic use , Nematoda/drug effects , Nematode Infections/veterinary , Acetylation , Thymol/pharmacology , Sheep , Haemonchus/drug effects , Anthelmintics/therapeutic use , Anthelmintics/pharmacology , Acetates/therapeutic use , Acetates/pharmacology , Nematode Infections/drug therapy
2.
An. acad. bras. ciênc ; 89(2): 1111-1120, Apr.-June 2017. tab, graf
Article in English | LILACS | ID: biblio-886682

ABSTRACT

ABSTRACT Myrciaria floribunda (H. West ex Willd.) O. Berg, Myrtaceae, is a native plant species of the Atlantic Rain Forest, from north to south of Brazil. The lyophilized ethyl acetate extract from the leaves of M. floribunda was investigated for its antiproliferative activity in tumor cell lines, antioxidant capacity and its total phenolic, flavonoid and tannin contents. Antiproliferative activity was tested in vitro against seven human cancer cells and against immortalized human skin keratinocytes line (HaCat, no cancer cell). Antioxidant activity was determined using 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and oxygen radical absorbing capacity (ORAC) assays and total phenolic, flavonoid and tannin contents were determined by spectrophotometric techniques. Ethyl acetate extract of M. floribunda exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 69.70 and 172.10 µg/mL. For HaCat cell, TGI value was 213.60 µg/mL. M. floribunda showed a strong antioxidant potential: EC50 of 45.89±0.42 µg/mL and 0.55±0.05 mmol TE/g for DPPH and ORAC, respectively. Total phenolic content was 0.23±0.013g gallic acid equivalents (GAE)/g extract and exhibited 13.10±1.60% of tannins content. The content of flavonoid was 24.08±0.44% expressed as rutin equivalents. These results provide a direction for further researches about the antitumoral potential of M. floribunda.


Subject(s)
Humans , Phenols/analysis , Flavonoids/analysis , Myrtaceae/chemistry , Cell Proliferation/drug effects , Antioxidants/pharmacology , Picrates , Biphenyl Compounds , Brazil , Cell Line, Tumor , Oxygen Radical Absorbance Capacity , Indicators and Reagents , Acetates/pharmacology , Acetates/chemistry
3.
Acta cir. bras ; 31(8): 557-563, Aug. 2016. tab, graf
Article in English | LILACS | ID: lil-792413

ABSTRACT

ABSTRACT PURPOSE: To determine the toxic effect of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) on reproductive system and the beneficial effects of Montelukast (ML) with histological and biochemical analysis. METHODS: Rats were randomly divided into four equal groups (control, TCDD, ML and TCDD+ML). Tissue samples were collected on day 60 and oxidative status and histological alterations were analyzed. RESULTS: The results showed a significant increase in oxidative and histological damage on uterine and ovarian tissues. Otherwise, the oxidative and histological damages caused by TCDD were prevented with ML treatment. CONCLUSION: The toxic effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin on female reproductive system were reversed with Montelukast treatment. Therefore, we claimed that ML treatment might be useful for TCDD toxicity.


Subject(s)
Animals , Female , Rats , Ovary/drug effects , Quinolines/pharmacology , Oxidative Stress/drug effects , Polychlorinated Dibenzodioxins/toxicity , Acetates/pharmacology , Antioxidants/pharmacology , Ovary/pathology , Superoxide Dismutase/metabolism , Uterus/pathology , Catalase/metabolism , Random Allocation , Rats, Wistar , Glutathione/metabolism , Ovarian Follicle/drug effects
4.
Braz. j. biol ; 76(2): 531-538, Apr.-June 2016. tab, graf
Article in English | LILACS | ID: lil-781389

ABSTRACT

Abstract The loss of leaves by plant species found in the Cerrado (Brazilian savanna) is an energetically expensive process due to adverse environmental conditions and predation by herbivory. The mature leaves have adaptations which minimize these events. However, the young individuals lack these structures and produce high leaf concentrations of secondary metabolites as a form of protection. These compounds can be used in bioprospection of natural herbicides. Thus, this study aimed to evaluate the phytotoxicity of hexane, ethyl acetate and aqueous extracts of young leaves from Blepharocalyx salicifolius (Kunth) O. Berg on the elongation of wheat coleoptiles (Triticum aestivum L.) and evaluate the potential phytotoxic of ethyl acetate extract on germination, growth and cell size of metaxylem of sesame (Sesamum indicum L.) seedlings. The hexane and ethyl acetate extracts inhibited the elongation of wheat coleoptiles at all concentrations; however, the most promising results were observed in coleoptile fragments treated with the ethyl acetate extract. This treatment changed the mean germination time and the synchrony of sesame seeds, inhibited the growth of shoots and roots, reduced the dry weight of seedlings, led to abnormalities in the seedlings and reduced the length of the metaxylem cells in the sesame seedlings. These results demonstrated the phytotoxic potential of young leaf extracts of B. salicifolius and the high phytotoxicity of the ethyl acetate extract in the initial development of S. indicum.


Resumo A perda das folhas pelas plantas do Cerrado é um processo energeticamente custoso devido às condições ambientais adversas e intensa predação por herbivoria. As folhas maduras possuem adaptações que minimizam esses eventos. Entretanto, os indivíduos jovens carecem dessas estruturas e produzem elevadas concentrações foliares de metabólitos secundários como forma de proteção. Esses compostos podem ser utilizados na bioprospecção de herbicidas naturais. Dessa forma, objetivamos com este estudo avaliar a fitotoxicidade dos extratos hexânico, acetato etílico e aquoso de folhas jovens de Blepharocalyx salicifolius (Kunth) O. Berg sobre o alongamento de coleóptilos estiolados de Triticum aestivum L. (trigo) e avaliar o potencial fitotóxico do extrato acetato etílico sobre a germinação, crescimento e comprimento das células do metaxilema de Sesamum indicum (gergelim). Os extratos hexânico e acetato etílico inibiram o alongamento dos coleóptilos em todas as concentrações testadas, entretanto os resultados mais promissores foram observados nos fragmentos submetidos ao extrato acetato etílico. Este extrato alterou o tempo médio de germinação e a sincronia das sementes de gergelim, inibiu o crescimento da parte aérea e subterrânea com redução da massa seca das plântulas, levou ao surgimento acentuado de anomalias e causou redução no comprimento médio das células do metaxilema de plântulas de gergelim. Assim, ficou comprovado o potencial fitotóxico dos extratos de folhas jovens de B. salicifolius e a acentuada fitotoxicidade do extrato acetato etílico sobre o desenvolvimento inicial de S. indicum.


Subject(s)
Triticum/drug effects , Triticum/physiology , Plant Leaves/drug effects , Germination/drug effects , Myrtaceae , Hexanes/pharmacology , Acetates/pharmacology , Brazil , Plant Extracts/pharmacology , Plant Roots/growth & development , Plant Roots/drug effects , Plant Leaves/growth & development , Seedlings/drug effects , Herbicides/pharmacology
5.
Braz. j. med. biol. res ; 49(4): e5031, 2016. tab, graf
Article in English | LILACS | ID: lil-774523

ABSTRACT

Cysteinyl leukotrienes (CysLTs) have been implicated in seizures and kindling; however, the effect of CysLT receptor antagonists on seizure frequency in kindled animals and changes in CysLT receptor expression after pentylenetetrazol (PTZ)-induced kindling have not been investigated. In this study, we evaluated whether the CysLT1 inverse agonist montelukast, and a classical anticonvulsant, phenobarbital, were able to reduce seizures in PTZ-kindled mice and alter CysLT receptor expression. Montelukast (10 mg/kg, sc) and phenobarbital (20 mg/kg, sc) increased the latency to generalized seizures in kindled mice. Montelukast increased CysLT1 immunoreactivity only in non-kindled, PTZ-challenged mice. Interestingly, PTZ challenge decreased CysLT2 immunoreactivity only in kindled mice. CysLT1 antagonists appear to emerge as a promising adjunctive treatment for refractory seizures. Nevertheless, additional studies are necessary to evaluate the clinical implications of this research.


Subject(s)
Animals , Male , Mice , Acetates/pharmacology , Anticonvulsants/pharmacology , Leukotriene Antagonists/pharmacology , Quinolines/pharmacology , Seizures/drug therapy , Acetates/therapeutic use , Anticonvulsants/therapeutic use , Blotting, Western , Convulsants , Kindling, Neurologic/drug effects , Leukotriene Antagonists/therapeutic use , Pentylenetetrazole , Phenobarbital/pharmacology , Phenobarbital/therapeutic use , Quinolines/therapeutic use , Receptors, Leukotriene/drug effects , Seizures/chemically induced , Time Factors , Treatment Outcome
6.
Arch. endocrinol. metab. (Online) ; 59(2): 141-147, 04/2015. tab, graf
Article in English | LILACS | ID: lil-746464

ABSTRACT

Objective Investigate the effect of GC-1 on tolerance to exercise in rats with experimental hypothyroidism. Materials and methods Hypothyroidism was induced with methimazole sodium and perchlorate treatment. Six groups with eight animals were studied: control group (C), hypothyroid group without treatment (HYPO); hypothyroidism treated with physiological doses of tetraiodothyronine (T4) or 10 times higher (10×T4); hypothyroidism treated with equal molar doses of GC-1 (GC-1) or 10 times higher (10×GC-1). After eight weeks, each animal underwent an exercise tolerance test by measuring the time (seconds), in which the rats were swimming with a load attached to their tails without being submerging for more than 10 sec. After the test, the animals were killed, and blood samples were collected for biochemical analysis, and the heart and soleus muscle were removed for weighing and morphometric analysis of the cardiomyocyte. Results Hypothyroidism significantly reduced tolerance to exercise and, treatment with GC-1 1× or T4 in physiological doses recover tolerance test to normal parameters. However, high doses of T4 also decreased tolerance to physical exercise. Conversely, ten times higher doses of GC-1 did not impair tolerance to exercise. Interestingly, hypothyroidism, treated or not with T4 in a physiological range, GC-1 or even high doses of GC-1 (10X) did not change cardiomyocyte diameters and relative weight of the soleus muscle. In contrast, higher doses of T4 significantly increased cardiomyocyte diameter and induced atrophy of the soleus muscle. Conclusion Unlike T4, GC-1 in high doses did not modify tolerance to physical exercise in the rats with hypothyroidism. .


Subject(s)
Animals , Acetates/pharmacology , Exercise Tolerance/drug effects , Hypothyroidism/drug therapy , Phenols/pharmacology , Thyroid Hormone Receptors beta/agonists , Exercise Tolerance/physiology , Hypothyroidism/blood , Hypothyroidism/chemically induced , Hypothyroidism/physiopathology , Methimazole , Muscle, Skeletal/drug effects , Myocytes, Cardiac/drug effects , Perchlorates , Rats, Wistar , Sodium Compounds , Swimming , Thyrotropin/blood , Thyroxine/administration & dosage , Thyroxine/blood , Triiodothyronine/blood
7.
Yonsei Medical Journal ; : 426-432, 2015.
Article in English | WPRIM | ID: wpr-141635

ABSTRACT

PURPOSE: The aim of this study was to investigate whether pathologic changes in zonula occludens-1 (ZO-1) are induced by interleukin-13 (IL-13) in the experimental minimal-change nephrotic syndrome (MCNS) model and to determine whether montelukast, a leukotriene receptor antagonist, has an effect on ZO-1 restoration in cultured human podocytes. MATERIALS AND METHODS: Human podocytes cultured on bovine serum albumin-coated plates were treated with different doses of IL-13 and montelukast and then examined for distribution using confocal microscopy and for ZO-1 protein levels using Western blotting. RESULTS: ZO-1 was internalized and shown to accumulate in the cytoplasm of human podocytes in an IL-13 dose-dependent manner. High doses (50 and 100 ng/mL) of IL-13 decreased the levels of ZO-1 protein at 12 and 24 h (both p<0.01; n=3), which were significantly reversed by a high dose (0.5 microM) montelukast treatment (p<0.01; n=3). CONCLUSION: Our results suggest that IL-13 alters the expression of ZO-1, and such alterations in the content and distribution of ZO-1 may be relevant in the pathogenesis of proteinuria in the MCNS model.


Subject(s)
Acetates/pharmacology , Blotting, Western , Dose-Response Relationship, Drug , Humans , Interleukin-13/pharmacology , Leukotriene Antagonists/pharmacology , Microscopy, Confocal , Podocytes/drug effects , Proteinuria/pathology , Quinolines/pharmacology , Tight Junctions , Zonula Occludens-1 Protein/metabolism
8.
Yonsei Medical Journal ; : 426-432, 2015.
Article in English | WPRIM | ID: wpr-141634

ABSTRACT

PURPOSE: The aim of this study was to investigate whether pathologic changes in zonula occludens-1 (ZO-1) are induced by interleukin-13 (IL-13) in the experimental minimal-change nephrotic syndrome (MCNS) model and to determine whether montelukast, a leukotriene receptor antagonist, has an effect on ZO-1 restoration in cultured human podocytes. MATERIALS AND METHODS: Human podocytes cultured on bovine serum albumin-coated plates were treated with different doses of IL-13 and montelukast and then examined for distribution using confocal microscopy and for ZO-1 protein levels using Western blotting. RESULTS: ZO-1 was internalized and shown to accumulate in the cytoplasm of human podocytes in an IL-13 dose-dependent manner. High doses (50 and 100 ng/mL) of IL-13 decreased the levels of ZO-1 protein at 12 and 24 h (both p<0.01; n=3), which were significantly reversed by a high dose (0.5 microM) montelukast treatment (p<0.01; n=3). CONCLUSION: Our results suggest that IL-13 alters the expression of ZO-1, and such alterations in the content and distribution of ZO-1 may be relevant in the pathogenesis of proteinuria in the MCNS model.


Subject(s)
Acetates/pharmacology , Blotting, Western , Dose-Response Relationship, Drug , Humans , Interleukin-13/pharmacology , Leukotriene Antagonists/pharmacology , Microscopy, Confocal , Podocytes/drug effects , Proteinuria/pathology , Quinolines/pharmacology , Tight Junctions , Zonula Occludens-1 Protein/metabolism
9.
Clinics ; 69(12): 854-861, 2014. tab, graf
Article in English | LILACS | ID: lil-732391

ABSTRACT

OBJECTIVES: The purpose of this study was to analyze the effects of soybean extracts obtained using different extraction methods on the skin of female rats. METHOD: A total of 64 female Sprague-Dawley rats were divided into 8 equal groups. Various extracts were administered to the female rats by oral gavage for one month. The groups comprised carboxymethyl cellulose-free control, carboxymethyl cellulose-plus control, 100-mg/kg n-hexane extract, 200-mg/kg n-hexane extract, 100-mg/kg ethyl acetate extract, 200-mg/kg ethyl acetate extract, 100-mg/kg ethanol extract and 200-mg/kg ethanol extract groups. The thickness of the collagen layer and the number of estrogen receptor-positive cells were evaluated. RESULTS: All the extract-treated groups showed a statistically significant decrease in the number of estrogen receptor-positive cells compared with the control groups. Regarding the thickness of the collagen layer, only the 200-mg/kg ethyl acetate extract-treated group showed a significant increase compared with the control groups (p<0.05). CONCLUSIONS: Our data suggest that oral intake of three different total soybean extracts might have positive estrogenic effects on the skin and that only a high-dose ethyl acetate extract can increase the expression of collagen, which may prove to be beneficial for postmenopausal facial skin. ...


Subject(s)
Animals , Female , Collagen/analysis , Plant Extracts/pharmacology , Receptors, Estrogen/analysis , Skin/drug effects , Soybeans/chemistry , Acetates/pharmacology , Chromatography, High Pressure Liquid , Collagen/drug effects , Ethanol/pharmacology , Hexanes/pharmacology , Immunohistochemistry , Phytoestrogens/pharmacology , Rats, Sprague-Dawley , Reference Values , Reproducibility of Results , Receptors, Estrogen/drug effects , Skin/chemistry , Time Factors
10.
Article in English | IMSEAR | ID: sea-157539

ABSTRACT

Background:Allergic rhinitis is one of the most common conditions in clinical practice. Motelukast and second generation antihistamine fexofenadine are routinely used in the management of allergic rhinitis. Individually both drugs have been found to be effective in allergic rhinitis. Fixed dose combination of montelukast 10 mg plus fexofenadine 120 mg is available in India is also used in the treatment of allergic rhinitis. Objective: To evaluate the efficacy and safety of montelukast and fexofenadine fixed dose combination in the management of patients with allergic rhinitis. Material and methods: Post marketing observational study was conducted in 809 patients from all over India. All the patients were treated with montelukast 10 mg plus fexofenadine 120 mg fixed dose combination once daily for 14 days. The primary outcome criteria was the change in total symptom score (Sum of total nasal symptom score and total ocular symptom score) at the end of study compared to baseline. The secondary outcome criteria included change in total nasal symptom score (nasal congestion, rhinorrhea, nasal itching, and sneezing) and total ocular symptom score (Itching/burning eyes, tearing/ watering eyes and eye redness) at the end of study compared to baseline and physician’s and patient’s global assessment for efficacy and tolerability. The patients were evaluated at baseline, day 7 and day 14 for efficacy evaluation while the safety parameters were assessed at screening and day 14. Results: The fixed dose combination of fexofenadine plus montelukast was significantly effective in reducing total symptom score, total nasal symptom score and total ocular symptom score (p<0.0001 for all parameters). The global assessment of efficacy evaluation by both patient and investigators demonstrated “excellent to good” efficacy in >95% of patients. Most of the study population reported “good” tolerability with the fixed drug combination. No adverse events were reported in the study. Conclusion: The fixed dose combination of fexofenadine plus montelukast was found to be efficacious and well tolerated in allergic rhinitis in Indian adult patients.


Subject(s)
Acetates/administration & dosage , Acetates/analogs & derivatives , Acetates/pharmacology , Adult , Drug Combinations , Female , Humans , India , Male , Middle Aged , Quinolines/administration & dosage , Quinolines/analogs & derivatives , Quinolines/pharmacology , Product Surveillance, Postmarketing , Rhinitis, Allergic/drug therapy , Rhinitis, Allergic/epidemiology , Terfenadine/administration & dosage , Terfenadine/analogs & derivatives , Terfenadine/pharmacology , Treatment Outcome
11.
Esculapio. 2013; 9 (1): 25-29
in English | IMEMR | ID: emr-143129

ABSTRACT

To compare the efficacy of levocetirizine with montelukast and levocetirizine alone in patients with persistent allergic rhinitis in our setup. Patients with symptoms of AR attending ENT clinic were registered and divided into two groups based on drug given. Patients with odd numbers were included in group A receiving levocetirizine 5mg with montelukast 10mg once daily while patients with even numbers were included in group B receiving only levocetirizine 5mg once daily. Data was collected at visit 1 prior to medication, visit 2 one week after medication and visit 3 two weeks after medication. Medication history review, nasal symptom assessment and anterior rhinoscopy were done at each visit. Patients were evaluated for rhinorrhea, sneezing, nasal itching and nasal obstruction on a scale. Total symptom complex score [TSCS] was calculated by adding scores of all four variables under study using proforma. Lower the score more effective will be the drug. One hundred twenty four patients were included in study; 63 were male and 61 were female. TSCS was 9 -10 in 73.3% patients at visit 1 in levocetirizine + montelukast group that improved to 4-5 in 28.3% and 3- 4 in 65% patients at visit 2 and 3 respectively. Patients receiving levocetirizine alone had TSCS of 9 to 10 in 52.9% at visit 1 with an improvement to 3-4 in 9.4% and 49.1% at visit 2 and visit 3 respectively. Levocetirizine with montelukast is superior to levocetirizine alone in controlling overall symptoms of AR.


Subject(s)
Humans , Male , Female , Cetirizine/pharmacology , Acetates/pharmacology , Cetirizine , Quinolines/pharmacology , Acetates , Quinolines , Leukotriene Antagonists , Combined Modality Therapy
12.
Electron. j. biotechnol ; 15(5): 6-6, Sept. 2012. ilus, tab
Article in English | LILACS | ID: lil-657665

ABSTRACT

The defence mechanisms that are activated by methyl jasmonate (MJ) in fruits are not well understood. In this work, we studied the expression of defence genes in papaya fruit that are induced by the exposure to MJ and/or low temperatures. The papaya fruits ‘Maradol’ were randomly divided into two groups: one group was the untreated control and the other was treated with 10-4 M of MJ. Half of the fruits from each of the two groups were stored after treatment for 5 days at 5ºC and 2 days at 20ºC. We studied the expression levels of the pdf1.1 and pdf1.2 genes by amplification from expression libraries created from the pulp and skin tissues of the papaya fruit. As a reference, the mRNA level of the 18s ribosomal gene was used. In the skin tissue, the expression levels of the pdf1.1 and pdf1.2 genes were higher immediately after MJ treatment compared to the control. Furthermore, the expression of pdf1.2 remained high after MJ treatment and subsequent storage compared to the control. It was therefore concluded that the activation of the pdf1.1 and pdf1.2 genes forms part of the molecular defence mechanism in fruits that is activated by exposure to MJ. To our knowledge, this is the first study that analyzes the gene expression in papaya fruit that is induced by the exogenous application of methyl jasmonate and cold treatment.


Subject(s)
Acetates/pharmacology , Cold Temperature , Carica , Carica/genetics , Cyclopentanes/pharmacology , Carica/metabolism , DNA, Complementary , Gene Expression , Oxylipins/pharmacology , Polymerase Chain Reaction , Temperature
13.
Bauru; s.n; 2012. 122 p. tab, graf.
Thesis in Portuguese | LILACS, BBO | ID: biblio-866223

ABSTRACT

O chumbo (Pb) é um metal pesado, tóxico e está presente em diversos sistemas biológicos. Quando absorvido pelo organismo na forma iônica (Pb2+) atua em vários órgãos e sistemas, podendo ocasionar alterações graves no sistema nervoso central. Em adição, tem sido relatado que o íon ferroso (Fe2+) pode apresentar, entre outros, um efeito protetor na neurotoxicidade causada pelo Pb2+. Portanto, o objetivo deste estudo foi avaliar os marcadores de estresse oxidativo no cérebro de ratos expostos com acetato de chumbo (Pb(C2H3O2)2) associado ou não ao sulfato ferroso (FeSO4). Assim, 36 ratos machos (Rattus norvergicus) recém desmamados, divididos em 6 grupos (G), de 6 animais cada, foram expostos durante 6 semanas. No grupo controle (G1) os animais ingeriram água deionizada; G2 e G3 receberam 0,26 mM e G4 e G5 1,05 mM de acetato de chumbo, somado a isso G3 e G5 foram suplementados com 20 mg de sulfato ferroso/Kg peso corporal a cada 2 dias; e para G6 utilizou-se água deionizada e sulfato ferroso. O cérebro dos animais foi coletado para a análise da atividade enzimática de catalase (CAT), superóxido dismutase (SOD), glutationa peroxidase (GPx), a concentração de glutationa reduzida (GSH), lipoperoxidação (TBARS), hidroperóxido de lipídio (HL) e das substâncias antioxidantes totais (SAT) (técnicas ABTS e DPPH). A atividade das enzimas GPx e SOD nos grupos experimentais diminuiu em relação ao controle, assim como ocorreu com a concentração de GSH (p<0,05). Quanto às análises de HL e CAT, a primeira apresentou tendência de aumento na concentração dos grupos experimentais sem exposição concomitante, já a segunda demonstrou discreta inclinação de aumento na atividade em relação ao controle (p>0,05). A dosagem de SAT-ABTS mostrou aumento nos grupos expostos com 1,05 mM de acetato de chumbo. Em relação à SAT-DPPH houve diminuição nos grupos experimentais (p<0,05). De acordo com os resultados, as enzimas SOD e GPX e a GSH são...


Lead (Pb2+) is a toxic heavy metal, found in all stages of the inert environment and in several biological systems. When uptaken by the organism, acts on several organs and systems and may cause severe damage in Central Nervous System. In addition, it has been reported that iron (Fe2+) may present, a protective effect on neurotoxicity caused by Pb2+. Therefore, the aim of this study was to evaluate the markers of oxidative stress in the brain of rats exposed with lead acetate (Pb(C2H3O2)2) associated or not with ferrous sulfate (FeSO4). Thus, 36 rats weaning (Rattus norvegicus) were, divided into 6 groups (G) of six animals and were exposed for six weeks.In the control group (G1), the animals received deionized water; G2 and G3 received 0,26 mM, G4 and G5 1,05 mM of lead acetate; in addition to this G3 and G5 were supplemented with 20mg of ferrous sulfate/Kg body weight every 2 days; G6 received deionized water and ferrous sulfate were used. The animals' brains were collected for analysis of the enzymatic activity of catalase (CAT), superoxide dismutase (SOD), glutathione peroxidase (GPx), the concentration of reduced glutathione (GSH), lipid peroxidation (TBARS), lipid hydroperoxide (LH) and total antioxidant substances (TAS) (ABTS and DPPH technics). The activity of the enzymes SOD and GPx in the experimental groups decrease compared to control, as well as the concentration of GSH (p<0.05). Concerning to the analysis of HL and CAT, the first tended to increase the concentration in experimental groups without concomitant exposure with FeSO4, while the second showed a slight tendency for increase in activity compared to control (p>0.05). The dosage of TAS-ABTS showed an increase in the groups exposed with 1,05 mM of lead acetate. Regarding the SAT- DPPH there was a decrease in the experimental groups (p <0.05). According to the results, the enzymes SOD and GPx and GSH were affected by lead acetate and exposure with ferrous...


Subject(s)
Animals , Male , Rats , Acetates/pharmacology , Antioxidants/analysis , Cerebrum , Lead/pharmacology , Ferrous Sulfate , Lead/analysis , Drinking Behavior , Rats, Wistar
14.
Bauru; s.n; 2012. 122 p. tab, graf.
Thesis in Portuguese | LILACS, BBO | ID: lil-673694

ABSTRACT

O chumbo (Pb) é um metal pesado, tóxico e está presente em diversos sistemas biológicos. Quando absorvido pelo organismo na forma iônica (Pb2+) atua em vários órgãos e sistemas, podendo ocasionar alterações graves no sistema nervoso central. Em adição, tem sido relatado que o íon ferroso (Fe2+) pode apresentar, entre outros, um efeito protetor na neurotoxicidade causada pelo Pb2+. Portanto, o objetivo deste estudo foi avaliar os marcadores de estresse oxidativo no cérebro de ratos expostos com acetato de chumbo (Pb(C2H3O2)2) associado ou não ao sulfato ferroso (FeSO4). Assim, 36 ratos machos (Rattus norvergicus) recém desmamados, divididos em 6 grupos (G), de 6 animais cada, foram expostos durante 6 semanas. No grupo controle (G1) os animais ingeriram água deionizada; G2 e G3 receberam 0,26 mM e G4 e G5 1,05 mM de acetato de chumbo, somado a isso G3 e G5 foram suplementados com 20 mg de sulfato ferroso/Kg peso corporal a cada 2 dias; e para G6 utilizou-se água deionizada e sulfato ferroso. O cérebro dos animais foi coletado para a análise da atividade enzimática de catalase (CAT), superóxido dismutase (SOD), glutationa peroxidase (GPx), a concentração de glutationa reduzida (GSH), lipoperoxidação (TBARS), hidroperóxido de lipídio (HL) e das substâncias antioxidantes totais (SAT) (técnicas ABTS e DPPH). A atividade das enzimas GPx e SOD nos grupos experimentais diminuiu em relação ao controle, assim como ocorreu com a concentração de GSH (p<0,05). Quanto às análises de HL e CAT, a primeira apresentou tendência de aumento na concentração dos grupos experimentais sem exposição concomitante, já a segunda demonstrou discreta inclinação de aumento na atividade em relação ao controle (p>0,05). A dosagem de SAT-ABTS mostrou aumento nos grupos expostos com 1,05 mM de acetato de chumbo. Em relação à SAT-DPPH houve diminuição nos grupos experimentais (p<0,05). De acordo com os resultados, as enzimas SOD e GPX e a GSH são...


Lead (Pb2+) is a toxic heavy metal, found in all stages of the inert environment and in several biological systems. When uptaken by the organism, acts on several organs and systems and may cause severe damage in Central Nervous System. In addition, it has been reported that iron (Fe2+) may present, a protective effect on neurotoxicity caused by Pb2+. Therefore, the aim of this study was to evaluate the markers of oxidative stress in the brain of rats exposed with lead acetate (Pb(C2H3O2)2) associated or not with ferrous sulfate (FeSO4). Thus, 36 rats weaning (Rattus norvegicus) were, divided into 6 groups (G) of six animals and were exposed for six weeks.In the control group (G1), the animals received deionized water; G2 and G3 received 0,26 mM, G4 and G5 1,05 mM of lead acetate; in addition to this G3 and G5 were supplemented with 20mg of ferrous sulfate/Kg body weight every 2 days; G6 received deionized water and ferrous sulfate were used. The animals' brains were collected for analysis of the enzymatic activity of catalase (CAT), superoxide dismutase (SOD), glutathione peroxidase (GPx), the concentration of reduced glutathione (GSH), lipid peroxidation (TBARS), lipid hydroperoxide (LH) and total antioxidant substances (TAS) (ABTS and DPPH technics). The activity of the enzymes SOD and GPx in the experimental groups decrease compared to control, as well as the concentration of GSH (p<0.05). Concerning to the analysis of HL and CAT, the first tended to increase the concentration in experimental groups without concomitant exposure with FeSO4, while the second showed a slight tendency for increase in activity compared to control (p>0.05). The dosage of TAS-ABTS showed an increase in the groups exposed with 1,05 mM of lead acetate. Regarding the SAT- DPPH there was a decrease in the experimental groups (p <0.05). According to the results, the enzymes SOD and GPx and GSH were affected by lead acetate and exposure with ferrous...


Subject(s)
Animals , Male , Rats , Acetates/pharmacology , Antioxidants/analysis , Cerebrum , Lead/pharmacology , Ferrous Sulfate , Lead/analysis , Drinking Behavior , Rats, Wistar
15.
Journal of Guilan University of Medical Sciences. 2011; 19 (76): 29-37
in Persian | IMEMR | ID: emr-110046

ABSTRACT

The beta-carbolines harmane, harmine and norharmane are the members of Harmala,s alkaloids group [Peganum harmala, Zygophillaceae]. The beta-carboline alkaloids adjoined to benzodiazepine site of the gamma-aminobutyric acid type A [GABA[A]]. These alkaloids also inhibited cyclooxygenase and lipoxygenase activities. These findings showed that the beta-carbolines should be able to reduce writhing nociception induced by acetic acid- in mice. To assess the effects of acute treatment with harmane, norharmane and harmine on the writhing induced by acetic acid in mice. The experiments were carried out on male BALB/C mice [20-25g]. Intraperitoneal [I.p] injection of acetic acid [0.6%] was performed in order to cause writhing behavior. This behavior was recorded by direct observation for a 30-minutes period. Decrease of writhing count is indicative of an anti-nociception. In order to avoid the possibility of a physicochemical interaction between them, Drugs were administered on opposite sides of peritoned. Intraperitoneal [I.p] injection of Harmane [5-20mg/kg] on 6-9 mice, norharmane [5-15mg/kg] on 8-9 mice and harmine [10-15mg/kg] on 8-9 mice in per group decreased the writhing behavior significantly [P<0.0001, P<0.0003 and P<0.0016, respectively]. The inhibitory effects of the mentioned drugs were antagonized by flumazenil [2 mg/kg]. Effects of harmane, norharmane and harmine on writhing response may be mediated through an inverse agonistic mechanism located in the benzodiazepine receptors


Subject(s)
Animals, Laboratory , Male , Harmine/analogs & derivatives , Behavior, Animal/drug effects , Treatment Outcome , Acetates/pharmacology , Receptors, GABA-A/drug effects , Mice, Inbred BALB C , Pain Perception , Pain Measurement
16.
Biol. Res ; 43(2): 225-231, 2010. ilus
Article in English | LILACS | ID: lil-567537

ABSTRACT

Objectives: The objective of this study is to determine the effects of Ethyl acetate fraction from Cudrania tricuspidata (EACT) on the interleukin-1b (IL-1b)-induced proliferation of rheumatoid synovial fbroblasts (RASFs) and production of matrix metalloproteinases (MMPs), cyclooxygenase (COX) and prostaglandin E2 (PGE2) by RASFs. Materials and Methods: The proliferation of RASFs was evaluated with CCK-8 reagent in the presence of IL-1b with/without EACT. The expression of MMPs, TIMP-1, COXs, PGE2 and intracellular MAPK signalings, including p-ERK, p-p38, p-JNK and NF-kB were examined by immunoblotting or semi-quantitative reverse transcription-polymerase chain reaction (RT-PCR) and ELISA in conditions as described above. Results: EACT inhibits IL-1β-induced proliferation of RASFs and MMP-1, 3, COX-2 mRNA and protein expression, PGE2 production induced with IL-1b. EACT also inhibits the phosphorylation of ERK-1/2, p38, JNK and activation of NF-kB by IL-1b. Conclusions: These results suggest that EACT might be involved in synovial fbroblast proliferation and MMPs, COX-2, and PGE2 production, which are involved in joint destruction in rheumatoid arthritis (RA), indicating that this might be a new therapeutic modality for management of rheumatoid arthritis.


Subject(s)
Humans , Acetates/pharmacology , Arthritis, Rheumatoid/pathology , Fibroblasts/drug effects , Interleukin-1beta/antagonists & inhibitors , Moraceae/chemistry , Cell Proliferation/drug effects , /biosynthesis , Dinoprostone/biosynthesis , Enzyme-Linked Immunosorbent Assay , Fibroblasts/pathology , Interleukin-1beta/pharmacology , Matrix Metalloproteinases/biosynthesis , Polymerase Chain Reaction
17.
J Environ Biol ; 2007 Jan; 28(1): 39-43
Article in English | IMSEAR | ID: sea-113357

ABSTRACT

Screening of test chemicals or formulations for antifouling (AF) activity is important to get first hand information on their nontoxic repelling activities. Especially spores of a fouling alga, Ulva pertusa were used in this study to test the AF efficiency of five organic chemicals. Coatings made with 100 microg cm2 of citral and eugenol significantly inhibited the spore attachment. A low concentration (1 microg cm2) of solanesol exhibited effective AF activity against spore attachment. Spore germination was sensitive to different AF candidates screened in this study. Based on the attachment and germination response of Ulva pertusa spores, AF efficiency of five organic AF candidates is discussed.


Subject(s)
Acetates/pharmacology , Eugenol/pharmacology , Germination/drug effects , Monoterpenes/pharmacology , Spores/drug effects , Terpenes/pharmacology , Ulva/drug effects
18.
Indian J Pediatr ; 2006 Apr; 73(4): 275-82
Article in English | IMSEAR | ID: sea-81833

ABSTRACT

Leukotriene modifiers (receptor antagonist and biosynthesis inhibitor) represent the first mediator specific therapeutic option for asthma. Montelukast, a leukotriene receptor antagonist is the only such agent approved for use in pediatric patients. Montelukast modifies action of leukotrienes, which are the most potent bronchoconstrictors, by blocking Cysteinyl leukotriene receptors. Systemic drug like mountelukast can reach lower airways and improves the peripheral functions which play a crucial role in the evolution of asthma. Review of existing literature showed that montelukast compared to placebo has proven clinical efficacy in better control of day time asthma symptoms, percentage of symptom free days, need for rescue drugs and improvement in FEV 1. Studies also demonstrated improvement in airway inflammation as indicated by reduction in fractional exhaled nitric oxide, a marker of inflammation. Studies comparing low dose inhaled corticosteroids (ICS) with montelukast are limited in children and conclude that it is not superior to ICS. For moderate to severe persistent asthma, montelukast has been compared with long acting beta agonists (LABA) as an add-on therapy to ICS, montelukast was less efficacious and less cost-effective. It has beneficial effects in exercise induced asthma and aspirin-sensitive asthma. Montelukast has onset of action within one hour. Patient satisfaction and compliance was better with montelukast than inhaled anti-inflammatory agents due to oral, once a day administration. The recommended doses of montelukast in asthma are- children 1-5 years: 4 mg chewable tablet, children 6-14 years: 5mg chewable tablet, ADULTS: 10mg tablet; administered once daily. The drug is well tolerated. Based on the presently available data montelukast may be an alternative treatment for mild persistent asthma as monotherapy where ICS cannot be administered. It is also an alternative to LABA as an add-on therapy to ICS for moderate to severe persistent asthma. The other indications for use of montelukast include: allergic rhinitis, exercise induced bronchoconstriction and aspirin-induced asthma.


Subject(s)
Acetates/pharmacology , Administration, Inhalation , Adolescent , Adrenal Cortex Hormones/therapeutic use , Asthma/drug therapy , Bronchial Diseases/drug therapy , Child , Constriction, Pathologic/drug therapy , Humans , Infant , Leukotriene Antagonists/pharmacology , Practice Guidelines as Topic , Quinolines/pharmacology , Randomized Controlled Trials as Topic , Rhinitis, Allergic, Seasonal/drug therapy
19.
Article in English | IMSEAR | ID: sea-46759

ABSTRACT

To study the hyoplipidemic activity of non-methoxy and methoxy substituted--alkyl indan acetic acids in normogenic and hypergenic animal models. The hyoplipidemic activity was evaluated using normogenic and hypergenic rat models. Indan acids synthesized in our laboratory (50 mg/kg) and the standard drug clofibrate (50 mg/kg) were used for this study. Dimethoxy substituted -methyl and -ethyl indan acetic acids (9 & 10) exhibited significant hypocholesterolemic activity in both animal models. Clofibrate showed cholesterol lowering activity of 18% in normogenic rats while test agents 9 and 10 produced a similar activity of 20% and 17% respectively. Liver cholesterol and liver weight of the animals tested were found normal in case of the test compounds while liver weight was increased by 15% in clofibrate treated rats. LDL and VLDL cholesterol levels were also affected by compounds No. 9 and 10. Compounds having a smaller alkyl groups (R = CH3, C2H5) at--carbon atom of the acetic acid moiety exhibited significant hypocholesterolemic activity.


Subject(s)
Acetates/pharmacology , Animals , Hypolipidemic Agents/pharmacology , Cholesterol, LDL/drug effects , Cholesterol, VLDL/drug effects , Clofibrate/pharmacology , Hyperlipidemias/drug therapy , Indans/pharmacology , Male , Models, Animal , Rats , Triglycerides
20.
Indian J Exp Biol ; 2005 Mar; 43(3): 247-53
Article in English | IMSEAR | ID: sea-59707

ABSTRACT

The present study was aimed to evaluate the effect of licofelone, a dual inhibitor of cycloxygenase1/2-5-lipoxygenase against indomethacin-induced gastric damage in rats and mice in order to assess the role of leukotrienes if any, in non-steroidal anti-inflammatory drugs (NSAIDs)-induced gastrointestinal inflammation. Acute pretreatment with licofelone reversed the indomethacin-induced gastric ulceration, neutrophil adhesion in mesentery venules, neutrophil count in blood, lipid peroxides and vascularity in the stomachs of mice and rats. Further, chronic pretreatment of licofelone also prevented indomethacin-induced gastric morphological changes and cellular infiltration in mesentery venules. Moreover, acute administration of indomethacin elevated leukotriene B4 levels in gastric mucosa, which was reversed by pretreatment with licofelone The results suggest that licofelone offered gastroprotection against NSAIDs-induced gastropathy through its effect on leukotrienes and by inhibiting extravasation of neutrophils.


Subject(s)
Acetates/pharmacology , Animals , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Anti-Ulcer Agents/pharmacology , Female , Humans , Indomethacin/adverse effects , Inflammation/drug therapy , Leukotriene B4/metabolism , Lipid Peroxidation , Male , Mesentery/metabolism , Mice , Neutrophils/drug effects , Pyrroles/pharmacology , Rats , Stomach Ulcer/chemically induced , Time Factors
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