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Peptic ulcers (PU) are a breach in the mucosa of the digestive tract and are related to several factors including an altered immune system and an unbalanced diet. Current treatment carries to long-term complications; therefore, the use of medicinal plants is an alternative for several inflammatory diseases including ulcerative lesions. Kalanchoë gastonis-bonnieri, is a succulent plant and, has been used in traditional medicine against gastric ulcers, inflammation, and cancer among others. The main goal of this work was to analyze the anti-ulcerogenic potential of extracts from leaves of K. gastonis-bonnieri in an assay of ethanol-induced gastric ulcers. An ethanolic extract was obtained by maceration from fresh leaves of K. gastonis-bonnieri, and fractions were obtained through bipartition and chemical fractioning. The chemical characterization of the extract was made through HPLC, GC-MS, and NMR. Total extract and fractions showed an anti-ulcerogenic effect in specimens of male ICR mice with a gastric ulcer index (UI) of 3.27-5.47. The recorded effect is attributed to the presence of terpenoid compounds such as ß-Amyrin acetate, which showed antioxidant properties and lessened formations of ulcers induced by ethanol administration in mice stomach.
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Introduction: Essential oilâbased nanoemulsions (NEs) are the subjects of extensive investigation due to their potential to address a variety of oral health issues. NEs are delivery systems that improve lipid medicine solubility and distribution to intended sites. The goal of the current study was to create and enhance a self-nanoemulsifying drug delivery paradigm based on calendula oil (CO) and decorated with chitosan (CS) that could deliver posaconazole (PSZ) for the treatment of gingivitis. Method: Employing a response-surface BoxâBehnken design, PSZ-CO-CS NEs were created with varying amounts of PSZ (10, 15, and 20 mg), percentages of CO (6%, 12%, and 18%), and percentages of CS (0.5%, 1.5%, and 2.5%). Results and conclusion: The optimized formulation resulted in a 22-mm bacterial growth suppression zone, 25-mm fungal growth inhibition zone, droplet sizes of 110 nm, and a viscosity of 750 centipoise (cP). Using the appropriate design, the ideal formulation was produced; it contained 20 mg of PSZ, 18% of CO, and 1.35% of CS. Furthermore, the optimal formulation had a more controlled drug release, larger inhibition zones of bacterial and fungal growth, and desirable rheologic properties. Additionally, the optimized formulation substantially lowered the ulcer index in rats when tested against other formulations. Thus, this investigation showed that PSZ-CO-CS NEs could provide efficient protection against microbially induced gingivitis.
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Abstract This study aimed to determine the antiulcerogenic and antioxidant activities of Psyllium (Plantago ovata Forssk) seed ethanolic extract in rats. We assessed the antioxidant potential using free radical scavenging on DPPH, -carotene bleaching activity, ferric reducing power, and hydroxyl radical scavenging activity. In the antiulcerogenic study, pre-treatment with Plantago ovata seeds ethanolic extract (POE) (400 mg/kg b.wt) significantly protected against ethanol-induced gastric ulcer in rats by decreasing the ulcer index value and preserving the integrity of the gastric mucosa. The oxidative stress status in the stomach tissues showed a significant increase in the antioxidant enzyme levels of superoxide dismutase, catalase, and glutathione peroxidase with a significant decrease in lipid peroxidation during pre-treatment with POE. In conclusion, the POE protects against gastric ulcer due to its antioxidant potential and presence of bioactive molecules.
Resumo O presente estudo teve como objetivo determinar as atividades antiulcerogênica e antioxidante das sementes de Psyllium (Plantago ovata Forssk) em ratos. O potencial antioxidante foi avaliado utilizando o método do sequestro do radical livre DPPH, autooxidação do -caroteno, poder redutor de ferro e atividade de sequestro do radical hidroxila. No estudo antiulcerogênico, o pré-tratamento com o extrato etanólico das sementes de Plantago ovata (POE) (400 mg/Kg b.wt) reduziu a úlcera gástrica induzida pelo etanol em ratos, diminuindo o valor do índice de úlcera e preservando a integridade da mucosa gástrica. O estudo do estresse oxidativo nos tecidos estomacais mostrou um aumento significativo dos níveis das enzimas antioxidantes superóxido dismutase, catalase e glutationa peroxidase, com uma diminuição significativa da peroxidação lipídica enquanto pré-tratamento com POE. Em conclusão, o POE protege contra úlcera gástrica devido aos seus potenciais antioxidantes e à presença de moléculas bioativas.
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This study aimed to determine the antiulcerogenic and antioxidant activities of Psyllium (Plantago ovata Forssk) seed ethanolic extract in rats. We assessed the antioxidant potential using free radical scavenging on DPPH, ß-carotene bleaching activity, ferric reducing power, and hydroxyl radical scavenging activity. In the antiulcerogenic study, pre-treatment with Plantago ovata seeds ethanolic extract (POE) (400 mg/kg b.wt) significantly protected against ethanol-induced gastric ulcer in rats by decreasing the ulcer index value and preserving the integrity of the gastric mucosa. The oxidative stress status in the stomach tissues showed a significant increase in the antioxidant enzyme levels of superoxide dismutase, catalase, and glutathione peroxidase with a significant decrease in lipid peroxidation during pre-treatment with POE. In conclusion, the POE protects against gastric ulcer due to its antioxidant potential and presence of bioactive molecules.
O presente estudo teve como objetivo determinar as atividades antiulcerogênica e antioxidante das sementes de Psyllium (Plantago ovata Forssk) em ratos. O potencial antioxidante foi avaliado utilizando o método do sequestro do radical livre DPPH, autooxidação do ß-caroteno, poder redutor de ferro e atividade de sequestro do radical hidroxila. No estudo antiulcerogênico, o pré-tratamento com o extrato etanólico das sementes de Plantago ovata (POE) (400 mg/Kg b.wt) reduziu a úlcera gástrica induzida pelo etanol em ratos, diminuindo o valor do índice de úlcera e preservando a integridade da mucosa gástrica. O estudo do estresse oxidativo nos tecidos estomacais mostrou um aumento significativo dos níveis das enzimas antioxidantes superóxido dismutase, catalase e glutationa peroxidase, com uma diminuição significativa da peroxidação lipídica enquanto pré-tratamento com POE. Em conclusão, o POE protege contra úlcera gástrica devido aos seus potenciais antioxidantes e à presença de moléculas bioativas.
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Ratos , Plantago , Úlcera Gástrica , Mucosa Gástrica , Fitoterapia , AntioxidantesRESUMO
The objective of this study was to assess the anti-inflammatory effects of ribes rubrum oil at three different doses (5, 10 and 15 ml/kg b.w/day) in adult male albino rats with indomethacin-induced stomach ulcers (IND). Forty rats (135 ± 5 g) categorized into 5 groups (n = 8), for 45 days. Group (1) normal control, thirty-two rats were gavaged IND as single oral dose (30 mg/Kg b.w) resulted in gastric ulcer, then distributed to four groups, group (2) IND-intoxicated control, Groups 3, 4 and 5 were administrated ribes rubrum oil at levels of (5, 10 & 15 ml/kg b.w) respectively. Administrated levels of ribes rubrum oil found to have remarkable elevation in food conversion efficiency in experimental rats, gastric juice pH, in compared to the drunken control group, gastric prostaglandin E2 and gastric cytochrome P450 reductase levels were lower. The levels of pro-inflammatory cytokines NO, TNF-, and IL-1 were dramatically reduced, which was related with an increase in blood hemoglobin (Hb), packed cell volume (PCV), and red blood cells (RBCs)in ulcerogenic rats compared to intoxicated control. Data showed that, the main components of ribes rubrum oil are ß-Pinene, γ-linolenic and Linalool oxide levels (25.9%, 23.10% and 10.5%, respectively) for their antioxidant activity. Findings showed that administrate ribes rubrum oil at dose 15 ml/kg followed by 10 ml/kg had the best results against ulcerogenic rats. In conclusion, the outcomes are consistent with the concept that ribes rubrum oil had a gastroprotective and antisecretory effects against gastric ulcer that may be attributed to the antioxidant properties of the oil that ameliorates the damage occur in gastric of rats.
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Candida albicans is the fungus responsible for oral candidiasis, a prevalent disease. The development of antifungal-based delivery systems has always been a major challenge for researchers. This study was designed to develop a nanostructured lipid carrier (NLC) of sesame oil (SO) loaded with miconazole (MZ) that could overcome the solubility problems of MZ and enhance its antifungal activity against oral candidiasis. In the formulation of this study, SO was used as a component of a liquid lipid that showed an improved antifungal effect of MZ. An optimized MZ-loaded NLC of SO (MZ-SO NLC) was used, based on a central composite design-based experimental design; the particle size, dissolution efficiency, and inhibition zone against oral candidiasis were chosen as dependent variables. A software analysis provided an optimized MZ-SO NLC with a particle size of 92 nm, dissolution efficiency of 88%, and inhibition zone of 29 mm. Concurrently, the ex vivo permeation rate of the sheep buccal mucosa was shown to be significantly (p < .05) higher for MZ-SO NLC (1472 µg/cm2) as compared with a marketed MZ formulation (1215 µg/cm2) and an aqueous MZ suspension (470 µg/cm2). Additionally, an in vivo efficacy study in terms of the ulcer index against C. albicans found a superior result for the optimized MZ-SO NLC (0.5 ± 0.50) in a treated group of animals. Hence, it can be concluded that MZ, through an optimized NLC of SO, can treat candidiasis effectively by inhibiting the growth of C. albicans.
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Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Candidíase Bucal/tratamento farmacológico , Miconazol/farmacologia , Sistemas de Liberação de Fármacos por Nanopartículas/química , Óleo de Gergelim/química , Animais , Antifúngicos/administração & dosagem , Antifúngicos/farmacocinética , Química Farmacêutica , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Lipídeos/química , Masculino , Miconazol/administração & dosagem , Miconazol/farmacocinética , Mucosa Bucal , Tamanho da Partícula , Distribuição Aleatória , Ratos , Ovinos , Solubilidade , Propriedades de SuperfícieRESUMO
INTRODUCTION: Natural oil-based nanoemulsions (NEs) have been widely investigated in many diseases that affect the oral cavity. NEs are delivery systems that enhance the solubility of lipid therapeutics and improve their delivery to target sites; they are known as self-nanoemulsifying drug delivery systems (SNEDDSs). The current investigation's aim was to produce an oregano essential oil-based nanoemulsion (OEO-SNEDD) that would have antibacterial and antifungal effects against oral microbiota and improve oral health. METHODS: Several OEO-SNEDDSs were developed using different percentages of OEO (10%, 14%, and 18%), percentages of a surfactant mixture Pluracare L64:Lauroglycol FCC (18%, 32%, and 36%), Smix ratios (1:2, 1:1, and 2:1), and hydrophilic-lipophilic balances (HLBs) of the surfactant mixture (8, 10, and 12) using the BoxâBehnken design. The optimized concentration of excipients was determined using a pseudoternary phase diagram to obtain the NEs. The formulations were evaluated for their droplet size, stability index, and antibacterial and antifungal activities. RESULTS: The NEs had a droplet size of 150 to 500 nm and stability index of 47% to 95%, and the produced formulation reached antibacterial and antifungal inhibition zones of up to 19 and 17 mm, respectively. The BoxâBehnken design was adopted to get the optimum formulation, which was 18% OEO, 36% Smix, 10.29 HLB of Smix, and a 1.25:1 Smix ratio. The optimized formulation had a lower ulcer index compared with various other formulations evaluated in rats. CONCLUSION: This study illustrated that OEO-SNEDDSs can provide good protection against oral microbial infections.
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Microbiota , Origanum , Animais , Sistemas de Liberação de Medicamentos , Emulsões , Ratos , TensoativosRESUMO
Madhuca longifolia, a tropical tree used as medicine and food, is known to have a beneficial effect against stomach gastric toxicity. Madhuca longifolia is used in treating cough, skin disease and nerve disorders. Diclofenac, a non-steroidal anti-inflammatory drug (NSAID), with overdosage and prolonged use, is known to cause gastric toxicity. Silymarin (SLY), a polyphenolic antioxidant flavonoid, is a derivative of Silybum marianum extracted from milk thistle seeds and fruits, has been widely used in the treatment of gastric ulcer. SLY was used as the standard drug to compare the effects with the Madhuca longifolia aqueous leaf extract treatment. The aim of the current study is to understand the effect of Madhuca longifolia aq. leaf extract on rat stomach and intestine against diclofenac-administered toxicity. Rats (n = 30) were divided into Group I normal control, Group II treated with diclofenac, Group III treated with diclofenac and Madhuca longifolia leaf extract, Group IV treated with diclofenac and silymarin, and Group V was treated with Madhuca longifolia leaf extract alone. After the study duration, rats were euthanized and tissue samples were analyzed for antioxidant, cytokine, protein expression levels and histopathological changes. Diclofenac treated rats had significant (p < 0.05) changes in levels of antioxidants, cytokines, protein expression and pathological changes as compared to rats treated with Madhuca longifolia. This study demonstrated that Madhuca longifolia leaf extract had gastroprotective activity in rats treated with diclofenac.
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Diclofenaco , Intestinos/efeitos dos fármacos , Madhuca , Extratos Vegetais , Estômago/efeitos dos fármacos , Animais , Antioxidantes/metabolismo , Citocinas/metabolismo , Diclofenaco/toxicidade , Madhuca/química , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Silimarina/farmacologiaRESUMO
Candidiasis is one of the frequently encountered opportunistic infections in the oral cavity and can be found in acute and chronic presentations. The study aimed to develop fluconazole-loaded sesame oil containing nanotransfersomes (FS-NTF) by the thin-layer evaporation technique to improve the local treatment of oral candidiasis. Optimization of the formulation was performed using the BoxâBehnken statistical design to determine the variable parameters that influence the vesicle size, entrapment efficiency, zone of inhibition, and ulcer index. Finally, the formulated FS-NTF was embedded within the hyaluronic acidâbased hydrogel (HA-FS-NTF). The rheological behavior of the optimized HA-FS-NTF was assessed and the thixotropic behavior with the pseudoplastic flow was recorded; this is desirable for an oral application. An in vitro release study revealed the rapid release of fluconazole from the HA-FS-NTF. This was significantly higher when compared with the fluconazole suspension and hyaluronic acid hydrogel containing fluconazole. Correspondingly, the ex vivo permeation was also found to be higher in HA-FS-NTF in sheep buccal mucosa (400 µg/cm2) when compared with the fluconazole suspension (122 µg/cm2) and hyaluronic acid hydrogel (294 µg/cm2). The optimized formulation had an inhibition zone of 14.33 ± 0.76 mm and enhanced antifungal efficacy for the ulcer index (0.67 ± 0.29) in immunocompromised animals with Candida infection; these findings were superior to those of other tested formulations. Hence, it can be summarized that fluconazole can effectively be delivered for the treatment of oral candidiasis when it is entrapped in a nanotransfersome carrier and embedded into cross-linked hyaluronic acid hydrogel.
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Gastric ulcer (GU) is the most common health concern that occurs due to alcohol consumption, smoking and physiological stress. Ethanol-induced GU in animal model resembles the pathophysiology of human ulcer. The present study was designed to investigate the cytoprotective and anti-inflammatory properties of tert-butylhydroquinone (tBHQ), a nuclear factor erythroid 2-related factor 2 (Nrf2) activator, against gastric mucosal damage induced by acute exposure of ethanol (5 ml/kg). The intervention of tBHQ (25 and 50 mg/kg, per os (po)) and omeprazole (20 mg/kg, po) was done for 10 consecutive days. Omeprazole was chosen as a standard drug because it is prescribed for the treatment of GU. Pretreatment of tBHQ decreased gastric mucosal lesion, ulcer index, apoptotic cells and lipid peroxidation level induced by ethanol. Furthermore, the intervention of tBHQ increased gastric mucosa integrity, pH, reduced glutathione, collagen and mucus-producing goblet cells. Intervention of tBHQ increased the expression of antioxidant markers such as Nrf2, haeme oxygenase-1 and catalase and decreased the expressions of inflammatory markers such as nuclear factor kappa-light-chain-enhancer of activated B cells and cyclooxygenase-2. The cytoprotective potential of tBHQ against gastric mucosal damage might be due to its ability to enhance cellular antioxidants and anti-inflammatory responses.
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Antioxidantes/farmacologia , Etanol/toxicidade , Heme Oxigenase (Desciclizante)/metabolismo , Hidroquinonas/farmacologia , Fator 2 Relacionado a NF-E2/metabolismo , Úlcera Gástrica/prevenção & controle , Animais , Modelos Animais de Doenças , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Masculino , Ratos Sprague-Dawley , Transdução de Sinais , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/metabolismoRESUMO
BACKGROUND: Gastric ulcer (GU) is a common gastrointestinal disease that can be induced by many factors. Finding an effective treatment method that contains fewer side effects is important. 20 (S)-ginsenoside Rg3 is a kind of protopanaxadiol and has shown superior antiinflammatory and antioxidant effects in many studies, especially cancer studies. In this study, we examined the treatment efficacy of 20 (S)-ginsenoside Rg3 on GU. METHODS: Three kinds of GU models, including an alcohol GU model, a pylorus-ligated GU model, and an acetic acid GU model, were used. Mouse endothelin-1 (ET-1) and nitric oxide (NO) levels in blood and epidermal growth factor (EGF), superoxide dismutase, and NO levels in gastric mucosa were evaluated. Hematoxylin and eosin staining of gastric mucosa and immunohistochemical staining of ET-1, inducible nitric oxide synthase (NOS2), and epidermal growth factor receptors were studied. Ulcer index (UI) scores and UI ratios were also analyzed to demonstrate the GU conditions in different groups. Furthermore, Glide XP from Schrödinger was used for molecular docking to clarify the interactions between 20 (S)-ginsenoside Rg3 and EGF and NOS2. RESULTS: 20 (S)-ginsenoside Rg3 significantly decreased the UI scores and UI ratios in all the three GU models, and it demonstrated antiulcer effects by decreasing the ET-1 and NOS2 levels and increasing the NO, superoxide dismutase, EGF, and epidermal growth factor receptor levels. In addition, high-dose 20 (S)-ginsenoside Rg3 showed satisfactory gastric mucosa protection effects. CONCLUSION: 20 (S)-ginsenoside Rg3 can inhibit the formation of GU and may be a potential therapeutic agent for GU.
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Loranthus acaciae (Loranthaceae) is a perennial green semi-parasitic plant used in ethnopharmacological medicine for healing wounds. The protective effect of L. acaciae on gastric ulcer induced by ethanol was investigated in a rat model. Ulcer index and total glutathione level were measured and histological and immunohistochemical studies for the expression of cyclooxygenase-2 were performed. Furthermore, chemical constituents of the flower extract were analyzed. Ulcer index was significantly lowered in L. acaciae-treated groups. Protection ratios were 75.9%, 98.9%, and 70.7% for 250 mg/kg and 500 mg/kg of L. acaciae and 40 mg/kg of esomeprazole, respectively. Histological examination revealed fewer hemorrhage in mucosa and less edema in submucosa of L. acaciae-treated groups compared with control. In the esomeprazole-treated group, there was mild disruption in the surface epithelium and mild hemorrhage. However, edema and leucocytes infiltration in the submucosa layer were present. Immunohistochemical staining of stomach sections for cyclooxygenase-2 (COX-2) was negative in the control group as well as in the L. acaciae-treated groups. Total glutathione level in mucosa layer of the stomach was higher in L. acaciae-treated groups compared with control. Liquid chromatography-mass spectrometric analysis revealed the presence of loranthin and rutin as the major constituents. It can be concluded that L. acaciae imparted a gastroprotective action against ethanol-induced ulcer in rats. Novelty 500 mg/kg L. acaciae protected the stomach by 98.9% from ulcerogenic effect of ethanol. L. acaciae increased total glutathione level but not COX-2 expression in gastric mucosa. Loranthin and rutin were the major constituents in L. acaciae flower extract.
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Loranthaceae/química , Extratos Vegetais/farmacologia , Úlcera Gástrica/tratamento farmacológico , Animais , Ciclo-Oxigenase 2/metabolismo , Esomeprazol/farmacologia , Etanol/efeitos adversos , Feminino , Flores/química , Mucosa Gástrica/efeitos dos fármacos , Glutationa/análise , Ratos , Ratos Wistar , Rutina , Úlcera Gástrica/induzido quimicamenteRESUMO
Peptic ulcer is a recurrent chronic illness and has become almost a hallmark of the so-called civilized life. In folk medicine, the Celastrus paniculatus plant has been used for the prevention and treatment of various diseases and gastrointestinal disturbances, including dyspepsia and stomach ulcers. The aim of this study is to evaluate the gastroprotective and antiulcer effects of Celastrus paniculatus seed oil (CPO) against several gastric ulcer models in rats. The gastroprotective and antiulcer effects of CPO were evaluated using pylorus-ligated ulcer ethanol- and indomethacin-induced ulcers using rantidine (40 mg/kg per os [PO]) as standard. Gastrointestinal motility was determined by gastric emptying time and gastrointestinal transit ratio. The results of the pharmacological studies of CPO (200 mg/kg, 400 mg/kg) demonstrated effective gastroprotection against ethanol- and indomethacin-induced ulcer models. In pylorus-ligated rats, the seed oil showed gastroprotective activity by decreasing total gastric juice volume and gastric acidity while increasing the gastric pH. The gastroprotection against ethanol and indomethacin is partially attributed to effective inhibition of proinflammatory cytokines, TNF-α and IL-6, and increase in the levels of IL-10. Treatment with CPO in ethanol-induced ulcer rats significantly (p < .05) decreased MDA (malondialdehyde) levels, which were accompanied by an increase in the activities of SOD (superoxide dismutase) and catalase. CPO reduced the rate of gastric emptying but had no effect on gastrointestinal transit. The present findings indicate that CPO has potent gastroprotective effects and support the folkloric usage of the seed oil to treat various gastrointestinal disturbances.
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Celastrus/química , Modelos Animais de Doenças , Óleos de Plantas/administração & dosagem , Úlcera Gástrica/prevenção & controle , Animais , Etanol/administração & dosagem , Feminino , Determinação da Acidez Gástrica , Esvaziamento Gástrico/efeitos dos fármacos , Suco Gástrico/química , Motilidade Gastrointestinal/efeitos dos fármacos , Trânsito Gastrointestinal/efeitos dos fármacos , Concentração de Íons de Hidrogênio , Indometacina/administração & dosagem , Interleucina-10/sangue , Interleucina-6/antagonistas & inibidores , Interleucina-6/sangue , Masculino , Medicina Tradicional , Fitoterapia , Piloro/cirurgia , Ratos , Ratos Wistar , Úlcera Gástrica/etiologia , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Fator de Necrose Tumoral alfa/sangueRESUMO
Aronia melanocarpa (Michx.) Ell. belongs to the Rosaceae family. The purpose of this study is to explore the gastroprotective effect of the Aronia melanocarpa hydro-alcoholic extract (AMHAE) against ethanol-induced gastric ulcer in a rat model. Different concentrations (50, 100, and 200 mg/kg) of AMHAE, or 30 mg/kg of omeprazole, significantly inhibited the gastric injury formation. The ethanol-induced ulcer group showed significant increases of malondialdehyde (MDA), myeloperoxidase (MPO), tumor necrosis factor (TNF)-α, nuclear factor-kappaB p65 (NF-κB p65), and monocyte chemoattractant protein (MCP)-1, and decreased activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-px), and interleukin (IL)-4. However, AMHAE (200 mg/kg) pretreatment significantly reversed the altered pathophysiological levels of these biomolecules to near normal stages. The gastroprotective activity of AMHAE was abolished by pretreatment with l-NAME, naloxone, capsazepine, and indomethacin, demonstrating the participation of nitric oxide (NO), opioids, TRPV (vanilloid receptor-related transient receptor potential), and prostaglandins in AMHAE-assisted gastroprotection against ethanol-induced gastric injuries. This gastroprotective effect of AMHAE might be due to the downregulation of TNF-α-based NF-κB, MCP-1 signaling and strong antioxidant properties.
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Quimiocina CCL2/metabolismo , Etanol/efeitos adversos , Proteínas de Choque Térmico HSP70/metabolismo , NF-kappa B/metabolismo , Photinia/química , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/metabolismo , Animais , Antiulcerosos/química , Antiulcerosos/farmacologia , Cromatografia Líquida de Alta Pressão , Modelos Animais de Doenças , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Masculino , Compostos Fitoquímicos/química , Extratos Vegetais/química , Substâncias Protetoras/farmacologia , Ratos , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/patologiaRESUMO
BACKGROUND: Ulcer can be developed inside the inner lining of the stomach (gastric ulcer) or the small intestine (duodenal ulcer). Both the ulcers are also cumulatively referred as peptic ulcers. It affects nearly 10% of world population. AIM: To investigate the antiulcer activity of ethanolic extract of Salvadora indica W. leaves (ESIL) on albino rats. MATERIALS AND METHODS: The present study was carried by pylorus ligation, ethanol and cysteamine induced ulcer models in albino rats. The antiulcer activity of ESIL (150, 300 and 600 mg/kg p.o. for 7 days) was compared with standard drugs (Ranitidine). In pyloric ligation induced ulcer model, the studied parameters were gastric volume, pH, total acidity, free acidity, and ulcer index whereas in ethanol and cysteamine induced ulcer model, the ulcer index was determined for severity of ulcers. The parameters studied were ulcer index, gastric juice volume, pH, free acidity and total acidity. RESULTS: In pyloric ligation model; the volume of gastric content, total/free acidity and pepsin activity was significantly decreased at p<0.05 and p<0.01 and pH of the gastric juice was significantly increased at p<0.05 and p<0.01 in ESIL treated groups as compared to control group. All the doses of ESIL showed dose dependent antiulcer effect as well as significant (p<0.05 and p<0.01) reduction in the ulcer index as compared to control group in all the experimental models. CONCLUSION: The results of the study indicate that the ESIL have better potential against ulcer which supports the traditional claims in folklore medicine.
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BACKGROUND: The search for an ideal and new antiulcer drug has been extended to herbals for novel molecules that decrease the incidence of relapse and afford better protection. OBJECTIVE: The present study was designed to investigate the protective effect of hydro-alcoholic extract of Ruta graveolens (RGE) Linn. leaves on indomethacin (IND) and pylorus ligation-induced gastric ulcer in Wistar rats. MATERIALS AND METHODS: The rats of all the six groups were deprived of food for 24 h. Then, the first group received 1 ml/kg/day p.o. of 1% carboxymethylcellulose calcium (CMC), second group 1 ml/kg/day p.o. of 1% CMC and third group 20 mg/kg/day p.o. of IND. Fourth and fifth groups received RGE 200 and 400 mg/kg/day p.o., respectively; while the sixth group 10 mg/kg/day p.o. omeprazole. After 30 min, last three groups received 20 mg/kg/day p.o. of IND also. All these treatments after food deprivation were repeated each day for 5 consecutive days. Pylorus ligation was performed on 6th day in last five groups. After 4 h, stomach by sacrifice of the rats was examined for ulcer index (UI) and gastric mucus. Gastric juice was assessed for acidity, pH and pepsin; while gastric tissues were assessed for thiobarbituric acid reactive substance (TBARS) and glutathione (GSH). RESULTS: Fifth group showed significant decrease in UI (10.33 ± 0.67), TBARS (0.33 ± 0.03 mmol/mg), free acidity (48.78 ± 5.12 meq/l/100 g), total acidity (99.33 ± 9.31 meq/l/100 g), and pepsin activity (8.47 ± 0.41 µg/ml) levels while it showed significant increase in mucus (412.4 ± 21.6 µg/g), GSH (57.9 ± 4.8 mmol/mg) and pH (3.32 ± 0.27) compared to third group. Percent protection in RGE 400 mg was found to be 63.32 compared to indomethacin. CONCLUSION: RGE possesses antiulcerogenic activity as it exhibits protective effect on gastric ulcer in rats.
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CONTEXT: The water extract of Boswellia sacra Flueck. (Burseraceae) is used in the treatment of gastric and hepatic disorders in the Arab countries. OBJECTIVE: The effect of Boswellia sacra water extract on gastric secretion and experimentally induced gastric ulcers in rats was studied. MATERIALS AND METHODS: Acetic acid-induced chronic gastric ulcers, pylorus ligation, aspirin-induced, ethanol-induced, and restraint plus cold stress-induced gastric ulcer models were employed. The effect on normal rats was also studied. The water extract of B. sacra was administered orally at doses of 2 and 5 ml/kg once daily ranging from single dose to 30 d treatment depending on the model. The extract was subjected to GC-MS analysis to determine the presence of various phytoconstituents. RESULTS: Boswellia sacra water extract (5 ml/kg, p.o (per os)) aggravated acetic acid-induced chronic ulcers, wherein an increase in ulcer index (p < 0.01) and ulcer score (p < 0.05) was observed. In pylorus-ligated rats, the extract increased gastric content volume (p < 0.01), free acidity (p < 0.01), total acidity (p < 0.01), ulcer index (p < 0.01), and pepsin activity (p < 0.05). There was no significant effect on the development of ethanol-induced and aspirin-induced ulcers while an increase in the development of stress-induced ulcers was observed (p < 0.01). The extract did not produce any ulcers when administered to normal rats. The dose of 2 ml/kg was less proulcerogenic compared with 5 ml/kg. The GC-MS analysis revealed the presence of several phytoconstituents that included menthol, 3-cyclohexen-1-ol, and octanoic acid. CONCLUSION: Boswellia sacra water extract has proulcerogenic activity due to its gastric hypersecretory effect.
Assuntos
Boswellia/química , Ácido Gástrico/metabolismo , Mucosa Gástrica/efeitos dos fármacos , Extratos Vegetais/efeitos adversos , Gomas Vegetais/química , Úlcera Gástrica/induzido quimicamente , Animais , Modelos Animais de Doenças , Feminino , Mucosa Gástrica/metabolismo , Masculino , Extratos Vegetais/isolamento & purificação , Ratos Wistar , Úlcera Gástrica/metabolismo , Água/químicaRESUMO
AIM: Lycopene, a carotenoid and hesperidin, a flavonoid are naturally occurring in vegetables and fruits. Synergistic effect of a combination of carotenoid and flavonoid has been reported due to its antioxidant activity. Therefore, the present study was aimed to evaluate the protective effect of this combination on pylorus ligation induced ulcers in rats. MATERIALS AND METHODS: Thirty Wistar albino rats were divided into five groups (n = 6). Rats were fasted for 24 h before pylorus ligation. After 24 h of fasting the rats were treated with hesperidin (100 mg/kg) and lycopene (2 mg/kg) and their combination 1h prior to surgery. After an hour under ether anesthesia pylorus ligation was performed, after 5 h the animals were sacrificed, stomach was dissected, and gastric contents were collected and measured. Total acidity and pH of gastric content was estimated. Ulcer index was calculated, and macroscopic examination of the stomach was carried out. RESULTS: The sham operated rats showed a significant increase in pH, volume of gastric content and total acidity and ulcer index. The rats pretreated with lycopene and hesperidin showed significant improvement in the ulcer conditions. However, rats treated with a combination of lycopene and hesperidin showed more significant restoration of gastric function as compared to sham operated rats. Moreover, a significant difference was also noted in rats treated with a combination as compared to lycopene and hesperidin treatment alone. CONCLUSION: Thus experimentally the combination was seen to treat ulcers by anti-secretory, neutralizing, cytoprotective and mainly due to its antioxidant property.
RESUMO
OBJECTIVE: This study was aimed to investigate the beneficial effects of quercetin (QCT) against trinitrobenzene sulfonic acid (TNBS) induced clinical, morphological, and biochemical alterations in rats. MATERIALS AND METHODS: Colitis in rats was induced by administration of TNBS (25 mg dissolved in 0.25 ml of 30% ethanol) 8 cm into the rectum of the rat using a catheter. The animals were divided into six experimental groups (n = 6); naive (saline only without TNBS administration), control (saline + TNBS), standard (sulfasalazine 25 mg/kg + TNBS), QCT (25) (QCT 25 mg/kg + TNBS), QCT (50) (QCT 50 mg/kg + TNBS), QCT (100) (QCT 100 mg/kg + TNBS). Sulfasalazine (25 mg/kg) and QCT (25, 50 and 100 mg/kg) were administered per oral for 11 days and the colonic damage was evaluated in terms of macroscopical (body weight, stool consistency, rectal bleeding, and ulcer index) and biochemical parameters (myeloperoxidase activity, lipid peroxidation, nitrite, and glutathione). RESULTS: Treatment with QCT (50, 100 mg/kg) for 10 days following TNBS administration significantly attenuated the clinical, morphological, and biochemical alterations induced by TNBS, whereas it was found to be not effective at its lower dose (25 mg/kg) throughout the experimental protocol. CONCLUSION: QCT attenuates the clinical, morphological and biochemical alterations induced by TNBS possibly via its antioxidant mechanism.