RESUMEN
Epoxiconazole is a worldwide fungicide used to control fungal diseases. Although to its hazardous effects in non-target species, little information is available in the literature to show the cardiotoxic effects of EPX in male rats. Thus, our investigation aimed to assess the outcomes of EPX exposure on some biochemical parameters, the generation of oxidative stress, DNA fragmentation and histopathological alterations in the heart tissue. EPX was administered orally at doses of 8, 24, 40 and 56 mg/kg body weight, representing, respectively NOEL (No observed effect level), NOEL× 3, NOEL× 5 and NOEL× 7 for 28 consecutive days in male Wistar rats. Our results show that EPX induced a significant decrease of cardiac acetylcholinesterase, an increase of biochemical markers, such as creatinine phosphokinase (CPK) and a perturbation of the lipid profile. Furthermore, EPX caused diverse histological modifications in the myocardium, including congestion of cardiac blood vessels, cytoplasmic vacuolization, leucocytic infiltration and hemorrhage. Indeed, we have shown that EPX induces increase of lipid peroxidation, protein oxidation levels and DNA damage. On the other hand, we have found an increase of the antioxidant enzymes activity such as catalase (CAT) and superoxide dismutase (SOD) activities. The glutathione peroxidase and glutathione S tranferase initially enhanced at the doses of 8, 24, and 40 mg/kg b.w. and then decreased at the dose of 56 mg/kg b.w. In conclusion, our work has shown that EPX causes cardiotoxic effects by altering redox status and damaging heart tissue.
Asunto(s)
Compuestos Epoxi/toxicidad , Lesiones Cardíacas , Triazoles/toxicidad , Acetilcolinesterasa/metabolismo , Animales , Antioxidantes/metabolismo , Catalasa/metabolismo , Glutatión/metabolismo , Lesiones Cardíacas/inducido químicamente , Peroxidación de Lípido , Estrés Oxidativo , Ratas , Ratas Wistar , Superóxido Dismutasa/metabolismoRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: The Cleomaceae family is known for its richness in secondary metabolites and different Cleome species are used in folk medicine. Cleome amblyocarpa and Cleome arabica are medicinal herbs used in Tunisia and other North Africa countries to treat various diseases such as diabetes, rheumatism, colic, pain and digestive disorders. AIM OF THE STUDY: To our knowledge, few data are available about the nutritional value, phytochemical components and biological effects of C. arabica and C. amblyocarpa cultivated in Tunisia. For this reason, the present survey aimed to determine the nutritional value, bioactive compounds and pharmacological properties of the leaves of these two species of Cleome. MATERIALS AND METHODS: To characterize and determine the bioactive compounds in both extracts of leaves of Cleome species, ultra-performance liquid chromatography-mass spectrometry (UPLC-MS) was used. The various nutritional parameters were analyzed, in particular the amounts of protein, carbohydrates, ash, fiber, and total lipids. Vitamin E and fatty acid profiles were also evaluated by HPLC-DAD-FLD and GC-FID, respectively. The acute toxic effects of leaf extracts in mice at concentrations of 100, 500 and 800 mg/kg body weight have been investigated. The anti-inflammatory effect of leaves extracts was examined by means of the in vitro and in vivo models. The in vivo anti-inflammatory test was assessed by means of the carrageenan induced paw edema in rats. For the in vitro anti-inflammatory assay, the red blood cells membrane stabilization and protein denaturation methods were employed. The analgesic effect of hydroalcoholic extracts of leaves was also assessed by acetic acid induced writhing model in mice. RESULTS: The phytochemical composition and the nutritional values of the leaves of C. amblyocarpa and C. arabica were determined. Our results revealed that the leaves of C. amblyocarpa are rich in flavonoids and glucosinolates. On the other hand, these latter metabolites are not present in the C. arabica extract and the leaves are characterized by the presence of flavones, methoxyflavones and their glycosides. Our findings revealed that the leaves of the two species contain a potential quantity of vitamins; proteins, carbohydrates and dietary fiber, and their hydroalcoholic extracts indicated substantial anti-inflammatory and antinociceptive activities in all the tests. Additionally, the data from the acute toxicity test proved that the leaf extracts did not cause any mortality or signs of toxicity in animals at doses up to 800 mg/kg CONCLUSIONS: The results obtained in this investigation demonstrated that the leaves of C. arabica and C. amblyocarpa are a valuable source of nutrients and active substances. Our observations support the traditional utilize of these two Cleome species for the treatment of painful diseases and as a source of natural anti-inflammatory agents.
Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Cleome/química , Hiperalgesia/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Extractos Vegetales/farmacología , Ácido Acético/toxicidad , África del Norte , Analgésicos/química , Analgésicos/uso terapéutico , Animales , Antiinflamatorios/química , Antiinflamatorios/uso terapéutico , Conducta Animal/efectos de los fármacos , Carragenina/toxicidad , Cromatografía Liquida , Edema/inducido químicamente , Edema/tratamiento farmacológico , Membrana Eritrocítica/efectos de los fármacos , Ácidos Grasos/análisis , Femenino , Hiperalgesia/inducido químicamente , Inflamación/inducido químicamente , Masculino , Ratones , Valor Nutritivo , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Hojas de la Planta/química , Plantas Medicinales/química , Desnaturalización Proteica/efectos de los fármacos , Ratas Wistar , Espectrometría de Masa por Ionización de Electrospray , Espectrometría de Masas en Tándem , Vitamina E/análisisRESUMEN
Cleome amblyocarpa Barr. and Murb is a medicinal plant widespread in North Africa and widely used in Tunisia to treat diabetes and colic. The non-volatile (polyphenols, flavonoids, tannins, and flavonols) and volatile compounds (GC-MS) of C. amblyocarpa leaves and stems have been studied. The antioxidant, antimicrobial, analgesic, and cytotoxic activities of hydroalcoholic extracts of C. amblyocarpa leaves and stems were also investigated. The major volatile components were ß-caryophyllene (46.9%), eugenol (25.6%), ethyl 3-methylpentanoate (16.2%), 7-epi-silphiperfol-5-ene (11.0%), and α-copaene (7.0%). The antioxidant activity has been evaluated using various in vitro assays, such as DPPH free radical scavenging activity, iron-chelating capability, and ability to inhibit lipid peroxidation (TBARS). The antibacterial and antifungal effectiveness of leaves and stems parts of Cleome amblyocarpa were investigated by means of the disc diffusion and microdilution techniques. The in vitro cytotoxicity of the hydroalcoholic extract of C. amblyocarpa on A549 and H1299 lung adenocarcinoma cells was determined using the crystal violet assay. The acute toxicity of the extracts on Swiss albino mice at the doses of 3000, 1500, and 500 mg/kg body weight was evaluated. The analgesic effect of leaves and stems extract was also determined by means of the acetic acid induced writhing test. The results indicated that the leaves have higher phenols, and flavonoids contents and potential antioxidant, antimicrobial, and anticancer activities in comparison to stem. In addition, the aerial part of C. amblyocarpa did not cause signs of toxicity or death in animals at doses up to 3000 mg/kg and have a significant analgesic activity.
Asunto(s)
Cleome , Animales , Antioxidantes/análisis , Flavonoides , Cromatografía de Gases y Espectrometría de Masas , Ratones , Extractos Vegetales , Hojas de la Planta/química , TúnezRESUMEN
Ephedra alata, known as a medicinal plant in China, was used in this study as aqueous extract from aerial parts, for diabetes mellitus treatment. This study was carried out on two parts, in vitro, we tested the effect of the studied extract on the inhibition of α-glucosidase and α-amylase activities, and in vivo on Wistar male rats receiving alloxan intraperitoneally at a rate of 125 mg/kg. Extract (100, 200, and 300 mg/kg of body weight) was administrated for 28 days by oral gavage. Blood glucose, amylase, lipase, and lipid profile level were determined. Oxidative stress was evaluated by enzymatic activities of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx), and by estimation of lipid peroxidation and protein carbonyl (PC) level. Histopathological changes in pancreas were investigated under photonic microscopy using immunohistochemical procedure. Our findings showed that aqueous extract inhibited in vitro both α-glucosidase and α-amylase activities and its use in vivo at 300 mg/kg of body weight restored pancreas weight and weight gain, ameliorated significantly (p Ë 0.05) biochemical parameters; it prevented the increase in lipid and protein oxidation and the decrease in enzymatic and non-enzymatic defense system. Histological study of treated animals showed a comparable healed regeneration of beta cells.
Asunto(s)
Ephedra/química , Inhibidores de Glicósido Hidrolasas/toxicidad , Extractos Vegetales/toxicidad , alfa-Amilasas/metabolismo , Animales , Glucemia/análisis , Catalasa/metabolismo , China , Diabetes Mellitus Experimental , Glutatión Peroxidasa/metabolismo , Hipoglucemiantes , Peroxidación de Lípido/efectos de los fármacos , Masculino , Estrés Oxidativo/fisiología , Páncreas/efectos de los fármacos , Ratas , Ratas Wistar , Superóxido Dismutasa/metabolismo , Pruebas de ToxicidadRESUMEN
Diabetes is a serious condition that is linked to the development of oxidative stress causing among many other effects, kidney failure and pancreatic disorders. However, traditional plant-based remedies can be considered an alternative to diabetes healing. In this context, this study was oriented towards evaluating the protective effect of the flowers of Opuntia microdasys Lehm. collected in Tunisia at a biochemical and histological level on kidneys and pancreas of a type 2 diabetic rats. Renal and pancreatic toxicities were induced in diabetic male Wistar rats by fructose alloxan. Diabetic rats were treated with an extract obtained from flowers collected at post-flowering stage (OFP) (100 and 200 mg kg-1 bw) and metformin (100 mg kg-1 bw) for 28 days. Oral administration of OFP at 200 mg kg-1 bw showed significant reduction of the uric acid, urea, creatinine, amylase, lipase, and glycated hemoglobin (HbAlc). The levels of SOD, CAT, and GPx were increased, while protein carbonyls and lipid peroxidation TBARS levels were reduced in the kidney and pancreas. The altered kidney and pancreas histology were restored in rats treated with OFP. Thus, the present study demonstrated that OFP has antihyperglycemic activity in fructose-alloxan-induced diabetic rats.
Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/uso terapéutico , Riñón/efectos de los fármacos , Opuntia/química , Páncreas/efectos de los fármacos , Extractos Vegetales/uso terapéutico , Aloxano , Animales , Glucemia/análisis , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/patología , Flores/química , Fructosa , Hipoglucemiantes/aislamiento & purificación , Riñón/metabolismo , Riñón/patología , Peroxidación de Lípido/efectos de los fármacos , Masculino , Estrés Oxidativo/efectos de los fármacos , Páncreas/metabolismo , Páncreas/patología , Extractos Vegetales/aislamiento & purificación , Ratas Wistar , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismo , TúnezRESUMEN
Opuntia sp. has long been used as a folk medicine to treat hepatitis and diabetes in Sicile (Italy). To extract the polyphenols from the flower of Opuntia microdasys Lehm. at post flowring stage and evaluate the antidiabetic activity in vitro and in vivo. The hepatoprotective activity of Opuntia microdasys aqueous flowers extract at post flowering stage (OFP) has been tested for their antidiabetic activity. On fructose-alloxan induced diabete in rat model, evaluating the inhibitory effects of OFP on some carbohydrate metabolizing enzymes, pancreatic α-amylase and intestinal α-glucosidase activities in vitro. The OFP extract showed inhibitory activity against α-glucosidase (IC50=0.17±0.012mg/ml) and α-amylase (IC50=2.55±0.41mg/ml). The inhibitory potential of OFP extract on these enzymes suggests a positive and probable role of this extract in the management and treatment of diabetes mellitus, particularly, for type 2. Oral administration of the OFP at 200mg/kg to diabetic male rats for 28days demonstrated a significant protective effect by lowering the levels of glucose (123.21±1.38mg/dL) and hepatic marker enzymes (AST, ALT, LDH, γ-GT, BT, PAL, TC, LDL-C, HDL-C and TG). OFP attenuated oxidative stress by decreasing the SOD, CAT, GPX activity and the levels of PC and MDA in the liver and restored the histological architecture of the rat liver. OFP has protective effects on the protection of liver, thereby reducing some of the causes of diabetes in experimental animals.