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1.
Inflammopharmacology ; 27(5): 985-996, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-29222687

RESUMO

The gastroprotective potential of the methanolic extracts from peels (MEPe), seeds (MESe) and pulp (MEPu) of Chrysophyllum cainito L. (Sapotaceae) fruits was evaluated in mice using ethanol/HCl- and indomethacin-induced ulcer, as well as the antiulcer effect of the juice and flour from this fruit. The lowest oral gastroprotective dose of MEPe, MESe and MEPu against ethanol/HCl was 3, 3 and 10 mg/kg, respectively. Moreover, all extracts increased mucin secretion at 176, 198 and 193%. Intraperitoneal administration of MEPe (0.3 mg/kg), MESe (0.3 mg/kg) and MEPu (1 mg/kg) also promoted gastroprotection against ethanol/HCl. In addition, MEPe (3 mg/kg, p.o), MESe (3 mg/kg, p.o) and MEPu (10 mg/kg, p.o) reduced indomethacin-induced gastric ulcer in mice by 78, 70 and 50%, respectively. Regarding the mode of action, the gastroprotective effect of MEPe was decreased by the pre-administration of N-ethylmaleimide (NEM, a sulfhydryl group chelator, 10 mg/kg, i.p), glibenclamide (a potassium channel blocker, 10 mg/kg, i.p), yohimbine (10 mg/kg, i.p, an alpha-adrenergic receptor antagonist, 10 mg/kg, i.p) and indomethacin (a cyclooxygenase inhibitor, 10 mg/kg, i.p). The gastroprotective effect of MESe was reduced by the pre-administration of NEM, glibenclamide, N-Nitro-L-arginine methyl ester (L-NAME, a nitric oxide synthase inhibitor, 70 mg/kg, i.p) and yohimbine, while MEPu had the gastroprotective effect decreased in animals pretreated with NEM and L-NAME. However, the extracts did not reduce gastric acid secretion. The supplementation with the flour from C. cainito fruit at 10% by 7 days, but not the juice intake, displayed gastroprotective potential, evidencing the fruit as a promising functional food. Together, the antiulcer effect of extracts of the C. cainito fruit in different experimental models was confirmed by the favoring of mucosal protective mechanisms among different, but complementary, modes of action. In parallel, the gastroprotective effects of the flour from C. cainito fruit were also described.


Assuntos
Antiulcerosos/farmacologia , Frutas/química , Mucosa Gástrica/efeitos dos fármacos , Sapotaceae/química , Úlcera Gástrica/tratamento farmacológico , Animais , Modelos Animais de Doenças , Etanol/química , Feminino , Indometacina/farmacologia , Camundongos , NG-Nitroarginina Metil Éster/farmacologia , Fitoterapia/métodos , Extratos Vegetais/farmacologia , Folhas de Planta/química
2.
Nutr Health ; 23(4): 289-298, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29214921

RESUMO

BACKGROUND: The constant pursuit of improved athletic performance characterizes high-performance sport and the use of medicinal plants as dietary supplements is becoming widespread among athletes to enhance long-term endurance performance. AIM: The present study evaluated the toxicity of Heteropterys tomentosa (HEHt) and its acute adaptogenic effects. METHODS: The in vitro safety profile was evaluated on CHO-k1 cells using the alamar Blue assay, at concentrations ranging from 3.125 to 200 µg/mL. In vivo acute oral toxicity was conducted in male and female mice with oral administration of graded doses of HEHt from 400 to 2000 mg/kg. A subchronic oral toxicity study was completed by oral administration of HEHt (50, 200 or 1000 mg/kg) and vehicle for 30 days in male Wistar rats. Clinical observations and toxicological related parameters were determined. Blood was collected for biochemical and hematological analyses, while histological examinations were performed on selected organs. Thereafter, an adaptogenic test consisting of progressive loads until exhaustion was conducted in rats ( n = 5/group) orally pre-treated with the vehicle and HEHt (25, 100 or 400 mg/kg). RESULTS: HEHt exhibited no cytotoxic effects on the CHO-k1 cells and, apparently, no acute toxicity in mice and no subchronic toxicity in rats. An ergogenic effect was observed only at the dose of 25 mg/kg compared with the vehicle in relation to time to exhaustion and exercise load ( p = .011 and .019, respectively). HEHt is safe at up to 400 mg/kg, contains astilbin and taxifolin as the major phytochemical compounds, and exhibited a potential adaptogenic effect. CONCLUSIONS: These results justify its anecdotal usage as a tonic, show that the hydroethanolic maceration of the root does not cause toxicity, and provide scientific evidence of its potential as a source of new adaptogenic substance(s).


Assuntos
Suplementos Nutricionais/efeitos adversos , Malpighiaceae/química , Substâncias para Melhoria do Desempenho/efeitos adversos , Extratos Vegetais/efeitos adversos , Raízes de Plantas/química , Animais , Comportamento Animal , Células CHO , Cricetulus , Etnofarmacologia , Fadiga/etiologia , Fadiga/prevenção & controle , Feminino , Flavonóis/administração & dosagem , Flavonóis/efeitos adversos , Flavonóis/metabolismo , Flavonóis/uso terapêutico , Masculino , Malpighiaceae/crescimento & desenvolvimento , Medicina Tradicional , Camundongos , Substâncias para Melhoria do Desempenho/administração & dosagem , Substâncias para Melhoria do Desempenho/metabolismo , Substâncias para Melhoria do Desempenho/uso terapêutico , Esforço Físico , Extratos Vegetais/administração & dosagem , Extratos Vegetais/metabolismo , Extratos Vegetais/uso terapêutico , Raízes de Plantas/crescimento & desenvolvimento , Quercetina/administração & dosagem , Quercetina/efeitos adversos , Quercetina/análogos & derivados , Quercetina/metabolismo , Quercetina/uso terapêutico , Distribuição Aleatória , Ratos Wistar , Testes de Toxicidade Aguda , Testes de Toxicidade Subcrônica
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