RESUMO
ETHNO-PHARMACOLOGICAL RELEVANCE: Pattanga is botanically equated as Caesalpinia sappan Linn. (Family: Caesalpiniaceae) and is used in Ayurveda system of medicine since ages. According to Ayurveda, useful part is Heartwood, which is bitter, astringent and acrid and is useful in vitiated conditions of vata and pitta, burning sensation, wounds, ulcers, leprosy, skin diseases, menorrhagia, leucorrhea, and diabetes. It is used as a major ingredient in Ayurvedic formulations and preparations like Patrangasava, Chandanadya Thalia, and Karpuradyarka. AIM OF THE STUDY: The present study is planned to evaluate the gastroprotective activity of the selected Ayurvedic drug using three different in vivo gastric ulcer models, so as to provide scientific evidence for the Ayurvedic claims. MATERIALS AND METHODS: For this study, Wistar albino rats fasted overnight were selected. The hydroalcoholic extract of Caesalpinia sappan heartwood at the dose level 250 and 500mg/kg body weight was selected and administered orally before necrotizing agents. Antioxidant and antiulcer parameters were evaluated and the stomach samples were subjected for histopathological studies. In addition, PGE2 estimation and protein expressions of COX-1, COX-2 and iNOS were analyzed by Western blot. The plant extract was subjected to LCMS/MS analysis. In addition, Cytoprotective effect in isolated gastric mucosal cells, TUNEL Assay, Acid neutralizing capacity assay, H+/K+ ATPase inhibitory assay were performed. RESULTS: The ulcer protection was found to be 92%, 86% and 64% against ethanol, NSAID and pylorus ligation induced ulcer respectively. The hydro-alcoholic extract of C. sappan heartwood exhibited cytoprotective effect with 76.82% reduction against indomethacin-induced cytotoxicity at the concentration of 25µg/ml. C. sappan showed 63.91% inhibition in H+/K+ ATPase inhibitory assay at the concentration 500µg/ml. CONCLUSIONS: Our results depict that Caesalpinia sappan heartwood possesses gastroprotective activity, possibly mediated through cytoprotection and antioxidant mechanisms. The data obtained in the present study provides scientific support for the traditional use of Caesalpinia sappan in the management of peptic ulcer.
Assuntos
Caesalpinia/química , Mucosa Gástrica/efeitos dos fármacos , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Úlcera Gástrica/tratamento farmacológico , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Antiulcerosos/química , Antiulcerosos/farmacologia , Antioxidantes/farmacologia , Ciclo-Oxigenase 1/metabolismo , Ciclo-Oxigenase 2/metabolismo , Dinoprostona/metabolismo , Etanol/química , Feminino , Mucosa Gástrica/metabolismo , ATPase Trocadora de Hidrogênio-Potássio/metabolismo , Indometacina/farmacologia , Proteínas de Membrana/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Fitoterapia/métodos , Extratos Vegetais/química , Substâncias Protetoras/química , Ratos , Ratos Wistar , Úlcera Gástrica/metabolismoRESUMO
This study investigates the effects of an ethanolic extract from the stem bark of Combretum leprosum Mart. & Eiche (Combretaceae) on experimental ulcers induced by ethanol and indomethacin and on gastric secretion and mucus content in pylorus-ligated rats. The effects were compared with those of ranitidine and carbenoxolone. Combretum leprosum orally administered elicited a complete inhibition of the appearance of gastric lesions induced by ethanol and a partial reduction when indomethacin was used as an ulcerogenic agent. Moreover, the protection against gastric ulceration induced by ethanol was decreased with indomethacin pretreatment. The intraduodenal administration of Combretum leprosum in four-hour pylorus-ligated rats increased the volume and pH of gastric juice while decreasing the acid output and produced a significant increase in gastric wall mucus content. The major compounds detected in a preliminary phytochemical screening were triterpenes, flavonoids, taninns and saponins. This study provides evidence that the ethanolic extract of Combretum leprosum possesses gastroprotective and anti-ulcerogenic effects, which are related to the inhibition of the gastric acid secretion and an increase of mucosal defensive factors such as mucus and prostaglandin.