RESUMEN
Momordicae Semen, Momordica cochinchinensis Springer (Cucurbitaceae), has long been known to effectively relieve boils, rheumatic pain, and hemorrhoids. In this study, we investigated whether Momordicae Semen extract (MSE) has anti-gastritis effects in various rodent models and also explored possible mechanisms for the gastroprotective effects of MSE. MSE provided remarkable protective effects, comparable to those of rebamipide, in ethanol- and diclofenac-induced acute gastritis. In addition, it has demonstrated protective effect in a Helicobacter pylori-insulted chronic gastritis model. MSE also showed wound healing effect on cutaneous injury of mice and stimulated calcitonin gene-related peptide and somatostatin receptors, which may be related to its anti-gastritis effects. In a single oral dose toxicity study, the approximate lethal dose of MSE was determined at >2000 mg/kg/day. The NOAEL was set to be 2000 mg/kg/day from the repeated oral dose toxicity study. Moreover, momordica saponin I, a major ingredient of MSE, treatment decreased gastric mucosa damage indices in the ethanol- and diclofenac-induced acute gastritis models. The results suggest that MSE could be a promising gastroprotective herbal medicine and momordica saponin I might be used as an active marker compound for MSE.
Asunto(s)
Antiulcerosos/farmacología , Mucosa Gástrica/efectos de los fármacos , Gastritis/tratamiento farmacológico , Momordica/química , Extractos Vegetales/farmacología , Cicatrización de Heridas/efectos de los fármacos , Alanina/análogos & derivados , Alanina/farmacología , Animales , Antiulcerosos/química , Péptido Relacionado con Gen de Calcitonina/metabolismo , Mucosa Gástrica/metabolismo , Gastritis/inducido químicamente , Gastritis/metabolismo , Infecciones por Helicobacter/tratamiento farmacológico , Infecciones por Helicobacter/metabolismo , Helicobacter pylori/efectos de los fármacos , Helicobacter pylori/metabolismo , Masculino , Ratones , Extractos Vegetales/química , Quinolonas/farmacología , Ratas , Ratas Sprague-Dawley , Receptores de Somatostatina/metabolismo , Saponinas/química , Saponinas/farmacología , Semillas/química , Piel/efectos de los fármacos , Piel/metabolismoRESUMEN
A chemical investigation of the n-butanol fraction of the inner bark of Betula platyphylla led to the isolation of seven diarylhepanoids, (-)-centrolobol (1), aceroside VII (2), aceroside VIII (3), (3R)-1,7-bis-(4-hydroxyphenyl)-3-heptanol-3-O-[2,6-bis-O-(ß-D-apiofuranosyl)-ß-D-glucopyranoside (4), 1,7-bis-(4-hydroxyphenyl)-5-hepten-3-one (5), platyphyllone (6) and platyphylloside (7). The antifibrotic effects of these isolates were evaluated with HSC-T6 cells by assessing cell proliferation. Among them, compounds 1, 2, 5 and 6 significantly inhibited the proliferation of HSCs in a dose-dependent manner at concentrations from 10 µM to 100 µM. Compound 5 in particular dramatically decreased the collagen content and increased the Caspase-3/7 activity. Taken together, the antifibrotic activity of B. platyphylla and its constituents might suggest therapeutic potential against liver fibrosis.