The Anti-gastropathic and Anti-rheumatic Effect of Niga-ichigoside F1 and 23-Hydroxytormentic Acid Isolated from the Unripe Fruits of Rubus coreanus in a Rat Model

Abstract

This study was undertaken to produce the clinical merits of two natural antinociceptive anti-inflammatory triterpenoids which synthetic anti-inflammatory drugs do not have. The triterpenoid glycoside niga-ichigoside F₁ (NIF₁) and its aglycone 23-hydroxytormentic acid (23-HTA), which were isolated from the unripe fruits of Rubus coreanus (Rosaceae), reduced rheumatoid arthritis (RA) factor and C-reactive protein (CRP) factor in Freund's complete adjuvant reagent-induced rats, suggesting that these two triterpenoids had an anti-rheumatic effect. It was also shown that treatment with NIF₁ or 23-HTA reduced gastric lesion extent, acidity and total gastric acid output induced by EtOH plus sodium salicylate in a gastric secretion test. Moreover, 23-HTA had a greater effect than the glycoside, NIF₁. To clarify the anti-gastropathic mechanism of these two compounds, their free radical scavenging activities in the gastric mucosa were examined in a rat EtOH–sodium salicylate-induced gastropathy model. The two compounds significantly increased superoxide dismutase and glutathione peroxidase activities, indicating that the healing effects of NIF₁ and 23-HTA against gastropathy are associated with free radical scavenging enzyme activities. These results support the notion that the long-term administration of NIF₁ or 23-HTA should overcome the adverse effects of synthetic anti-inflammatory drugs.