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This study evaluated the gastroprotective potential of methanolic extract from fruits of Campomanesia reitziana (MECR) and its isolated chalcone dimethyl cardamonin (DMC). The phenolic compound in the extract, and the free radical scavenging activity of MECR and DMC, were quantified. The gastroprotective activity of MECR (30-300 mg/kg, p.o) and DMC (1 and 3 mg/kg, p.o) was determined by ethanol/HCl-induced gastric ulcers in mice. Histological, histochemical, and biochemical analyses were performed in the ulcerated tissue. MECR showed a high content of phenolic compounds, including DMC, and was able to scavenge DPPH radicals by 29.58% at 1000 μg/mL. However, DCM (1-1000 μg/mL) did not reduce DPPH radicals. Pre-treatment with MECR at doses of 100 and 300 mg/kg reduced the gastric lesions by 35.07 and 79.47%, respectively (ulcerated-vehicle group 10.72 ± 0.88 mm). Moreover, the extract increased the mucin content by 1044.44% and superoxide dismutase activity by 20.04%, and decreased the lipoperoxide levels by 39.39%, compared to the ulcerated-vehicle group (0.27 ± 0.04 pixels × 10/field; 57.37 ± 1.59 U SOD/mg of protein and 29.57 ± 2.99 mmol LOOH/mg of tissue, respectively). However, MECR did not prevent the depletion of reduced glutathione or the decrease in catalase activity. Pre-treatment with DMC, at 1 and 3 mg/kg, also reduced the gastric ulcers by 53.83 and 52.64%, respectively. In summary, these findings confirm the gastroprotective activity of MECR and DMC, and open an interesting field concerning the gastroprotective potential of dimethyl cardamonin, given its potent antinociceptive and anti-inflammatory activity already described.

The methanolic extract from Campomanesia reitziana fruits and the main active principle, identified as 4',6'-dihydroxy-3',5'-dimethyl-2'-methoxy chalcone or dimethyl cardamonin (1), exhibited pronounced antinociceptive effects against two models of pain in mice. Compound 1 caused dose-dependent inhibition of abdominal constrictions, with a calculated ID50 value of 8.1 (6.5-10.1) μmol/kg (i.p.), being about 16-fold more potent than two reference analgesic drugs. Methanolic extract and 1 were also effective against the formalin model, inhibiting both phases of pain, causing reductions of 39.9% and 26.8% (extract, 10 mg/kg) and 52.9% and 57.6% (compound 1, 5 mg/kg) for the first and second phases, respectively.

This study evaluated the gastroprotective value of the methanol extracts from fruits of Morus nigra L. (black mulberry (MEMN)) and Rubus niveus Thunb (raspberry (MERN)). The total phenolic compounds and flavonoids were measured, as well as the in vitro 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenger activity. The gastroprotective effects of the extracts against 60% ethanol/0.3 M HCl were evaluated in mice. After that, the lipid hydroperoxides and reduced glutathione levels at ulcerated tissue were determined. The effects of extracts on H+/K+-ATPase activity were also verified. The extracts exhibited high contents of polyphenols; however, MERN presented 1.5-fold higher levels. The presence of flavonoids also was confirmed. In addition, MEMN (IC50 = 13.74 μg/mL) and MERN (IC50 = 14.97 μg/mL) scavenged DPPH radical. The MEMN reduced the ulcer area only at 300 mg/kg (p.o.) by 64.06%. Interestingly, MERN decreased the ulcer area in a superior potency (ED50 = 20.88 mg/kg), reducing the ulcer area by 81.86% at 300 mg/kg, and increased the gastric mucin levels. The antioxidant effects of extracts were evidenced by reduced lipoperoxides and increased reduction of glutathione amount in the gastric mucosa. However, MEMN or MERN did not change the H+/K+-ATPase activity. These results confirm that M. nigra and R. niveus are berries with a gastroprotective value by strengthening of gastric protective factors.

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