The antidiabetic activity of Cissus sicyoides (Vitaceae) was investigated in KK-Ay mice, an animal model of genetically type 2 diabetes with hyperinsulinemia. The water extract of Cissus sicyoides (CS) (500 mg/kg body weight) improved hyperglycemia after an oral administration of maltose in KK-Ay mice. CS significantly reduced maltase activity in small intestine of KK-Ay mice. CS reduced the blood glucose of KK-Ay mice 2 weeks after repeated administration without changing plasma insulin level. These results suggest that the antidiabetic activity of CS is derived, at least in part, due to the inhibition of maltase activity.

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The inhibitory activities of 19 Chinese formulae on osteoclast formation and bone resorption in vitro were investigated. The inhibitory activity on osteoclast formation was evaluated using a mouse bone marrow cell culture in which osteoclast-like multinucleated cells were formed in the presence of parathyroid hormone (PTH). The inhibitory activity on bone resoption was evaluated using PTH-induced resorption of ⁴⁵Ca from ⁴⁵Ca-prelabeled neonatal mouse parietal bone. Among the 19 Chinese formulae, nine showed a strong inhibitory activity on osteoclast formation at a concentration of 50μg/ml, and three of the nine also showed a strong inhibitory activity on bone resorption. Among these three formulae, Bu-Shen-Jian-Gu-Tang showed the most promising activity in a dose-dependent manner on the inhibition of bone resorption. A further in vivo experiment in ovariectomized (OVX) model rats using peripheral quantitative computed tomography (pQCT) revealed its preventive effect on bone loss.

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We examined the preventive effect of Saikokeishito extract (TJ-10), a traditional Kampo medicine, on acute gastric mucosal lesion progression in rats treated once with compound 48/80 (C48/80), a mast cell degranulator. Rats treated with C48/80 (0.75 mg/kg, i.p.) received TJ-10 (0.13, 0.65 or 1.3 g/kg, p.o.) 0.5 h after the treatment at which time gastric mucosal lesions appeared. At 0.5 h after C48/80 treatment, the gastric mucosa of the treated rats had increased myeloperoxdiase (an index of neutrophil infiltration) and xanthine oxidase activities and thiobarbituric acid reactive substances (an index of lipid peroxidation) content. At 3 h after C48/80 treatment, the gastric mucosa of the treated rats showed progressive lesions and further increases in myeloperoxdiase and xanthine oxidase activities and thiobarbituric acid reactive substances content and decreases in vitamin E, ascorbic acid, and adherent mucus contents and Se-glutathione peroxidase activity. Post-administered TJ-10 attenuated all these changes found at 3 h after C48/80 treatment dose-dependently. However, Post-administered TJ-10 had no effect on the changes in serum serotonin and histamine concentrations and gastric mucosal blood flow following mast cell degranulation caused by C48/80 treatment. TJ-10 inhibited in vitro gastric mucosal myeloperoxidase activity but had little effect on in vitro gastric mucosal xanthine oxidase activity. These results indicate that TJ-10 prevents the progression of C48/80-induced acute gastric mucosal lesions in rats possibly by attenuating enhanced neutrophil infiltration and oxidative damage and destruction of the defensive barrier in the gastric mucosa.

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The antimetastatic effect of fermented brown rice by Aspergillus oryzae(FBRA), a processed food, was examined in an animal model of metastasis to the liver using mouse colon cancer cells. Mice fed a diet containing 10% FBRA were inoculated with colon 26-L5 cells via the portal vein on day 14. Liver metastasis on day 28 was significantly inhibited by the FBRA-containing diet without an increase in body weight. To investigate the immunostimulatory activity, the cellular functions of macrophages were examined. Intracellular glutathione levels were increased in peritoneal macrophages (PEMs) prepared from mice fed FBRA for 18 days. FBRA did not induce the production of interferon-γ (IFN-γ) by itself, though enhanced the ability of PEMs to produce IFN-γ, but not interleukin-12 or tumor necrosis factor-α, in response to lipopolysaccharide (LPS). These results indicated that oral administration of FBRA inhibited the metastasis of colon 26-L5 cells to the liver through a mechanism leading to a Th1-dominant immune state and activation of macrophages via anti-oxidative properties.

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