Effect of the tyrosinase inhibitor (S)-N-trans-feruloyloctopamine from garlic skin on tyrosinase gene expression and melanine accumulation in melanoma cells.

In our searching for novel tyrosinase inhibitors from natural sources, (S)-N-trans-feruloyloctopamine isolated from garlic skin was found to be a potential mushroom tyrosinase inhibitor. Here, we examined the effects of the potential tyrosinase inhibitor in B16F10 cells on intracellular melanin contents, cytotoxicity, and the signaling mechanism involved in the expression of tyrosinase. The results showed the inhibitor displayed little or no cytotoxicity at all concentrations examined and decreased the relative melanin contents in a dose-dependent manner in the α-MSH-stimulated B16F10 cells. Real-time PCR and Western blot analysis showed that it inhibits melanogenesis signaling by down-regulates mRNA and protein expression levels of tyrosinase, which leads to a lower melanin contents. These results suggested that (S)-N-trans-feruloyloctopamine was an ideal tyrosinase inhibitor, and could be used in food and medical industry.

Two cinnamoyloctopamine antioxidants from garlic skin attenuates oxidative stress and liver pathology in rats with non-alcoholic steatohepatitis.

Hepatic oxidative stress plays a key role in the development of non-alcoholic steatohepatitis (NASH), therefore, treatment approaches that address the antioxidant is helpful in the therapy of patients with NASH. N-trans-coumaroyloctopamine (1) and N-trans-feruloyloctopamine (2) were identified as the primary antioxidant constituents of garlic skin with high antioxidant activities. The aim of this study was to elucidate the protective effect and mechanism of the antioxidants on NASH in rats. The results provide morphological and molecular biological evidences for the protective role of the antioxidant 2 in ameliorating oxidative stress and hepatic apoptosis in experimental NASH for the first time. Mechanism study indicated that the antioxidant 2 significantly reduced the expression of COX-2 mRNA and protein by western blot, RT-PCR and immunohistochemical techniques.

Anti-tumor effects and apoptosis induction by Realgar bioleaching solution in Sarcoma-180 cells in vitro and transplanted tumors in mice in vivo.

BACKGROUND: Realgar which contains arsenic components has been used in traditional Chinese medicine (TCM) as an anticancer drug. However, neither Realgar nor its formula are soluble in water. As a result, high dose of Realgar has to be administered to achieve an effective blood medicine concentration, and this is associated with adverse side effects. The objective of the present study was to increase the solubility of a formula using hydrometallurgy technology as well as investigating its effects on in vitro and in vivo cell proliferation and apoptosis in Sarcoma-180 cell line. MATERIALS AND METHODS: Antiproliferative activity of Realgar Bioleaching Solution (RBS) was evaluated by MTT assay. Further, effects of RBS on cell proliferation and apoptosis were studied using flow cytometry and transmission electron microscopy. Kunming mice were administered RBS in vivo, where arsenic specifically targeted solid tumors. RESULTS: The results indicated that RBS extract potently inhibited the tumor growth of Sarcoma-180 cell line in a dose-dependent manner. Flow cytometry and transmission electron microscopy further indicated that RBS significantly induced cell apoptosis through the inhibition of cell cycle pathway in a dose-dependent manner. Further, on RBS administration to mice, arsenic was specifically targeted to solid tumors CONCLUSIONS: RBS could substitute for traditional Realgar or its formula to work as a potent tool in cancer treatment.

[Comparison of effects of Wujia Bugu decoction) and alendronate sodium on protection the bone loss of hindlimb unloaded rats].

OBJECTIVE: To compare the effects of Wujia Bugu decoction and Alendronate sodium on protecting bone and muscle loss of hindlimb unloaded rats lasting three weeks. METHODS: March to May, 2009, 40 male Wistar rats with age of 6-week, were randomized divided to four groups (10 rats in each group): hindlimb unloaded group treated with Chinese medicine (HUC), hindlimb unloaded group treated with alendronate sodium (HUA), control group (CON), as well as hindlimb unloaded group (HU). During the experiment, rats of HUC was given Wujia Bugu decoction (including the Ciwujia, Shudihuang, Huainiuxi, Muli, etc. with the concentration of 0.704 g/ml) 10 ml/kg weight once a day, HUA was given quantitative alendronate sodium slice dissolve suspension (0.9 mg/ml) once a week. CON and HU were given double-distilled water. The experiment lasted 4 weeks,from the second to the forth week, rats in HU, HUC, HUA were hindlimb unloaded. All rats were sacrificed at the fourth weekend, the content of Ca, P and the activation of ALP in serum, Bone mineral density (BMD) of humerus and femurs, Biomechanical property of tibia and humerus, as well as the weight index of biceps and sural muscles were measured. RESULTS: Compared with CON, serum Ca of HU was significantly increased (P < 0.05), BMD, mechanical properties, muscle index of hindlimb were significantly reduce (P < 0.01), the serum Ca of HUA significantly increased (P < 0.05). Serum ALP of HUC was significantly higher than other three groups (P < 0.01). Compared with HU, femoral BMD of HUC and HUA significantly increased, tibial maximum load, maximum deflection and elastic load had increased tendency; calf muscle atrophy of HUC and HUA was alleviate 50% and 12.5% respectively (P > 0.05), humeral BMD had no significant difference, while the maximum deflection (P < 0.01) and elastic deflection (P < 0.05) in humerus of HUA were significantly lower. CONCLUSION: Herbal prescription and alendronate sodium can effectively protect the bone and muscle loss of hindlimb unloaded rats, improve its mechanical structure. Herbal prescription has advantages of relieving mechanical properties change. The effects of Wujia Bugu decoction and alendronate sodium are similar in treating space weightlessness bone loss.