RESUMEN
Ethylene-glycol (EG) induced nephrolithiasis is a known model of kidney stone in experimental rodents.Nephrolithiasis is treatable with an antilithiatic and lithotriptic drug. Decoction of Crinum giganteum Andrews(CG) bulb, a medicinal herb is used in folklore medicine to manage urinary tract diseases including kidney stone.The antilithiatic effects of Crinum giganteum Andrews bulb extract was investigated using biochemical andhistological parameters on ethylene-glycol nephrolithiatic rat model and compared with cystone (a knownantilithiatic drug). Twenty rats were randomized into a control group (N=4) which received water (vehicle) andexperimental groups (N-16) that received 1% ethylene-glycol in water and subdivided into negative control (only1% EG in drinking water) and treatment groups which were given 200mg/kg/bw, 400mg/kg/bw of ethanolic bulbextracts of CG and 100mg/kg/bw of cystone orally for 21 days. The EG elevated urinary and serum calcium,protein and creatinine, and reduced magnesium concentrations. These were accompanied by microcrystal depositsin kidney sections. But, the ethanolic bulb extract and cystone treatments reversed the above biochemical andhistopathological effects. The ethanolic bulb extract of CG exhibited comparable antilithiatic effect with cystoneon ethylene-glycol-induced nephrolithiasis. Thus, the extract showed positive indication of its use in folkloremedicine.
RESUMEN
OBJECTIVE: To prepare the microcrystalline glucose transporter-1(GLUT-1)inhibitor BAY-876 and determine its pharmacological properties and examine the slow-release characteristics and in vivo anti-tumor efficiency of BAY-876-microcrystal on mice liver tumor model. METHODS: The tumor model of HCC cells in liver of nude mice was established. The model mice were administrated BAY-876 by means of intragastric administration for three days, and then the liver of mice were photographed and examined by PET / CT. The solubilizing solution or microcrystalline BAY-876 was prepared. BAY-876-solution or microcrystal was injected into subcutaneous tumors. Blood and tumor tissue were taken from mice at different times, and the content of BAY-876 was detected. On this basis, BAY-876-solution or microcrystal was injected into the tumor in liver of nude mice, and the livers were tested by PET / CT at different times. RESULTS: BAY-876-microcrystal can inhibit the cell growth of HCC cells. BAY-876-microcrystal can take long-term effect and slow-release in tissue. A single administration of BAY-876 in HCC liver can achieve the inhibition of HCC tumors CONCLUSION: The microcrystal BAY-876 is prepared, which can long-term inhibit the tumor growth in liver of nude mice.
RESUMEN
OBJECTIVE: To prepare the microcrystal of defactinib and identify the in vivo activity of defactinib-microcrystal on hepatocellular carcinoma (HCC) cells using PET (positron emission computed tomography) methods. METHODS: The protein level of focal adhesion kinase (FAK) in HCC cell lines was examined by Western blot. The solubilizing solution or microcrystal of defactinib was prepared. MHCC97-H cells, which express highest level of FAK, were injected to nude mice to form the subcutaneous tumor. The solubilizing solution or microcrystal of defactinib was injected into tumor tissues. The clearance curve or anti-tumor efficiency of solubilizing solution or microcrystal of defactinib was identified by LC-MS /MS or PET/CT methods. Mice were injected with 300 μCi(11.1 MBq)18F-FDG and analyzed by PET after 50 min. RESULTS: The solubilizing solution or microcrystal of defactinib was successfully prepared. MHCC97-H expresses highest level of FAK than HCC other cell lines. defactinib slowly released by defactinib-microcrystal. Treatment of defactinib-microcrystal sustainably attenuated the absorbing of 18F-FDG in MHCC97-H cells. CONCLUSION: The solubilizing solution or microcrystal of defactinib is successfully prepared. A method to identify the in vivo activity of FAK inhibitor is also established.
RESUMEN
OBJECTIVE: To obtain the microcrystal agents of sorafenib and examine the in vivo anti-tumor efficiency of sorafenib-microcrystal on hepatocellular carcinoma cells. METHODS: The solubilizing solution or microcrystal of sorafenib was obtained. A highly aggressive HCC cell line, MHCC97-H, was used to form the subcutaneous or intra-hepatic tumor model in nude mice. Sorafenib-solution or microcrystal was injected into tumors. The clearance curve or anti-tumor efficiency of solubilizing solution or microcrystal was identified. Endogenous of EMT related indicators was identified by qPCR. RESULTS: Sorafenib slowly released in tumor tissues by sorafenib-microcrystal but not sorafenib-solution. Treatment of sorafenib-microcrystal inhibited the in vivo growth of MHCC97-H cells. CONCLUSION: The microcrystal agents of sorafenib is prepared. This work also establishes the in vivo anti-tumor efficiency of sorafenib-microcrystal on HCC cells.