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1.
Chinese Pharmaceutical Journal ; (24): 303-311, 2019.
Article in Chinese | WPRIM | ID: wpr-858070

ABSTRACT

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.

2.
Chinese Pharmaceutical Journal ; (24): 906-911, 2018.
Article in Chinese | WPRIM | ID: wpr-858319

ABSTRACT

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.

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