Preparation of Microcrystalline Glucose Transporter 1 Inhibitor BAY-876 and Its Anti-tumor Effect in Vivo / 中国药学杂志

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.