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临床上穿心莲大多应用于治疗呼吸系统疾病、心血管系统疾病和胃肠道系统疾病等.现今,临床上多存在同时使用两种甚至两种以上的药物,引起体内代谢酶UGTs的代谢抑制,从而引发药物-药物相互作用.本实验主要研究由实验室合成的穿心莲内酯化合物A:zfx-45-7对UGT2B7酶的抑制作用,采用4-甲基伞形酮(4-MU)葡萄糖醛酸化抑制法,以4-MU作为底物对UGT2B7代谢穿心莲化合物的抑制能力做了初步的筛查,测得其残余活性小于20%,继续实验测定抑制常数K_1值为0.15μm0l/L,从而为进一步合成穿心莲药物做出理论和基础实验准备.
Most of the clinical application of andrographis for the treatment of respiratory diseases, cardiovascular system diseases and gastrointestinal diseases, etc .. Nowadays, there are many clinical use of two or even more than two kinds of drugs, causing metabolic inhibition of metabolic enzymes UGTs, thus Induced drug-drug interaction.In this experiment, we investigated the inhibition of UGT2B7 enzyme by andrographolide A: zfx-45-7 synthesized in the laboratory, using 4-methylumbelliferone (4-MU) glucuronidation Inhibition method to 4-MU as a substrate for UGT2B7 metabolic Andrographis paniculata compounds were tested for its ability to inhibit the residual activity was measured less than 20%, continued to determine the inhibition constant K_1 value of 0.15μm0l / L, so as to further Synthetic Andrographis medicine to make the theory and basic experimental preparation.