药物体外代谢研究III- PHASE II酶研究
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药物代谢酶Elimination pathways of top 200 drugs
实例
Conjugation with phase II enzymes Detoxification & Antioxidant
UGTs结构特征
UGTs are a family of membrane-bound enzymes that are concentrated in the endoplasmic reticulum (ER) and nuclear envelope of hepatocytes.
How to remove the latency
Detergent : Toxon-X Brij-58
Pore-forming peptides: Filipin
人体内主要UGTs代谢亚型酶Williams J.A. et al. DMD 2004; 32:1201-08
◆改善微循环丹参酮I
丹参酮IIA
隐丹参酮
原儿茶醛(PAL)丹参素丹酚酸B (Sal B)主要活性物质脂溶性成分
水溶性成分◆抗凝血
15000002000000COMTs SULTs UGTs 0n m
,
m
V
CHO CHO
MS/MS
1. Metabolism of PAL by 12 commercially avaluable
and other UGTs activities in 15 individual HLMs 2. Inhibitory effects of inhibitors on PAL
glucuronidation in HLMs and rUGTs, respectively
Kinetic characteristics and prediction of in vivo CL Phenylbutazone for UGT1A6;Androsterone for UGT1A9