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中文摘要：
利用超高效液相色谱-串联质谱（UPLC—MS／MS）的多反应监测（MRM）技术，结合多探针底物方法，对单酯型及双酯型乌头类生物碱组分对细胞色素P450（CYP450）亚型的活性影响进行了研究；同时利用超高效液相色谱一四极杆一飞行时问串联质谱（UPLC-Q—TOF—MS／MS）对单酯型和双酯型乌头类生物碱组分在CYP450中的代谢指纹图谱进行了研究．活性影响研究结果表明，单酯型生物碱组分对CYP2C及2D的抑制能力较强，其IC50值分别为7．44和6．74μmol／L；双酯型生物碱组分对CYP1A2，3A，2C和2D均有较弱的抑制作用，其IC50值分别为39．48，70．44，17．36和86．04μmol／L．代谢指纹图谱显示，双酯型生物碱组分在大鼠肝微粒体中有6个特异性产物可以作为该反应的特征峰．
英文摘要：
The effects of the components of monoester and diester diterpenoid alkaloids （ MDAs, DDAs） on the activities of hepatic microsomal CYP450 isozymes（CYP1A2, CYP2C, CYP2EI, CYP2D, CYP3A） were studied by ultra performance liquid chromatography-tandem mass spectrometry（UPLC-MS/MS） combined with cocktail probe substrate＇s method. The metabolic fingerprints of MDAs and DDAs＇ components were studied in rat liver microsomes using UPLC-Q-TOF/MS/MS. The results showed that the components of MDAs had strong inhibitory effects on the activities of CYP2C and 2D, the ICso value was 7.44 and 6. 74 μmoL/L, respectively. The components of DDAs had weaker inhibitory effects on the activities of CYP1A2, 3A, 2C and 2D, the IC50 value was 39.48, 70. 44, 17.36 and 86. 04 μmoL/L, respectively. Six metabolites of DDAs in rat liver rnicrosomes were identified using UPLC-Q-TOF-MS/MS. They can be used as marked peaks for meta- bolic fingerprint of aconite alkaloids components.
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