Endogenous sterols

A number of CYPs take part in cholesterol biosynthesis and elimination, thus playing an important role in maintaining cholesterol homeostasis. Under normal physiological conditions, cholesterol intake (diet or synthesized de novo from acetyl CoA) equals cholesterol elimination (degraded to bile salts, secreted in bile and used in steroid hormone synthesis). These processes are under tight regulatory control and any disruption leads to increased cholesterol levels resulting in cardiovacular disease. The CYPs involved in cholesterol homeostasis could serve as potential targets for cholesterol-lowering drugs (Lewis 2004, Guengerich 2006, Pikuleva 2006).

众多细胞色素P450（CYPs）参与胆固醇的生物合成与排泄，因此在维持胆固醇稳态中扮演着至关重要的角色。在正常的生理状态下，胆固醇的摄入（源自饮食或由乙酰辅酶A重新合成）与胆固醇的排泄（降解为胆汁酸，随胆汁分泌并参与类固醇激素的合成）保持平衡。这些过程受到严格的调控，任何调控失衡都将导致胆固醇水平升高，进而引发心血管疾病。参与胆固醇稳态的CYPs可作为降胆固醇药物潜在的治疗靶点（Lewis 2004，Guengerich 2006，Pikuleva 2006）。