Schisandrin B (SinB) and Schisandrol B (SolB) are two abundant compounds with similar structures in Schisandra sphenanthera widely used for hepatic diseases in Asian countries. They are also pharmacologically active components in many other traditional Chinese medicines. However, induction features of cytochrome P450 (CYP) by SinB and SolB were not well established. The present study aimed to investigate the CYP profile induced by SinB and SolB, and the role of nuclear factors pregnane X receptor (PXR) and constitutive androstane receptor (CAR). Wild-type (WT) and Pxr-null (KO) mice were administered SinB and SolB respectively for 5 days. CYP induction analysis was carried out and underlying mechanism was explored. CYP2b was sharply induced by SinB and SolB in WT and KO mice. CYP3a was moderately induced in WT mice, but not in KO mice. No significant induction of CYP2c or UDP glucuronosyltransferases was observed. Edema related with slight hepatomegaly was found in both WT and KO mice, which was found reversible and non-inflammatory. These data suggest SinB and SolB induced CYP3a moderately in a PXR-dependent way. In contrast, they both sharply induced CYP2b, which was supposed to be associated with nuclear factor CAR not PXR. Non-inflammatory and reversible edema contributed to hepatomegaly induced by SinB and SolB. The complicated CYP induction of SinB and SolB might cause drug-drug interactions in the clinic.

五味子B（SINB）和五味子醇B（SolB）是两种丰富的化合物与类似结构华中五味子广泛用于在亚洲国家肝脏疾病。它们还是许多其他传统中药的药理活性成分。但是，尚不能很好地确定SinB和SolB对细胞色素P450（CYP）的诱导特性。本研究旨在调查由SinB和SolB诱导的CYP谱，以及核因子孕烷X受体（PXR）和组成型雄甾烷受体（CAR）的作用。野生型（WT）和Pxr-将无效（KO）小鼠分别给予SinB和SolB 5天。进行了CYP诱导分析，并探讨了潜在的机制。CYP2b被WT和KO小鼠的SinB和SolB强烈诱导。CYP3a在WT小鼠中被中等诱导，但在KO小鼠中未被诱导。没有观察到CYP2c或UDP葡萄糖醛酸转移酶的显着诱导。在WT和KO小鼠中均发现了与轻度肝肿大相关的水肿，被发现是可逆的和非炎性的。这些数据表明SinB和SolB以PXR依赖性的方式适度诱导CYP3a。相反，他们俩都强烈诱导CYP2b，这被认为与核因子CAR而不是PXR有关。非炎性和可逆性水肿是由SinB和SolB诱导的肝肿大的原因。CYP对SinB和SolB的复杂诱导可能会在临床中引起药物相互作用。