Inhibition of Rat CYP1A2 and CYP2C11 by Honokiol, a Component of Traditional Chinese Medicine

Quantitation of Diclofenac, Tolbutamide, and Warfarin as Typical CYP2C9 Substrates in Rat Plasma by UPLC-MS/MS and Its Application to Evaluate Linderane-Mediated Herb-Drug Interactions

“…Tolbutamide is mainly metabolized by CYP2C9 in the liver. Hence, it is often applied as a substrate of CYP2C9 to explore the changes of enzyme activity [ 20 ]. The results of the previous studies showed that LDR could irreversibly inhibit the enzyme activity after being inactivated because of the mechanism-based activity of CYP2C9 in vitro .…”

“…Unfortunately, about 129 severe bleeding events were reported in the two groups [ 19 ]. In addition, honokiol, the main component of Magnolia officinalis , could significantly increase the t 1/2 and AUC of tolbutamide, mainly because of the inhibitory effect of honokiol on the activity of CYP2C9 [ 20 ]. It is obvious that DDIs based on the inhibition of the activity of CYP2C9 are frequently reported.…”

Honokiol attenuates acetaminophen-induced acute liver injury by inhibiting hepatic CYP1A2 activity and improving liver mitochondrial dysfunction

“…Honokiol (Hon) is one of the main active components of M. officinalis , and has many pharmacological activities, such as anti-oxidative stress, liver protection, anti-inflammatory, anticancer and so on ( Caballero et al, 2020 , Chi et al, 2020 , Wang et al, 2020 , Zhai et al, 2020 ). It has been reported that Hon strongly inhibited human CYP1A2-mediated phenacetin O -deethylation ( Jeong et al, 2013 ), as well as the activities of CYP1A2 and CYP2C11 in rat liver microsome, with inhibition constant values of 1.6 μmol/L and 16.5 μmol/L, respectively ( Li et al, 2019 ). Our previous work also revealed that Hon decreased the enzyme activities of CYP1A2 and CYP2E1 in diabetic rat liver ( Wang et al, 2018 ).…”