Tian, Min; Zhou, Shenzhi; Li, Wei; Li, Jiaru; Yang, Lan; Peng, Ying; Zheng, Jiang published an article in 2021, the title of the article was Metabolic activation of aegeline mediated by CYP2C19.Name: N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide And the article contains the following content:
Aegeline (AGL) is a natural alkaloidal amide mainly isolated from the leaves and fruits of tropical plant Aegle marmelos, with multiple pharmacol. activities. As one component of several dietary supplements, AGL caused a series of acute and chronic liver injuries. Nevertheless, the mechanisms of AGL-induced hepatotoxicity remain unclear. This study was conducted to identify reactive metabolite(s), to determine related metabolic pathways, and define the possible association of the bioactivation with AGL cytotoxicity. A demethylation metabolite (M1) and a GSH conjugate (M2) were detected in rat liver microsomal incubations containing AGL and GSH. The two metabolites were both found in bile of rats and rat primary hepatocytes after AGL administration. Recombinant P 450 enzyme incubations showed that CYP2C19 was the principal enzyme catalyzing this metabolic activation. Ticlopidine, a selective inhibitor of CYP2C19, decreased the formation of M1 and M2 in hepatocytes and attenuated the susceptibility of hepatocytes to the cytotoxicity of AGL. The results suggest that AGL was metabolized to a p-quinone methide intermediate which could in part participate in AGL-induced cytotoxicity. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).Name: N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide
The Article related to aegeline cytochrome p metabolic activation, aegeline, cyp2c19, cytotoxicity, metabolic activation, quinone methide intermediate, Placeholder for records without volume info and other aspects.Name: N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics