Metabolism of Drugs. L. The In Vitro Study on Metabolism of Brucine and 4-Substituted Veratroles

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Interesting selective demethylation of brucine and 4-substituted veratroles, which was found to occur as major metabolism in rabbits, was further investigated by in vitro systems. Using 9000×g. supernatant fraction of rabbit liver homogenate, it was shown that demethylation of brucine and 4-nitroveratrole was catalyzed by so called "liver microsomal drug metabolizing enzyme systems, " and it took place predominantly at the meta-position of the lactam group of brucine and at the para-position of nitro group of 4-nitroveratrole at pH 7.5,coinciding with the in vivo results.^<1,2> On the other hand, 4-acetamidoveratrole underwent mostly deacetylation by the same fraction. In addition, demethylation of 4-nitroveratrole studied further by rabbit liver microsomes, and it was found that NADH was even more effective than NADPH as the cofactor if added sufficiently to the incubation mixture.
公益社団法人日本薬学会の論文
1964-10-25