2 sources
Mechanism of action
To evaluate the hepatoprotective activity of spices, 21 different spices were fed to rats with liver damage caused by lipopolysaccharide (LPS) plus d-galactosamine (D-GalN). As assessed by plasma aminotranferase activities, nutmeg showed the most potent hepatoprotective activity. Bioassay-guided isolation of the active compound from nutmeg was carried out in mice by a single oral administration of the respective fractions. Myristicin, one of the major essential oils of nutmeg, was found to possess extraordinarily potent hepatoprotective activity. Myristicin markedly suppressed LPS/D-GalN-induced enhancement of serum TNF-alpha concentrations and hepatic DNA fragmentation in mice. These findings suggest that the hepatoprotective activity of myristicin might be, at least in part, due to the inhibition of TNF-alpha release from macrophages. ...
Mouse hepatoma Hepa-1c1c7 (Hepa-1) cells were treated with myristicin to assess the role of myristicin in the process of Cyp1a-1 induction. Treatment of Hepa-1 cells with myristicin increased Cyp1a-1 transcription in a dose-dependent manner as shown by analysis of 7-ethoxyresorufin O-deethylase activity, Cyp1a-1 protein level, and Cyp1a-1 mRNA. Myristicin, however, did not competitively displace [3H]2,3,7,8-tetrachlorodibenzo-p-dioxin from the Hepa-1 cytosolic aryl hydrocarbon (Ah) receptor in a competitive Ah receptor binding analysis using sucrose density gradient sedimentation and did not affect formation of DNA-protein complexes between the Ah receptor and its DRE target in a gel mobility shift assay using oligonucleotides corresponding to DRE 3 of the Cyp1a-1. ...
Pharmacokinetics
Metabolism
In mice, the major metabolic pathway for ... myristicin includes cleavage of the methylenedioxyphenol residue and exhalation of the methylene carbon atom as carbon dioxide.
Myristicin yields 3-methoxycatechol probably in mouse, housefly; yields 1-(3-methoxy-4,5-methylenedioxyphenyl)-3-piperidyl-1-propanone in rat, guinea pig; yields 1-(3-methoxy-4,5-methylenedioxyphenyl)-3-pyrrolidinyl-1-propanone in rat, guinea pig. /From table/
Myristicin was converted into 3-methoxy-4,5-methylenedioxyamphetamine during perfusion of isolated rat liver or incubation with rat liver homogenates.
2 N-containing metabolites of myristicin were excreted in the urine of rats and guinea pigs following oral or ip admin. In the rats the metabolite was 3-piperidyl-1,3-methoxy-4,5-mehtylenedioxyphenyl)-1-propanone while the major metabolite in the guinea pig was 3-pyrrolidinyl-1(3-methoxy-4,5-methylenedioxy-phenyl)-1-propanone.
For more Metabolism/Metabolites (Complete) data for MYRISTICIN (8 total), please visit the HSDB record page.
Myristicin has known human metabolites that include 5-allyl-1-methoxy-2,3-dihydroxybenzene.
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