Disease relevance of Halomon

• OBJECTIVES: To characterize the enzymes responsible for and metabolites produced from the metabolism of halomon, a halogenated monoterpene that is isolated from the red algae Portieria hornemanii and has in vitro activity in the NCI screen against brain, renal, and colon cancer cell lines [1].

High impact information on Halomon

• Human hepatic microsomes metabolized halomon and required NADPH to do so [1].
• Further separation of murine hepatic S9 fractions produced a microsomal fraction that contained all of the halomon-metabolizing activity; cytosol had none [1].
• MATERIALS AND METHODS: Mouse and human liver fractions, prepared by homogenization and differential centrifugation, were incubated with halomon, extracted with toluene, and analyzed by gas chromatography [1].
• CONCLUSIONS: Halomon is metabolized by mouse and human hepatic cytochrome P-450 enzymes, the identities of which remain unknown [1].
• Population estimates of parameters describing halomon plasma pharmacokinetics in female CD2F1 mice were developed with a standard two-stage technique and also by simultaneous modeling of data from 20-, 60-, 90-, and 135-mg/kg i.v. studies in female mice [2].

Biological context of Halomon

• Halomon bioavailability was 45%, 47%, and 4% after i.p., s.c., and enteral dosing, respectively [2].
• Plasma pharmacokinetics, bioavailability, and tissue distribution in CD2F1 mice of halomon, an antitumor halogenated monoterpene isolated from the red algae Portieria hornemannii [2].

Anatomical context of Halomon

• Both murine and human hepatic microsomes produced a metabolite of halomon [1].
• Halomon concentrations were also determined in the brains, hearts, lungs, livers, kidneys, spleens, skeletal muscles, fat, red blood cells, and, if present, testes of mice given 135 mg/kg i.v. Halomon plasma pharmacokinetics were well fit by a two-compartment, open linear model and were linear between 20 and 135 mg/kg [2].

Associations of Halomon with other chemical compounds

• RESULTS: In the presence of NADPH, mouse-liver 9,000-g supernatant (S9) fractions metabolized halomon, but boiled S9 fractions did not [1].

Analytical, diagnostic and therapeutic context of Halomon

• Plasma halomon concentrations were measured with a gas-chromatography system using electron-capture detection [2].

References