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Chemical Compound Review:

Chalcone, 3 (E)-3-(4-hydroxyphenyl)-1- phenyl-prop-2-en...

Synonyms: CHEMBL7747, AC1NQZY1, Bio-0682, SureCN1375837, NSC-170282, ...

Kohno, Y. et al., Valla, A. et al.

Valla, Valla, Cartier, Le Guillou, Labia, Florent, Charneau, Schrevel, Potier,

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High impact information on NSC170282

The oxidase activities leading to 4-hydroxychalcone and 4'-hydroxychalcone were enhanced in liver microsomes of 3-methylcholanthrene- and phenobarbital-treated rats, respectively [1].
When chalcone and trans-4-phenyl-3-buten-2-one (PBO) were incubated with liver microsomes of untreated rats in the presence of NADPH, 4-hydroxychalcone and trans-4-(4-hydroxyphenyl)-3-buten-2-one (4-OH-PBO), respectively, were formed as major metabolites [1].
The 4-hydroxy-chalcone-like (compound 6a, derived from beta-ionone) exhibits a good and reproducible inhibitory effect on the in vitro culture of Plasmodium falciparum, with an IC 50 lower than 10 microM for inhibition of 3H-hypoxanthine uptake by parasites (respectively, 4.93 and 8.47 microM for strains K1 and Thaï) [2].

References

Metabolism of the alpha,beta-unsaturated ketones, chalcone and trans-4-phenyl-3-buten-2-one, by rat liver microsomes and estrogenic activity of the metabolites. Kohno, Y., Kitamura, S., Sanoh, S., Sugihara, K., Fujimoto, N., Ohta, S. Drug Metab. Dispos. (2005) [Pubmed]
New syntheses and potential antimalarial activities of new 'retinoid-like chalcones'. Valla, A., Valla, B., Cartier, D., Le Guillou, R., Labia, R., Florent, L., Charneau, S., Schrevel, J., Potier, P. European journal of medicinal chemistry. (2006) [Pubmed]

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