Chemoprotective isothiocyanates

Details Chemoprotective isothiocyanates Chemoprotective isothiocyanates

1997-05-02

2000-07-18

McKane, Joseph

Drug, bio-affecting and body treating compositions

Enzyme or coenzyme containing

426 49, 426 52, 426547, 426615, 424648, 424655, 514514, 514515, 558 17, A61K 3843, C07C33104

Patent

active

RE0367842

ABSTRACT:
Sulforaphane has been isolated and identified as a major and very potent phase II enzyme inducer in broccoli (Brassica oleracea italica). Sulforaphane is a monofunctional inducer, inducing phase II enzymes selectively without the induction of aryl hydrocarbon receptor-dependent cytochromes P-450 (phase I enzymes). Analogues differing in the oxidation state of sulfur and the number of methylene groups were synthesized, and their inducer potencies were measured. Sulforaphane is the most potent of these analogues. Other analogues having different substituent groups in place of the methylsulfinyl group of sulforaphane were also synthesized and assessed. Of these, the most potent are 6-isothiocyanato-2-hexanone and exo-2-acetyl-6-isothiocyanatonorbornane.

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