Chemoprotective isothiocyanates
    6.
    再颁专利
    Chemoprotective isothiocyanates 失效
    化学保护异硫氰酸酯

    公开(公告)号:USRE36784E

    公开(公告)日:2000-07-18

    申请号:US850387

    申请日:1997-05-02

    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.

    Abstract translation: 已经分离出了萝卜硫烷,并将其鉴定为西兰花中的主要且非常有效的II期酶诱导剂(Brassica oleracea italica)。 Sulforaphane是单功能诱导剂,不依赖于芳基受体依赖的细胞色素P-450(I期酶)的诱导而选择性地诱导II期酶。 合成了硫的氧化态和亚甲基数的不同的类似物,测定了它们的诱导效力。 磺吡烟是这些类似物中最有效的。 还合成了具有不同取代基的其他类似物代替萝卜硫代甲基亚磺酰基,并进行了评估。 其中最有效的是6-异硫氰酸根合-2-己酮和外-2-乙酰基-6-异硫氰基降冰片烷。

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