Sulforaphane is currently found in vegetables in the anti-cancer ability is one of the best active ingredients, it does not directly present in vegetables, a kind of isothiocyanates compounds but when chewing or harvested by myrosinase enzyme release solution is obtained. It has extensive biological activities, such as can induce beneficial phase Ⅱ enzyme activity, inhibition of enzyme activity, thus effectively preventing cancer, in addition to strong light protective effect, in recent years the incidence of cancer is higher and higher, so the radish sulfur has broad market prospects, more and more attention. Chemical synthesis of sulforaphane a series of derivatives in the beginning, generated by 1,4- dibromobutane with phthalic imide reaction of alkane two a potassium salt, and potassium thioacetate reaction of ester, ester with the acid catalyzed hydrolysis of the important intermediate of mercaptan, mercaptan and different bromination reaction generating sulfide using Gabriel method, Bo amine, amine and carbon disulfide, methyl sulfonyl chloride reaction of isothiocyanates, finally by m-CPBA oxidation by sulforaphane derivatives, MTT method was used to test anticancer activity.
萝卜硫素是目前在蔬菜中发现的抗癌能力最好的活性成分之一,它并不直接存在于蔬菜中,而是在咀嚼或收割的时候由释放出的黑芥子酶酶解得到的一种异硫氰酸酯化合物。它具有广泛的生物活性,如可以诱导产生对身体有益的Ⅱ相酶的活性,抑制Ⅰ相酶的活性,从而有效地预防癌症,除此之外还有较强的光防护作用,近年来癌症发病率越来越高,因此萝卜硫素有广阔的市场前景,越来越引起人们的关注。本文用化学合成法合成萝卜硫素一系列衍生物,开始用1,4-二溴丁烷与邻苯二甲酰亚胺钾盐反应生成烷烃,后与硫代乙酸钾反应生成酯,所得的酯用酸催化水解得到硫醇这一重要中间体,硫醇与不同的溴代物反应生成硫醚,用Gabriel法制得伯胺,伯胺与二硫化碳、甲基磺酰氯反应生成异硫氰酸酯,最后用m-CPBA氧化得到萝卜硫素衍生物,后用MTT法测试抗癌活性。
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Sulforaphane is found in vegetables cancer-fighting ability of the best active ingredients, it does not directly present in vegetables, but in chewing or harvest time by the release of myrosinase enzyme obtained a kind of isothiocyanate compounds. It has a wide range of biological activity, such as health benefits can induce phase Ⅱ enzyme activity, inhibition phase Ⅰ enzyme activity, thus effectively preventing cancer, in addition to a strong protective effect of light in recent years, cancer increasing incidence, therefore sulforaphane known broad market prospects, more cause for concern. This synthesis method using chemical sulforaphane derivative series, starting with 1,4 - dibromo-butane with potassium phthalimide reaction alkane, after reaction with potassium thioacetate ester, and the resulting acid catalyzed ester hydrolysis of the key intermediate thiol, thiol reaction bromide different sulfide, with Gabriel method were primary amine, a primary amine with carbon disulfide, the reaction of methyl sulfonyl chloride isothiocyanate, Finally, m-CPBA oxidation of sulforaphane derivatives tested by MTT assay after anticancer activity.
Sulforaphane is currently found in vegetables in the anti-cancer ability is one of the best active ingredients, it does not directly present in vegetables, a kind of isothiocyanates compounds but when chewing or harvested by myrosinase enzyme release solution is obtained. It has extensive biological activities, such as can induce beneficial phase Ⅱ enzyme activity, inhibition of enzyme activity, thus effectively preventing cancer, in addition to strong light protective effect, in recent years the incidence of cancer is higher and higher, so the radish sulfur has broad market prospects, more and more attention. Chemical synthesis of sulforaphane a series of derivatives in the beginning, generated by 1,4- dibromobutane with phthalic imide reaction of alkane two a potassium salt, and potassium thioacetate reaction of ester, ester with the acid catalyzed hydrolysis of the important intermediate of mercaptan, mercaptan and different bromination reaction generating sulfide using Gabriel method, Bo amine, amine and carbon disulfide, methyl sulfonyl chloride reaction of isothiocyanates, finally by m-CPBA oxidation by sulforaphane derivatives, MTT method was used to test anticancer activity.答案来自me~~~~~~~~~~~~~~
Sulforaphane is found in vegetables, anti-cancer ability to one of the best active ingredient, it does not exist in vegetables directly, but rather in chewing or the harvest by the release of myrosinase digestion of a isothiocyanates compounds. It has extensive biological activity, such as can be induced to body good Ⅱ phase enzyme activity, the activity of the enzyme inhibition Ⅰ phase, thus effectively prevent cancer, in addition to strong light protection, and cancer incidence in recent years, more and more high, so the radish sulfur has broad market prospect, more and more aroused people's concern. This paper use chemical synthesis method of synthesis of sulforaphane, a series of derivatives with 1, 4 - dibromobutane with phthalates formyl imine potassium reacts alkanes, after reaction with thioacetic acid potassium generated ester, the ester catalyzed by acid hydrolysis is mercaptan this important intermediates, mercaptan and different bromine generation reaction sulfur ether, by Gabriel, primary amine, primary amine and carbon disulfide, methyl sulfonyl chloride reaction generates isothiocyanates, finally with the m - CPBA oxidation sulforaphane derivatives, antitumor activity by determined by MTT method after testing.