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二烯丙基二硫化物在大鼠体内的代谢:两种新代谢产物的鉴定

In vivo metabolism of diallyl disulphide in the rat: identification of two new metabolites.

作者信息

Germain E, Auger J, Ginies C, Siess M-H, Teyssier C

机构信息

Unité Mixte de Recherche de Toxicologie Alimentaire, Institut National de Recherche Agronomique, BP 86510, 17 rue Sully, F-21065 Dijon cedex, France.

出版信息

Xenobiotica. 2002 Dec;32(12):1127-38. doi: 10.1080/0049825021000017902.

Abstract
  1. Diallyl disulphide (DADS), a compound formed from the organosulphur compounds present in garlic, is known for its anticarcinogenic effects in animal models. 2. The aim was to identify and analyse the metabolites produced in vivo after a single oral administration of 200 mg kg(-1) DADS to rats. The organic sulphur metabolites present in the stomach, liver, plasma and urine were measured by gas chromatography coupled with mass spectrometry over 15 days. 3. Data indicate that DADS is absorbed and transformed into allyl mercaptan, allyl methyl sulphide, allyl methyl sulphoxide (AMSO) and allyl methyl sulphone (AMSO(2)), which are detected throughout the excretion period. Overall, the highest amounts of metabolites were measured 48-72h after the DADS administration. AMSO(2) is the most abundant and persistent of these compounds. The levels of all the sulphur compounds rapidly decline within the first week after administration and disappear during the second week. Only AMSO and AMSO(2) are significantly excreted in urine. 4. These potential metabolites are thought to be active in the target tissues. Our data warrant further studies to check this hypothesis.
摘要
  1. 二烯丙基二硫化物(DADS)是一种由大蒜中存在的有机硫化合物形成的化合物,其在动物模型中的抗癌作用已为人所知。2. 目的是鉴定和分析大鼠单次口服200 mg kg⁻¹ DADS后体内产生的代谢产物。在15天内,通过气相色谱-质谱联用技术测定胃、肝脏、血浆和尿液中存在的有机硫代谢产物。3. 数据表明,DADS被吸收并转化为烯丙基硫醇、烯丙基甲基硫醚、烯丙基甲基亚砜(AMSO)和烯丙基甲基砜(AMSO₂),在整个排泄期均能检测到。总体而言,在给予DADS后48 - 72小时测得的代谢产物量最高。AMSO₂是这些化合物中含量最丰富且持续时间最长的。所有硫化合物的水平在给药后的第一周内迅速下降,并在第二周内消失。只有AMSO和AMSO₂在尿液中有明显排泄。4. 这些潜在的代谢产物被认为在靶组织中具有活性。我们的数据值得进一步研究以验证这一假设。

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