生熟大黄总提取物灌胃给药后游离蒽醌在SD大鼠组织中的分布差异研究

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大黄应用范围广、疗效确切,然而近年来国内外实验报道大黄中蒽醌成分具有肝、肾细胞毒性。本文对比研究了生熟大黄总提取物灌胃给药后游离蒽醌在正常SD大鼠组织中的分布。肝、脾和肾组织中游离蒽醌类成分含量采用UPLC-MS/MS法测定。生熟大黄总提物(相当于生药量14.69 g.kg-1)灌胃给药,连续12周。结果表明,游离蒽醌在生大黄组大鼠组织中的分布浓度高于熟大黄组;大黄游离蒽醌在同一组织中的分布浓度顺序大致为大黄酸>大黄素>芦荟大黄素;大黄酸在肝、脾和肾组织中的分布浓度明显高于芦荟大黄素和大黄素,且大黄酸在生大黄组的组织分布浓度明显高于熟大黄组;停药恢复4周后,大黄游离蒽醌在组织中检测不到。结果提示生大黄的组织毒性可能高于熟大黄;大黄酸可能是大黄主要的毒性物质之一;大黄游离蒽醌在组织中可能无蓄积毒性。炮制过程不仅影响了有效成分的含量还可能影响其成分的组成,通过影响吸收和作用过程中成分之间的相互作用,致使生大黄组动物组织中游离蒽醌的分布浓度高于熟大黄组,这与传统中医药理论炮制减毒的思想认识基本一致。 Rhubarb has a wide range of applications and exact therapeutic effects. However, anthraquinone components in rhubarb have been reported to have liver and kidney cytotoxicity in recent years. In this paper, we compared the distribution of free anthraquinones in normal SD rats after oral administration of the total extract of rhubarb. The contents of free anthraquinones in liver, spleen and kidney were determined by UPLC-MS / MS. Health cooked rhubarb extract (equivalent to crude drug dose 14.69 g.kg-1) administered orally for 12 weeks. The results showed that the concentration of free anthraquinone in the tissue of the rhubarb group was higher than that in the mature rhubarb group. The order of distribution of free anthraquinone in the same tissue was roughly rhein> emodin> aloe-emodin; The concentration distribution of liver, spleen and kidney was significantly higher than that of aloe-emodin and emodin, and the tissue distribution of rhein in the rhubarb group was significantly higher than that of the mature rhubarb group. After resuming for 4 weeks, Not detected in the organization. The results suggest that the tissue toxicity of rhubarb may be higher than that of ripe rhubarb; rhein may be one of the main toxic substances rhubarb; anthraquinones rhubarb may be no accumulation in the tissue toxicity. Processing process not only affected the content of active ingredients may also affect the composition of its composition, by affecting the absorption and interaction between the ingredients in the process of action, resulting in the crude rhubarb tissue free anthraquinone concentration distribution of cooked rhubarb group, This is consistent with traditional Chinese medicine theory concocted thinking of attenuating.
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