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倍半萜类化合物氧化β-石竹烯和反式橙花叔醇对小鼠体内外源性物质代谢酶的影响。

The impact of sesquiterpenes β-caryophyllene oxide and trans-nerolidol on xenobiotic-metabolizing enzymes in mice in vivo.

作者信息

Lněničková Kateřina, Svobodová Hana, Skálová Lenka, Ambrož Martin, Novák Filip, Matoušková Petra

机构信息

a Faculty of Pharmacy, Charles University , Hradec Králové , Czech Republic.

出版信息

Xenobiotica. 2018 Nov;48(11):1089-1097. doi: 10.1080/00498254.2017.1398359. Epub 2017 Nov 10.

Abstract
  1. Sesquiterpenes, constituents of plant essential oil, are popular bioactive compounds due to the positive effect on human health, but their potential toxicity and possible herb-drug interactions are often omitted. In our in vivo study, we followed up the effect of p.o. administration of two sesquiterpenes β-caryophyllene oxide (CAO) and trans-nerolidol (NER) on various xenobiotic-metabolizing enzymes in mice liver and small intestine. 2. To spot the early effect of studied compounds, enzymatic activity and mRNA levels were assessed 6 and 24 h after single dose. 3. CAO and NER markedly increased cytochromes P450 (CYP2B, 3A, 2C) activity and mRNA levels in both tissues. Liver also showed elevated activity of aldo-ketoreductase 1C and carbonyl reductase after treatment. Contrary, sesquiterpenes decreased NAD(P)H:quinone oxidoreductase 1 activity in small intestine. Among conjugation enzymes, only liver sulfotransferase activity was increased by sesquiterpenes. 4. Our results document that single dose of sesquiterpenes modulate activities and expression of several xenobiotic-metabolizing enzymes.
摘要
  1. 倍半萜类化合物是植物精油的成分,因其对人体健康有积极作用而成为受欢迎的生物活性化合物,但它们的潜在毒性和可能的药草-药物相互作用常常被忽视。在我们的体内研究中,我们追踪了口服两种倍半萜类化合物氧化β-石竹烯(CAO)和反式橙花叔醇(NER)对小鼠肝脏和小肠中各种外源性物质代谢酶的影响。2. 为了发现所研究化合物的早期作用,在单次给药后6小时和24小时评估酶活性和mRNA水平。3. CAO和NER显著增加了两种组织中细胞色素P450(CYP2B、3A、2C)的活性和mRNA水平。处理后,肝脏中醛酮还原酶1C和羰基还原酶的活性也有所升高。相反,倍半萜类化合物降低了小肠中NAD(P)H:醌氧化还原酶1的活性。在结合酶中,只有肝脏磺基转移酶的活性因倍半萜类化合物而增加。4. 我们的结果表明,单次剂量的倍半萜类化合物可调节几种外源性物质代谢酶的活性和表达。

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