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三种不同的Mitragyna speciosa korth 叶提取物对 II 相药物代谢酶-谷胱甘肽转移酶(GSTs)的体内外作用。

In vitro and in vivo effects of three different Mitragyna speciosa korth leaf extracts on phase II drug metabolizing enzymes--glutathione transferases (GSTs).

机构信息

Centre for Drug Research, Universiti Sains Malaysia, 11800 USM Penang, Malaysia.

出版信息

Molecules. 2010 Jan 20;15(1):432-41. doi: 10.3390/molecules15010432.

Abstract

In the present study, we investigate the effects of three different Mitragyna speciosa extracts, namely methanolic, aqueous and total alkaloid extracts, on glutathione transferase-specific activity in male Sprague Dawley rat liver cytosol in vitro and in vivo. In the in vitro study, the effect of Mitragyna speciosa extracts (0.01 to 750 microg/mL) against the specific activity of glutathione transferases was examined in rat liver cytosolic fraction from untreated rats. Our data show concentration dependent inhibition of cytosolic GSTs when Mitragyna speciosa extract was added into the reaction mixture. At the highest concentration used, the methanolic extract showed the highest GSTs specific activity inhibition (61%), followed by aqueous (50%) and total alkaloid extract (43%), respectively. In in vivo study, three different dosages; 50, 100 and 200 mg/kg for methanolic and aqueous extracts and 5, 10 and 20 mg/kg for total alkaloid extract were given orally for 14 days. An increase in GST specific activity was generally observed. However, only Mitragyna speciosa aqueous extract with a dosage of 100 mg/kg showed significant results: 129% compared to control.

摘要

在本研究中,我们研究了三种不同的美沙酮提取物,即甲醇、水和总生物碱提取物,对雄性 Sprague Dawley 大鼠肝胞浆谷胱甘肽转移酶特异性活性的体外和体内影响。在体外研究中,我们在未处理大鼠的肝胞浆部分中,检查了美沙酮提取物(0.01 至 750 微克/毫升)对谷胱甘肽转移酶特异性活性的影响。我们的数据显示,当美沙酮提取物加入反应混合物中时,细胞溶质 GSTs 呈浓度依赖性抑制。在使用的最高浓度下,甲醇提取物显示出最高的 GSTs 特异性活性抑制(61%),其次是水提取物(50%)和总生物碱提取物(43%)。在体内研究中,我们分别给予 50、100 和 200mg/kg 的甲醇和水提取物,以及 5、10 和 20mg/kg 的总生物碱提取物,连续口服 14 天。通常观察到 GST 特异性活性增加。然而,只有美沙酮水提取物的剂量为 100mg/kg 时显示出显著的结果:与对照组相比增加了 129%。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3416/6256986/d89e07614cd3/molecules-15-00432-g001.jpg

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