Use of silkworms for identification of drug candidates having appropriate pharmacokinetics from plant sources.
Use of silkworms for identification of drug candidates having appropriate pharmacokinetics from plant sources.
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DOI：
10.1186/1471-2210-10-7
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发表时间：
2010-06-11
期刊：
影响因子：
--
通讯作者：
Sekimizu K
中科院分区：
文献类型：
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作者：
Asami Y;Horie R;Hamamoto H;Sekimizu K
我们使用蚕来评估候选药物的治疗效果。我们以前的研究表明，化学品在蚕和哺乳动物体内有共同的药代动力学机制。本研究试图建立一种利用家蚕来鉴定植物提取物中的化学物质的方法，这些化学物质可以从肠道吸收，也可以稳定地存在于体液中。用高效液相色谱法分析了从橙子皮中提取的中草药清剂的丙酮提取物在家蚕血淋巴中的含量。经质谱和核磁共振谱分析，确定化合物为川陈皮素、七甲氧基黄酮和橘子素。据报道，这些化合物在哺乳动物血液中稳定。这些化合物在家蚕血淋巴中的半衰期分别为18、26和34 h。这些发现表明，蚕可以用作模型动物，以容易地鉴定具有适当药代动力学行为的化合物。
We use silkworms to evaluate therapeutic effects of drug candidates. Our previous reports have revealed that there are common mechanisms of pharmacokinetics of chemicals in silkworms and mammals. In this report, we attempt to establish a method by using silkworms to identify chemicals from plant extracts which are absorbed from intestine and also stably exist in body fluids. Three compounds were detected in the silkworm hemolymph by HPLC analysis after midgut injection of acetone extracts of seihi, an herbal medicine obtained from orange peel. Analyses with MS and NMR revealed that the compounds were nobiletin, heptamethoxyflavone, and tangeretin. These compounds are reported to be stable in mammalian blood. The half-life of each of these compounds in the silkworm hemolymph was 18, 26 and 34 h, respectively. These findings suggest that silkworms can be used as a model animal to easily identify compounds with appropriate pharmacokinetic behavior.