Detection of baicalin metabolites baicalein and oroxylin-a in mouse pancreas and pancreatic xenografts.
Detection of baicalin metabolites baicalein and oroxylin-a in mouse pancreas and pancreatic xenografts.
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DOI：
10.1097/mpa.0b013e318232e130
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发表时间：
2012-05
期刊：
影响因子：
2.9
通讯作者：
Go VL
中科院分区：
文献类型：
--
作者：
Lu QY;Zhang L;Moro A;Chen MC;Harris DM;Eibl G;Go VL
黄芩由于其潜在的多种治疗作用，一直是研究的热点。本研究在异种移植动物模型中，检测黄芩素、枸杞素、oroxylin A及其葡萄糖醛酸苷/硫酸盐结合代谢物在血浆、结肠、小肠、肺、肝、胰腺、肾脏和前列腺组织以及胰腺肿瘤中的分布。此外，我们还检测了黄芩苷在这些组织中的代谢稳定性。以裸鼠皮下注射3×106人胰腺癌MiaPaCa-2细胞制备小鼠异种移植瘤模型。试验小鼠随机分为对照饲粮（AIN76A）和1% SB饲粮（每组8只），试验期13周。采用高压液相色谱法，酶解后提取小鼠组织中黄芩素、枸杞素、oroxlin A及其偶联物的含量。大量黄芩苷（34-63%）在吸收过程中被甲基化成oroxylin A及其缀合物。虽然血浆中主要含有黄芩素、沃草素和欧oxylin A的偶联物，但在研究的所有其他组织和肿瘤中都发现了苷元和偶联物。在靶组织中发现了大量的生物活性代谢物积累，这表明SB作为胰腺癌的预防或辅助补充剂具有很大的潜力。
Scutellaria baicalensis has been a subject of research interests due to its potential multiple therapeutic benefits. This study was to examine the distribution of baicalein, wogonin, oroxylin A and their glucuronide/sulfate conjugated metabolites in plasma, colon, small intestine, lung, liver, pancreas, kidney, and prostate tissues and in pancreatic tumor in a xenograft animal model. In addition, we examined metabolic stability of baicalin in these tissues. A mouse xenograft model was prepared by injection of 3×106 human pancreatic cancer MiaPaCa-2 cells subcutaneously into nude mice. Mice were randomly allocated to control diet (AIN76A) and 1% SB diet (n=8 per group) for 13 weeks. Levels of baicalein, wogonin, oroxylin A, and their conjugates in mouce tissues were measured by high-pressure liquid chromatography following enzymatic hydrolysis and then extraction. A substantial amount of baicalin (34–63%) was methylated to oroxylin A and its conjugates in various organs during absorption. While plasma contained predominantly conjugates of baicalein, wogonin, and oroxylin A, both aglycones and conjugates were found in all other tissues investigated and in tumor. Substantial accumulation of bioactive metabolites are found in target tissues, suggesting strong potential for SB use as a preventive or adjuvant supplement for pancreatic cancer.