National Center of Mass Spectrometry in Changchun, Jilin Province Key Laboratory of Chinese Medicine Chemistry and Mass Spectrometry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China; University of Chinese Academy of Sciences, Beijing 100039, China.
National Center of Mass Spectrometry in Changchun, Jilin Province Key Laboratory of Chinese Medicine Chemistry and Mass Spectrometry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China.
Chin J Nat Med. 2018 Jun;16(6):418-427. doi: 10.1016/S1875-5364(18)30075-X.
Radix Scutellaria is widely applied to the treatment of diabetes mellitus in China. Its main bioactive constituents contain baicalin, wogonoside, oroxyloside, and their aglycones. To investigate the effect of type 2 diabetes mellitus on both pharmacokinetics and tissue distribution of these flavonoid compounds, the six flavonoids in plasma and tissues from the normal and type 2 diabetic rats after oral administration of Radix Scutellaria extract were simultaneously measured by ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method. The results showed that baicalin, wogonoside, and oroxyloside had higher C and AUC values (P < 0.05) in type 2 diabetic rats than that in normal rats and the tissue-distribution behaviors of the six flavonoid compounds in hearts, livers, spleens, lungs, kidneys, brains, pancreas, fat and muscle of the type 2 diabetic rats showed obviously differences from the normal rats (P < 0.05). In conclusion, the differences in the pharmacokinetics of oroxyloside and tissue distribution of the six flavanoids in Radix Scutellaria extract between diabetic and normal rats were found for the first time. The results from the present study provided a crucial basis for a better understanding of in vivo anti-diabetic mechanism of action of the six flavonoids from Radix Scutellaria.
黄芩在临床上被广泛用于治疗糖尿病。其主要生物活性成分包括黄芩苷、黄芩素、汉黄芩苷及其苷元。为研究 2 型糖尿病对黄芩提取物中这 6 种黄酮类化合物药代动力学和组织分布的影响，采用超高效液相色谱-串联质谱（UPLC-MS/MS）法同时测定正常和 2 型糖尿病大鼠灌胃黄芩提取物后血浆和组织中的 6 种黄酮类化合物。结果表明，2 型糖尿病大鼠体内黄芩苷、黄芩素和汉黄芩苷的 C 和 AUC 值均高于正常大鼠（P < 0.05），6 种黄酮类化合物在心脏、肝脏、脾脏、肺脏、肾脏、大脑、胰腺、脂肪和肌肉中的组织分布行为也明显不同于正常大鼠（P < 0.05）。综上所述，首次发现 2 型糖尿病大鼠体内汉黄芩苷的药代动力学和黄芩提取物中 6 种黄酮类化合物的组织分布存在差异。本研究结果为更好地理解黄芩中 6 种黄酮类化合物的体内抗糖尿病作用机制提供了重要依据。
