Isolation of Luteolin and Luteolin-7-O-glucoside from Dendranthema morifolium Ramat Tzvel and Their Pharmacokinetics in Rats

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• 作者：Lie-Chwen Lin ; Yu-Feng Pai ; Tung-Hu Tsai
• 刊名：Journal of Agricultural and Food Chemistry
• 出版年：2015
• 出版时间：September 9, 2015
• 年：2015
• 卷：63
• 期：35
• 页码：7700-7706
• 全文大小：304K
• ISSN：1520-5118

文摘

Luteolin and luteolin-7-O-glucoside were isolated from the ethanolic extract of Dendranthema morifolium Ramat Tzvel. The structures of these analytes were identified by nuclear magnetic resonance (¹H and ¹³C NMR) and mass spectrometry. Ethanolic and water extracts contained luteolin-7-O-glucoside at 4.19 and 6.56%, respectively. However, the level of luteolin was only 0.19% in the ethanolic extract, and luteolin was not detected in the water extract. To examine the pharmacokinetics and bioavailability of luteolin and luteolin-7-O-glucoside in rats, parallel studies of luteolin (10 mg/kg, iv; and 100 mg/kg, po) and luteolin-7-O-glucoside (10 mg/kg, iv; and 1 g/kg, po) were conducted. The analytes were detected by high-performance liquid chromatography coupled with a photodiode array detector. A phenyl-hexyl (150 脳 4.6 mm iv; 5.0 渭m) column was used to separate the analytes from the biological samples. The pharmacokinetic data demonstrate that the areas under the concentration curves (AUCs) of luteolin were 261 卤 33 and 611 卤 89 (min 渭g/mL) after luteolin administration (10 mg/kg, iv; and 100 mg/kg, po, respectively). The oral bioavailability of luteolin was 26 卤 6%. The AUCs of luteolin-7-O-glucoside were 229 卤 15 and 2109 卤 350 (min 渭g/mL) after administration of luteolin-7-O-glucoside (10 mg/kg, iv; and 1 g/kg, po, respectively). The oral bioavailability of luteolin-7-O-glucoside was approximately 10 卤 2%. In the group that received luteolin-7-O-glucoside orally, a biotransformed luteolin product was detected, but this product was not detected in the group that received luteolin-7-O-glucoside intravenously. The biotransformation ratio of luteolin to luteolin-7-O-glucoside (the AUC ratio of metabolite/parent compound) was approximately 48.78 卤 0.12%. These results demonstrate that luteolin-7-O-glucoside is primarily hydrolyzed to luteolin in the gastrointestinal tract and then absorbed into the systemic circulation.