| 柚皮苷的人肠内菌生物转化(英文) |
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| 引用本文： | 冉丽,吴帅,徐嵬,张友波,杨秀伟.柚皮苷的人肠内菌生物转化(英文)[J].中国药学,2013,22(4):329-333. |
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| 作者姓名： | 冉丽 吴帅 徐嵬 张友波 杨秀伟 |
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| 作者单位： | 北京大学医学部天然药物及仿生药物国家重点实验室;药学院天然药物学系,北京100191 |
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| 基金项目： | National Sciences and Technology Program of China （Grant No. 2011BAI07B08）; “Major New Medicine Project” in Mega-projects of Science Research of China （Grant No. 2009ZX09301-010） |
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| 摘 要： | 柚皮苷(1)是酸橙中含量最高的二氢黄酮苷类化合物, 将其与人肠内菌丛共温孵, 从温孵物中通过色谱方法得到原形化合物1和四个转化产物 (2-5), 根据谱学数据确定它们分别为柚皮苷-6"-乙酰物(2)、柚皮素(3)、根皮酸(4)和间苯三酚(5)。在1的糖苷链葡萄糖基6位能够特异性地发生乙酰化作用。1口服难以吸收。本文结果为阐明其生物利用度低提供了实验依据, 推测表现其生物活性的物质基础主要是其肠内菌生物转化产物3。肠内菌丛所致1的生物转化的继发结果,是它的转化产物吸收进入体循环发挥生物学作用, 此结果为进一步或再评价其体内过程、作用或毒性及其生物利用度提供了有用的信息。
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| 关 键 词： | 柚皮苷 柚皮素 柚皮苷-6"-乙酰物 生物转化 人肠内菌丛 |
Biotransformation of naringin by human intestinal flora |
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| Li Ran,Shuai Wu,Wei Xu,Youbo Zhang,Xiuwei Yang.Biotransformation of naringin by human intestinal flora[J].Journal of Chinese Pharmaceutical Sciences,2013,22(4):329-333. |
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| Authors: | Li Ran Shuai Wu Wei Xu Youbo Zhang Xiuwei Yang |
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| Affiliation: | ＊ State Key Laboratory of Natural and Biomimetic Drugs,＂ Department of Natural Medicines, School of Pharmaceutical Sciences Peking University Health Science Center, Beijing 100191, China |
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| Abstract: | Naringin （1）, the highest-content flavanone glycoside in sour oranges, was incubated with human intestinal flora, and four biotransforrnation products （2-5） were obtained from the incubated mixture by chromatographic methods. The chemical structures of the four products were elucidated as naringin-6＂acetate （2）, naringenin （3）, phloretic acid （4）, and phloroglucinol （5） on the basis of their spectroscopic data. Naringin-6＂-acetate was specifically formed by acetylation at C6-OH of glucosyl group of 1. The result obtained in the present research could account for the lower bioavailability of 1 after oral administration, suggesting that some biological properties of 1 in vivo may be mediated by its intestinal flora converted product 3. The biotransforrnation of 1 by intestinal flora leading to their systemic absorption deserves further attention and may provide valuable insights into pre-systemic drug metabolism, delivery or toxicity. |
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| Keywords: | Naringin Naringenin Naringin-6-acetate Biotransformation Human intestinal flora |
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