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林产化学与工业 ›› 2016, Vol. 36 ›› Issue (1): 112-118.doi: 10.3969/j.issn.0253-2417.2016.01.016

• 研究报告 • 上一篇    下一篇

桉叶月见草素B的单体制备及其体内外稳定性研究

曹素芳1, 陈运娇1, 陈洪璋2, 欧阳文3, 叶锡光1, 曹庸1, 赵力超1   

  1. 1. 华南农业大学 食品学院, 广东 广州 510642;
    2. 无限极(中国)有限公司, 广东 新会 529100;
    3. 湖南中医药大学 药学院, 湖南 长沙 410208
  • 收稿日期:2014-12-24 出版日期:2016-02-25 发布日期:2016-03-18
  • 通讯作者: 赵力超(1979-),男,副教授,博士,主要从事功能食品的高新加工技术研究;E-mail:zlc@scau.edu.cn。 E-mail:zlc@scau.edu.cn
  • 作者简介:曹素芳 (1989-),女,湖南宜章人,硕士生,主要从事食品化学与营养方向研究工作
  • 基金资助:
    国家自然科学基金资助项目(31301445);林业重大公益性行业科研专项(201104003-03);广东省自然科学基金博士启动项目(2015A030310118)

Preparation and in vitro and in vivo Stability of Oenothein B from Eucalyptus Leaves

CAO Su-fang1, CHEN Yun-jiao1, CHEN Hong-zhang2, OUYANG Wen3, YE Xi-guang1, CAO Yong1, ZHAO Li-chao1   

  1. 1. College of Food Science, South China Agricultural University, Guangzhou 510642, China;
    2. Infinitus(China) Co. Ltd., Xinhui 529100, China;
    3. School of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, China
  • Received:2014-12-24 Online:2016-02-25 Published:2016-03-18

摘要: 采用乙醇提取、大孔树脂吸附、中压柱层析和制备液相等方法从桉叶中分离得到月见草素B(OEB)单体,并对其结构进行了鉴定,分析了OEB在不同极性溶剂中的溶解度,同时考察了热处理条件、pH值及酶的作用对OEB损失率的影响,然后追踪了其在小鼠体内代谢过程,以综合评价OEB的体内外稳定性。结果表明:桉叶醇提所得粗提物经大孔树脂吸附、柱层析及制备液相纯化后可获得OEB单体化合物,纯度 94.85%,得率(以桉叶干质量计)2.50%;OEB在水中的溶解度大于其他有机溶剂,热处理温度、pH值、酶的种类及浓度均对OEB的稳定性有影响,高温(>80℃)、碱性条件(pH值>7)和胰蛋白酶、脂肪酶对OEB的损失率影响更大,损失率最大可达 98.85%;OEB在离体血浆作用后出现新组分且损失明显;OEB在小鼠体内的代谢过程表明其在体内胃肠道中均不稳定、易分解,不能直接进入血液,也不能以原型化合物的形式抵达粪便及尿液中。由此可见,OEB在体内外均不稳定,这将为阐明OEB的体内代谢途径及进一步提高其稳定性提供理论依据。

关键词: 桉叶, 月见草素B, 单体制备, 稳定性

Abstract: Oenothein B(OEB) has strong anti-oxidative and antineoplastic activities.It can be developed into functional health food, food antioxidant and other products.Few researches are done on its application because of a scarcity of nature resources and its low bioavailability.In this article, a method of large scale preparation of OEB from eucalyptus leaves was studied by extracting with ethanol, adsorbing through the macroporous resin, medium pressure column chromatography and preparative liquid phase.The structure of OEB was further identified.In addition, the solubility of OEB was analyzed in different polar solvents.Meanwhile, the loss ratio of OEB was measured by dealing with heating temperature, pH values and enzymes.Finally, the metabolic process of OEB was traced in mice to estimate the stability of OEB in vivo and in vitro comprehensively.The results showed that OEB could be purified by column chromatography and pre-HPLC with the purity of 94.85% and the yield of 2.50% in weight of dried eucalyptus.OEB was easily decomposed with maximum 98.85% by solvents, heating temperature, pH and enzymes with different types and concentration.OEB was disappeared clearly and new components appeared after affecting with plasma in vitro.It was also indicated that OEB was unstable in mice and easy to decompose.It could not be absorbed directly into the blood, and also could not arrive in the feces and urine in the form of prototype compounds.Therefore, OEB is unstable in vivo and in vitro.This result provides theoretical basis for elucidating the metabolic pathway in vivo and in vitro as well as for further study on the improvement of OEB stability.

Key words: Eucalyptus leaves, oenothein B, monomer preparation, stability

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