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Triterpenoids with -glucosidase inhibitory activity and cytotoxic activity from the leaves of Akebia trifoliata

机译:来自葡萄氨酸酶抑制活性的三萜类化合物和来自Akebia Trifoliata叶子的细胞毒性活性

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摘要

Ten pentacyclic triterpenoids including a new multiflorane triterpene acid, 2,3,23-trihydroxymultiflor-7-en-28-oic acid (1), and a new lupane triterpene monoglucoside named akebiaoside C (2), were obtained from the leaves of Akebia trifoliata. Their structures were elucidated by extensive spectroscopic analysis, and they were all isolated from the leaves of A. trifoliata for the first time. These compounds, except 4 and 5, showed in vitro -glucosidase inhibitory activity much stronger than acarbose. Especially, 2, 3, 6, 8 and 10 displayed in vitro -glucosidase inhibitory activity with IC50 values from 0.004 to 0.081 mM, which were close or even more potent than corosolic acid (IC50 0.06 mM). Triterpenoids 1, 8 and 10 were further revealed to show moderate in vitro cytotoxic activity against human tumor A549, HeLa and HepG2 cell lines, with IC50 values ranging from 26.5 to 51.9 M. Compound 9 selectively showed in vitro cytotoxicity toward HeLa and HepG2 cell lines, with IC50 values of 81.49 and 73.47 M, respectively. These findings provided new data to support that the leaves of A. trifoliata are a rich source in bioactive triterpenoids highly valuable to be developed for medicinal usage.
机译:包括新的多氯胺酸,2,3,23-三羟基葡聚糖-7-28-甲酸(1)的十个五胞苷三萜类化合物,以及名为AkebiaSide C(2)的新的Lupane Triterpene单氟葡糖苷,是从Akebia的叶片获得的Trifoliata。通过广泛的光谱分析阐明了它们的结构,它们首次从A. Trifoliata的叶子中分离出来。除了4和5之外,这些化合物的体外 - 葡糖苷酶抑制活性比缺氧更强大。特别是2,3,6,8和10在体外 - 葡糖苷酶抑制活性中显示,IC 50值为0.004至0.081mm,其比碳酸酸(IC50 0.06mm)紧密甚至更有效。进一步揭示三萜1,8和10,以表现对人肿瘤A549,He1和HepG2细胞系的中度体外细胞毒性活性,IC 50值范围为26.5至51.9M.化合物9选择性地向HeLa和HepG2细胞体外显示体外细胞毒性,IC50值分别为81.49和73.47米。这些发现提供了新数据,以支持A. Trifoliata的叶子是生物活性三萜类的富源,对于药用使用而言,具有高价值。

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  • 来源
    《RSC Advances》 |2018年第70期|共7页
  • 作者单位

    South China Agr Univ Coll Forestry &

    Landscape Architecture Guangdong Key Lab Innovat Dev &

    Utilizat Forest P State Key Lab Conservat &

    Utilizat Subtrop Agrobi Guangzhou 510642 Guangdong Peoples R China;

    South China Agr Univ Coll Forestry &

    Landscape Architecture Guangdong Key Lab Innovat Dev &

    Utilizat Forest P State Key Lab Conservat &

    Utilizat Subtrop Agrobi Guangzhou 510642 Guangdong Peoples R China;

    Guangdong Acad Forestry Guangdong Prov Key Lab Silviculture Protect &

    Uti Guangzhou 510520 Guangdong Peoples R China;

    Chinese Acad Sci South China Bot Garden Guangdong Prov Key Lab Appl Bot Guangzhou 510650 Guangdong Peoples R China;

    South China Agr Univ Coll Forestry &

    Landscape Architecture Guangdong Key Lab Innovat Dev &

    Utilizat Forest P State Key Lab Conservat &

    Utilizat Subtrop Agrobi Guangzhou 510642 Guangdong Peoples R China;

    South China Agr Univ Coll Forestry &

    Landscape Architecture Guangdong Key Lab Innovat Dev &

    Utilizat Forest P State Key Lab Conservat &

    Utilizat Subtrop Agrobi Guangzhou 510642 Guangdong Peoples R China;

    Chinese Acad Sci South China Bot Garden Guangdong Prov Key Lab Appl Bot Guangzhou 510650 Guangdong Peoples R China;

    South China Agr Univ Coll Forestry &

    Landscape Architecture Guangdong Key Lab Innovat Dev &

    Utilizat Forest P State Key Lab Conservat &

    Utilizat Subtrop Agrobi Guangzhou 510642 Guangdong Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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