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来自 Desmos cochinchinensis 的杂种黄烷-查耳酮、芳香酶和脂氧合酶抑制剂。

Hybrid flavan-chalcones, aromatase and lipoxygenase inhibitors, from Desmos cochinchinensis.

机构信息

Chulabhorn Graduate Institute, and the Center for Environmental Health, Toxicology and Management of Chemicals (ETM), Chemical Biology Program, Vibhavadi-Rangsit Road, Bangkok 10210, Thailand.

出版信息

Phytochemistry. 2011 Nov;72(16):2062-7. doi: 10.1016/j.phytochem.2011.07.002. Epub 2011 Jul 28.

Abstract

Hybrid flavan-chalcones, desmosflavans A (1) and B (2), together with three known compounds, cardamonin (3), pinocembrin (4) and chrysin (5), were isolated from leaves of Desmos cochinchinensis. Cardamonin (3) and chrysin (5) exhibited potent antioxidant activity with 15.0 and 12.2 ORAC units. Desmosflavans A (1) and B (2), pinocembrin (4), and chrysin (5) were found to be inhibitors of aromatase with respective IC50 values of 1.8, 3.3, 0.9, and 0.8 μM. Desmosflavan A (1) inhibited lipoxygenase with the IC50 value of 4.4 μM. Desmosflavan A (1) exhibited cytotoxic activity with IC50 values of 0.29-3.75 μg/mL, while desmosflavan B (2) showed IC50 values of 1.71-27.0 μg/mL.

摘要

从 Desmos cochinchinensis 的叶子中分离得到了混合黄酮查耳酮、德斯莫斯黄酮 A(1)和 B(2),以及三种已知化合物,小豆蔻素(3)、松属素(4)和白杨素(5)。小豆蔻素(3)和白杨素(5)表现出很强的抗氧化活性,分别具有 15.0 和 12.2 的 ORAC 单位。德斯莫斯黄酮 A(1)和 B(2)、松属素(4)和白杨素(5)被发现是芳香酶抑制剂,其 IC50 值分别为 1.8、3.3、0.9 和 0.8 μM。德斯莫斯黄酮 A(1)对脂氧合酶的抑制作用,IC50 值为 4.4 μM。德斯莫斯黄酮 A(1)具有细胞毒性活性,IC50 值为 0.29-3.75 μg/mL,而德斯莫斯黄酮 B(2)的 IC50 值为 1.71-27.0 μg/mL。

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