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波罗蜜中异戊烯基取代多酚作为培养的黑色素瘤细胞中黑色素生物合成抑制剂的构效关系

Structure-activity relationship of prenyl-substituted polyphenols from Artocarpus heterophyllus as inhibitors of melanin biosynthesis in cultured melanoma cells.

作者信息

Arung Enos Tangke, Shimizu Kuniyoshi, Kondo Ryuichiro

机构信息

Department of Forest Product, Faculty of Forestry, Mulawarman University, Samarinda, East Kalimantan, 75123, Indonesia.

出版信息

Chem Biodivers. 2007 Sep;4(9):2166-71. doi: 10.1002/cbdv.200790173.

Abstract

A series of prenylated, flavone-based polyphenols, compounds 1-8, were isolated from the wood of Artocarpus heterophyllus. These compounds, which have previously been shown not to inhibit tyrosinase activity, were found to be active inhibitors of the in vivo melanin biosynthesis in B16 melanoma cells, with little or no cytotoxicity. To clarify the structural requirement for inhibition, some structure-activity relationships were studied, in comparison with related compounds lacking prenyl side chains. Our experiments indicate that both prenyl and OH groups, as well as the type of substitution pattern, are crucial for the inhibition of melanin production in B16 melanoma cells.

摘要

从菠萝蜜的木材中分离出了一系列基于黄酮的异戊烯化多酚化合物1-8。这些化合物此前已被证明不抑制酪氨酸酶活性,但被发现是B16黑色素瘤细胞体内黑色素生物合成的活性抑制剂,几乎没有细胞毒性。为了阐明抑制作用的结构要求,与缺乏异戊烯侧链的相关化合物相比,研究了一些构效关系。我们的实验表明,异戊烯基和羟基以及取代模式的类型对于抑制B16黑色素瘤细胞中的黑色素生成至关重要。

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