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使用基于昆虫细胞的阻抗谱探究樟芝分离物的抑制作用:抑制作用与化学结构的关系

Probing inhibitory effects of Antrodia camphorata isolates using insect cell-based impedance spectroscopy: inhibition vs chemical structure.

作者信息

Male Keith B, Rao Yerra Koteswara, Tzeng Yew-Min, Montes Johnny, Kamen Amine, Luong John H T

机构信息

Biotechnology Research Institute, National Research Council Canada, Montreal, Quebec, Canada.

出版信息

Chem Res Toxicol. 2008 Nov;21(11):2127-33. doi: 10.1021/tx800202a.

DOI:10.1021/tx800202a
PMID:18816072
Abstract

A continuous online technique based on electric cell-substrate impedance sensing (ECIS) was used for probing inhibitory effects on Spodoptera frugiperda Sf9 insect cells exposed to structurally similar compounds isolated and purified from the fruiting bodies of the fungus Antrodia camphorata. Such chemicals consisted of three ergostane-related steroids and five lanosta-related triterpenes, which are known for their diverse properties and use in the formulation of nutraceuticals and functional foods. The half-inhibition concentration (ECIS(50)), the level at which 50% inhibition of the resistance response was obtained, was determined from the response function to establish inhibitory effects of the different isolates. A slight change in their chemical structures resulted in significant effects on inhibition as probed by impedance spectroscopy. The ergostane-related steroids were mostly inhibitory, but replacing their ketone groups with hydrogen or hydroxyl groups significantly reduced the inhibition. Similarly, the addition of methyl or carboxymethyl groups also lowered the inhibition. Removal of the double bond conjugation within the rings (sulfurenic acid) of the isolate drastically reduced the inhibition.

摘要

一种基于细胞-基质阻抗传感(ECIS)的连续在线技术被用于探究从樟芝子实体中分离纯化出的结构相似化合物对草地贪夜蛾Sf9昆虫细胞的抑制作用。这类化学物质包括三种与麦角甾烷相关的类固醇和五种与羊毛甾烷相关的三萜,它们因其多样的特性以及在营养保健品和功能性食品配方中的应用而闻名。通过响应函数确定半数抑制浓度(ECIS(50)),即获得50%抗性反应抑制水平时的浓度,以确定不同分离物的抑制效果。正如通过阻抗谱所探测的那样,它们化学结构的轻微变化会对抑制产生显著影响。与麦角甾烷相关的类固醇大多具有抑制作用,但用氢或羟基取代其酮基会显著降低抑制作用。同样,添加甲基或羧甲基基团也会降低抑制作用。分离物环内(亚硫酸)双键共轭的去除极大地降低了抑制作用。

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