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穿心莲中的新穿心莲内酯作为一种有潜力的天然化学增敏剂。

Neoandrographolide from Andrographis paniculata as a potential natural chemosensitizer.

机构信息

Institute of Pharmacy/Pharmacognosy, Center for Molecular Biosciences Innsbruck, Leopold-Franzens University of Innsbruck, Innsbruck, Austria.

出版信息

Planta Med. 2010 Oct;76(15):1698-700. doi: 10.1055/s-0030-1249876. Epub 2010 May 5.

Abstract

Extracts of the traditional medicinal herb Andrographis paniculata and its main constituents are described in the literature as showing anticancer activity. The aim of this study was to isolate the main constituents of a commercially available phytotherapeutic preparation of A. paniculata and to determine their chemosensitizing potential in a leukemia cell line. Chromatographic separation steps resulted in the isolation of the diterpenes andrographolide (1) and 14-deoxy-11,12-didehydroandrographolide (3) and the diterpene glucoside neoandrographolide (2). The combination of these constituents with suboptimal concentrations of etoposide revealed compound 2 as chemosensitizer in S-Jurkat and X chromosome-linked inhibitor of apoptosis protein (XIAP)-overexpressing Jurkat cells, a model for chemoresistance.

摘要

传统药用植物穿心莲及其主要成分在文献中被描述为具有抗癌活性。本研究的目的是从市售穿心莲植物制剂中分离主要成分,并在白血病细胞系中测定其化学增敏作用。色谱分离步骤得到二萜穿心莲内酯(1)和 14-去氧-11,12-二脱氢穿心莲内酯(3)以及二萜糖苷新穿心莲内酯(2)。这些成分与依托泊苷亚最佳浓度联合使用,结果表明成分 2 是 S-Jurkat 和 X 染色体连接的凋亡蛋白抑制剂(XIAP)过表达 Jurkat 细胞的化学增敏剂,这是一种化疗耐药模型。

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