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基于前列腺癌细胞系差异行为的植物和真菌提取物激素(雄激素和抗雄激素)及细胞毒性活性的多重读数分析。

Multiple readout assay for hormonal (androgenic and antiandrogenic) and cytotoxic activity of plant and fungal extracts based on differential prostate cancer cell line behavior.

作者信息

Bobach Claudia, Schurwanz Jana, Franke Katrin, Denkert Annika, Van Sung Tran, Kuster Ricardo, Mutiso Patrick Chalo, Seliger Barbara, Wessjohann Ludger A

机构信息

Leibniz Institute of Plant Biochemistry, Weinberg 3, D-06120 Halle (Saale), Germany; Ontochem GmbH, H.-Damerow-Str.4, D-06120 Halle (Saale), Germany.

Leibniz Institute of Plant Biochemistry, Weinberg 3, D-06120 Halle (Saale), Germany.

出版信息

J Ethnopharmacol. 2014 Aug 8;155(1):721-30. doi: 10.1016/j.jep.2014.06.008. Epub 2014 Jun 16.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Prostate cancer is one of the most diagnosed forms of cancer among men in western regions. Many traditional applications or phytotherapeutic concepts propose to inhibit the proliferation of prostate cancer cells. In order to detect influences of plant or fungal extracts and derived fractions on androgen receptor signaling pathways, a differentiating cell proliferation assay was established, which enables the simultaneous detection of hormonal and cytotoxic effects.

MATERIAL AND METHODS

The well characterized prostate cancer cell lines LNCaP and PC-3 were used in a multiple readout assay. In all, 186 fractions of 23 traditionally used organisms were screened regarding their effects on proliferation of the two prostate cancer cell lines. The fractions were prepared by accelerated solvent extraction followed by gradient extrography. Extracts of the potential hormonally active plants Cibotium barometz, Heteropterys chrysophylla, and Sideroxylon obtusifolium (= Bumelia sartorum) were phytochemically investigated.

RESULTS

Fractions from Cibotium barometz, Cortinarius rubellus, Cyrtomium falcatum, Heteropterys chrysophylla, Nephrolepis exaltata, Salvia miltiorrhiza, Sideroxylon obtusifolium, Trichilia emetica, and Trimeria grandifolia exhibited hormonal influences on prostate cancer cells. Cytotoxic activity towards human cell lines was detected for the first time for fractions from Aglaia spectabilis (A. gigantea), Nephrolepis exaltata and Cortinarius brunneus.

CONCLUSIONS

The differential behavior of the two prostate cancer cell lines allows the discrimination between potential androgenic or antiandrogenic activities and effects on the estrogen or glucocorticoid receptor as well as cytotoxic activities. The combined cell lines assay can help to assess the biological activities of material used in traditional medicine.

摘要

民族药理学相关性

前列腺癌是西方地区男性中最常被诊断出的癌症形式之一。许多传统应用或植物治疗理念都提出要抑制前列腺癌细胞的增殖。为了检测植物或真菌提取物及其衍生馏分对雄激素受体信号通路的影响,建立了一种鉴别细胞增殖测定法,该方法能够同时检测激素和细胞毒性作用。

材料与方法

在多重读数测定中使用了特征明确的前列腺癌细胞系LNCaP和PC-3。总共筛选了23种传统使用的生物体的186个馏分,以研究它们对两种前列腺癌细胞系增殖的影响。这些馏分通过加速溶剂萃取然后梯度萃取法制备。对具有潜在激素活性的植物金毛狗脊、金黄异翅藤和钝叶铁线子(= 沙托鲁姆布梅利亚)的提取物进行了植物化学研究。

结果

金毛狗脊、红绒盖牛肝菌、镰叶贯众、金黄异翅藤、高肾蕨、丹参、钝叶铁线子、吐根美登木和大叶藜的馏分对前列腺癌细胞表现出激素影响。首次检测到来自美丽鹧鸪花(= 巨大鹧鸪花)、高肾蕨和褐绒盖牛肝菌的馏分对人类细胞系具有细胞毒性活性。

结论

两种前列腺癌细胞系的不同行为使得能够区分潜在的雄激素或抗雄激素活性以及对雌激素或糖皮质激素受体的影响以及细胞毒性活性。联合细胞系测定有助于评估传统医学中所用材料的生物活性。

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