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乳香酸在体外对恶性细胞系的细胞生长抑制和凋亡诱导活性。

Cytostatic and apoptosis-inducing activity of boswellic acids toward malignant cell lines in vitro.

作者信息

Hostanska Katarina, Daum Gerhard, Saller Reinhard

机构信息

Departmment of Internal Medicine, University Hospital Zürich, Rämistrasse 100, 8091 Zürich, Switzerland.

出版信息

Anticancer Res. 2002 Sep-Oct;22(5):2853-62.

Abstract

Boswellic acids from frankincense were indentified as the active compounds which inhibit leukotriene biosynthesis, 5-lipoxygenase and exert antiproliferative activity toward a variety of malignant cells. Because of the relevance for the clinical application, we tested the ethanolic extract of Boswellia serrata gum resin containing a defined amount of boswellic acids for its cytotoxic, cytostatic and apoptotic activity on five leukemia (HL-60, K 562, U937, MOLT-4, THP-1) and two brain tumor (LN-18, LN-229) cell lines by WST-1 assay and flow cytometry. The Boswellia serrata extract induced dose-dependent antiproliferative effects on all human malignant cells tested with GI50 values (extract concentration producing 50% cell growth inhibition) between 57.0 and 124.1 micrograms/ml. In three haematological cell lines (K562, U937, MOLT-4) the effect of total extract expressed in GI50 was 2.8-, 3.3- and 2.3-times more potent (p < 0.05) than pure 3-O-acetyl-11-keto-beta-boswellic acid (AKBA). Morphological changes after 24-27 hours and the detection of apoptotic cells by AnnexinV-binding and/or by the detection of propidium iodide-labelled DNA with flow cytometry, confirmed the apoptotic cell death. The results of this study suggest the effectiveness of Boswellia serrata extract with defined content of boswellic acids.

摘要

乳香中的乳香酸被鉴定为具有抑制白三烯生物合成、5-脂氧合酶以及对多种恶性细胞发挥抗增殖活性的活性化合物。鉴于其与临床应用的相关性,我们通过WST-1检测法和流式细胞术,测试了含有一定量乳香酸的锯叶乳香树胶树脂乙醇提取物对五种白血病(HL-60、K562、U937、MOLT-4、THP-1)和两种脑肿瘤(LN-18、LN-229)细胞系的细胞毒性、细胞生长抑制和凋亡活性。锯叶乳香提取物对所有测试的人类恶性细胞均诱导出剂量依赖性的抗增殖作用,其GI50值(产生50%细胞生长抑制的提取物浓度)在57.0至124.1微克/毫升之间。在三种血液学细胞系(K562、U937、MOLT-4)中,以GI50表示的总提取物的作用比纯3-O-乙酰基-11-酮-β-乳香酸(AKBA)强2.8倍、3.3倍和2.3倍(p<0.05)。24至27小时后的形态学变化以及通过膜联蛋白V结合和/或通过流式细胞术检测碘化丙啶标记的DNA来检测凋亡细胞,证实了凋亡性细胞死亡。本研究结果表明了具有特定乳香酸含量的锯叶乳香提取物的有效性。

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