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瑞香叶状忍冬中的细胞毒鞣花单宁。

Cytotoxic ellagitannins from Reaumuria vermiculata.

机构信息

Department of Phytochemistry and Plant Systematics, National Research Center, Dokki, Cairo, Egypt.

出版信息

Fitoterapia. 2012 Oct;83(7):1256-66. doi: 10.1016/j.fitote.2012.06.007. Epub 2012 Jun 26.

Abstract

Three ellagitannins and one disulfated flavonol were isolated from the aerial parts of Reaumuria vermiculata L. Besides that, 16 known compounds were characterized as well. The structures of all compounds were elucidated on the basis of spectroscopic data including 1D and 2D NMR and ESI HR-FTMS. The in vivo antioxidant activity using the oxygen radical absorbance capacity (ORAC) method, of the extract, its column fractions and two of the isolated ellagitannins was accomplished. In addition, a possible cytotoxicity of the extract and two of the new ellagitannins on HaCaT human keratinocytes and the activity of both compounds against the prostate cancer cell line (PC-3) were also assessed, whereby a potent cytotoxicity with IC₅₀ less than 1 μg/ml was determined for both compounds. Besides, the extract exhibited a potential cytotoxic effect against four different solid tumor cell lines, namely liver (Huh-7), colorectal (HCT-116), breast (MCF-7) and prostate (PC-3). The IC₅₀s were found to be substantially low (ranged from 1.3±0.15 to 2.4±0.22 μg/ml) with relatively low resistance possibility reaching to 0% in the case of Huh-7 cell.

摘要

从软紫草(Reaumuria vermiculata L.)的地上部分分离得到了三种鞣花单宁和一种二硫酸化黄酮醇,此外还鉴定了 16 种已知化合物。所有化合物的结构均基于包括 1D 和 2D NMR 以及 ESI HR-FTMS 在内的光谱数据阐明。采用氧自由基吸收能力(ORAC)法测定了提取物、其柱馏分和两种分离出的鞣花单宁的体内抗氧化活性。此外,还评估了提取物和两种新鞣花单宁对 HaCaT 人角质形成细胞的可能细胞毒性以及这两种化合物对前列腺癌细胞系(PC-3)的活性,结果表明这两种化合物均具有很强的细胞毒性,IC₅₀值均小于 1 μg/ml。此外,提取物对四种不同的实体瘤细胞系(肝(Huh-7)、结肠直肠(HCT-116)、乳腺(MCF-7)和前列腺(PC-3))表现出潜在的细胞毒性作用。IC₅₀ 值均相当低(范围为 1.3±0.15 至 2.4±0.22 μg/ml),耐药性相对较低,在 Huh-7 细胞中耐药率达到 0%。

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