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月见草脱脂种籽提取物含五没食子酰葡萄糖和原花青素,能增强长春新碱的细胞毒性。

Oenothera paradoxa defatted seeds extract containing pentagalloylglucose and procyanidins potentiates the cytotoxicity of vincristine.

机构信息

Department of Pharmacognosy and Molecular Basis of Phytotherapy, Faculty of Pharmacy, Medical University of Warsaw, Poland.

出版信息

J Physiol Pharmacol. 2010 Oct;61(5):637-43.

PMID:21081808
Abstract

The purpose of the study was a comparison of Oenothera paradoxa Hudziok defatted seeds extract (EPE) effect with the activity of individual constituents of the extract: pentagalloylglucose (PGG), gallic acid, (+)-catechin and the procyanidin fraction, as well as an assessment of the combined effect of EPE and vincristine (VCR) in the absence or presence of MRP1 (indomethacin) and P-glycoprotein (verapamil) inhibitors, on two human cancer cell lines, metastatic melanoma (HTB-140) and hepatoma (HepG2). The presence of EPE, PGG and procyanidins caused a marked reduction in viability (MTT assay) and rise in mortality (LDH release assay) of HTB-140 cells. The combined use of EPE (25 μg/mL) and VCR (1 μM) in HTB-140 and HepG2 cells produced an increased cytotoxicity as compared to vincristine alone - by more than 4 and 1.5 times, respectively. In HTB-140 cells, the level of intracellular ATP (measured by bioluminescence) was lowered over 7-fold as a result of exposure to the combination of EPE and VCR, while the addition of MRP-1 inhibitor did not cause an increased cytotoxicity or further lowering of the ATP level. Our results demonstrate that EPE, containing PGG and procyanidins, significantly increased the sensitivity of cancer cells, particularly the melanoma cells, to the action of vincristine.

摘要

本研究旨在比较月见草 paradoxa Hudziok 去脂种子提取物 (EPE) 的作用与提取物中各成分的活性:五没食子酰葡萄糖 (PGG)、没食子酸、(+)-儿茶素和原花青素,以及评估 EPE 和长春新碱 (VCR) 在缺乏或存在多药耐药相关蛋白 1 (吲哚美辛) 和 P-糖蛋白 (维拉帕米) 抑制剂时对两种人癌细胞系(转移性黑色素瘤[HTB-140]和肝癌[HepG2])的联合作用。EPE、PGG 和原花青素的存在导致 HTB-140 细胞活力(MTT 测定)明显降低和死亡率(LDH 释放测定)升高。与单独使用长春新碱相比,EPE(25μg/mL)和 VCR(1μM)在 HTB-140 和 HepG2 细胞中的联合使用产生了更高的细胞毒性,分别超过 4 倍和 1.5 倍。在 HTB-140 细胞中,由于 EPE 和 VCR 的联合作用,细胞内 ATP 水平(通过生物发光测量)降低了 7 倍以上,而添加 MRP-1 抑制剂并没有导致细胞毒性增加或进一步降低 ATP 水平。我们的结果表明,EPE 含有 PGG 和原花青素,可显著提高癌细胞,特别是黑色素瘤细胞对长春新碱作用的敏感性。

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