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海葵毒素的抗肿瘤活性。

Antitumor activity of equinatoxin.

作者信息

Giraldi T, Ferlan I, Romeo D

出版信息

Chem Biol Interact. 1976 Jun;13(3-4):199-203. doi: 10.1016/0009-2797(76)90073-9.

Abstract

Equinatoxin, a highly basic protein extracted from Actinia equina, causes an increase in the survival time of mice bearing the ascitic form of Ehrlich carcinoma, whereas it has no effect on L1210 leukaemia. When tested for in vitro cytotoxicity by the dye exclusion test, it shows a potent activity on both tumour cell lines, with ED50 of a few ng/ml. Higher concentrations produce an extensive lysis of the cells. The cytotoxic effects of Equinatoxin are inhibited by phospholipids, thus suggesting that its mechanism of action may be related to interactions with lipids or other charged components of cell membrane. The observed lack of in vivo activity against L1210 leukaemia presumably is due to poor systemic absorption of the protein and/or neutralization by serum factors.

摘要

海葵毒素是一种从红海葵中提取的高碱性蛋白质,它能使患艾氏腹水癌的小鼠存活时间延长,而对L1210白血病则没有作用。通过染料排斥试验检测其体外细胞毒性时,它对两种肿瘤细胞系均表现出强大活性,半数有效剂量为几纳克/毫升。较高浓度会导致细胞大量裂解。海葵毒素的细胞毒性作用受到磷脂的抑制,因此表明其作用机制可能与和细胞膜脂质或其他带电荷成分的相互作用有关。观察到的对L1210白血病缺乏体内活性大概是由于该蛋白质的全身吸收不良和/或被血清因子中和。

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