γ-亚麻酸和二十碳五烯酸对尿激酶活性的影响。

The effect of gamma-linolenic acid and eicosapentaenoic acid on urokinase activity.

作者信息

du Toit P J, van Aswegen C H, du Plessis D J

机构信息

Wolmarans Research Laboratory, Department of Urology, HF Verwoerd Hospital, Pretoria, South Africa.

出版信息

Prostaglandins Leukot Essent Fatty Acids. 1994 Aug;51(2):121-4. doi: 10.1016/0952-3278(94)90087-6.

DOI:10.1016/0952-3278(94)90087-6

PMID:7972265

Abstract

Urokinase (UK) is an important protease enzyme in carcinogenesis, and is involved in the invasion and metastasis of cancer. Thus, regulation of UK activity is likely to be important in healthy cell metabolism. As it has been reported that a decrease in delta 6-desaturated essential fatty acid (EFA) metabolites occurs in malignant cells and that gamma-linolenic acid (GLA) and eicosapentaenoic acid (EPA) exert antimutagenic effects, the effects of GLA and EPA on UK activity have been investigated in this study. Both GLA (n-6) and EPA (n-3) acted as competitive inhibitors of UK with Ki values of 120 and 96 microM respectively. No modification of plasmin activity occurred with either 1.4 x 10(-4) M GLA or EPA. These results could explain why malignant cells with decreased EFA concentrations show increased UK activity. The addition of EFAs to available therapeutic regimens may be worth considering in the treatment of cancer.

摘要

尿激酶（UK）是致癌过程中一种重要的蛋白酶，参与癌症的侵袭和转移。因此，调节UK活性在健康细胞代谢中可能很重要。据报道，恶性细胞中δ-6-去饱和必需脂肪酸（EFA）代谢产物减少，且γ-亚麻酸（GLA）和二十碳五烯酸（EPA）具有抗诱变作用，本研究对GLA和EPA对UK活性的影响进行了调查。GLA（n-6）和EPA（n-3）均作为UK的竞争性抑制剂，其抑制常数（Ki）值分别为120和96微摩尔。1.4×10⁻⁴ M的GLA或EPA均未引起纤溶酶活性的改变。这些结果可以解释为什么EFA浓度降低的恶性细胞显示UK活性增加。在癌症治疗中，将必需脂肪酸添加到现有的治疗方案中可能值得考虑。