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羊蹄甲激肽释放酶抑制剂对内皮细胞增殖及细胞内钙浓度的影响。

Effect of bauhinia bauhinioides kallikrein inhibitor on endothelial proliferation and intracellular calcium concentration.

作者信息

Bilgin M, Burgazli K M, Rafiq A, Mericliler M, Neuhof C, Oliva M L, Parahuleva M, Soydan N, Doerr O, Abdallah Y, Erdogan A

机构信息

Department of Cardiology and Angiology, Justus-Liebig-University of Giessen, Giessen, Germany.

出版信息

Eur Rev Med Pharmacol Sci. 2014;18(1):46-51.

Abstract

OBJECTIVES

Proteinase inhibitors act as a defensive system against predators e.g. insects, in plants. Bauhinia bauhinioides kallikrein inhibitor (BbKI) is a serine proteinase inhibitor, isolated from seeds of Bauhinia bauhinioides and is structurally similar to plant Kunitz-type inhibitors but lacks disulfide bridges. In this study we evaluated the antiproliferative effect of BbKI on endothelial cells and its impact on changes in membrane potential and intracellular calcium.

MATERIALS AND METHODS

HUVEC proliferation was significantly reduced by incubation with BbKI 50 and 100 µM 12% and 13%. Furthermore, BbKI (100 µM) exposure caused a significant increase in intracellular Ca2+ concentration by 35% as compared to untreated control.

RESULTS

The intracellular rise in calcium was not affected by the absence of extracellular calcium. BBKI also caused a significant change in the cell membrane potential but the antiproliferative effect was independent of changes in membrane potential.

CONCLUSIONS

BBKI has an antiproliferative effect on HUVEC, which is independent of the changes in membrane potential, and it causes an increase in intracellular Ca2+.

摘要

目的

蛋白酶抑制剂在植物中作为抵御捕食者(如昆虫)的防御系统。羊蹄甲胰激肽释放酶抑制剂(BbKI)是一种丝氨酸蛋白酶抑制剂,从羊蹄甲种子中分离得到,其结构与植物库尼茨型抑制剂相似,但缺乏二硫键。在本研究中,我们评估了BbKI对内皮细胞的抗增殖作用及其对膜电位和细胞内钙变化的影响。

材料与方法

用50和100μM的BbKI孵育后,人脐静脉内皮细胞(HUVEC)的增殖显著降低,分别降低了12%和13%。此外,与未处理的对照组相比,暴露于100μM的BbKI会导致细胞内Ca2+浓度显著增加35%。

结果

细胞内钙的升高不受细胞外钙缺失的影响。BbKI还引起细胞膜电位的显著变化,但抗增殖作用与膜电位的变化无关。

结论

BbKI对HUVEC具有抗增殖作用,该作用与膜电位的变化无关,且会导致细胞内钙增加。

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