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一种来自黄皮(Clausena lansium)种子的具有抗增殖、HIV逆转录酶抑制和抗真菌活性的同二聚体孢粉素型胰蛋白酶抑制剂。

A homodimeric sporamin-type trypsin inhibitor with antiproliferative, HIV reverse transcriptase-inhibitory and antifungal activities from wampee (Clausena lansium) seeds.

作者信息

Ng Tzi B, Lam Sze K, Fong Wing P

机构信息

Department of Biochemistry, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong, China.

出版信息

Biol Chem. 2003 Feb;384(2):289-93. doi: 10.1515/BC.2003.032.

Abstract

A homodimeric trypsin inhibitor with a molecular mass of 54 kDa was isolated from the seeds of Clausena lansium (Lour) Skeels with a very simple procedure comprising extraction with an aqueous buffer and ion exchange chromatography on CM-cellulose. It inhibited trypsin with an IC50 of 2.2 nM but was without any inhibitory effect on chymotrypsin and proteinase K. The uptake of MTT by human leukemia HL60 and hepatoma Hep G2 cells was inhibited with an IC50 of 100 microM. Translation in the cell-free rabbit reticulocyte lysate system was inhibited with an IC50 of 3.6 microM. The activity of HIV-1 reverse transcriptase was reduced in the presence of the trypsin inhibitor. The trypsin inhibitor exerted antifungal activity toward Physalospora piricola but not Mycosphaerella arachidicola, Botrytis cinerea, Fusarium oxysporum or Coprinus comatus.

摘要

通过一个非常简单的程序从黄皮(Clausena lansium (Lour) Skeels)种子中分离出一种分子量为54 kDa的同二聚体胰蛋白酶抑制剂,该程序包括用水性缓冲液提取和在CM - 纤维素上进行离子交换色谱。它抑制胰蛋白酶的IC50为2.2 nM,但对胰凝乳蛋白酶和蛋白酶K没有任何抑制作用。人白血病HL60细胞和肝癌Hep G2细胞对MTT的摄取受到抑制,IC50为100 microM。在无细胞兔网织红细胞裂解物系统中的翻译受到抑制,IC50为3.6 microM。在胰蛋白酶抑制剂存在的情况下,HIV - 1逆转录酶的活性降低。该胰蛋白酶抑制剂对梨孢炭疽菌具有抗真菌活性,但对花生尾孢菌、灰葡萄孢菌、尖孢镰刀菌或毛头鬼伞没有抗真菌活性。

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