蓝藻微囊藻中的多种毒素产生：有毒蛋白酶抑制剂蓝藻肽菌素 1020 的分离。

Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.

机构信息

Department of Chemistry, University of Basel, St. Johanns-Ring 19, CH-4056 Basel, Switzerland.

出版信息

J Nat Prod. 2010 May 28;73(5):980-4. doi: 10.1021/np900818c.

PMID:20405925

Abstract

The isolation and structure of cyanopeptolin 1020 (hexanoic acid-Glu-N[-O-Thr-Arg-Ahp-Phe-N-Me-Tyr-Val-]) from a Microcystis strain is reported. Very potent picomolar trypsin inhibition (IC(50) = 670 pM) and low nanomolar values against human kallikrein (4.5 nM) and factor XIa (3.9 nM) have been determined for cyanopeptolin 1020. For plasmin and chymotrypsin, low micromolar concentrations were necessary for 50% inhibition. Cyanopeptolin 1020 was found to be toxic against the freshwater crustacean Thamnocephalus platyurus (LC(50) = 8.8 microM), which is in the same range as some of the well-known microcystins. These data support the hypothesis that cyanopeptolins can be considered as a second class of toxins in addition to the well-established microcystins in Microcystis.

摘要

从一种微囊藻菌株中分离得到了蓝藻肽 1020（己酸-Glu-N[-O-Thr-Arg-Ahp-Phe-N-Me-Tyr-Val-]），并对其结构进行了研究。蓝藻肽 1020 对胰蛋白酶具有很强的皮摩尔级抑制活性（IC₅₀=670 pM），对人激肽释放酶（4.5 nM）和因子 XIa（3.9 nM）的抑制活性也达到纳摩尔级。对于纤溶酶和糜蛋白酶，需要低微摩尔浓度才能达到 50%的抑制率。蓝藻肽 1020 对淡水甲壳动物 T. platyurus（LC₅₀=8.8 μM）具有毒性，与一些著名的微囊藻毒素处于同一范围。这些数据支持了这样一种假设，即蓝藻肽除了已被广泛认可的微囊藻毒素外，还可以被视为微囊藻中的第二类毒素。