Psammaplin A, a chitinase inhibitor isolated from the Fijian marine sponge Aplysinella rhax

Psammaplin A, a chitinase inhibitor isolated from the Fijian marine sponge Aplysinella rhax
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DOI:
10.1016/s0968-0896(01)00372-8
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发表时间:
2002-04-01
影响因子:
3.5
通讯作者:
van Aalten, DMF
van Aalten, DMF
中科院分区:
医学3区
文献类型:
--
作者:
Tabudravu, JN;Eijsink, VGH;van Aalten, DMF

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几种溴化酪氨酸衍生化合物。采用生物测定导向分离方法,从斐济海绵Aplysinella rhax中分离得到3种沙门冬素A(1)、K(2)、L(3)和Bisaprasin(4)。其结构经核磁共振和质谱学确证。Psammaplin A对粘质沙雷氏菌的几丁质酶B有适度的抑制作用,这种抑制方式是非竞争性的,结晶学研究表明,活性部位附近结合了一个无序的Psammaplin A分子。有趣的是,沙参甲素被发现是一种有效的抗真菌药物。(C)2002爱思唯尔科学有限公司。保留所有权利。
Several brominated tyrosine derived compounds. psammaplins A (1), K (2) and L (3) as well as bisaprasin (4) were isolated from the Fijian marine sponge Aplysinella rhax during a bioassay guided isolation protocol. Their structures were determined using NMR and MS techniques. Psammaplin A was found to moderately inhibit chitinase B from Serratia marcescens, the mode of inhibition being non-competitive, Crystallographic studies suggest that a disordered psammaplin A molecule is bound near the active site. Interestingly, psammaplin A was found to be a potent antifungal agent. (C) 2002 Elsevier Science Ltd. All rights reserved.