Lyngbyastatin 4, a dolastatin 13 analogue with elastase and chymotrypsin inhibitory activity from the marine cyanobacterium Lyngbya confervoides
Lyngbyastatin 4, a dolastatin 13 analogue with elastase and chymotrypsin inhibitory activity from the marine cyanobacterium Lyngbya confervoides
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DOI：
10.1021/np060471k
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发表时间：
2007-01-01
影响因子：
5.1
通讯作者：
Luesch, Hendrik
中科院分区：
文献类型：
--
作者：
Matthew, Susan;Ross, Cliff;Luesch, Hendrik
Lyngbyastatin 4(1)是一种新的沉积肽，含有不寻常的氨基酸同型酪氨酸和3-氨基-6-羟基-2-哌啶酮（Ahp）残基，从佛罗里达大西洋海岸的海洋蓝藻Lyngbya confervoides中分离得到。通过核磁共振谱分析确定了其总体结构，通过手性高效液相色谱分析确定了其不对称中心的构型。Lyngbyastatin 41)是海兔分离的dolastatin 13和几种海洋蓝藻代谢产物的类似物，进一步支持了许多dolastatin起源于蓝藻的观点。Lyngbyastatin 4(1)比其他丝氨酸蛋白酶选择性抑制弹性酶和凝乳胰蛋白酶，IC50值分别为0.03 μ M和0.30 μ M。
Lyngbyastatin 4 (1), a new depsipeptide containing the unusual amino acid homotyrosine and a 3-amino-6-hydroxy-2-piperidone (Ahp) residue, was isolated from a collection of the marine cyanobacterium Lyngbya confervoides off the Florida Atlantic coast. Its gross structure was determined by NMR spectroscopy, and the configurations of asymmetric centers were assigned after chiral HPLC analysis of hydrolysis products. Lyngbyastatin 4 1) is an analogue of the sea hare isolate dolastatin 13 and several marine cyanobacterial metabolites, further supporting the notion that many of the dolastatins are of cyanobacterial origin. Lyngbyastatin 4 (1) selectively inhibits elastase and chymotrypsin in vitro over other serine proteases with IC50 values of 0.03 and 0.30 mu M, respectively.