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Two Marine Cyanobacterial Aplysiatoxin Polyketides, Neo-debromoaplysiatoxin A and B, with K+ Channel Inhibition Activity
Organic Letters ( IF 4.9 ) Pub Date : 2018-01-18 00:00:00 , DOI: 10.1021/acs.orglett.7b03672 Bing-Nan Han 1, 2 , Ting-Ting Liang 3 , Lawrence Jordan Keen 1 , Ting-Ting Fan 1 , Xiao-Dan Zhang 1 , Lin Xu 1 , Qi Zhao 4 , Shu-Ping Wang 2 , Hou-Wen Lin 2
Organic Letters ( IF 4.9 ) Pub Date : 2018-01-18 00:00:00 , DOI: 10.1021/acs.orglett.7b03672 Bing-Nan Han 1, 2 , Ting-Ting Liang 3 , Lawrence Jordan Keen 1 , Ting-Ting Fan 1 , Xiao-Dan Zhang 1 , Lin Xu 1 , Qi Zhao 4 , Shu-Ping Wang 2 , Hou-Wen Lin 2
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The isolation and structure elucidation of two cyanobacterial debromoaplysiatoxin (DAT) analogues, neo-debromoaplysiatoxin A (1) and neo-debromoaplysiatoxin B (2), were reported and found to possess 6/10/6 and 6/6/6 fused-ring systems, respectively, which are rarely seen among aplysiatoxins. Both compounds exhibited potent blocking activity against Kv1.5 with IC50 values of 6.94 ± 0.26 and 0.30 ± 0.05 μM, respectively. These findings suggest the potential of aplysiatoxin analogues in modulating ionic channels and also provide links between the DAT target, protein kinase C, and cell regulation.
中文翻译：
两个具有K +通道抑制活性的海洋蓝藻海藻毒素多酮化合物，新皮溴海藻毒素A和B。
据报道，分离并阐明了两种蓝细菌脱溴通毒素（DAT）类似物，新-溴通毒素A（1）和新-溴通毒素B（2），并发现它们具有6/10/6和6/6/6稠合环分别在aplysiatoxins中很少见到的系统。两种化合物均显示出对Kv1.5的有效阻断活性，IC 50值分别为6.94±0.26和0.30±0.05μM。这些发现表明了aplysiatoxin类似物在调节离子通道中的潜力，并且还提供了DAT靶标，蛋白激酶C和细胞调节之间的联系。
更新日期：2018-01-18
中文翻译：
两个具有K +通道抑制活性的海洋蓝藻海藻毒素多酮化合物，新皮溴海藻毒素A和B。
据报道，分离并阐明了两种蓝细菌脱溴通毒素（DAT）类似物，新-溴通毒素A（1）和新-溴通毒素B（2），并发现它们具有6/10/6和6/6/6稠合环分别在aplysiatoxins中很少见到的系统。两种化合物均显示出对Kv1.5的有效阻断活性，IC 50值分别为6.94±0.26和0.30±0.05μM。这些发现表明了aplysiatoxin类似物在调节离子通道中的潜力，并且还提供了DAT靶标，蛋白激酶C和细胞调节之间的联系。
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