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Pyrrolactams from Marine Sponge Stylissa massa Collected from Myanmar and Their Anti-Vpr Activities
Chemical & Pharmaceutical Bulletin ( IF 1.5 ) Pub Date : 2021-07-01 , DOI: 10.1248/cpb.c21-00227
Nwet Nwet Win 1 , Takeshi Kodama 1 , Aung Aung Aye 2 , Khine Zar Wynn Lae 3 , Hla Ngwe 3 , Nang Mya Han 2 , Ikuro Abe 4, 5 , Hiroyuki Morita 1
Affiliation  

A new brominated pyrrolactam stylissaol A (1) together with four known analogues, 2-bromoaldisine, aldisine, spongiacidin D, and Z-hymenialdisine, were isolated from the EtOAc extract of marine sponge Stylissa massa collected in Myanmar. The absolute configuration at C-10 of 1 was determined as R by the electronic circular dichroism (ECD) data. Among the isolated compounds, 2-bromoaldisine showed anti-Viral Protein R (Vpr) activity against TREx-HeLa-Vpr cells with an effective dose of 10 µM and its potency was comparable to that of positive control damnacanthal.

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中文翻译:

来自缅甸的海洋海绵 Stylissa massa 的吡咯内酰胺及其抗 Vpr 活动

从缅甸收集的海海绵Stylissa massa的 EtOAc 提取物中分离出一种新的溴化吡咯内酰胺 stylissaol A ( 1 ) 以及四种已知的类似物 2-溴醛酸、醛缩醛、海绵酸 D 和Z -hymenialdisine 。在C-10的绝对构型1被确定为[R由电子圆二色性(ECD)的数据。在分离的化合物中,2-bromoaldisine 显示出对 TREx-HeLa-Vpr 细胞的抗病毒蛋白 R (Vpr) 活性,有效剂量为 10 µM,其效力与阳性对照damacanthal 相当。

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更新日期:2021-06-30
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