Pulchranin A, isolated from the Far-Eastern marine sponge, Monanchora pulchra: the first marine non-peptide inhibitor of TRPV-1 channels
作者:Alla G. Guzii、Tatyana N. Makarieva、Yuliya V. Korolkova、Yaroslav A. Andreev、Irina V. Mosharova、Ksenya M. Tabakmaher、Vladimir A. Denisenko、Pavel S. Dmitrenok、Ekaterina K. Ogurtsova、Alexandr S. Antonov、Hyi-Seung Lee、Eugene V. Grishin
DOI:10.1016/j.tetlet.2012.12.099
日期:2013.3
A new marine guanidine-containing compound, pulchranin A (1) was isolated from the marine sponge Monanchora pulchra. Its structure was elucidated by detailed NMR and MS analyses. The Mosher’s method did not allow determination of the absolute configuration of the carbinol center in 1, but after conversion of 1 into the bis-MTPA esters of 1,3-diol 2, the same method was successfully used to solve the
从海洋海绵Monanchora pulchra中分离出一种新的含海洋胍的化合物pulchranin A(1)。通过详细的NMR和MS分析阐明了其结构。Mosher方法无法确定1中甲醇中心的绝对构型,但是在将1转化为1,3-二醇2的双MTPA酯后,成功地使用了相同的方法来解决该问题。化合物1作为TRPV1受体的抑制剂具有活性,EC 50值为41.2μM。