PF1270A, B and C, novel histamine H3 receptor ligands produced by Penicillium waksmanii PF1270
PF1270A, B and C, novel histamine H3 receptor ligands produced by Penicillium waksmanii PF1270
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DOI：
10.1038/ja.2007.85
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发表时间：
2007-11-01
影响因子：
3.3
通讯作者：
Yaguchi, Takashi
中科院分区：
文献类型：
--
作者：
Kushida, Nobuaki;Watanabe, Naoko;Yaguchi, Takashi
从真菌菌株PF1270的发酵液中分离得到3个新的组胺H3受体(H3R)配体：PF1270A(1)、PF1270B(2)和PF1270C(3)。经形态特征鉴定，该菌株为魏氏青霉。这些化合物是从发酵液中通过溶剂提取和层析纯化得到的。通过光谱分析和X-射线晶体分析确定了它们的结构。它们具有五环螺二酮骨架。1、2和3对大鼠H3R的亲和力分别为0.058、0.17和0.19mU M，对人H3R的亲和力分别为0.047、0.12和0.22mU M。此外，1、2和3是有效的激动剂，其EC50值分别为0.12、0.15和0.20微米。
Three novel histamine H3 receptor (H3R) ligands, PF1270A (1), PF1270B (2) and PF1270C (3) were isolated from the culture broth of the fungal strain PF1270. The strain was identified as Penicillium waksmanii on the basis of morphological characteristics. These compounds were obtained from the culture broth by solvent extraction and chromatographic purification. Their structures were established by spectroscopic methods and X-ray crystallographic analysis. They possess pentacyclic spiroindolinone skeletons. 1, 2 and 3 displayed high affinity for the rat H3R (Ki=0.058, 0.17 and 0.19 mu M, respectively) and human H3R (Ki=0.047, 0.12 and 0.22 mu M, respectively). Moreover, 1, 2 and 3 acted as potent agonists with the EC50 values of 0.12, 0.15 and 0.20 mu M, respectively.