Asperdichrome, an unusual dimer of tetrahydroxanthone through an ether bond, with protein tyrosine phosphatase 1B inhibitory activity, from the Okinawan freshwater Aspergillus sp TPU1343
Asperdichrome, an unusual dimer of tetrahydroxanthone through an ether bond, with protein tyrosine phosphatase 1B inhibitory activity, from the Okinawan freshwater Aspergillus sp TPU1343
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DOI：
10.1016/j.tetlet.2015.12.111
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发表时间：
2016-02-17
影响因子：
1.8
通讯作者：
Namikoshi, Michio
中科院分区：
文献类型：
--
作者：
Yamazaki, Hiroyuki;Ukai, Kazuyo;Namikoshi, Michio
从曲霉TPU1343的培养液中分离出一种新的通过醚键连接的双四羟基anthone，命名为asperdichrome(1)，与两种已知的二聚体聚酮，二氯酸D(2)和F(3)。这种真菌是从日本冲绳的一份淡水样本中分离出来的。根据其光谱数据对其结构进行了分析，并与相关化合物进行了比较。化合物1和3（异源二聚体）抑制蛋白酪氨酸磷酸酶1B （PTP1B）活性，IC50值分别为6.0 μ M和9.6 μ M。化合物2（同二聚体）对PTP1B的活性降低（15.7 μ M时抑制40%）。这是首次研究四羟基蒽酮对PTP1B的抑制作用。(C) 2015 Elsevier Ltd.版权所有。
A new unusual bis-tetrahydroxanthone connected through an ether bond, named asperdichrome (1), was isolated from a culture broth of Aspergillus sp. TPU1343 together with two known dimeric polyketides, secalonic acids D (2) and F (3). The fungus was isolated from a freshwater sample in Okinawa, Japan. The structure of 1 was elucidated on the basis of its spectroscopic data and comparisons were made with related compounds. Compounds 1 and 3 (heterodimers) inhibited the activity of protein tyrosine phosphatase 1B (PTP1B) with IC50 values of 6.0 and 9.6 mu M, respectively. Compound 2 (homodimer) showed reduced activity against PTP1B (40% inhibition at 15.7 mu M). This is the first study on the inhibitory activities of tetrahydroxanthones against PTP1B. (C) 2015 Elsevier Ltd. All rights reserved.