Cladosporamide A, a new protein tyrosine phosphatase 1B inhibitor, produced by an Indonesian marine sponge-derived Cladosporium sp.
Cladosporamide A, a new protein tyrosine phosphatase 1B inhibitor, produced by an Indonesian marine sponge-derived Cladosporium sp.
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DOI：
10.1007/s11418-018-1193-y
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发表时间：
2018-03
影响因子：
3.3
通讯作者：
H. Rotinsulu;H. Yamazaki;Shino Sugai;N. Iwakura;D. Wewengkang;D. Sumilat;M. Namikoshi
中科院分区：
文献类型：
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作者：
H. Rotinsulu;H. Yamazaki;Shino Sugai;N. Iwakura;D. Wewengkang;D. Sumilat;M. Namikoshi
Cladosporamide A(1)是一种新的蛋白酪氨酸磷酸酶（PTP） 1B抑制剂，与一种已知的烯丙基黄酮衍生物(2)一起从印度尼西亚海绵体cladosporiumsp培养液中分离得到。采用溶剂萃取、ODS柱层析、制备型高效液相色谱法（ODS）对TPU1507进行分析。利用一维和二维核磁共振数据对其结构进行了分析。化合物1适度抑制PTP1B和t细胞PTP （TCPTP）活性，ic50值分别为48 μM和54 μM。2对PTP1B （IC50= 11 μM）的抑制活性约为对TCPTP （IC50= 27 μM）的2倍。
Cladosporamide A (1), a new protein tyrosine phosphatase (PTP) 1B inhibitor, was isolated together with a known prenylated flavanone derivative (2) from the culture broth of an Indonesian marine sponge-derivedCladosporiumsp. TPU1507 by solvent extraction, ODS column chromatography, and preparative HPLC (ODS). The structure of1was elucidated based on 1D and 2D NMR data. Compound1modestly inhibited PTP1B and T-cell PTP (TCPTP) activities with IC50values of 48 and 54 μM, respectively. The inhibitory activity of2against PTP1B (IC50= 11 μM) was approximately 2-fold stronger than that against TCPTP (IC50= 27 μM).