A new protein tyrosine phosphatase 1B inhibitory α-pyrone-type polyketide from Okinawan plant-associated Aspergillus sp. TMPU1623

Hiroyuki Yamazaki; Kenta Takahashi; Natsuki Iwakura; Tatsuki Abe; Masanari Akaishi; Satomi Chiba; Michio Namikoshi; Ryuji Uchida

doi:10.1038/s41429-018-0054-y

A new protein tyrosine phosphatase 1B inhibitory α-pyrone-type polyketide from Okinawan plant-associated Aspergillus sp. TMPU1623

J Antibiot (Tokyo). 2018 Aug;71(8):745-748. doi: 10.1038/s41429-018-0054-y. Epub 2018 Apr 20.

Authors

Hiroyuki Yamazaki¹, Kenta Takahashi², Natsuki Iwakura², Tatsuki Abe², Masanari Akaishi², Satomi Chiba², Michio Namikoshi², Ryuji Uchida³

Affiliations

¹ Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan. yamazaki@tohoku-mpu.ac.jp.
² Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan.
³ Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan. uchidar@tohoku-mpu.ac.jp.

PMID: 29679041
DOI: 10.1038/s41429-018-0054-y

Abstract

A new polyenyl-α-pyrone polyketide, aspopyrone A (1), was isolated from a culture broth of Okinawan plant-associated Aspergillus sp. TMPU1623 by solvent extraction, ODS column chromatography, and preparative HPLC (ODS). The structure of 1 was assigned based on NMR experiments. Compound 1 exhibited protein tyrosine phosphatase (PTP) 1B and T-cell PTP (TCPTP) inhibitory activities with IC₅₀ values of 6.7 and 6.0 μM, respectively.

MeSH terms

Aspergillus / metabolism
Polyketides / pharmacology*
Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors*
Pyrones / antagonists & inhibitors*

Substances

Polyketides
Pyrones
Protein Tyrosine Phosphatase, Non-Receptor Type 1