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Study about fluostatins: efficient preparation of fluostatin A and discovery of fluostatin derivatives from Streptomyces sp. TA-3391

The Journal of Antibiotics volume 78, pages 552–559 (2025)Cite this article

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Abstract

Fluostatins are a class of compounds having four unique ring systems. They were originally isolated as dipeptidyl peptidase III (DPP3) inhibitors, and various derivatives and activities have been reported. In this study, fluostatin A, which is difficult to prepare by fermentative production, was effectively prepared by the transformation of fluostatin B. A new derivative, fluostatin Y, and a new naturally occurring derivative, fluostatin B2, were obtained, and their structures were determined. Furthermore, the bioactivity, DPP3 inhibitory activity, and antibacterial and cytotoxic activities were examined.

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Acknowledgements

We are grateful to Dr. K. Iijima, Dr. S. Adachi, Mrs. Y. Kubota and Dr. R. Sawa (Microbial Chemistry Research Center) for MS and NMR measurement. We also thank Dr. T. Kimura (Microbial Chemistry Research Center) for a single crystal X-ray diffraction.

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Authors and Affiliations

  1. Institute of Microbial Chemistry (BIKAKEN), Shinagawa-ku, Tokyo, Japan

    Shigehiro Tohyama, Masaki Hatano, Chigusa Hayashi & Masayuki Igarashi

  2. Funakoshi Co. Ltd., Bunkyo-ku, Tokyo, Japan

    Seiji Nukui

  3. Institute of Microbial Chemistry (BIKAKEN), Numazu, Numazu, Shizuoka, Japan

    Isao Momose

Authors
  1. Shigehiro Tohyama
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  2. Seiji Nukui
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  6. Masayuki Igarashi
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Correspondence to Shigehiro Tohyama.

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Tohyama, S., Nukui, S., Hatano, M. et al. Study about fluostatins: efficient preparation of fluostatin A and discovery of fluostatin derivatives from Streptomyces sp. TA-3391. J Antibiot 78, 552–559 (2025). https://doi.org/10.1038/s41429-025-00841-8

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