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<p>α-Glucosidase is considered an ideal target for the treatment of type 2 diabetes mellitus. <i>Streptomyces</i> species are known to produce a plethora of bioactive metabolites. On the basis of genomic information, the one strain many compounds (OSMAC) strategy and various chromatographic separation techniques, two compounds, bezerramycin A (<b>1</b>) and elloxazinone A (<b>2</b>), were identified from among <i>Streptomyces</i> sp. CB00316 metabolites. The α-glucosidase inhibitory activities of the isolated compounds were evaluated and compound <b>2</b> showed the strongest activity, with an IC<sub>50</sub> value of 74.31 ± 3.74 µM. In silico molecular docking and molecular dynamics simulations confirmed the in vitro activities of these α-glucosidase inhibitors. In addition, we investigated the biosynthetic gene clusters and metabolic pathways of compounds <b>1</b> and <b>2</b>. These findings highlight the potential of phenoxazines as lead compounds to combat the development of type 2 diabetes.</p>

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Discovery of phenoxazine congeners as novel α-glucosidase inhibitors and identification of their biosynthetic gene cluster from Streptomyces sp. CB00316

  • 期刊论文

  • 发表日期：

    2025年4月29日

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  • Lin Jiang,
  • Pingzhi Huang,
  • Aijie Li,
  • Bin Fen,
  • Yani Zhong,
  • Caijun Tang,
  • Guangling Wu,
  • Wenlei Wang,
  • Yuhan Chen,
  • Jian Pan,
  • Genyun Tang,
  • Hong Pu

摘要

α-Glucosidase is considered an ideal target for the treatment of type 2 diabetes mellitus. Streptomyces species are known to produce a plethora of bioactive metabolites. On the basis of genomic information, the one strain many compounds (OSMAC) strategy and various chromatographic separation techniques, two compounds, bezerramycin A (1) and elloxazinone A (2), were identified from among Streptomyces sp. CB00316 metabolites. The α-glucosidase inhibitory activities of the isolated compounds were evaluated and compound 2 showed the strongest activity, with an IC50 value of 74.31 ± 3.74 µM. In silico molecular docking and molecular dynamics simulations confirmed the in vitro activities of these α-glucosidase inhibitors. In addition, we investigated the biosynthetic gene clusters and metabolic pathways of compounds 1 and 2. These findings highlight the potential of phenoxazines as lead compounds to combat the development of type 2 diabetes.