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<p>The DPPH radical scavenging, <i>α</i>-glucosidase inhibitory, nitric oxide (NO) inhibitory, and cytotoxic activities of the extracts from fruiting bodies of wood-rot basidiomycete <i>Fulvifomes fastuosus</i> were evaluated in this study. While the CH<sub>2</sub>Cl<sub>2</sub> extract was biologically inactive, chromatographic fractionation led to the isolation of two chlorinated hydroquinone derivatives, drosophilin A methyl ether (DAME; <b>1</b>) and drosophilin A (DA; <b>2</b>). The EtOAc-partitioned fraction, obtained from the partitioning of the MeOH extract, exhibited strong <i>α</i>-glucosidase and NO inhibitory activities. Further investigation led to the isolation of inoscavin A (<b>3</b>) as the major constituent, along with inoscavin E (<b>4</b>) and polyphenols (<b>5</b>–<b>7</b>). Inoscavin A demonstrated potent <i>α</i>-glucosidase inhibition (IC<sub>50</sub> = 3.22 µM), surpassing acarbose by 59-fold, and exhibited non-competitive inhibition kinetics (<i>K</i>ᵢ = 3.25 µM). Molecular docking studies supported an allosteric binding mode. It also displayed favorable drug-likeness and ADMET (absorption, distribution, metabolism, excretion, and toxicity) profiles, including good solubility, high intestinal absorption, low central nervous system (CNS) penetration, and absence of hepatotoxicity. These results suggest that <i>F. fastuosus</i> is a promising source of antidiabetic agents, with inoscavin A as a principle active compound.</p><p></p>

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Potent α-glucosidase inhibitory activity of inoscavin A from fruiting bodies of Fulvifomes fastuosus: Mechanism of action, molecular docking and ADMET

  • 期刊论文

  • 发表日期：

    2025年8月30日

查看全文
  • Khemika Singmahan,
  • Chiraphat Takpho,
  • Nadtanet Nunthaboot,
  • Worrawat Promden,
  • Ruchilak Rattarom,
  • Khwanyuruan Naksuwankul,
  • Kusavadee Sangdee,
  • Aphidech Sangdee,
  • Masahiko Isaka,
  • Prapairat Seephonkai

摘要

The DPPH radical scavenging, α-glucosidase inhibitory, nitric oxide (NO) inhibitory, and cytotoxic activities of the extracts from fruiting bodies of wood-rot basidiomycete Fulvifomes fastuosus were evaluated in this study. While the CH2Cl2 extract was biologically inactive, chromatographic fractionation led to the isolation of two chlorinated hydroquinone derivatives, drosophilin A methyl ether (DAME; 1) and drosophilin A (DA; 2). The EtOAc-partitioned fraction, obtained from the partitioning of the MeOH extract, exhibited strong α-glucosidase and NO inhibitory activities. Further investigation led to the isolation of inoscavin A (3) as the major constituent, along with inoscavin E (4) and polyphenols (5–7). Inoscavin A demonstrated potent α-glucosidase inhibition (IC50 = 3.22 µM), surpassing acarbose by 59-fold, and exhibited non-competitive inhibition kinetics (Kᵢ = 3.25 µM). Molecular docking studies supported an allosteric binding mode. It also displayed favorable drug-likeness and ADMET (absorption, distribution, metabolism, excretion, and toxicity) profiles, including good solubility, high intestinal absorption, low central nervous system (CNS) penetration, and absence of hepatotoxicity. These results suggest that F. fastuosus is a promising source of antidiabetic agents, with inoscavin A as a principle active compound.