New Polyketide and Butenolide Derivatives from the Mangrove Fungus Aspergillus spelaeus SCSIO 41433

Mar Drugs. 2025 Jun 13;23(6):251. doi: 10.3390/md23060251.

Abstract

Two new racemic mixtures, including a polyketide, (±)-penilactone F (1), and a butenolide, (±) phenylbutyrolactone IIa (2), were isolated from the mangrove sediment-derived strain Aspergillus spelaeus SCSIO 41433. Additionally, 20 known compounds were isolated, including four penicillin-like compounds (11-14), three alkaloids (15-17), one sesquiterpene (18), and four phenolic acids (19-22). Their structures were elucidated through NMR spectroscopy, HRESIMS, X-ray diffraction, and ECD calculations. In the PDE4 inhibitory activity and anticancer cell activity assays, compounds 2, 3, 5, 8, 9, 11-14, and 16 exhibited weak PDE4 inhibitory activity at a concentration of 10 µM, Compound 11 demonstrated potent inhibitory effects against six cancer cell lines (MDA-MB-231, MDA-MB-435, HCT116, SNB-19, PC3, and A549), with IC50 values ranging from 3.4 to 23.7 µM.

Keywords: PDE4 inhibitors; alkaloids; anticancer; butenolides; mangrove sediment-derived fungi.

MeSH terms

  • 4-Butyrolactone* / analogs & derivatives
  • 4-Butyrolactone* / chemistry
  • 4-Butyrolactone* / isolation & purification
  • 4-Butyrolactone* / pharmacology
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / isolation & purification
  • Antineoplastic Agents* / pharmacology
  • Aspergillus* / chemistry
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Phosphodiesterase 4 Inhibitors* / chemistry
  • Phosphodiesterase 4 Inhibitors* / isolation & purification
  • Phosphodiesterase 4 Inhibitors* / pharmacology
  • Polyketides* / chemistry
  • Polyketides* / isolation & purification
  • Polyketides* / pharmacology

Substances

  • 4-Butyrolactone
  • Polyketides
  • Antineoplastic Agents
  • butenolide
  • Phosphodiesterase 4 Inhibitors