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Elaiophylin is a natural macrodiolide macrolide antibiotic isolated from actinomycetes such as Streptomyces melanosporus and related Streptomyces species, characterized by a C2-symmetric 16-membered lactone scaffold and potent bioactivity across multiple systems. It functions as a late-stage autophagy inhibitor that promotes autophagosome accumulation but blocks autophagic flux by impairing lysosomal cathepsin activity, leading to SQSTM1/p62 buildup and cancer cell death, and also acts as a mitophagy inhibitor linked to downregulation of SIRT1 and altered FoxO3a or Nrf2 signaling in various tumor models including ovarian cancer, uveal melanoma, and lung adenocarcinoma. Beyond its antitumor properties, elaiophylin has been reported to exert antibacterial, antifungal, anthelmintic, immunosuppressive, anti‑inflammatory, antiviral, α‑glucosidase inhibitory, and testosterone 5‑reductase–inhibitory actions, and more recently to activate AMPK and improve metabolic parameters in obese and diabetic models, making it a versatile research tool and an early-stage investigational lead rather than an approved pharmaceutical product.
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