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| Autores principales: | , , , , , , , , , , , , |
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| Formato: | Artículo científico |
| Lenguaje: | en |
| Publicado: |
Journal of natural products
2025
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| Materias: | |
| Acceso en línea: | https://pubmed.ncbi.nlm.nih.gov/41124213/ |
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- Discovery of Na1.7 Inhibitors through the Screening of Marine Natural Product Extracts. Adewole, Adetola H Chhetri, Bhuwan Khatri Abdelwahab, Ghada M Bhanushali, Riya Sweeney-Jones, Anne Marie Greene, Madison Shim, Jaehoon Asef, Carter K Vaelli, Patric Barrett, Lee Fernández, Facundo M Quave, Cassandra L Kubanek, Julia Biological Products Molecular Structure Animals Porifera Marine Biology Drug Discovery NAV1.7 Voltage-Gated Sodium Channel Humans Rhodophyta Glycolipids Anthozoa High-Throughput Screening Assays Automated high-throughput screening of a prefractionated extract library of marine macroorganisms identified 239 hits (hit rate 2.5%), including a marine algal extract that blocked the Na1.7 channel in a fluorescent-based flux assay. Bioactivity-guided chemical investigation led to the isolation of two glycoglycerolipids ( and ). In preliminary screening, showed stronger Na1.7 inhibition, while secondary screening using patch-clamp electrophysiology, which measures ion movement across membranes, revealed as more potent. This study identified some ion channel modulators from diverse taxonomic origins, including red algae, sponges, and corals, many of which are underexplored and represent promising leads for future drug discovery.