Discovery of Na <sub>v</sub> 1.7 Inhibitors through the Screening of Marine Natural Product Extracts

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 Na<sub>v</sub>1.7 channel in a fluorescent-based flux assay. Bioactivity-guided chemical investigation led to the isolation of two glycoglycerolipids (<b>1</b> and <b>2</b>). In preliminary screening, <b>1</b> showed stronger Na<sub>v</sub>1.7 inhibition, while secondary screening using patch-clamp electrophysiology, which measures ion movement across membranes, revealed <b>2</b> 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.

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Publication Details

Journal
Journal of Natural Products
Published
2025-10-22
DOI
https://doi.org/10.1021/acs.jnatprod.5c00978
Primary Topic
Marine Sponges and Natural Products
Type
article
Field-Weighted Citation Impact
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article

Discovery of Na v 1.7 Inhibitors through the Screening of Marine Natural Product Extracts

Cassandra L. Quave, Carter K. Asef, Madison Greene, Facundo M. Fernández et al.
Journal of Natural Products
Marine Sponges and Natural Products
article

Discovery of Na v 1.7 Inhibitors through the Screening of Marine Natural Product Extracts

Cassandra L. Quave, Carter K. Asef, Madison Greene, Facundo M. Fernández, Riya Bhanushali, Adetola H. Adewole, Patric M Vaelli, Ghada M. Abdelwahab, Anne Marie Sweeney-Jones, Julia Kubanek, Bhuwan K. Chhetri, Jaehoon Shim, Lee Barrett
article en

Abstract

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 Na<sub>v</sub>1.7 channel in a fluorescent-based flux assay. Bioactivity-guided chemical investigation led to the isolation of two glycoglycerolipids (<b>1</b> and <b>2</b>). In preliminary screening, <b>1</b> showed stronger Na<sub>v</sub>1.7 inhibition, while secondary screening using patch-clamp electrophysiology, which measures ion movement across membranes, revealed <b>2</b> 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.

Journal of Natural ProductsVol. 88(11)
Boston Children's Hospital (US), Georgia Institute of Technology (US), Harvard University (US), Emory University (US), Office of the Assistant Secretary for Health (US), Institute of Neurobiology (BG), Parker Hannifin (United States) (US)
Openalex Percentile: Top 68%
Marine Sponges and Natural Products
DOIOpen Access PDFOpenAlex
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Discovery of Na <sub>v</sub> 1.7 Inhibitors through the Screening of Marine Natural Product Extracts — Cassandra L. Quave, Carter K. Asef, et al. · Journal of Natural Products (2025) | TGRS Research Map | TGRS