Discovery of Na_v1.7 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_v1.7 channel in a fluorescent-based flux assay. Bioactivity-guided chemical investigation led to the isolation of two glycoglycerolipids (1 and 2). In preliminary screening, 1 showed stronger Na_v1.7 inhibition, while secondary screening using patch-clamp electrophysiology, which measures ion movement across membranes, revealed 2 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.