Current treatments for pain and inflammation, such as opioids and NSAIDs, are associated with dependency and adverse side effects. The opioid crisis, characterized by the misuse of opioids, particularly synthetic variants like fentanyl and tramadol, has led to a significant number of deaths, underscoring the urgency to develop alternative pain management strategies. Similarly, the long-term use of anti-inflammatory drugs such as corticosteroids and NSAIDs is often limited due to poor tolerance and adverse reactions. Thus, there is a growing need for alternative therapies that offer effective pain and inflammation relief with fewer side effects.

In a recent study published in Communications Biology, researchers screened 1,444 plant extracts, primarily from native species in California and the United States Virgin Islands, against the Kv1.3 (expressed in T-cells and linked to inflammation) and Kv7.2/7.3 channels (expressed in nociceptive neurons and linked to pain). This high-throughput screening, using FLIPR and automated patch clamp (SyncroPatch 384), identified a subset of extracts that both inhibited Kv1.3 and activated Kv7.2/7.3 channels, suggesting dual anti-inflammatory and analgesic effects.

Notably, extracts from witch hazel and fireweed were among the top candidates, with their actions attributed to hydrolysable tannins. These tannins exhibit polymodal modulation of multiple K+ channel types, contributing to their dual therapeutic actions.

Indeed, previous studies have shown that tannic acid increases Kv1.1 and Kv1.2 currents. In contrast, in this study, the authors found that tannic acid strongly inhibits Kv1.3. In silico docking and mutagenesis experiments revealed that the differential effects of hydrolysable tannins on Kv1 isoforms (Kv1.1, Kv1.2, and Kv1.3) are due to sequence divergence in pore-proximal extracellular linkers.

In summary, this research highlights the potential of botanical extracts as dual-action analgesic and anti-inflammatory agents through the modulation of specific K+ channels. It also illustrates a successful strategy to screen botanical extracts for potential therapeutic effects.

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Find the full article here: Polymodal K+ channel modulation contributes to dual analgesic and anti-inflammatory actions of traditional botanical medicines

Learn more about the SyncroPatch 384, our newest generation automated patch clamp system: https://www.nanion.de/products/syncropatch-384/