Common ivy is better known as a garden invader or a rather attractive indoor plant that's prone to triggering allergic reactions or irritation. Now, for the first time, it's been found to be extremely effective in blocking pain signals – by invading a key pain receptor.
Scientists at Leipzig University in Germany have made what they deem an "important advancement" in finding new, safe pain relief therapeutics, by experimenting with extracts of ivy (Hedera helix). The evergreen vine, also known as English ivy and easily identified by its leaves, has long been considered a holistic way to treat inflammation and respiratory issues, and is readily available in refined medicinal form.
Testing thousands of substances for potential pain-relief activity, the team of researchers led by Professor Annette Beck-Sickinger from Leipzig's Institute of Biochemistry found that one such triterpenoid that occurs in the plant's leaves, binds to the receptor that regulates pain in the human body.
Triterpenoids, which are found in plants, fungi and animals, as well as sedimentary rocks, are organic compounds that are known to have anti-inflammatory and antiviral properties. This one, hederagenin, has a particularly effective way of blocking the activity of the neuropeptide FF receptor 1 (NPFFR1). This receptor protein is most commonly found in the spine and in the brain, and regulates pain signals and perception.
When hederagenin binds to the receptor, it essentially silences the signaling pathway to communicate messages of pain to the brain. As such, it holds great potential as a safe, effective treatment for chronic pain in particular.
“These findings make a significant contribution to understanding the activation mechanism of NPFFR1 and may facilitate the rational design of future therapeutics for chronic pain," said Beck-Sickinger. "They demonstrate the importance of basic research in translating findings into applications."
Because NPFFR1 has a lot of similar receptors, the fact hederagenin is specifically attracted to its properties makes this discovery a big step forward in pain research.
"The elucidation of key residues causing selectivity not only enhances the understanding of ligand-receptor interactions within the NPFF receptor system but also paves the way for rational drug design strategies aimed at optimizing therapeutic efficacy and minimizing off-target effects in the modulation of nociceptive signaling pathways," the researchers noted in the study.
The study was published in the journal Angewandte Chemie International Edition.
Source: Leipzig University
