Sunflower Peptide as ‘Template’ for Potential Analgesic

AHA Publisher — Thu, 15 Jul 2021 07:00:46 +0000

Medical University of Vienna via EurekAlert – A naturally occurring peptide in sunflower seeds was synthetically optimised and has now been identified as a potential drug for treating abdominal pain or inflammation (in the gastrointestinal tract, abdominal area and/or internal organs). That is the finding of an international study led by Christian Gruber from MedUni Vienna’s Institute of Pharmacology (Center for Physiology and Pharmacology), which was conducted jointly with the University of Queensland and Flinders University in Australia and has now been published. The scientific aim of the study is to find analgesics that are only active in the periphery and do not cross the blood-brain barrier, as an alternative to commonly used synthetic opioids. Gruber explains the background: “Morphine was one of the first plant-based medicines and was isolated from the dried latex of poppies more than 200 years ago. It binds to opioid receptors in the brain and is still regarded as the main pillar of pain therapy. However, there is a high risk of opioid addiction, and an overdose – as a result of this strong dependency – inhibits the breathing centre in the brain, which can result in respiratory depression and, in the worst case, in death.” For this reason, researchers throughout the world are trying to make analgesics safer and to find active drug molecules that do not have the typical opioid side-effects. Sunflower extracts were to some extent used in traditional medicine for their anti-inflammatory and analgesic properties. In the current study, the scientists from Austria and Australia, primarily PhD student Edin Muratspahi?, isolated the plant molecule that may be responsible for this effect. Medicinal chemistry methods were then used to optimise the so-called sunflower trypsin inhibitor-1 (SFTI-1), one of the smallest naturally occurring cyclic peptides, by ‘grafting’ an endogenous opioid peptide into its scaffold. A total of 19 peptides were chemically synthesized based on the original SFTI-1 blueprint and pharmacologically tested. “One of these variants turned out to be our lead candidate for as potential innovative analgesic molecule, especially for pain in the gastrointestinal tract or in the peripheral organs. This peptide is extremely stable, highly potent and its action is restricted to the body’s periphery. Its use is therefore expected to produce fewer of the typical side-effects associated with opioids,” point out Gruber and Muratspahi?. The mode-of-action of the peptide is via the so-called kappa opioid receptor; this cellular protein is a drug target for pain relief, but is often associated with mood disorders and depression. The sunflower peptide does not act in the brain, hence there is much less risk of dependency or addiction. Furthermore, it selectively activates only the molecular signalling pathway that influences pain transmission but does not cause the typical opioid side-effects. The data of the animal model in the current study are very promising: the scientists see great potential for using this peptide in the future to develop a safe medication – which could be administered orally in tablet form – to treat pain in the gastrointestinal tract, and this drug could potentially also be used for related painful conditions, e.g. for inflammatory bowel disease. Using Nature’s Blueprint The research of this MedUni Vienna laboratory led by Christian Gruber exploits the concept of using Nature’s blueprint to develop optimised drugs. “We are searching through large databases containing genetic information of plants and animals, decoding new types of peptide molecules and studying their structure, with a view to testing them pharmacologically on enzymes or membrane receptors and ultimately utilizing them in the disease model,” explains Gruber. Finally, potential drug candidates are chemically synthesised in a slightly modified form based on the natural blueprint, to obtain optimised pharmacological properties. To read the original article click here.

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Seeking a Treatment for IBS Pain in Tarantula Venom

AHA Publisher — Thu, 01 Jul 2021 07:00:34 +0000

American Chemical Society via EurekAlert – For patients who have inflammatory bowel syndrome (IBS), the condition is literally a pain in the gut. Chronic — or long-term — abdominal pain is common, and there are currently no effective treatment options for this debilitating symptom. In a new study in ACS Pharmacology & Translational Science, researchers identify a new potential source of relief: a molecule derived from spider venom. In experiments with mice, they found that one dose could stop symptoms associated with IBS pain. The sensation of pain originates in electrical signals carried from the body to the brain by cells called neurons. Tiny channels in the surfaces of neurons help them transmit these signals by allowing positively charged sodium ions to pass into the cell. There are numerous types of sodium channels, and some pain-killing drugs work by blocking them. However, existing treatments interfere with channels indiscriminately and can only be used briefly — not for chronic pain. Stuart Brierley, Glenn King and colleagues wanted to find a way to selectively target the channels activated during chronic IBS pain. The researchers focused on a particular sodium channel they suspected was responsible for chronic IBS pain. Then, to block it, they turned to the richest known source of molecules that alter the activity of sodium channels: spider venom. In the venom of a Peruvian tarantula, they discovered a molecule that they named Tsp1a, which had promising blocking activity. To test its potential as a treatment, the researchers used mice that had an IBS-related condition, and they monitored the mice during the experiment to detect a reflex associated with pain. A single Tsp1a treatment delivered into the mice’s colons significantly reduced the occurrence of this reflex, indicating pain relief. What’s more, Tsp1a appeared highly selective and did not interfere with other body functions, suggesting it could be used safely in humans. While Tsp1a shows promise as a potential treatment for chronic IBS pain, thorough studies of its activity in the body and the immune system’s reaction to it will be critical, the researchers write. To read the original article click here.

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Sunflower Peptide as ‘Template’ for Potential Analgesic

Seeking a Treatment for IBS Pain in Tarantula Venom