Inflammation is a normal and expected physiological response to tissue trauma or infection. However, for a large portion of the population, these responses occur on a far more extensive and disruptive scale. Now that medical practitioners generally better understand the signs and symptoms of widespread and chronic inflammatory disorders—from obvious disorders such as rheumatoid arthritis and psoriasis to the lesser-understood connections between inflammation and diabetes, heart disease, and even cancer—the degree and occurrence of such cases represents a public health problem on a larger scale than imagined. As such, the push to discover simple but effective treatment methods is stronger than ever.
At present, as the pathogenesis of inflammatory and immunological diseases is unclear, there are few effective therapeutic drugs available in clinical practice. In such a context, the appropriate preclinical research techniques and models are required to help companies and researchers further develop and evaluate new drugs. Our Preclinical Pharmacodynamics Department has been deeply involved in this field for years, developing reliable animal-based efficacy evaluation models aimed at different targets and pathways, thus facilitating the clinical transformation of new drugs.
Modern Western steroidal and nonsteroidal treatments lack the efficiency needed to make them effective in manageable doses, and larger doses have shown to cause too many adverse reactions to make them viable as long-term options. As it happens, several natural remedies, with a few synthesized twists, have shown a great deal of treatment potential, leading to the emergence of a class of biomolecular and phytochemical agents, including isoprenoids, phenolic compounds, and the increasingly popular flavonoids.
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A team of researchers from Quebec’s Université Laval—Sébastien Cardinal, Jabrane Azelmat, Daniel Grenier, and Normand Voyer—has turned its attention to these centuries-old plant-based treatments to see if these natural remedies can produce reliable and repeatable results. The team isolated a compound found in maple syrup, called quebecol, and found that, in in vitro bioassays, it has demonstrated strong potential as a chemopreventative and chemotherapeutic agent.
To test the idea, molecules of quebecol were split into sub-molecules, designated North and South. These reduced and isolated molecule combinations were tested in a series of experiments involving additional benzyl groups and tetrasubstituted alkenes to target individual compounds. The quebecol and its derivatives were tested for anti-inflammatory activity using leukocytes, human macrophages that are essential immune system elements and whose usefulness in chronic inflammatory pathologies has been well-established. The leukocytes’ interleukin secretions, either amplified or reduced at various stages of the inflammatory process and thereby producing an accurate measure of inflammatory response, can establish therapeutic efficacy in treatments for both acute and chronic inflammatory disorders as well as some autoimmune diseases.
The team’s results showed that the maple-derived quebecol compound does indeed produce an anti-inflammatory response in trials by inhibiting the leukocyte secretion of certain cytokines, specifically interleukin-6 and TNF-α, a compound that is crucial in the regulation of inflammatory responses and related disorders. The results also identified a relationship between structure and activity, most importantly the response and activity observed in quebecol1, a molecule derived from the North substructure.
The ease of synthesizing this kind of compound may hold the key to developing a whole new class of effective plant-based anti-inflammatory compounds. The team is now working on preparing and developing such compounds, as well as ascertaining the potential in multiple quebecol analogs.
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