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Rusotäpläjuurekas (Rhodocollybia maculata), κ-opioidiagonistia tuottava sieni

Poissa Arvalis

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Tuoreen tutkimuksen mukaan rusotäpläjuurekkaan (jota ilmeisesti tavataan myös Suomessa) sisältämä (Salvia divinorumin vaikuttavan aineen salvinoriini A:n sukuinen) kollybolidiksi nimetty aine toimii (kuten salvinoriini A) erittäin potenttina κ-opioidireseptorin agonistina.

Collybolide is a novel biased agonist of κ-opioid receptors with potent antipruritic activity (Gupta et al., 2015)

Lainaus
In recent years, the κ-opioid receptor (κOR) has become an attractive therapeutic target for the treatment of a number of disorders including depression, visceral pain, and drug addiction. A search for natural products with novel scaffolds targeting κOR has been intensive. Here, we report the discovery of a natural product (Colly) from the fungus Collybia maculata as a novel scaffold that contains a furyl-δ-lactone core structure similar to that of Salvinorin A, another natural product isolated from the mint Salvia divinorum. We show that Colly functions as a κOR agonist with antinociceptive and antipruritic activity. Interestingly, Colly exhibits biased agonistic activity, suggesting that it could be used as a backbone for the generation of novel therapeutics targeting κOR with reduced side effects.
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