11β,13-Dihydrolactucopicrin is a sesquiterpene lactone and the main bitter component of chicory root. 11β,13-Dihydrolactucopicrin inhibits yeast α-glucosidase activity ( IC50 = 27.49 μM) and inhibits Crz1 activation and nuclear accumulation. 1β,13-Dihydrolactucopicrin possesses blood-brain barrier penetration capacity in an in vitro HBMEC blood-brain barrier model and can generate cysteine-conjugated metabolites within brain microvascular endothelial cells. 11β,13-Dihydrolactucopicrin can regulate the lncRNA H19/miR-21-3p signaling axis; it upregulates the expression of ABCG2 and lncRNA H19, downregulates miR-21-3p, inhibits the release of IL-6, TNF-α, and hs-CRP pro-inflammatory mediators, and alleviates urate-induced inflammatory injury in renal epithelial cells. 11β,13-Dihydrolactucopicrin can be used in research on diabetes and renal urate deposition [1] [2] [3] [4].
In Vitro, 11β,13-dihydrolactucopicrin (10 μM; 4 h) exhibited moderate permeability in Caco-2 monolayer cells, with the apical concentration decreasing by 29.9%, and no cysteine adduct was formed[1]. 11β,13-dihydrolactucopicrin (12.5-100 μM; 3 h) has a maximum non-toxic concentration of 12.5 µM in Saccharomyces cerevisiae[1]. 11β,13-dihydrolactucopicrin exhibited moderate inhibitory activity against the calcineurin-Crz1 pathway in Saccharomyces cerevisiae YAA5, with an inhibition rate of 26% at 12.5 µM[1]. 11β,13-Dihydrolactucopicrin (compound 5) inhibited yeast α-glucosidase with an IC50 of 27.49 μM, showing limited inhibitory activity, possibly because its phenyl group hinders binding to the enzyme[2]. 11β,13-Dihydrolactucopicrin (predicted by molecular docking) showed good binding activity with the ABCG2 protein, exhibiting the lowest binding energy among the tested compounds[3]. 11β,13-dihydrolactucopicrin (5 μM; 2 h) can be transported across the in vitro BBB model of HBMEC, with a transport percentage between 10% and 20%[4]. 11β,13-Dihydrolactucopicrin (10 μM; 24 h) attenuates inflammation and enhances ABCG2 expression in UA- and LPS-stimulated NRK-52E cells, while uniquely upregulating lncRNA H19 and downregulating miR-21-3p[3].
References:
[1]. Matos MS, et al. Assessing the Intestinal Permeability and Anti-Inflammatory Potential of Sesquiterpene Lactones from Chicory. Nutrients. 2020 Nov 19;12(11):3547.
[2]. Fan H, et al. Isolation and identification of terpenoids from chicory roots and their inhibitory activities against yeast α-glucosidase. European Food Research and Technology, 2017, 243: 1009-1017.
[3]. An X Y, et al. Investigation of Pharmacological Mechanisms and Active Ingredients of Cichorium intybus L. in Alleviating Renal Urate Deposition via lncRNA H19/miR-21-3p Regulation to Enhance ABCG2 Expression. International Journal of Molecular Sciences, 2025, 26(16):7892.
[4]. Ávila-Gálvez MÁ, et al. Costunolide and parthenolide: Novel blood-brain barrier permeable sesquiterpene lactones to improve barrier tightness. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2023 Nov;167:115413.
In Vitro, 11β,13-dihydrolactucopicrin (10 μM; 4 h) exhibited moderate permeability in Caco-2 monolayer cells, with the apical concentration decreasing by 29.9%, and no cysteine adduct was formed[1]. 11β,13-dihydrolactucopicrin (12.5-100 μM; 3 h) has a maximum non-toxic concentration of 12.5 µM in Saccharomyces cerevisiae[1]. 11β,13-dihydrolactucopicrin exhibited moderate inhibitory activity against the calcineurin-Crz1 pathway in Saccharomyces cerevisiae YAA5, with an inhibition rate of 26% at 12.5 µM[1]. 11β,13-Dihydrolactucopicrin (compound 5) inhibited yeast α-glucosidase with an IC50 of 27.49 μM, showing limited inhibitory activity, possibly because its phenyl group hinders binding to the enzyme[2]. 11β,13-Dihydrolactucopicrin (predicted by molecular docking) showed good binding activity with the ABCG2 protein, exhibiting the lowest binding energy among the tested compounds[3]. 11β,13-dihydrolactucopicrin (5 μM; 2 h) can be transported across the in vitro BBB model of HBMEC, with a transport percentage between 10% and 20%[4]. 11β,13-Dihydrolactucopicrin (10 μM; 24 h) attenuates inflammation and enhances ABCG2 expression in UA- and LPS-stimulated NRK-52E cells, while uniquely upregulating lncRNA H19 and downregulating miR-21-3p[3].
References:
[1]. Matos MS, et al. Assessing the Intestinal Permeability and Anti-Inflammatory Potential of Sesquiterpene Lactones from Chicory. Nutrients. 2020 Nov 19;12(11):3547.
[2]. Fan H, et al. Isolation and identification of terpenoids from chicory roots and their inhibitory activities against yeast α-glucosidase. European Food Research and Technology, 2017, 243: 1009-1017.
[3]. An X Y, et al. Investigation of Pharmacological Mechanisms and Active Ingredients of Cichorium intybus L. in Alleviating Renal Urate Deposition via lncRNA H19/miR-21-3p Regulation to Enhance ABCG2 Expression. International Journal of Molecular Sciences, 2025, 26(16):7892.
[4]. Ávila-Gálvez MÁ, et al. Costunolide and parthenolide: Novel blood-brain barrier permeable sesquiterpene lactones to improve barrier tightness. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2023 Nov;167:115413.