Glaucine

Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a K_i of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer^{[1][2][3][4][5][6]}. IC50 & Target:Ki: 3.4 µM (Phosphodiesterase 4 (PDE4))^[1]
α-adrenoceptor^[1]
Ca²⁺ channel^[1]
Dopamine D1/D2 receptors^[2]
In Vitro:Glaucine (0.1 μM-1 mM; 30 min) produces a concentration-dependent inhibition of both spontaneous tension and histamine (HY-B1204)-induced tension in isolated human bronchial tissues^[1].
Glaucine (10 μM-1 mM; 30 min) concentration-dependently inhibits the concentration of calcium ions in isolated human bronchial tissues induced by potassium depolarization^[1].
Glaucine (0.1-3 mM; 120 min) concentration-dependently inhibits the release of peroxidase from human eosinophils^[1].
Glaucine (0-50 μM; 24 and 48 h) inhibits the proliferation of MCF-7 cells induced by Phorbol 12-myristate 13-acetate (HY-18739) in a concentration-dependent manner^[4].
Glaucine (0-30 μM; 36 h) significantly blocks the expression and activity of MMP-9 in MCF-7 cells induced by Phorbol 12-myristate 13-acetate (HY-18739) in a dose-dependent manner^[4].
Glaucine (0-30 μM; 24 h) significantly inhibits the invasion of MDA-MB-231 cells in a dose-dependent manner^[4].
In Vivo:Glaucine (5-10 mg/mL; inhale; 3 min) inhibits acute bronchoconstriction and microvascular leakage at all airway levels induced by inhalation of aerosol antigens in guinea pigs sensitized with ovalbumins (HY-W250978)^[5].
Glaucine (10-100 mg/kg; p.o.; 60 min) can effectively inhibit carrageenan (HY-125474)-induced paw edema and LPS (HY-D1056)-induced fever in rats, as well as acetic acid (HY-Y0319)-induced abdominal contraction in mice^[6].