Galegine (hemisulfate)

Galegine hemisulfate, a guanidine derivative, contributes to weight loss in mice. Galegine hemisulfate activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hemisulfate has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains^[1][2]. In Vitro:Pre-treatment with Galegine (10 μM-3 mM; 5 h) hemisulfate produces a concentration-dependent stimulation of insulin-independent glucose uptake by 3T3-L1 adipocytes without any effect on cell viability. Incubation with Galegine (1 μM-1 mM, 5 h) hemisulfate produces a concentration-dependent stimulation of glucose uptake into L6 myotubes, again without any effect on cell viability^[1].
Galegine (0.3-300 μM; 24 hours) hemisulfate produces a slight reduction in basal glycerol release and a more marked reduction in Isoprenaline (HY-108353)-stimulated glycerol release from 3T3-L1 adipocytes. Incubation of H4IIE rat hepatoma cells with Galegine (10 or 300 μM) hemisulfate for up to 6 hours produces a time-dependent activation of AMPK measured in cell lysates, with maximal activation at 360 min and twofold activation still evident at 24 hous in the presence of 300 μM Galegine hemisulfate. The effect of 300 ΜM Galegine hemisulfate is markedly greater than that of 10 μM. Incubation with Galegine hemisulfate for 1 hour produces a concentration-dependent activation of AMPK in both 3T3L-1 adipocytes and L-6 myotubes. Galegine hemisulfate also produces a concentration-dependent activation of the enzyme in a human kidney cell line (HEK293)^[1]. In Vivo:Galegine (63 mg/kg; feed; daily for 11 days) hemisulfate produces a significant reduction in body weight^[1].