5α-Cyprinol sulfate is an orally active bile salt and heterospecific pheromone. 5α-Cyprinol sulfate promotes lipid digestion in fish. 5α-Cyprinol sulfate inhibits taurocholic acid uptake mediated by apical bile salt transporters in rat ileum. 5α-Cyprinol sulfate can be used in studies of fish toxic acute renal failure [1] [2].
In Vivo, 5α-Cyprinol sulfate (1 μmol/min/kg; i.v.; single infusion) administered intravenously to anesthetized rats induces hemolysis, hemobilia, and death[2]. 5α-Cyprinol sulfate (1-4 μmol/min/kg; i.v. into perfused liver; 20-minute infusion) administered to isolated perfused rat livers shows a maximum biliary secretion rate (Tmax) of 0.5 μmol/kg/min, reduces bile flow at the higher dose, and competitively inhibits taurocholate hepatic uptake and secretion[2].
In Vitro, 5α-Cyprinol sulfate (100 μM; 15 min at 37°C) completely inhibits sodium-dependent taurocholate uptake in COS-7 cells transiently transfected with the ileal apical bile salt transporter (asbt) after 15 minutes of incubation at 37°C[2].
References:
[1]. Hahn MA, et al. 5α-cyprinol sulfate, a bile salt from fish, induces diel vertical migration in Daphnia. Elife. 2019;8:e44791. Published 2019 May 2.
[2]. Goto T, et al. Physicochemical and physiological properties of 5alpha-cyprinol sulfate, the toxic bile salt of cyprinid fish. J Lipid Res. 2003;44(9):1643-1651.
In Vivo, 5α-Cyprinol sulfate (1 μmol/min/kg; i.v.; single infusion) administered intravenously to anesthetized rats induces hemolysis, hemobilia, and death[2]. 5α-Cyprinol sulfate (1-4 μmol/min/kg; i.v. into perfused liver; 20-minute infusion) administered to isolated perfused rat livers shows a maximum biliary secretion rate (Tmax) of 0.5 μmol/kg/min, reduces bile flow at the higher dose, and competitively inhibits taurocholate hepatic uptake and secretion[2].
In Vitro, 5α-Cyprinol sulfate (100 μM; 15 min at 37°C) completely inhibits sodium-dependent taurocholate uptake in COS-7 cells transiently transfected with the ileal apical bile salt transporter (asbt) after 15 minutes of incubation at 37°C[2].
References:
[1]. Hahn MA, et al. 5α-cyprinol sulfate, a bile salt from fish, induces diel vertical migration in Daphnia. Elife. 2019;8:e44791. Published 2019 May 2.
[2]. Goto T, et al. Physicochemical and physiological properties of 5alpha-cyprinol sulfate, the toxic bile salt of cyprinid fish. J Lipid Res. 2003;44(9):1643-1651.