Teprenone (Geranylgeranylacetone)

Cell experiment:

Human umbilical vein endothelial cells (HUVECs) are seeded onto 48-well plates at a density of 1 × 102 cells/well before Teprenone and/or radiation treatment. Cell viability is determined at 48 h after treatment using 0.5 mg/mL MTT solution in serum-free media. This solution is incubated with the cells for 2 h in the 37°C humidified atmosphere containing 5% CO2. Then, the MTT solution is removed, and the cells are dissolved in 100 µL of DMSO. Optical densities of the supernatants are measured at 540 nm with an ELISA spectrophotometer[3].

Animal experiment:

Male Wister strain rats weighing approximately 250 g are individually housed in wire-mesh cages in a room maintained at 23°C on a 12-hour light-dark cycle. Rats are allowed free access to a standard laboratory chow. Teprenone (200 mg/kg; as emulsion with 5% gum arabic and 0.008% α-tocopherol) or vehicle (5% gum arabic emulsion containing 0.008% α-tocopherol) is given orally in a volume of 5 mL/kg through a metal tubing attached to a 6-mL syringe. Two hours later, rats are placed in restraint cages and then vertically immersed in water at 23°C to the level of the xyphoid process. The rats are killed by decapitation at the indicated times[1].

References:

[1]. Hirakawa T, et al. Geranylgeranylacetone induces heat shock proteins in cultured guinea pig gastric mucosal cells and rat gastric mucosa. Gastroenterology. 1996 Aug;111(2):345-57.
[2]. Caprioli J, et al. Retinal ganglion cell protection with geranylgeranylacetone, a heat shock protein inducer, in a rat glaucoma model. Trans Am Ophthalmol Soc. 2003;101:39-50; discussion 50-1.
[3]. Han NK, et al. Geranylgeranylacetone Ameliorates Intestinal Radiation Toxicity by Preventing Endothelial Cell Dysfunction. Int J Mol Sci. 2017 Oct 7;18(10).