Teprenone, an Anti-ulcer Drug, is an Inducer of Heat Shock Proteins (HSPs)

Ulcer is caused by discontinuity or break in a bodily membrane, which can damage normal function of the affected organ. Besides, it is induced by sloughing out of inflamed necrotic tissue. Ulcer includes genital ulcers, pressure ulcers, diabetic foot ulcers, gastric ulcers, and so on. Heat shock proteins (HSPs) are important molecules in inflammatory, infectious and tumoral processes. Additionally, Many researches show that HSP70 associated with gastric cancer and duodenal ulcer in a population at high risk of gastric cancer.

Teprenone is an anti-ulcer agent, acting by promoting epithelial regeneration by increasing the mucosal hexosamine content to protect mucosal. In addition, it also is an inducer of HSPs.

Teprenone (1 μM) significantly prevents ethanol-induced exfoliation, and reduces lactate dehydrogenase (LDH) release in gastric mucosal cells. it can gradually increase HSC70 level, and rapidly accumulates the stress-inducible HSP90, HSP70, and HSP60 concentrations within 30-60 min at 1 μM. Besides, Teprenone also activates the heat shock factor 1.

In oral experiments, Teprenone (200 mg/kg) results in the accumulation of HSP70 mRNA in rats. Teprenone (50 and 100 mg/kg; p.o., twice daily) significantly decreases the ulcer index by approximately 30% in acetic acid-induced ulcer rats. As well as, Teprenone remarkably increases the concentration and secretion of the high-molecular-weight glycoprotein (HMG). it is inferred that Teprenone strengthens the defensive force of gastric mucosa by increasing the HMG with a polymeric structure.

In conclusion, Teprenone is a potent anti-ulcer drug and an inducer of HSPs.

[1] Ferrer-Ferrer M, et al. Arch Med Res. 2013;44(6):467-474.
[2] Hirakawa T, et al. Gastroenterology. 1996;111(2):345-357.
[3] Ito M, et al. Jpn J Pharmacol. 1986;41(1):117-125.