Abstract
Suramin exerts antitumour effects by interfering with the biological activity of several growth factors. It is also known that growth factors, including epidermal growth factor, play a primary role in the protection of gastric mucosa and promotion of ulcer healing. In the present study, the penetration of suramin into the stomach as well as the influence exerted by this drug on ethanol-induced gastric mucosal damage were investigated. Suramin was administered by the intraperitoneal route to male rats every other day for fourteen days. Animals were then used for:
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1.
Assessment of suramin levels in plasma and tissues;
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Histomorphometric evaluation of ethanol-induced gastric mucosal damage;
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Measurement of gastric acid secretion after pylorus ligation.
The concentrations of suramin in plasma, stomach and kidney were 158±18.8 μg/ml, 179.7±33.0 μg/g and 1480.9±85.8 μg/g (n=6), respectively. Suramin did not induce gastric mucosal damage under basal conditions. However, the drug markedly enhanced ethanol-induced necrotic damage at all times tested. In addition, suramin significantly enhanced gastric acid output induced by pylorus ligation in conscious rats. Suramin is characterized by an unusually long half-life and a remarkable accumulation in kidney, whereas, in the majority of other organs, the drug reaches levels that are 8–10 times lower than those found in renal tissue. The data obtained in the present study are consistent with this pharmacokinetic profile and suggest that suramin concentration achieved in gastric tissue, which is known to inhibit the proliferation of several cell lines in vitro, is high enough to induce an impairment of mucosal protective mechanisms.
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Blandizzi, C., Danesi, R., Gherardi, G. et al. Effect of suramin on ethanol-induced gastric mucosal injury: Relationship between tissue distribution and severity of damage. Inflammopharmacology 4, 331–340 (1996). https://doi.org/10.1007/BF02755786
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DOI: https://doi.org/10.1007/BF02755786