Evaluation of Biological Activity of Two Steroid Derivatives on Glucose Levels Using a Diabetic Model

Abstract

In this study, three steroid derivatives (compounds 2-4) were prepared from an estrone derivative (compound 1) to evaluate their biological activity on glucose concentration using a diabetic model. Besides, the compounds 1 and 4 were bound to technetium-99m (Tc-99m) via a radioimmunoassay method to evaluate the biodistribution of either compounds 1 and 4 in different organs over time (15, 30, 45, and 60 min). The results showed that both compounds 1 and 4 increase glucose levels compared with either compounds 2 and 3. In addition, other data showed that the biodistribution of the Tc-99m-compound 4 conjugate in all organs was higher compared with Tc-99m- compound 1 complex. In conclusion, compound 4 had greater hypoglycemic effects, and its biodistribution was wider than 1. The data suggest that amino groups may be important to the hypoglycemic activity of compound 4, and this could be related to their higher lipophilicity degree compared with compound 1.