# Antidiabetic Activity and Inhibitory Effects of Derivatives of Advanced Aminoguanidine Glycation

## TL;DR

This study explores modified versions of aminoguanidine to reduce diabetes complications by lowering blood sugar and preventing harmful chemical reactions in the body.

## Contribution

The paper introduces 19 new aminoguanidine derivatives with potential antidiabetic and antiglycant effects.

## Key findings

- Some derivatives showed reduced cytotoxicity and effective antiglycant activity in vitro.
- In vivo tests revealed potential antidiabetic effects and protection against diabetes-related complications.
- Histopathological and biochemical analyses confirmed the safety and efficacy of selected derivatives.

## Abstract

Aminoguanidine is a drug that prevents the formation
of AGEs by
reacting with initial glycation products and is effective in improving
proteinuria and vessel elasticity, preventing diabetic retinopathy,
and treating patients with diabetic nephropathy. Structural modifications
of this molecule were carried out, and 19 derivatives were studied
to present a potential hypoglycemic and antiglicante effect, preventing
such complications for diabetics. For this purpose, an in vitro cytotoxicity
test was initially carried out by colorimetric assay with MTT [3-(4,5-dimethylthiazol-2-yl)-2,5
diphenyltetrazolium], in macrophages of the J774 lineage. The AGEs
were produced in vitro from the junction of glucose with bovine serum
albumin and tested for evaluation of the antiglicante activity with
reading in a fluorescence spectrophotometer. Derivatives with the
best in vitro response were submitted to in vivo acute toxicity tests
with Wistar rats and later evaluation of their antidiabetic and antiglycant
potential in rats with streptozotocin-induced diabetes. After euthanasia,
the heart, kidney, liver, and pancreas were removed for histopathological
examination, and the blood for blood count and glycated hemoglobin,
glucose, insulin, triglycerides, total cholesterol, HDL cholesterol,
serum albumin, fructosamine, TGO, TGP, and GGT were collected. It
is possible to conclude that the studied derivatives have the potential
for the production of a drug that can be produced with them or associated
with them and that is capable of reducing the glycemic indices and,
at the same time, having an antiglicant action protecting individuals
from macro- and microvascular complications.