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17.2.22

ALLOXAN & STREPTOZOTOCIN: THEIR MECHANISM OF ACTION IN DIABETES INDUCTION

1.     Alloxan & Streptozotocin-induced diabetes is a form of insulin-dependent diabetes mellitus that occurs as a result of alloxan administration or injection to animals. It has been successfully induced in a variety of animal species; rabbits, mice, rats, monkeys, cats and dogs. Alloxan & Streptozotocin has been administered in single or multiple doses, through different routes (intraperitoneal, intravenous and subcutaneous); with single intraperitoneal administration apparently the most employed mode.

2.     Alloxan is a toxic glucose analogue, which selectively destroys insulin-producing cells in the pancreas (that is, beta cells) when administered to rodents. Alloxan is a classical diabetogenic chemical that exerts selective cytotoxic influences on pancreatic β-cells, resulting in the destruction of β-cells and type 1 diabetes.

3.     Alloxan selectively inhibits glucose-induced insulin secretion through specific inhibition of glucokinase, the glucose sensor of the beta-cell which facilitates phosphorylation of glucose to glucose-6-phosphate. Inhibition of glucokinase reduces glucose oxidation and ATP generation, thereby suppressing the ATP signal that triggers insulin secretion. Inhibition of glucokinase is achieved within 1 min of exposure to alloxan.

4.     It causes insulin-dependent diabetes by inducing ROS formation in a cyclic reaction with its reduction product, dialuric acid, resulting in the selective necrosis of beta cells.

5.     After administration of Alloxan, in the first 2 hours, blood glucose rises. This transient hyperglycaemia is thought to be due to sudden glycogen breakdown in the liver. The second phase is a hypoglycaemic phase which may be severe enough to lead to death if it is not prevented or treated with supplemental glucose. Hypoglycaemia is due to a sudden outpouring of insulin from dying beta cells. Hypoglycaemia generally appears after 6 hours. Hypoglycaemia is more pronounced in fasted animals.


6.     Streptozotocin is a naturally occurring alkylating antineoplastic agent that is particularly toxic to the insulin-producing beta cells of the pancreas in mammals.

7.     Streptozotocin is selectively accumulated in pancreatic beta cells via the low-affinity GLUT2 glucose transporter in the plasma membrane. Thus, insulin-producing cells that do not express this glucose transporter are resistant to Streptozotocin.

8.     Toxicity of Streptozotocin is dependent upon the DNA alkylating activity of its methylni-trosourea moiety. The transfer of the methyl group from streptozotocin to the DNA molecule causes damage, which along a defined chain of events, results in the fragmentation of the DNA. DNA methylation is ultimately responsible for beta cell death, but it is likely that protein methylation contributes to the functional defects of the beta cells after exposure to streptozotocin.

9.     Both alloxan and streptozotocin induce insulin deficiency. While the mechanisms of beta cell-selective action through uptake via the GLUT2 glucose transporter and beta-cell death via necrosis are identical, ROS in the case of alloxan and DNA alkylation in the case of streptozotocin mediate the toxic action of these glucose analogues.

10. Due to its chemical properties, in particular the greater stability, streptozotocin is the agent of choice for reproducible induction of a diabetic metabolic state in experimental animals.    Alloxan, on the other hand, as a model compound of ROS mediated beta-cell toxicity, is the agent with the greater impact upon the understanding of ROS mediated mechanisms of beta-cell death in type 1 and type 2 diabetes mellitus.

Key Points for Streptozotocin & Alloxan preparation and induction in laboratory animals

·         Streptozotocin and Alloxan are available in powder form. As both chemicals are very sensitive to light, temperature and humidity, they should be kept under tightly closed containers and should be protected from light.

·         For the preparation of a solution of these chemicals, weigh the appropriate amount of compound and place it in an aluminium foil wrapped container under an icebox. Ice cold citrate buffer prepared in autoclaved water should be used for the preparation of the solution.

·         All steps of the solution preparation should be performed in a dark room to protect the compound from light.

·         When you add the buffer in powdered chemicals, it started to degrade. So, you should use the solution at the earliest.

·         Solution should be filtered through 0.22 uM nylon syringe to remove any particulate matter from solution. 

·         Streptozotocin and alloxan should be induced by the intraperitoneal route. The dose of Streptozotocin and Alloxan is 50 to 60 mg/kg.

·         Before induction of diabetes, animals should be kept on fasting for 12 to 15 hours. After induction, blood glucose level (BGL) should be measured after 4, 24, 72 hours of induction and insulin injection should be given when BGL is too high. If diabetes is not induced in any animal, re-induce in that individual animal.

·         After diabetes-inducing agent induction, provide 10% dextrose water solution to the animals for 24 hours to protect them from hypoglycaemia.

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