AICAR – Dosage
AICAR is an analogue of the natural molecule adenosine monophosphate. It can selectively activate AMP-activated protein kinase (AMPK) in many connective tissues. This metabolic regulator can control the metabolic pathway of glucose and lipids and is always activated in conditions of reduced energy availability. Due to these effects on the body, AICAR is considered a potential therapy for diabetes, and it can also be used to protect against cardiac ischemia or in cases of heart failure. Peptide also has antioxidant properties and can inhibit proinflammatory cytokines, which may be useful in treating various diseases and conditions.
Dosage Chart
| Timeline | Week 1-4 | Week 4-6.5 |
|---|---|---|
| 6.5 week protocol for skeletal muscle research | 500 mg/kg body weight (1 injections) |
Lower dose (1 injection) |
About the Peptide
AICAR is an analogue of adenosine monophosphate, which is a natural molecule, while the peptide itself can be synthesized in the laboratory. Its main function is the activation of AMP-activated protein kinase (AMPK) in adipocytes (fat cells), hepatocytes (liver cells), skeletal muscle, and many other tissues. Activation of this enzyme achieves various effects and potential beneficial properties. One of them is the regulation of glucose and lipid metabolism and the inhibition of various pro-inflammatory cytokines.
In addition to acting as a metabolic regulator, it can also inhibit anabolic processes. Another crucial effect is reflected in the promotion of differentiation of mesenchymal stem cells into active cell forms, as well as the inhibition of certain enzymes (acetyl-CoA carboxylase, malonyl-CoA) and the increase in fatty acid oxidation and glucose uptake. Due to these properties that the peptide exerts on the body, AICAR is considered a potential part of therapy for diabetes type 2 (by increasing the metabolic activity of tissues). It can also be used to protect against cardiac ischemia that occurs after a heart attack or in cases of heart failure. The peptide also has antioxidant properties that are crucial to potentially slowing down the physiological signs of aging. Numerous studies are underway on the use of this compound in many autoimmune diseases, cancers, and other inflammatory conditions.
List of Uses and Potential Benefits of AICAR
AICAR and Cardioprotective Effect
The cardioprotective effect is extremely beneficial, and since there were scientific assumptions that AICAR had such a property, studies were conducted to determine this.
One of the many studies used a molecule known as doxorubicin (DOX). This powerful chemotherapeutic agent causes serious cardiotoxic effects and dangers to the cardiovascular system that can lead to heart failure. DOX was used to cause heart damage and induce a state of heart failure in the rats used for this study, and then the animals were treated with AICAR. Adenosine monophosphate-dependent kinase (AMPK) regulates mitochondrial biogenesis (and thus energy metabolism) and enhances fatty acid oxidation. Scientists hypothesized that impaired mitochondrial function could be crucial to the cardiotoxic effect caused by DOX, so they attempted to restore mitochondrial function by activating AMPK, which led to a cardioprotective effect. Since the main function of AICAR is to activate this enzyme, the peptide could lead to an improvement in the case of heart failure.
The results of the study showed that AICAR could improve cardiac systolic function and cardiac mitochondrial fatty acid oxidation. A key potential effect of this peptide is preventing myocardial mass loss. In rats treated with DOX, pathways related to protein synthesis were disrupted, and after treatment with this peptide, they were normalized.
This treatment also prevented dyslipidemia and excessive body weight loss, which may be crucial in preserving myocardial mass. Therefore, AICAR can potentially be used as a cardioprotective agent in heart failure to preserve cardiac function and mass.
Potential Therapy for Type 2 Diabetes
Type 2 diabetes is a disease of glucose metabolism in which insulin receptors become resistant to insulin, leading to elevated blood sugar levels. Treatment options primarily include diet and sometimes drug therapy. This study aimed to examine the effect of AICAR, whose main function is the activation of AMPK, and its effect on metabolic syndrome and type 2 diabetes. This condition was induced by a high-fat diet in the mice model used for the study. The parameters monitored were body weight, glucose, and insulin levels. Internal organs and visceral fat were also assessed.
All animals showed signs of metabolic syndrome or type 2 diabetes, weight gain, hyperglycemia, hyperinsulinemia, increased abdominal fat volume, and changes in internal organs. Treatment with AICAR resulted in a reduction in body weight, abdominal fat mass, and improved visceral image. Inflammation in adipose tissue results from insulin resistance, and AICAR can reduce tissue inflammation and thus improve insulin receptor sensitivity. As a result of this mechanism of action, blood sugar homeostasis could be normalized. This peptide has shown potential therapeutic effects in the treatment of metabolic syndrome and type 2 diabetes.
Anti-Inflammatory Properties
The anti-inflammatory effect is helpful because it can be used for any condition that has an inflammatory process as its cause. Scientists have studied the effect of this peptide on various conditions, one of which was chronic pain, and inflammation can often be the cause. Scientists assumed that the activation of AMPK could alleviate the intensity of pain, and knowing that AICAR is the main activator of this enzyme, they monitored the therapeutic effect of the peptide on this condition. The assumption was that the mechanism of action could be achieved by inhibiting pro-inflammatory cytokines (interleukin-1β). The immune response in experimental animals is easily induced by complete Freund's adjuvant (CFA). This molecule is a driver of pathological changes and causes inflammatory pain. Four days after pain induction and the application of AICAR, the main parameters (most reflect the intensity of pain) were measured.
In the results, peptides showed analgesic effects and reduced pain intensity by inhibiting pro-inflammatory cytokines. Scientists assume that due to the reduction of interleukin-1β expression and, in general, the activation of AMPK, this amino acid sequence may have a potential therapeutic effect on chronic inflammatory pain.
Cancer Research
AMPK is believed to have many effects on reducing the amount of cancer cells and tumor survival rates. Scientists assume that by activating this enzyme, tumor cells that are exposed to this environment will start to die over time, slowing down their metabolism. AICAR (as the main activator of this enzyme) can be used together with other chemotherapy drugs to further enhance its effect.
The results of studies on rat models have shown that the peptide can potentially reduce the dosage of other chemotherapeutic drugs, reduce their side effects, and also act on tumors that are not recommended for chemotherapy.
AICAR Dosage Calculator
Depending on the purpose for which the peptide is used, the dosage, treatment time, and method of administration vary. Studies have investigated dosage for different purposes. For example, it is assumed that a dose of 1 mg/kg AICAR per day with injections as the method of administration during the 13 weeks leads to improvement in blood sugar homeostasis, which suggests that this could be a dosing method in the treatment of type 2 diabetes and metabolic syndrome.
Another example refers to the increase in the amount of protein in skeletal muscle by activating AMPK. The treatment period lasts 6.5 weeks, of which 4 weeks are administered daily injections of AICAR (500 mg/kg), and for the remaining 2.5 weeks, the dose is reduced. The results showed the regulation of mitochondrial function and an increase in the amount of protein in skeletal muscle in response to training.
Another dosing method is a daily intraperitoneal injection of AICAR (0.7 g/kg body weight) for 4 to 8 weeks. The dose can vary from 0.5 to 1.0 g/kg of body weight, but the mentioned value is optimal for research on fat tissue metabolism. This treatment may reduce the volume of adipose tissue, all due to the activation of AMPK.
Conclusion
According to research, AICAR shows various potential beneficial effects. Some of the described are possible therapeutic effects on Type 2 Diabetes and potentially positive effects on cardiovascular health. In addition, the peptide may contain anti-inflammatory properties that can be used for various conditions. AICAR also has a possible effect on cancer cells. The main function of this peptide, the activation of AMPK, is responsible for these and other properties. The dosage depends on the purpose of use but ranges from 0.5-1g/kg body weight. Certainly, AICAR will be the subject of much research in the future.