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Diamine Oxidase Inhibitor: Aminoguanidine

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Understanding the Role and Impact of Aminoguanidine in Histamine Degradation and Health

Picture this: You’re at a family gathering, enjoying a feast of aged cheeses, cured meats, and pickled vegetables. Everyone is having a great time, but a few hours later, you find yourself doubled over in discomfort, battling a runny nose, rashes, and abdominal pain.

This isn’t a case of food poisoning, but a manifestation of histamine intolerance. The key player in this scenario? An enzyme called Diamine Oxidase (DAO).

Aminoguanidine has emerged as a significant player in the field of histamine degradation and health management as an effective inhibitor of diamine oxidase. The role of aminoguanidine extends beyond histamine regulation, with implications for cellular health, endothelial function, and more.

Understanding Diamine Oxidase and Aminoguanidine

Diamine Oxidase

DAO (aka copper amine oxidase) plays a crucial role in the degradation of histamine — a biogenic amine involved in various physiological processes. The DAO enzyme is found in abundance in endothelial cells and fibroblasts, among other cell types.

However, substances like aminoguanidine can affect the activity of this enzyme. Aside from aminoguanidine, these are other substances that can also affect DAO activity:

SubstanceCommonly Found In
MetamizolPainkillers (Dipyrone)
Acetyl Salicylic AcidAspirin
DiphenhydramineAntihistamines (Tylenol, Advil, Benadryl, Dimetapp and others)
PromethazinePhenergen, Promacot
PropafenoneAnti-arrhythmics (Rythmol)
QuinidineAnti-arrhythmics (Nuedexta)
TheophyllineAnti-asthmatics (Theo 24, Theochron, Elixophyllin, aminophylline, and Uniphyl)


Aminoguanidine is a diamine oxidase inhibitor that reduces the activity of the DAO enzyme. This process allows for an increase in histamine levels in the body, which can lead to a condition known as histamine intolerance. Symptoms associated with this condition are abdominal pain, rashes, and even anaphylaxis in severe cases.

Aminoguanidine has also been studied for its potential benefits in treating various conditions that include:

  • Protection against diabetes-induced impairment in vascular dynamics
  • Improved vascular elasticity and decreased vascular permeability
  • Prevention of experimental diabetic nephropathy
  • Reduction of diabetes-associated cardiac fibrosis
  • Prevention of complications caused by experimental diabetes and aging
  • Inhibition of aortic hydrogen peroxide production, VSMC NOX activity, and hypercontractility

Aminoguanidine Mechanism of Inhibition

Aminoguanidine inhibits DAO by binding to its copper-containing active site, which prevents the enzyme from carrying out its function. This can lead to an increase in histamine levels in various tissues, including the heart and the conjunctiva.

The inhibition of diamine oxidase by aminoguanidine can influence the concentration of histamine in various tissues, including the large bowel. This is due to the role of DAO in the metabolic degradation of histamine.

Implications of Aminoguanidine Treatment

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Aminoguanidine treatment has been found to have various effects on cellular mechanisms. For instance, it has been observed to influence the growth of fibroblasts in culture. It is also known to be one of the nitric oxide synthase inhibitors. It can reduce the production of nitric oxide, a reactive nitrogen species that can cause cellular damage and contribute to conditions such as endothelial dysfunction and others including:

1. Aminoguanidine and Metabolic Disorders

Aminoguanidine has been linked to various metabolic disorders. It has been suggested that alterations in food consumption and the resulting changes in cellular concentrations of various compounds can influence the effects of aminoguanidine.

For example, the presence of advanced glycation endproducts (AGEs) in one’s diet can enhance the effects of aminoguanidine. AGEs are compounds that can cause cellular damage and contribute to various metabolic disorders.

2. Aminoguanidine and Polyamines

Aminoguanidine has been found to interact with polyamines, such as spermidine, and these interactions can influence the oxidative degradation of these compounds. Specifically, aminoguanidine has been shown to reduce the level of putrescine, a type of polyamine. This reduction in putrescine levels can have various implications for cellular mechanisms, including those involved in the adaptive response to stress

3. Aminoguanidine in Abiotic-Stress Responses

Aminoguanidine has been found to modulate abiotic-stress responses in various organisms by influencing the activities of polyamine oxidase, an enzyme involved in the metabolism of polyamines.

For instance, aminoguanidine can reduce the activity of this enzyme, leading to alterations in the levels of polyamines. This can have various effects on the organism’s ability to respond to abiotic stress.

4. The Impact of Aminoguanidine on Endothelial Dysfunction

Endothelial dysfunction is a condition characterized by the impaired functioning of the endothelial cells lining the blood vessels. This condition is also a key factor in the development of cardiovascular diseases.

In studies, aminoguanidine treatment has been shown to improve endothelial function by reducing the production of nitric oxide synthase inhibitors and other harmful compounds. This suggests that aminoguanidine may have potential therapeutic benefits for conditions related to endothelial dysfunction.

Side Effects of Aminoguanidine Treatment

While aminoguanidine has various therapeutic effects, it can also lead to certain side effects. These can vary among individuals and may include:

  1. Gastrointestinal Disturbance: Some individuals undergoing aminoguanidine treatment have reported experiencing gastrointestinal disturbances which could include symptoms such as nausea, vomiting, or abdominal discomfort.
  2. Abnormalities in Liver Function Tests: Aminoguanidine treatment has been associated with abnormalities in liver function tests. This could potentially indicate an impact on liver health.
  3. Flu-like Symptoms: Some individuals have reported experiencing flu-like symptoms during aminoguanidine treatment which include fever, chills, fatigue, body aches, and cough.
  4. Development of Antinuclear Antibody: Aminoguanidine treatment has been linked to the development of antinuclear antibodies. These are proteins produced by the immune system that mistakenly target and attack the body’s own tissues.
  5. Rare Vasculitis: Aminoguanidine treatment has been associated with the development of a rare form of vasculitis. This condition occurs when there is inflammation of the blood vessels. If not properly managed, vasculitis can lead to serious complications.

Embrace Health and Balance with SeeBeyond Shop

At SeeBeyond Shop, we understand the intricate dance between histamine, diamine oxidase (DAO), and aminoguanidine. We’ve harnessed the power of scientific research to create our specialized supplements, designed to boost DAO levels and promote efficient histamine breakdown. Our DAO-HIST supplement is crafted to help you manage histamine levels and support your overall well-being.

Don’t let histamine imbalance dictate your life. Reach out to our team of professionals at SeeBeyond Shop today. Let us guide you on your journey towards vibrant health, helping you navigate the complexities of DAO and aminoguanidine. It’s time to see beyond histamine intolerance and embrace a future of health and balance.

We are offering 30 minutes for free to talk to one of SeeBeyond's Functional Medicine Practitioners to create a personalized regimen.

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