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Tetrahydrobiopterin (BH4) powder is a natural compound with molecular formula C8H10N2O and CAS 17528-72-2. It also has a certain effect on anti fatigue agents. It can promote muscle metabolism and energy generation, while inhibiting the release of fatigue factors, thereby improving the body's endurance and anti fatigue ability. Tetrahydrobiopterin, as a natural compound, also plays a certain role in the synthesis of alkaloids as a raw material. It can be used to synthesize various alkaloids, such as ephedrine, vincristine, etc. These alkaloids have extensive application value in the pharmaceutical field, such as anti-tumor, anti-inflammatory, antibacterial, etc. Tetrahydrobiopterin has various effects in nutritional supplements, including supplementing nutrients, enhancing immunity, antioxidant effects, promoting metabolism, and maintaining cardiovascular health. These functions are of great significance for maintaining human health and preventing diseases.
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tetrahydrobiopterin (BH4) powder is a naturally occurring enzyme cofactor with the chemical formula C9H15N5O3 and a molecular weight of 241.25. As an essential cofactor of aromatic amino acid hydroxylase and nitric oxide synthase (NOS), BH4 plays a central role in physiological processes such as neurotransmitter synthesis, vascular function regulation, immune response, and antioxidant defense.
Medical field: Treatment of genetic metabolic diseases and neurotransmitter related diseases
Targeted therapy for phenylketonuria (PKU)
It is a coenzyme of phenylalanine hydroxylase (PAH), involved in the metabolism of phenylalanine to tyrosine. PKU patients experience intellectual disability and neurological damage due to phenylalanine accumulation caused by PAH gene mutations. About 10% -15% of PKU patients are sensitive to BH4 supplementation therapy (referred to as "BH4 reactive PKU"). Oral administration of Sapropterin (BH4 dihydrochloride form) can significantly reduce blood phenylalanine concentration, reduce dietary restriction requirements, and improve quality of life. In 2007, saxagliptin was approved by the US FDA, becoming the first PKU targeted therapy drug.
Assistive management of hyperphenylalaninemia (HPA)
BH4 deficiency (BH4D) is a group of rare genetic diseases, including 6-propanoyltetrahydropterin synthase deficiency (PTPS), dihydropteridine reductase deficiency (DHPR), etc., which lead to disorders in BH4 synthesis or regeneration, abnormal phenylalanine metabolism, and neurotransmitter (such as dopamine and serum) deficiency. BH4 supplementation therapy can correct neurotransmitter imbalances, alleviate symptoms such as abnormal muscle tone and convulsions, and prevent neurodevelopmental delay.
Potential interventions for autism and attention deficit hyperactivity disorder (ADHD)
Clinical studies have shown that some BH4 deficient PKU patients have ADHD symptoms, and BH4 supplementation can improve attention and behavioral control. In addition, BH4 may have a positive impact on social disorders and repetitive behavior in individuals with autism by regulating serotonin synthesis, but further validation is needed.
Neuroscience field: Protecting neurons and regulating cognitive function
Exploration of Treatment for Neurodegenerative Diseases
BH4 is a coenzyme of tyrosine hydroxylase (TH) and tryptophan hydroxylase (TPH), involved in dopamine and serotonin synthesis. In Parkinson's disease, BH4 enhances TH activity, increases substantia nigra dopamine levels, and alleviates motor symptoms; In Alzheimer's disease, BH4 may reduce β - amyloid protein induced neuronal damage through antioxidant effects. Animal experiments have shown that BH4 supplementation can improve cognitive function in mice with memory impairment models.
Breakthrough in the Mechanism of Pain Management
In 2013, a study by Boston Children's Hospital found that BH4 is a key regulator of neuropathic pain and inflammatory pain. tetrahydrobiopterin (BH4) powder promotes mitochondrial iron supply, enhances T cell activation, and intensifies pain signal transmission; Inhibiting BH4 synthesis can block the pain pathway. This discovery provides a theoretical basis for the development of new analgesic drugs, such as SPR antagonists.
The protective effect of cerebral ischemia and trauma
BH4 improves endothelial function after cerebral ischemia by maintaining nitric oxide (NO) synthesis, reducing brain edema and neuronal death. In addition, BH4 can inhibit oxidative stress in ischemia-reperfusion injury, protect key brain regions such as the hippocampus, and promote neurological function recovery.
Cardiovascular field: Regulating vascular function and myocardial protection
Intervention for vascular endothelial dysfunction
BH4 is an essential cofactor of endothelial nitric oxide synthase (eNOS), promoting NO synthesis and maintaining vasodilation function. Under pathological conditions such as diabetes and hypertension, BH4 oxidation leads to uncoupling of eNOS, producing superoxide instead of NO, which leads to vascular endothelial dysfunction. BH4 supplementation can restore the bioavailability of NO, improve hemodynamics and reduce the risk of atherosclerosis.
Potential treatments for pulmonary arterial hypertension (PAH)
The level of BH4 in pulmonary blood vessels of PAH patients decreases, and eNOS activity decreases, leading to pulmonary vasoconstriction and remodeling. Animal experiments have shown that BH4 supplementation can inhibit the proliferation of pulmonary artery smooth muscle cells and alleviate symptoms of pulmonary arterial hypertension. In addition, BH4 further reduces pulmonary vascular resistance by regulating the renin-angiotensin system.
Protection against myocardial hypertrophy and ischemia-reperfusion injury
Under conditions of excessive cardiac load or ischemia, BH4 reduces myocardial hypertrophy and dysfunction by inhibiting mitochondrial oxidative stress and myocardial cell apoptosis. BH4 can also promote myocardial cell survival and reduce myocardial infarction area by activating the PI3K/Akt/mTOR pathway.
In the field of immune regulation: enhancing anti-tumor immune response
Metabolic regulation of T cell activation
In 2018, Nature reported that tetrahydrobiopterin (BH4) powder controls T cell proliferation and activation by regulating mitochondrial iron balance. Activation of T cells requires a large amount of mitochondrial energy, while BH4 promotes iron supply and supports mitochondrial biosynthesis. In the tumor microenvironment, a decrease in BH4 levels can inhibit T cell function and promote tumor immune escape. Supplementing BH4 or overexpressing its synthase (GCH1) can enhance the anti-tumor activity of CD8 ⁺ T cells and inhibit tumor growth.
Intervention potential for autoimmune diseases
BH4 may have therapeutic effects on autoimmune diseases such as rheumatoid arthritis and multiple sclerosis by regulating the balance of T cell subsets. Inhibiting BH4 synthesis can reduce the proliferation of self reactive T cells and alleviate inflammatory reactions.
Industrial and Biotechnology Fields: Synthetic Intermediates and Environmental Applications
Pharmaceutical intermediates and synthetic biology
BH4 and its derivatives are used as key pharmacophores in the design of novel drugs such as kinase inhibitors and G protein coupled receptor (GPCR) modulators. In addition, the synthetic pathway of BH4, such as the GTP cyclohydrolase I catalytic step, provides a model for the biosynthesis of high-value compounds.
Environmental Remediation and Agricultural Applications
BH4 analogues (such as tetrahydropyrimidine) have stress resistance and can protect microorganisms and plants from extreme environments such as salt alkali and drought. In agriculture, BH4 derivatives have been explored as plant growth regulators or biopesticides to promote crop stress resistance.
Cosmetics and functional materials
BH4 analogs (such as Ecidone) are widely used in anti-aging skincare and sun protection products due to their excellent cell protection function, which can resist environmental damage such as ultraviolet radiation and pollution. In addition, the electronic properties of BH4 make it a potential component for materials such as organic semiconductors and fluorescent probes.
BH4, as a multifunctional cofactor, has applications spanning across the fields of medicine, neuroscience, cardiovascular protection, immune regulation, and industrial biotechnology.
Tetrahydrobiopterin (BH4) powder CAS Number 17528-72-2 manufactured by BLOOM TECH GMP polit factory.
Remark: BLOOM TECH(Since 2008), ACHIEVE CHEM-TECH is the subsidiary of us.
Tetrahydrobiopterin is an important coenzyme involved in a series of biological reactions including tryptophan and tyrosine hydroxylation. Its biosynthesis usually involves three main enzymatic reaction steps, which are catalyzed by GTP cyclase (GTPCH), 6-pyridone 2-carboxylate reductase (PCBD), and aldehyde dehydrogenase (SR).
This is the first step in the synthesis of tetrahydrobiopterin. GTP cyclase catalyzes the cyclization and deamination reaction of GTP (guanosine triphosphate) to produce 7,8-dihydroguanosine triphosphate.
GTP → (GTPCH) → 7,8-dihydropterin triphosphate
In this step, 7,8-dihydroguanylic acid is obtained from 6-Pyridone-5,6,7,8-tetrahydroguanylic acid through 6-Pyridone-2-carboxylate reductase.
7,8-dihydropterin triphosphate → (PCBD) → 6-pyruvyl-5,6,7,8-tetrahydropterin
Finally, 6-pyridone 5,6,7,8-tetrahydroguanylic acid generates tetrahydrobiopterin under the action of aldehyde dehydrogenase.
6-pyruvoyl-5,6,7,8-tetrahydropterin → (SR) → C9H17Cl2N5O3
This is just a basic overview of tetrahydrobiopterin biosynthesis. Each step involves complex enzymatic and chemical processes, including enzyme activity, substrate specificity, reaction mechanisms, and so on. If you need more detailed information, I suggest you consult relevant professional literature or consult biochemical experts.
FAQ
What is the role of tetrahydrobiopterin?
Tetrahydrobiopterin (BH4) is an essential cofactor for the aromatic amino acid hydroxylases, which are essential in the formation of neurotransmitters, and for nitric oxide synthase. It is presently used clinically to treat some forms of phenylketonuria (PKU) that can be ameliorated by BH4 supplementation.
What supplements increase BH4?
A complementary strategy would be to increase BH4 synthesis or limit its oxidative degradation. As an example, folic acid (vitamin B), and in particular its active metabolites 5-methyltetrahydrofolate, may reduce BH4 oxidation and increase the recycling of BH2 to BH4 by increasing DHFR activity.
How is BH4 produced?
De Novo Pathway of BH4 Synthesis
In the de novo pathway, BH4 is synthesized from GTP by three enzymes, namely GTP cyclohydrolase I (GCH1), 6-pyruvyl-tetrahydrobiopterin synthase (PTPS) and methotrexate reductase (SR).
What is the role of BH4 in PKU?
BH4 supplementation enhances residual PAH enzyme activity and increases metabolism of plasma Phe to tyrosine in some patients with PKU. In 1999, oral BH4 therapy was demonstrated to reduce plasma Phe in PKU patients.
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