Carcinine dihydrochloride for Anti-glycation Antioxidation Anti-photoaging and Skin Brightening

1. Description

Carcinine dihydrochloride is a naturally occurring peptide derivative composed of a β-alanine residue and histamine; its chemical structure is that of the dihydrochloride form of β-alanine histamine, which contains an imidazole ring. It appears as a white to beige powder with the molecular formula C₈H₁₆Cl₂N₄O and a molecular weight of approximately 255.14 Da. This compound is highly soluble in water (solubility ≥ 15 mg/mL) and soluble in dimethyl sulfoxide and ethanol. It must be stored in a sealed container, protected from light, and refrigerated at 2–8°C. The powder can be stored for 3 years at –20°C and for 2 years at 4°C; when dissolved in a solvent, it can be stored for 6 months at –80°C. Casinine is widely distributed in mammalian tissues such as the brain, muscles, intestines, and liver. It is a selective histamine H₃ receptor antagonist with 100–1,000 times higher selectivity for H₂ and H₁ receptors. Additionally, this compound exhibits antioxidant and chemoattractant activity.

2. Application

(1) Research on neurodegenerative diseases: Used in studies of neurodegenerative diseases such as Parkinson’s disease and Alzheimer’s disease to explore its mechanisms of action in protecting dopaminergic neurons, reducing neuroinflammation, and inhibiting pathological protein aggregation.

(2) Research on ophthalmic diseases: Used in studies of oxidative stress-induced retinal damage to evaluate its efficacy in protecting photoreceptor cells from oxidative damage.

(3) Inflammation and Immunity Research: As a histamine H₃ receptor antagonist, it is used to study the regulation of inflammatory responses and immune modulation mechanisms, including the reduction of pro-inflammatory cytokine production and the regulation of immune cell activity.

(4) Cardiovascular Disease Research: Used to investigate its positive inotropic effects and its potential to regulate cardiac function (heart rate and myocardial contractility).

(5) Metabolic Disease Research: Used to investigate its regulatory effects on blood glucose and lipid levels, exploring potential applications in metabolic diseases such as diabetes.

(6) Sports Nutrition Research: As a structural analog of carnosine (β-alanine-L-histidine), it is used to investigate its potential role in muscle buffering capacity and resistance to exercise-induced fatigue.

3. Main Efficacy

(1) Selective histamine H3 receptor antagonism: As a highly selective histamine H3 receptor antagonist, its affinity for H3 receptors is significantly higher than its affinity for H2 and H1 receptors. By blocking presynaptic H3 receptors, it promotes the synthesis and release of histamine, thereby regulating various physiological functions such as wakefulness, cognition, and appetite.

(2) Antioxidant and lipid peroxidation product scavenging effects: It scavenges 4-hydroxy-nonenal, a toxic byproduct of lipid oxidation, thereby reducing oxidative stress-induced cellular damage. It exhibits a protective effect against oxidative damage in photoreceptor cells.

(3) Chemo-modulator activity: As a chemo-modulator, it reduces non-enzymatic glycation of proteins and maintains their normal folding state.

(4) Neuroprotective effects: Through the scavenging of 4-hydroxy-2-nonenal and its antioxidant activity, it protects dopaminergic neurons and retinal photoreceptor cells from oxidative damage.

(5) Metabolic Regulatory Effects: It can lower blood glucose and lipid levels and improve disorders of glucose and lipid metabolism, suggesting its potential application in metabolic diseases such as diabetes and hyperlipidemia.