1. What is Melatonin?
Melatonin is a naturally occurring hormone produced by the pineal gland in the brain, primarily in response to darkness. It plays a critical role in regulating the body’s circadian rhythm—our internal biological clock that governs sleep-wake cycles. Melatonin is widely used as a supplement to improve sleep quality, manage jet lag, and support healthy aging. It also acts as an antioxidant and immune modulator.
2. Melatonin Structure
Molecular Formula：C13H16N2O2
Molecular Weight：232.28g/mol
CAS Number：73-31-4
3. Melatonin Research
Melatonin (N acetyl 5 methoxytryptamine) is an endogenous indoleamine hormone produced primarily by the pineal gland in response to darkness, with peak levels at night. It regulates the circadian rhythm, especially the sleep–wake cycle, via MT₁/MT₂ receptors in the suprachiasmatic nucleus (SCN) 【https://onlinelibrary.wiley.com/doi/10.1111/jpi.12525?utm_source=chatgpt.com】.
⚙️ 【1】Mechanisms:
Circadian entrainment: Activates MT₁/MT₂ GPCRs, reducing cAMP/cGMP signaling and modulating PKA/PKC pathways to promote sleepiness and regulate body temperature 【https://en.wikipedia.org/wiki/Melatonin_receptor_agonist?utm_source=chatgpt.com】.
Potent antioxidant: Directly scavenges ROS (e.g., hydroxyl, superoxide, nitric oxide) and induces antioxidant enzymes like SOD, catalase, GPx 【https://pmc.ncbi.nlm.nih.gov/articles/PMC9907215/?utm_source=chatgpt.com】【https://en.wikipedia.org/wiki/Melatonin?utm_source=chatgpt.com】.
Anti-inflammatory & immunomodulation: Inhibits NF κB, COX 2, and iNOS; lowers pro-inflammatory cytokines while boosting anti-inflammatory mediators 【https://www.nature.com/articles/s41419-019-1556-7?utm_source=chatgpt.com】【https://onlinelibrary.wiley.com/doi/10.1111/jpi.12525?utm_source=chatgpt.com】.
Mitochondrial protection: Concentrates within mitochondria to enhance redox homeostasis and limit apoptosis 【https://zh.wikipedia.org/wiki/%E8%A4%AA%E9%BB%91%E7%B4%A0?utm_source=chatgpt.com】.
Metabolites like AMK/AFMK: Contribute additional neuroprotective, antiproliferative, and antioxidant effects【https://en.wikipedia.org/wiki/N1-Acetyl-5-methoxykynuramine?utm_source=chatgpt.com】.
【2】Clinical Effects & Evidence:
Shortens sleep-onset latency (~6 min), modestly improves sleep duration, especially in delayed sleep phase and jet lag 【https://en.wikipedia.org/wiki/Melatonin?utm_source=chatgpt.com】.
Approved as Circadin (slow-release melatonin) for insomnia in over-55 adults, improving sleep quality .
Supports REM sleep behavior disorder management, preferred over clonazepam for safety 【https://en.wikipedia.org/wiki/Melatonin_as_a_medication_and_supplement?utm_source=chatgpt.com】.
Enhances preoperative anxiety reduction, athletic recovery, and mood stabilization 【https://pubmed.ncbi.nlm.nih.gov/40278958/】.
Emerging cognitive benefits in mild cognitive impairment and Alzheimer’s disease models via antioxidative and amyloid β reduction pathways.
✅ Why Consider Melatonin?
⏳ Sleep quality & circadian support: Helps fall asleep faster, resets sleep–wake cycles, eases jet lag.
🛡️ Antioxidant powerhouse: Scavenges free radicals, upregulates antioxidant enzymes, protects mitochondria .
🌡️ Anti-inflammatory effects: Reduces NF κB, COX 2, iNOS activity, and pro-inflammatory cytokines
🧠 Neuroprotection & cognitive support: Linked to better memory, mitochondrial health, and neurodegenerative disease defense .
🫀 Immune regulation: Modulates lymphocyte, NK cell, macrophage activity, immunoglobulin balance .
🔄 Multiple roles: Eye health, cardiovascular regulation, metabolic signaling, reproductive rhythm modulation .
4. Future Research
A. Neurodegenerative & Aging Studies
Trials in Alzheimer’s show improved cognition and sleep quality; mechanisms include mitochondrial protection and amyloid reduction .
Aging research targets AMK’s role in maintaining hippocampal memory and neuronal health 【https://en.wikipedia.org/wiki/N1-Acetyl-5-methoxykynuramine?utm_source=chatgpt.com】.
B. Immune and Autoimmune Disorders
Investigating melatonin’s therapeutic roles in autoimmune diseases, allergies, and inflammatory bowel disease via immune and barrier modulation .
C. Cancer Prevention & DNA Repair
Emerging studies in shift workers show boosted DNA repair and reduced UV damage risk; pilot trials indicate up to 80% repair increase .
D. Cardiometabolic & Reproductive Health
Potential benefits in hypertension, metabolic syndrome, PCOS, and hormone regulation.
E. Novel Delivery Formats
Development of receptor-selective MT₁/MT₂ agonists, transdermal patches, nanocarriers, and chronotherapeutic formulations aiming for precision application .
5. Application Area
| Use Case | Description |
| Sleep & Jet Lag | Treatment for insomnia, shift work disorder, delayed sleep phase, jet lag resetting |
| Cognitive & Psychiatric | Adjunct in mild cognitive impairment, Alzheimer’s, anxiety, OCD, bipolar conditions |
| Immuno & Inflammatory | Supports chronic inflammation, allergy, autoimmune disease, gut barrier repair |
| Antioxidant & Cellular Protection | Reduces oxidative damage in radiation exposure, mitochondrial disorders, age-related decline |
| Reproductive Health | Modulates menstrual cycles, TSH, seasonal hormone rhythms and PCOS |
| Sports & Recovery | Supports pre-/post-surgical recovery, athletic stress adaptation, inflammation mitigation |
6. Safety & Dosing Considerations
Dosage range: 0.5–10 mg daily; typically 2–4 mg taken 30 min before bedtime.
Side effects: Drowsiness, dizziness, headache, nausea; rare endocrine effects (e.g., reproductive hormone shifts).
Long-term data: Generally safe, non-addictive; avoid use in pregnancy without medical advice .
Drug interactions: Caution with sedatives, antihypertensives, and immune-modifying agents.
Regulatory status: Prescription circadin is approved in some countries; OTC formulations vary in purity and dosing accuracy.
✅ Summary
Melatonin, beyond being the “sleep hormone”, is a multifaceted therapeutic agent offering antioxidant, anti-inflammatory, neuroprotective, and immunoregulatory benefits. Trusted for short-term sleep aid and circadian alignment, it also shows promise in age-related cognitive decline, DNA repair, and metabolic health. With ongoing research into selective analogs and advanced delivery methods, melatonin remains a cornerstone in integrative wellness and chrono-therapeutics.
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The products offered on this website are furnished for in-vitro studies only. In-vitro studies(Latin: in glass) are performed outside of the body. These products are not medicines or drugs and have not been approved by the FDA to prevent, treat or cure any medical condition, ailment or disease. Bodily introduction of any kind into humans or animals is strictly forbidden by law.
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