Melatoninとは？用途・使用量・代替品・規格

Melatonin, chemically known as N-Acetyl-5-methoxytryptamine, has the chemical formula C13H16N2O2, molecular weight 232.28, and CAS number 73–31–4. Melatonin is an amine hormone secreted by the pineal gland in mammals, belonging to the tryptophan derivative family, and plays a central role in regulating circadian rhythms and the sleep-wake cycle. The secretion of melatonin follows a distinct circadian rhythm: during the day, light inhibits secretion, keeping the person awake; at night, darkness promotes secretion, inducing drowsiness. As humans age, the pineal gland calcifies and atrophies, leading to a significant decrease in melatonin production—from peak levels in childhood to lower levels in old age, which is a major reason for declining sleep quality in the elderly. Melatonin is also involved in various physiological processes including antioxidant defense, immune regulation, and endocrine regulation, making it a multifunctional endogenous hormone. Melatonin appears as a white to off-white crystalline powder, odorless, with a slightly bitter taste. Within the recommended dosage range, melatonin has a good safety profile. Due to its significant efficacy in improving sleep quality, regulating circadian rhythms, and alleviating jet lag, melatonin has become one of the fastest-growing star products in the global dietary supplement and health supplement market. In China, melatonin is generally classified as a health supplement or dietary supplement. According to China‘s health supplement ingredient catalog, the daily dosage of melatonin is 1–3 mg.

Melatonin is known as the “hormone of life” and the “core molecule of sleep regulation,” occupying a rapidly rising core position in the global dietary supplement, health supplement, and pharmaceutical fields. Its most prominent core advantages include: high biocompatibility as an endogenous hormone, superior sleep regulation efficacy, broad physiological regulatory functions, good safety profile, and continuously optimized production processes. 1 High biocompatibility as an endogenous hormone Melatonin is an endogenous hormone naturally secreted by the human body, offering outstanding advantages such as natural, gentle action, and high safety. Compared to chemically synthesized sleep aids, melatonin has no drug dependence or withdrawal symptoms (within the recommended dosage range), does not cause next-day drowsiness or other side effects, and has no toxic effects on the human nervous system or organs. Since it originates from the human body itself, exogenous melatonin supplementation can mimic natural sleep rhythms, helping users establish healthy sleep patterns rather than inducing forceful sleep. 2 Superior sleep regulation efficacy The core application value of melatonin lies in its function of regulating sleep and circadian rhythms. Melatonin activates melatonin receptors MT1 and MT2 in the brain, shortening sleep latency and prolonging deep sleep duration, especially suitable for individuals with short-term insomnia caused by stress, schedule disruption, or aging. Clinical studies have shown that taking 1 mg of melatonin 2 hours before bedtime effectively improves sleep quality, shortens sleep latency, reduces the number of awakenings during sleep, and increases sleep efficiency and quality. Additionally, melatonin is particularly effective in treating circadian rhythm sleep disorders in patients with dementia, especially those with sundowning syndrome. Melatonin is also used to alleviate jet lag caused by long-distance travel, help adjust the biological clock, and is suitable for shift workers, night shift workers, and those needing to adapt to new sleep schedules. 3 Broad physiological regulatory functions Melatonin is not only a sleep-regulating hormone but also participates in various physiological processes. Melatonin has powerful antioxidant effects, scavenging free radicals, enhancing antioxidant enzyme activity, preventing cellular oxidative damage, and slowing the aging process. Numerous clinical studies have indicated that melatonin possesses excellent antioxidant efficacy, with its main functions including promoting collagen synthesis, boosting the immune system, and reducing oxidative stress. Melatonin has a bidirectional regulatory effect on the immune system, affecting the growth and development of immune organs, regulating humoral and cellular immunity, as well as cytokine secretion. Melatonin also regulates the cardiovascular system, with increased nighttime melatonin secretion being negatively correlated with decreased cardiovascular activity, helping to prevent arrhythmias caused by ischemia-reperfusion injury and regulating blood flow. Furthermore, melatonin regulates mood, protects nerve cells, and has anti-inflammatory and anti-apoptotic effects. 4 Good safety profile Within the recommended dosage range, melatonin has a good safety profile. According to China‘s health supplement ingredient catalog, the daily dosage of melatonin is 1–3 mg. When used appropriately for specific populations (such as those with circadian rhythm disruption due to jet lag, shift work, or aging), it effectively improves sleep quality. Compared to prescription sleeping pills, melatonin is non-addictive and has a good long-term safety record. 5 Continuously optimized production processes Melatonin production processes have evolved from early chemical synthesis to synthetic biology fermentation, achieving a leap from traditional chemical synthesis to green bio-manufacturing. Based on synthetic biology technology, microbial cell factories produce natural product functional substances, solving problems associated with traditional botanical extraction, such as limited sources, quality control difficulties, complex components, and environmental pollution. Chinese enterprises have achieved the world‘s first large-scale bio-manufacturing of melatonin, filling domestic and international gaps with a market share exceeding 70%, driving the industry into a green, efficient, and sustainable development stage.