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melatonin

✓ Approved

Clinigen Group · MTNR1A · 小分子

什么是 melatonin？

melatonin 是一种小分子，由Clinigen Group研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

公司Clinigen Group
药物类别小分子
分子靶点MTNR1A, MTNR1B
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Clinigen Group

作用机制

分子靶点

melatonin 作用于 2 个分子靶点：

MTNR1Amelatonin receptor 1A (MEL-1A-R, MT1)
MTNR1Bmelatonin receptor 1B (FGQTL2, MT2)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

melatonin 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersInsomnia✓ Approved
Psychiatric disordersSleep disorder✓ Approved

相关研究文献

PubMedJournal of cellular and molecular medicine2026-06-13

Hierarchical Disruption of the Tryptophan-Melatonin Axis Contributes to Glioma Progression Through AKT/ERK/STAT3 Signalling.

Tan Bo B, Yao Suqiu S, He Shuangyin S, Chen Tao T et al.

Melatonin signalling, mediated by membrane receptors and tightly regulated biosynthetic enzymes, is a key component of circadian and neuroendocrine control in the brain. However, whether the tryptophan-melatonin axis remains hierarchically intact during glioma progression and how its disruption affects downstream signalling remain unclear. In this study, transcriptomic data from TCGA, CGGA, and GTEx were integrated to characterize the expression patterns of melatonin receptors (MTNR1A and MTNR1B) and biosynthetic enzymes (AANAT and ASMT) across normal brain tissue, lower-grade glioma and glioblastoma. Protein expression was validated by immunohistochemistry, and functional consequences were investigated through gain- and loss-of-function experiments in glioma cells, followed by proliferation, migration, invasion, apoptosis and signalling analyses. Multi-layered analyses revealed a coordinated disruption of the tryptophan-melatonin axis during glioma progression. Expression of AANAT, ASMT, MTNR1A and MTNR1B progressively declined with increasing tumour grade and was associated with poor prognosis. Immunohistochemistry confirmed reduced MTNR1A and ASMT protein expression in glioma tissues. Restoration of these factors suppressed glioma cell proliferation, migration and invasion while promoting apoptosis. Mechanistically, these effects were accompanied by inhibition of AKT, ERK and STAT3 signalling. These findings demonstrate that hierarchical disruption of receptor- and synthesis-dependent melatonin signalling is a defining molecular feature of glioma and may contribute to malignant progression through activation of AKT/ERK/STAT3 pathways, providing new insights into the biological and therapeutic relevance of the tryptophan-melatonin axis in glioma.

PMID 42286740
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PubMedBMC plant biology2026-06-13

Melatonin activates the ZjERF34-ZjMYB1 regulatory pathway to promote flavonoid biosynthesis and salt tolerance in jujube (Ziziphus jujuba Mill.).

Wen Cuiping C, Wang Zhongtang Z, Wang Chao C, Qiu Liguo L et al.

Flavonoids are essential secondary metabolites that contribute to fruit nutritional quality and stress adaptation. Jujube (Ziziphus jujuba Mill.) accumulates abundant flavonoids; however, the regulatory mechanisms by which melatonin (MT) modulates flavonoid biosynthesis remain poorly understood. In this study, exogenous MT treatment markedly promoted flavonoid accumulation in jujube leaves and triggered dynamic changes in endogenous MT levels, implying a regulatory function of MT in this process. Transcriptomic and correlation analyses identified ZjMYB1 as a key MT-responsive regulator strongly associated with flavonoid accumulation. Functional characterization revealed that silencing ZjMYB1 significantly decreased flavonoid content and downregulated genes in the phenylpropanoid pathway, whereas its overexpression enhanced flavonoid accumulation in jujube and heterologous systems. ZjMYB1 directly activated the key structural genes ZjF3H and ZjFLS by binding to MYB cis-elements in their promoters. Furthermore, the MT-responsive transcription factor ZjERF34 was identified as an upstream regulator of ZjMYB1. ZjERF34 directly targets the ZjMYB1 promoter to enhance its transcription, as demonstrated by Y1H, GUS staining, and dual-luciferase assays, establishing a hierarchical ERF-MYB regulatory network. In addition, ZjMYB1 overexpression significantly enhanced salt tolerance, correlating with increased flavonoid accumulation and upregulation of stress-responsive genes. Collectively, our findings reveal a MT-ZjERF34-ZjMYB1-ZjF3H/FLS regulatory module that links hormonal signaling with flavonoid biosynthesis and abiotic stress responses, providing new insights and potential molecular targets for improving fruit quality and stress resilience in horticultural crops.

PMID 42286505
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PubMedInorganic chemistry2026-06-12

Axial Coordination of Melatonin in Magnesium Porphyrin: Structural Insights, Excited-State Dynamics, and Photostability.

Choudhury Abdul K AK, Bhuyan Jagannath J

Axial coordination of biologically relevant ligands offers an effective strategy for tuning the photophysical and redox behavior of magnesium porphyrins, widely used as models for chlorophyll a. Herein, we report the first example of a melatonin-coordinated magnesium porphyrin, [MgT(4-Cl)PP(MT)],1 [T(4-Cl)PP = 5,10,15,20-tetrakis(4-chlorophenyl)porphyrin, MT = melatonin], in which melatonin binds axially to the Mg(II) center through its carbonyl oxygen atom with the Mg-OMT distance of 2.008 Å, resulting in a penta-coordinated square-pyramidal geometry. Compound 1 was characterized by UV-visible spectroscopy, NMR, MALDI-TOF, FTIR, and single-crystal XRD. Moreover, the redox properties were studied using cyclic voltammetry. Photophysical studies reveal that melatonin coordination significantly alters the excited-state dynamics of the porphyrin, resulting in reduced fluorescence lifetime and suppressed singlet oxygen generation, which correlate with enhanced resistance toward photoinduced degradation. The melatonin-bound complex also exhibits improved antioxidant activity relative to the parent magnesium porphyrin. Notably, freshly isolated spinach chlorophyll a exhibits similar resistance to oxidative stress and photodegradation in the presence of melatonin. Complementary density functional theory calculations and electrostatic analyses provide insight into ligand-induced modulation of the porphyrin π-electronic framework. Overall, these results demonstrate that axial coordination of melatonin offers an effective strategy for tuning the photochemical stability and reactivity of magnesium porphyrins.

PMID 42281461
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PubMedNutrients2026-06-12

Hypnotic Effects of Hypericum perforatum L. and Melissa officinalis L. Through Adenosine and Melatonin Receptors.

Jee Hye Jin HJ, Lee Suk Jin SJ, Yoo Jae Ryeong JR, Kim Hye-Jin HJ et al.

Sleep disorders, particularly insomnia, represent a major public health concern, while currently available hypnotic drugs are often limited by adverse effects and poor long-term tolerability. In this study, we investigated the sleep-promoting effects of a mixture of Hypericum perforatum L. and Melissa officinalis L. extract (HME) and its underlying mechanisms in male ICR and C57BL/6 mice. In a pentobarbital-induced sleep model in mice, sleep onset latency and total sleep time were measured. Pharmacological studies using various antagonists and agonists were conducted to elucidate receptor-mediated mechanisms. Immunohistochemical and immunofluorescence analyses were performed to assess neuronal activity, and cortical mRNA expression was evaluated by quantitative analysis. HPLC analysis was used to identify the major constituents of HME, and their pharmacological profiles were functionally evaluated. HME significantly reduced sleep onset latency and prolonged total sleep time. These hypnotic effects were shown to be mediated through adenosine and melatonin receptor signaling pathways. Immunohistochemical and immunofluorescence analyses showed that HME suppressed neuronal activity in wake-promoting cholinergic and orexinergic neurons of the basal forebrain and lateral hypothalamus, while enhancing activation of sleep-promoting GABAergic neurons in the ventrolateral preoptic nucleus. At the molecular level, HME increased cortical mRNA expression levels of adenosine A1 receptor, adenosine A2A receptor, melatonin receptor 1, and melatonin receptor 2. From the HPLC analysis, rosmarinic acid and hyperoside were identified as the major constituents of HME. Functional evaluation of these compounds revealed complementary pharmacological profiles, with hyperoside primarily acting through adenosine receptors and rosmarinic acid engaging both adenosine and melatonin receptor pathways. These findings suggest that HME enhances both sleep initiation and maintenance through adenosine and melatonin receptor signaling pathways, thereby supporting its potential as a multitarget therapeutic agent for improving sleep quality.

PMID 42280309
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PubMedJournal of clinical medicine2026-06-12

Effect of Melatonin as an Adjunct to NSPT on Periodontal and Systemic Outcomes in Patients with Type 2 Diabetes Mellitus: A Systematic Review and Meta-Analysis of RCTs.

Angelopoulou Thaleia T, Bobetsis Yiorgos A YA

Background/Objectives: In recent years, a wide range of adjunctive therapies have been employed in conjunction with non-surgical periodontal therapy (NSPT) to enhance treatment outcomes. Among them, melatonin, a hormone with well-documented antioxidant, anti-inflammatory, and immunomodulatory properties, has emerged as a potential adjunctive therapeutic agent. The purpose of the present systematic review was to investigate whether systemic melatonin supplementation, when combined with NSPT, provides any additional periodontal and systemic benefits in patients diagnosed with type 2 diabetes mellitus (T2DM). Methods: Articles indexed in PubMed, Web of Science, Scopus, and the Cochrane Library were systematically retrieved, with additional screening of gray literature, covering all records available up to February 2026. This systematic review included randomized controlled trials (RCTs) evaluating the effect of adjunctive systemic melatonin administration in conjunction with NSPT on clinical and biochemical periodontal parameters and systemic outcomes related to glycemic control, oxidative stress, and inflammation in patients with T2DM compared with NSPT alone or combined with placebo. Three RCTs were eligible for qualitative synthesis, and two placebo-controlled RCTs were included in the quantitative synthesis. Risk of bias and quality of evidence assessments were performed. Results: With a low level of certainty, systemic melatonin supplementation in conjunction with NSPT demonstrated significantly more pronounced improvements in periodontal and systemic outcomes than those observed following NSPT or NSPT combined with placebo. Meta-analysis demonstrated statistically significant improvements in PPD and CAL, as well as in HbA1c and serum hs-CRP, favoring adjunctive melatonin supplementation. Conclusions: Adjunctive systemic melatonin supplementation in combination with NSPT may have a beneficial impact in patients with T2DM. However, the limited number of available studies, relatively small sample sizes, risk of bias concerns, and low quality of evidence limit the confidence that can be placed in these findings. Future research should focus on conducting more well-designed, sufficiently powered, large-scale RCTs employing standardized treatment protocols and longer observation periods.

PMID 42278933
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PubMedAnimals : an open access journal from MDPI2026-06-12

Oxidative Stress and Blood Parameters During Shearing in Sheep Treated with Melatonin.

Carcangiu Vincenzo V, Luridiana Sebastiano S, Cocco Raffaella R, Trimasse Othmane O et al.

Shearing is a stressful procedure for sheep, combining isolation, restraint, and the mechanical action of shearing, which activates the hypothalamic-pituitary-adrenal axis and induces oxidative stress. This study investigated whether melatonin-a pleiotropic hormone with well-documented antioxidant properties-administration could modulate the stress response and oxidative stress in Sarda sheep during shearing. Forty lactating ewes (aged 3-5 years, mean body weight 41 ± 1.1 kg) were randomly assigned to four groups (n = 10 each): two groups received a subcutaneous melatonin implant (18 mg); two remained untreated as controls. Within each category, one group was shorn and the other subjected only to restraint. Blood samples were collected before, during, and after shearing to measure cortisol, glucose, reactive oxygen metabolites (ROMs), biological antioxidant potential (BAP), and oxidative stress index (OSI). Procedures elevated cortisol, glucose, ROMs, and OSI in all groups, but melatonin treatment significantly reduced these parameters and increased BAP relative to untreated animals at all sampling points (p < 0.05). No significant differences were observed between shorn and unshorn animals within the same treatment, suggesting that the handling, restraint, and isolation associated with the shearing procedure represent the major sources of stress, rather than the mechanical act of shearing itself. In conclusion, melatonin administration blunts the stress response and reduces oxidative stress in sheep during routine shearing-related handling procedures, suggesting its potential as a practical tool to improve animal welfare during routine management practices.

PMID 42278132
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