In vitro Evaluation of Endocrine‐Related Adverse Effects of 5‐Fluoroindole Derived Melatonin Analogues with Antioxidant Activity DOI Open Access
Elif Ince Ergüç, Hanifa Fatullayev,

Bita Entezari

et al.

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 12, 2024

Melatonin (MLT) is a natural indolic hormone with well documented antioxidant properties, but it can also modulate the estrogen signaling pathway by inhibiting aromatase enzyme and receptor modulating activity. This dual activity raises concerns about potential endocrine-related adverse effects when using MLT its analogues as therapeutic agents in prevention treatment of oxidative stress related diseases. In this study, 34 novel 5-fluoroindole derivatives were synthesized evaluated for their antioxidant, modulatory, inhibitory activities.Three compounds (4c, 5c, 6c) demonstrated significant activity, compound 4c showing highest efficacy reducing intracellular reactive oxygen species (ROS) 65 % CHO-K1 cells displaying DPPH radical scavenging comparable to standard BHT. However, these same exhibited antiestrogenic E-Screen assay, IC

Language: Английский

Melatonin’s Impact on Wound Healing DOI Creative Commons
Eun‐Hwa Sohn, Su‐Nam Kim, Sung Ryul Lee

et al.

Antioxidants, Journal Year: 2024, Volume and Issue: 13(10), P. 1197 - 1197

Published: Oct. 2, 2024

Melatonin (5-methoxy-N-acetyltryptamine) is an indoleamine compound that plays a critical role in the regulation of circadian rhythms. While melatonin primarily synthesized from amino acid tryptophan pineal gland brain, it can also be produced locally various tissues, such as skin and intestines. Melatonin's effects target tissues mediated through receptor-dependent mechanisms. Additionally, exerts actions via receptor-independent pathways. In biological systems, its endogenous metabolites often produce similar effects. injuries are common daily life, promoting optimal wound healing essential for patient well-being healthcare outcomes. Beyond regulating rhythms neuroendocrine hormone, may enhance (1) potent antioxidant properties, (2) anti-inflammatory actions, (3) infection control, (4) vascular reactivity angiogenesis, (5) analgesic (pain-relieving) effects, (6) anti-pruritic (anti-itch) This review aims to provide comprehensive overview scientific studies demonstrate melatonin's potential roles supporting effective healing.

Language: Английский

Citations

2

Melanogenesis Is Directly Affected by Metabolites of Melatonin in Human Melanoma Cells DOI Open Access

Jack K. S. Möller,

Kinga Linowiecka, Maciej Gagat

et al.

International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 24(19), P. 14947 - 14947

Published: Oct. 6, 2023

Melatonin (N-acetyl-5-methoxytryptamine, MEL), its kynurenic (N1-acetyl-N2-formyl-5-methoxykynurenine, AFMK) and indolic derivatives (6-hydroxymelatonin, 6(OH)MEL 5-methoxytryptamine, 5-MT) are endogenously produced in human epidermis. Melatonin, by the pineal gland, brain peripheral organs, displays a diversity of physiological functions including anti-inflammatory, immunomodulatory, anti-tumor capacities. Herein, we assessed their regulatory effect on melanogenesis using amelanotic (A375, Sk-Mel-28) highly pigmented (MNT-1, melanotic) melanoma cell lines. We discovered that subjected compounds decrease downstream pathway melanin synthesis causing significant drop cyclic adenosine monophosphate (cAMP) level, microphthalmia-associated transcription factor (MITF) resultant collapse tyrosinase (TYR) activity, content comparatively to N-phenylthiourea (PTU, positive control). observed reduction pigment melanosomes visualized transmission electron microscopy. Finally, role G-protein-coupled seven-transmembrane-domain receptors. Obtained results revealed nonselective MT1 MT2 receptor antagonist (luzindole) or selective (4-P-PDOT) did not affect dysregulation indicating receptor-independent mechanism. Our findings, together with current state art, provide convenient experimental model study complex relationship between metabolites melatonin control pigmentation serving as future rationale strategy for targeted therapies melanoma-affected patients.

Language: Английский

Citations

4

In vitro Evaluation of Endocrine‐Related Adverse Effects of 5‐Fluoroindole Derived Melatonin Analogues with Antioxidant Activity DOI Open Access
Elif Ince Ergüç, Hanifa Fatullayev,

Bita Entezari

et al.

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 12, 2024

Melatonin (MLT) is a natural indolic hormone with well documented antioxidant properties, but it can also modulate the estrogen signaling pathway by inhibiting aromatase enzyme and receptor modulating activity. This dual activity raises concerns about potential endocrine-related adverse effects when using MLT its analogues as therapeutic agents in prevention treatment of oxidative stress related diseases. In this study, 34 novel 5-fluoroindole derivatives were synthesized evaluated for their antioxidant, modulatory, inhibitory activities.Three compounds (4c, 5c, 6c) demonstrated significant activity, compound 4c showing highest efficacy reducing intracellular reactive oxygen species (ROS) 65 % CHO-K1 cells displaying DPPH radical scavenging comparable to standard BHT. However, these same exhibited antiestrogenic E-Screen assay, IC

Language: Английский

Citations

1