In vitro Evaluation of Endocrine-Related Adverse Effects of 5-Fluoroindole Derived Melatonin Analogues with Antioxidant Activity.

IF 2.3 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Chemistry & Biodiversity Pub Date : 2024-11-11 DOI:10.1002/cbdv.202402050

Elif Ince Erguc, Hanifa Fatullayev, Bita Entezari, Betul Tekiner, Sibel Suzen, Hande Gurer-Orhan

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Abstract

Melatonin (MLT) is a natural indolic hormone and its antioxidant activity has been reported through various mechanisms. MLT interacts with the estrogen signaling pathway by inhibiting aromatase enzyme, and it has been suggested that these new compounds may have endocrine-related adverse effects due to their selective estrogen modulator activity. In this study, we investigated the aromatase inhibitory and estrogen receptor agonist/antagonist effects as well as possible antioxidant activity of MLT analogue 5-floro indole derivatives for being potential drug candidates in the prevention and treatment of oxidative stress related diseases. Among the 34 compounds tested, three compounds showed antioxidant effect through radical scavenging activity and reducing the formation of intracellular reactive oxygen species. They also showed varying potencies of antiestrogenic and/or aromatase inhibitory activity which should be considered as a potential untargeted effect of MLT and its analogues.

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体外评估具有抗氧化活性的 5-氟吲哚衍生褪黑素类似物与内分泌相关的不良反应。

褪黑素（MLT）是一种天然吲哚类激素，其抗氧化活性已通过各种机制得到报道。MLT 通过抑制芳香化酶与雌激素信号通路相互作用，有人认为这些新化合物可能因其选择性雌激素调节剂活性而产生与内分泌相关的不良反应。在这项研究中，我们研究了 MLT 类似物 5-氯吲哚衍生物的芳香化酶抑制和雌激素受体激动剂/拮抗剂效应以及可能的抗氧化活性，以作为预防和治疗氧化应激相关疾病的潜在候选药物。在测试的 34 种化合物中，有三种化合物通过自由基清除活性和减少细胞内活性氧的形成而显示出抗氧化作用。它们还显示出不同效力的抗雌激素和/或芳香化酶抑制活性，这应被视为 MLT 及其类似物的潜在非靶向效应。

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来源期刊

Chemistry & Biodiversity 环境科学-化学综合

CiteScore

3.40

自引率

10.30%

发文量

475

审稿时长

2.6 months

期刊介绍： Chemistry & Biodiversity serves as a high-quality publishing forum covering a wide range of biorelevant topics for a truly international audience. This journal publishes both field-specific and interdisciplinary contributions on all aspects of biologically relevant chemistry research in the form of full-length original papers, short communications, invited reviews, and commentaries. It covers all research fields straddling the border between the chemical and biological sciences, with the ultimate goal of broadening our understanding of how nature works at a molecular level. Since 2017, Chemistry & Biodiversity is published in an online-only format.