Phiphatwatcharaded Chawapon, Puthongking Ploenthip, Chaiyarit Ponlatham, Johns Nutjaree Pratheepawanit, Sakolchai Sumon, Mahakunakorn Pramote
Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen, 40002, Thailand; Melatonin Research Group, Khon Kaen University, Khon Kaen 40002, Thailand.
Research Group of Chronic Inflammatory Oral Diseases and Systemic Diseases Associated with Oral Health, Khon Kaen University, Khon Kaen, 40002, Thailand; Department of Oral Diagnosis, Faculty of Dentistry, Khon Kaen University, Khon Kaen, 40002, Thailand.
Arch Oral Biol. 2017 Jul;79:55-61. doi: 10.1016/j.archoralbio.2017.02.022. Epub 2017 Mar 7.
Aim of this in vitro study was to evaluate the anti-oxidant activity of indole ring modified melatonin derivatives as compared with melatonin in primary human gingival fibroblast (HGF) cells.
Anti-oxidant activity of melatonin (MLT), acetyl-melatonin (AMLT) and benzoyl-melatonin (BMLT) was evaluated by5 standard methods as follows: 2, 2-diphenyl-1-picrylhydrazyl (DPPH); ferric ion reducing antioxidant power (FRAP); superoxide anion scavenging; nitric oxide (NO) scavenging; and thiobarbituric acid reactive substances (TBARs).Evaluation of cellular antioxidant activity (CAA) and protectivity against HO induced cellular damage was performed via MTT assay in HGF cells.
According to the standard anti-oxidant assays, the antioxidant power of AMLT and BMLT were slightly less than MLT in FRAP and superoxide scavenging assays. In the NO scavenging and TBARs assays, BMLT and AMLT were more potent than MLT, whereas DPPH assays demonstrated that MLT was more potent than others. BMLT and AMLT had more potent anti-oxidant and protective activities against HOin HGF cells as compared with MLT.
MLT derivatives demonstrated different anti-oxidant activities as compared with MLT, depending upon assays. These findings imply that N-indole substitution of MLT may help to improve hydrogen atom transfer to free radicals but electron transfer property is slightly decreased. Anti-oxidant and protective effects of melatonin derivatives (AMLT and BMLT) on human gingival fibroblasts imply the potential use of these molecules as alternative therapeutics for chronic inflammatory oral diseases.
本体外研究的目的是评估吲哚环修饰的褪黑素衍生物与褪黑素相比在原代人牙龈成纤维细胞（HGF）中的抗氧化活性。
通过以下5种标准方法评估褪黑素（MLT）、乙酰褪黑素（AMLT）和苯甲酰褪黑素（BMLT）的抗氧化活性：2,2-二苯基-1-苦基肼（DPPH）；铁离子还原抗氧化能力（FRAP）；超氧阴离子清除；一氧化氮（NO）清除；以及硫代巴比妥酸反应性物质（TBARs）。通过MTT法在HGF细胞中评估细胞抗氧化活性（CAA）和对HO诱导的细胞损伤的保护作用。
根据标准抗氧化试验，在FRAP和超氧清除试验中，AMLT和BMLT的抗氧化能力略低于MLT。在NO清除和TBARs试验中，BMLT和AMLT比MLT更有效，而DPPH试验表明MLT比其他物质更有效。与MLT相比，BMLT和AMLT在HGF细胞中对HO具有更强的抗氧化和保护活性。
与MLT相比，MLT衍生物根据试验表现出不同的抗氧化活性。这些发现表明，MLT的N-吲哚取代可能有助于改善向自由基的氢原子转移，但电子转移性质略有下降。褪黑素衍生物（AMLT和BMLT）对人牙龈成纤维细胞的抗氧化和保护作用表明这些分子有可能作为慢性炎症性口腔疾病的替代疗法。
