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首页> 外文期刊>The Open Drug Discovery Journal >In Vitro Assessment of the Tolerance Profile, the Metabolism and the Potential Depigmenting Activity of New Retinoid Derivatives
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In Vitro Assessment of the Tolerance Profile, the Metabolism and the Potential Depigmenting Activity of New Retinoid Derivatives

机译：体外评估新类维生素A衍生物的耐受性，代谢和潜在的色素沉着活性

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Background: In spite of the numerous depigmenting agents available, there is an inverse relationship betweensafety and efficiency. Natural retinoids exert depigmenting activities in vivo, but have a narrow therapeutic window. Thereis thus a need for a new class of depigmenting agents that would be both safe and useful.Objective: The aim of the study was to analyse the potential interest of new retinoid derivatives as topical depigmentingagents.Methods: The tolerance profile of the new retinoids was analysed in murine BDVII keratinocytes and murine B16melanocytes using the MTT assay. The uptake and the metabolism of the retinoids were analysed in keratinocytes andmelanocytes by HPLC/UV. The cellular content of melanin was determined in melanocytes using a photometric assay.Results: Methyl- and t-butyl-4-oxoretinoate, arbutin retinoate and retinoic acid were shown to have the best depigmentingpotential according to the ratio between the IC50 for MTT assay and that for melanin content. Retinaldehyde, 4-hydroxyretinaldehyde and methyl-4-hydroxyretinoate have a good depigmenting potential too, although the therapeuticwindow is narrower due to a higher toxicity.Conclusion: 4-Oxoesters of retinoic acid, arbutin retinoate and 4-hydroxyretinaldehyde derivatives offer a new family ofdepigmenting agents acting via a different pathway than tyrosinase inhibitors.
机译：背景：尽管有许多脱色剂，但安全性和效率之间存在反比关系。天然类维生素A在体内发挥脱色素活性，但治疗范围狭窄。因此，需要一类既安全又有用的新型脱色剂。目的：本研究的目的是分析作为局部脱色剂的新类视黄醇衍生物的潜在兴趣。方法：新类视黄醇的耐受性使用MTT分析对鼠BDVII角质形成细胞和鼠B16黑素细胞进行了分析。通过HPLC / UV分析角质形成细胞和黑素细胞中类维生素A的摄取和代谢。用光度法测定黑素细胞中黑色素的含量。结果：根据MTT测定的IC50与IC50之间的比值，甲基和叔丁基-4-氧杂环丁酸酯，熊果苷视黄酸酯和视黄酸具有最佳的脱色潜能。对于黑色素含量。视黄醛，4-羟基视黄醛和4-羟基视黄酸甲酯也具有良好的脱色潜力，尽管由于毒性更高而使治疗范围更窄。结论：视黄酸的4-羟基酯，熊果素视黄酸酯和4-羟基视黄醛衍生物提供了一个新的脱色素家族通过与酪氨酸酶抑制剂不同的途径起作用的药物。

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