合成对 MG-63 人类成骨细胞样细胞具有增强抗氧化和细胞抑制特性的羟基酪醇类似物及其对骨骼健康的潜在影响。

IF 4.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Archiv der Pharmazie Pub Date : 2024-11-16 DOI:10.1002/ardp.202400469
Eleftheria A Georgiou, Ioanna Kalpaktsi, Katerina Gioti, Maria Choleva, Elizabeth Fragopoulou, Alexios-Leandros Skaltsounis, Roxane Tenta, Ioannis K Kostakis
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引用次数: 0

摘要

研究人员合成了 16 种新型羟基酪醇(HT)类似物,这些类似物在 HT 脂肪族侧链的 C-1 位进行了取代,并评估了它们对 MG-63 类人成骨细胞的细胞抑制活性及其抗氧化性。结果表明,与作为阳性对照的 HT 相比,这些类似物具有明显更高的抑制活性。其中,环取代化合物的作用尤为突出,对 MG-63 细胞具有很强的自由基清除能力和显著的细胞抑制作用。这些研究结果表明,环取代 HT 类似物在开发新型抗氧化剂方面大有可为,有望应用于骨生理学领域。
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Synthesis of hydroxytyrosol analogs with enhanced antioxidant and cytostatic properties against MG-63 human osteoblast-like cells and their potential implications for bone health.

Sixteen novel hydroxytyrosol (HT) analogs with substitutions at the C-1 position of the HT aliphatic side chain were synthesized and evaluated for their cytostatic activity against MG-63 human osteoblast-like cells and for their antioxidant properties. The results revealed that these analogs exhibited significantly higher inhibitory activity compared with HT, which served as the positive control. Among these, the cyclo-substituted compounds stood out as particularly potent, demonstrating strong radical scavenging abilities and notable cytostatic effects against MG-63 cells. These findings suggest that the cyclo-substituted HT analogs hold considerable promise for the development of novel antioxidants with potential applications in bone physiology.

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来源期刊
Archiv der Pharmazie
Archiv der Pharmazie 医学-化学综合
CiteScore
7.90
自引率
5.90%
发文量
176
审稿时长
3.0 months
期刊介绍: Archiv der Pharmazie - Chemistry in Life Sciences is an international journal devoted to research and development in all fields of pharmaceutical and medicinal chemistry. Emphasis is put on papers combining synthetic organic chemistry, structural biology, molecular modelling, bioorganic chemistry, natural products chemistry, biochemistry or analytical methods with pharmaceutical or medicinal aspects such as biological activity. The focus of this journal is put on original research papers, but other scientifically valuable contributions (e.g. reviews, minireviews, highlights, symposia contributions, discussions, and essays) are also welcome.
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