Comparative effects of curcuminoids on endothelial heme oxygenase-1 expression: Ottho-methoxy groups are essential to enhance heme oxygenase activity and protection
Comparative effects of curcuminoids on endothelial heme oxygenase-1 expression: Ottho-methoxy groups are essential to enhance heme oxygenase activity and protection
复制标题
DOI：
10.1038/emm.2006.46
复制
发表时间：
2006-08-31
影响因子：
12.8
通讯作者：
Chung, Hun-Taeg
中科院分区：
文献类型：
--
作者：
Jeong, Gil-Saeng;Oh, Gi-Su;Chung, Hun-Taeg
最近，据报道，姜黄素被认为是一种有效的抗氧化剂，可作为细胞保护性血红素加氧酶（HO）-1的无应激且无细胞毒性的诱导剂。在这项研究中，比较了天然存在的姜黄素，例如纯姜黄素、去甲氧基姜黄素 (DMC) 和双去甲氧基姜黄素 (BDMC)，它们调节人内皮细胞中 HO-1 表达和细胞保护活性的潜在能力。所有三种姜黄素均可诱导不同水平的 HO-1 表达和 HO 活性。 HO活性的排序为姜黄素、DMC和BDMC。与针对 H2O2 诱导的细胞损伤的内皮保护作用相比，姜黄素的细胞保护能力最高，其次是 DMC 和 BDMC。有趣的是，类姜黄素提供的细胞保护作用与其增强过氧化氢活性的能力密切相关。考虑到三种类姜黄素之间的主要区别在于甲氧基的数量（BDMC 没有，DMC 没有，姜黄素有 2 个），因此表明芳香环邻位上甲氧基的存在对于增强人内皮细胞中 HO-1 的表达和细胞保护至关重要。我们的结果可能有助于设计更有效的 HO-1 诱导剂，这些诱导剂可以被认为是开发预防或治疗氧化损伤引起的内皮疾病的治疗方法中有前途的药物。
Recently, it has been reported that curcumin, which is known as a potent antioxidant, acts as a non-stressful and non-cytotoxic inducer of the cytoprotective heme oxygenase (HO)-1. In this study, naturally occurring curcuminoids, such as pure curcumin, demethoxycurcumin (DMC) and bis-demethoxycurcumin (BDMC), were compared for their potential ability to modulate HO-1 expression and cytoprotective activity in human endothelial cells. All three curcuminoids could induce HO-1 expression and HO activity with differential levels. The rank order of HO activity was curcumin, DMC and BDMC. In comparison with endothelial protection against H2O2-induced cellular injury, cytoprotective capacity was found to be highest with curcumin, followed by DMC and BDMC. Interestingly, cytoprotective effects afforded by curcuminoids were considerably associated with their abilities to enhance HO activity. Considering that the main difference among the three curcuminoids is the number of methoxy groups (gone for BDMC, one for DMC, and two for curcumin), the presence of methoxy groups in the ortho position on the aromatic ring was suggested to be essential to enhance HO-1 expression and cytoprotection in human endothelial cells. Our results may be useful in designing more efficacious HO-1 inducers which could be considered as promising pharmacological agents in the development of therapeutic approaches for the prevention or treatment of endothelial diseases caused by oxidative damages.