University of Pennsylvania Perelman School of Medicine, Pulmonary, Allergy and Critical Care Division, Philadelphia, Pennsylvania 19104.
Radiat Res. 2014 Jul;182(1):102-10. doi: 10.1667/RR13635.1. Epub 2014 Jun 19.
Secoisolariciresinol diglucoside (SDG) is the major lignan in wholegrain flaxseed. However, extraction methods are complex and are associated with low yield and high costs. Using a novel synthetic pathway, our group succeeded in chemically synthesizing SDG (S,S and R,R enantiomers), which faithfully recapitulates the properties of their natural counterparts, possessing strong antioxidant and free radical scavenging properties. This study further extends initial findings by now investigating the DNA-radioprotective properties of the synthetic SDG enantiomers compared to the commercial SDG. DNA radioprotection was assessed by cell-free systems such as: (a) plasmid relaxation assay to determine the extent of the supercoiled (SC) converted to open-circular (OC) plasmid DNA (pBR322) after exposure of the plasmid to gamma radiation; and (b) determining the extent of genomic DNA fragmentation. Exposure of plasmid DNA to 25 Gy of γ radiation resulted in decreased supercoiled form and increased open-circular form, indicating radiation-induced DNA damage. Synthetic SDG (S,S) and SDG (R,R), and commercial SDG at concentrations of 25-250 μM significantly and equipotently reduced the radiation-induced supercoiled to open-circular plasmid DNA in a dose-dependent conversion. In addition, exposure of calf thymus DNA to 50 Gy of gamma radiation resulted in DNA fragments of low-molecular weight (<6,000 bps), which was prevented in a dose-dependence manner by all synthetic and natural SDG enantomers, at concentrations as low as 0.5 μM. These novel results demonstrated that synthetic SDG (S,S) and SDG (R,R) isomers and commercial SDG possess DNA-radioprotective properties. Such properties along with their antioxidant and free radical scavenging activity, reported earlier, suggest that SDGs are promising candidates for radioprotection for normal tissue damage as a result of accidental exposure during radiation therapy for cancer treatment.
肠内脂二葡萄糖甙(SDG)是亚麻籽全谷物中的主要木质素。然而,提取方法复杂,且产量低、成本高。我们的研究小组通过一种新的合成途径,成功地化学合成了 SDG(S,S 和 R,R 对映体),其忠实地再现了天然对应物的特性,具有很强的抗氧化和自由基清除特性。本研究进一步扩展了最初的发现,现在研究了与商业 SDG 相比,合成 SDG 对映体的 DNA 辐射防护特性。通过无细胞系统评估 DNA 辐射防护,例如:(a)质粒松弛测定法,用于确定在将质粒暴露于γ辐射后超螺旋(SC)转化为开环(OC)质粒 DNA(pBR322)的程度;(b)确定基因组 DNA 片段化的程度。将质粒 DNA 暴露于 25 Gy 的γ射线会导致超螺旋形式减少,开环形式增加,表明辐射引起 DNA 损伤。合成 SDG(S,S)和 SDG(R,R)以及商业 SDG 在 25-250 μM 的浓度下,以剂量依赖性方式显著且等效地减少了辐射诱导的超螺旋到开环质粒 DNA 的转化。此外,将小牛胸腺 DNA 暴露于 50 Gy 的γ射线会导致低分子量(<6000 bps)的 DNA 片段,所有合成和天然 SDG 对映体都以剂量依赖性方式防止了这种情况,浓度低至 0.5 μM。这些新的结果表明,合成 SDG(S,S)和 SDG(R,R)对映体和商业 SDG 具有 DNA 辐射防护特性。这些特性以及它们之前报道的抗氧化和自由基清除活性表明,SDG 是治疗癌症放射治疗中意外辐射导致正常组织损伤的潜在放射保护候选物。