Milackova Ivana, Rackova Lucia, Majekova Magdalena, Mrvova Natasa, Stefek Milan
Institute of Experimental Pharmacology and Toxicology, Slovak Academy of Sciences, Dubravska cesta 9, 841 04 Bratislava, Slovak Republic.
Gen Physiol Biophys. 2015 Jan;34(1):51-64. doi: 10.4149/gpb_2014028. Epub 2014 Nov 4.
Many natural and synthetic quinones and naphthoquinones possess a variety of beneficial pharmacological properties. In plants, the cytotoxic properties of quinones serve in their defensive roles against invading bacteria, fungi and parasites. In this regard many quinones as well as polyphenols, exerting generally toxicity at high dosages, are able to induce favorable hormetic responses at a low dosage. The novel chloronaphthoquinone derivative of quercetin (CHNQ) showed a profound cytotoxicity followed by enhancement of intracellular generation of oxidants in human neonatal B-HNF-3 fibroblasts. Its synthetic precursors, quercetin and 2-chloro-3-hydroxy-[1,4]naphthoquinone, failed to induce these effects, and paradoxically, only CHNQ at a low concentration provided partial protection of the cells against oxidative challenge. Thus, the novel quinonoid-polyphenol CHNQ might have a merit in the search for new prospective agents in prevention and management of ageing and ageing-related pathologies.
许多天然和合成的醌类及萘醌类化合物具有多种有益的药理特性。在植物中,醌类的细胞毒性特性在其抵御入侵细菌、真菌和寄生虫的防御作用中发挥作用。在这方面,许多醌类以及多酚类化合物,虽然在高剂量时通常具有毒性,但在低剂量时能够诱导出有利的 hormetic 反应。新型槲皮素氯萘醌衍生物(CHNQ)在人新生儿 B - HNF - 3 成纤维细胞中表现出显著的细胞毒性,随后细胞内氧化剂生成增加。其合成前体槲皮素和 2 - 氯 - 3 - 羟基 - [1,4]萘醌未能诱导这些效应,而且矛盾的是,只有低浓度的 CHNQ 能为细胞提供部分抗氧化应激保护。因此,新型醌类 - 多酚化合物 CHNQ 在寻找预防和管理衰老及衰老相关病症的新潜在药物方面可能具有价值。