Shin Hyeon-Cheol, Hwang Hye Jeong, Kang Kee Jung, Lee Bong Ho
Laboratory of Aging and Degenerative Diseases, Hanbat National University, Daejon 305-719, Korea.
Arch Pharm Res. 2006 Feb;29(2):165-71. doi: 10.1007/BF02974279.
Osteoarthritis is thought to be induced by the ageing-related loss of homeostatic balance between degeneration and repair mechanism around cartilage tissue in which inflammatory mediators such as reactive oxygen species, cytokines and prostaglandins are prone to over-production under undesirable physiological conditions. Phlorotannins are unique polyphenolic compounds bearing dibenzo-1,4-dioxin skeleton which are not found in terrestrial plants but found only in some brown algal species such as Ecklonia and Eisenia families. Phlorotannin-rich extracts of Ecklonia cava including LAD103 showed significant antioxidant activities such as DPPH radical scavenging, ferric ion reduction, peroxynitrite scavenging, and inhibition of LDL oxidation, indicating their possible antioxidative interference both in onset and downstream consequences of osteoarthritis. LAD103 also showed significant down regulation of PGE2 generation in LPS-treated RAW 246.7 cells, and significant inhibition of human recombinant interleukin-1alpha-induced proteoglycan degradation, indicating its beneficial involvement in pathophysiological consequences of osteoarthritis, the mechanism of which needs further investigation. Since LAD103 showed strong therapeutic potentials in arthritic treatment through several in vitro experiments, it is highly encouraged to perform further mechanistic and efficacy studies.
骨关节炎被认为是由软骨组织周围退变与修复机制之间与衰老相关的稳态平衡丧失所诱发，在不良生理条件下，诸如活性氧、细胞因子和前列腺素等炎症介质易于过度产生。间苯三酚单宁是一类独特的具有二苯并 - 1,4 - 二恶英骨架的多酚化合物，在陆生植物中未发现，仅在一些褐藻物种如昆布属和艾氏藻属中存在。包括LAD103在内的海蕴富含间苯三酚单宁的提取物表现出显著的抗氧化活性，如清除DPPH自由基、还原铁离子、清除过氧亚硝酸盐以及抑制低密度脂蛋白氧化，表明它们可能在骨关节炎的发病及下游后果中发挥抗氧化干预作用。LAD103在脂多糖处理的RAW 246.7细胞中还显示出显著下调前列腺素E2的生成，并显著抑制人重组白细胞介素 - 1α诱导的蛋白聚糖降解，表明其在骨关节炎病理生理后果中具有有益作用，其作用机制有待进一步研究。由于LAD103通过多项体外实验在关节炎治疗中显示出强大的治疗潜力，因此强烈鼓励开展进一步的机制和疗效研究。
