Dipartimento di Scienze del Farmaco, Faculty of Pharmacy, University of Catania, V.le A. Doria 6, 95125 Catania, Italy.
Med Chem. 2013 Feb;9(1):84-90. doi: 10.2174/157340613804488378.
5-Arylidene-2-oxo-4-thiazolidinones and 2-phenylimino analogues were evaluated for their antidegenerative activity on human chondrocyte cultures stimulated by IL-1β and for their inhibitory capability against matrix metalloproteinase- 13. Our results indicated that 5-arylidene-4-thiazolidinone derivatives 1-9 exhibit antidegenerative activity and could block multiple cartilage destruction during the osteoarthritic process. Out of the selected compounds, (5-arylidene- 2,4-dioxothiazolidin-3-yl)acetic acids 7-9 showed significant effectiveness in reducing NO release and restoring normal levels of GAGs in chondrocytes treated with IL-1β. Moreover, benzoic acids 1, 5 and 6 proved to be effective MMP-13 inhibitors and were able to restore normal levels of GAGs.
5-芳亚甲基-2-氧代-4-噻唑烷酮和 2-苯亚氨基类似物被评估其对 IL-1β 刺激的人软骨细胞的抗退行性活性，以及对基质金属蛋白酶-13 的抑制能力。我们的结果表明，5-芳亚甲基-4-噻唑烷酮衍生物 1-9 具有抗退行性活性，可阻止骨关节炎过程中多种软骨破坏。在所选择的化合物中，（5-芳亚甲基-2,4-二氧代噻唑烷-3-基）乙酸 7-9 显示出在降低 NO 释放和恢复 IL-1β 处理的软骨细胞中 GAGs 正常水平方面的显著效果。此外，苯甲酸 1、5 和 6 被证明是有效的 MMP-13 抑制剂，并且能够恢复 GAGs 的正常水平。
