Heo Cheol Ho, Roh Eun Ji, Kim Jaehee, Choi Hyemin, Jang Ho Yeon, Lee Giseong, Lim Chang Su, Han Inbo
Department of Applied Chemistry, Kookmin University, Seoul 02707, Republic of Korea.
Pure Chem Co., Ltd., Knu Start-up CUBE, Chunchenon 24341, Republic of Korea.
J Funct Biomater. 2023 Mar 29;14(4):192. doi: 10.3390/jfb14040192.
Cyclooxygenase-2 (COX-2) is a biomolecule known to be overexpressed in inflammation. Therefore, it has been considered a diagnostically useful marker in numerous studies. In this study, we attempted to assess the correlation between COX-2 expression and the severity of intervertebral disc (IVD) degeneration using a COX-2-targeting fluorescent molecular compound that had not been extensively studied. This compound, indomethacin-adopted benzothiazole-pyranocarbazole (), was synthesized by introducing indomethacin-a compound with known selectivity for COX-2-into a phosphor with a benzothiazole-pyranocarbazole structure. exhibited relatively high fluorescence intensity in cells pretreated with lipopolysaccharide, which induces inflammation. Furthermore, we observed significantly higher fluorescence in tissues with artificially damaged discs (modeling IVD degeneration) compared to normal disc tissues. These findings indicate that can meaningfully contribute to the study of the mechanism of IVD degeneration in living cells and tissues and to the development of therapeutic agents.
环氧化酶-2（COX-2）是一种已知在炎症中过度表达的生物分子。因此，在众多研究中它被视为一种具有诊断价值的标志物。在本研究中，我们尝试使用一种尚未被广泛研究的靶向COX-2的荧光分子化合物，来评估COX-2表达与椎间盘（IVD）退变严重程度之间的相关性。这种化合物，吲哚美辛修饰的苯并噻唑-吡喃咔唑（），是通过将对COX-2具有已知选择性的化合物吲哚美辛引入具有苯并噻唑-吡喃咔唑结构的荧光团中合成的。在经脂多糖预处理（诱导炎症）的细胞中表现出相对较高的荧光强度。此外，与正常椎间盘组织相比，我们在人工损伤椎间盘（模拟IVD退变）的组织中观察到显著更高的荧光。这些发现表明，能够对活细胞和组织中IVD退变机制的研究以及治疗药物的开发做出有意义的贡献。
