Kumar Akhil, George Jiya Mary, Sharma Sushank, Koyyadi Sundar, Sharma Suchinder K, Verwilst Peter, Bhatia Alka, Patro Sourabha Kumar, Aggarwal Anjali, Gupta Shipra, Sharma Sheetal, Sharma Amit
Department of Experimental Medicine and Biotechnology, Postgraduate Institute of Medical Education and Research, Sector 12, Chandigarh 160012, India.
Oral Health Sciences Centre, Postgraduate Institute of Medical Education and Research, Sector 12, Chandigarh 160012, India.
ACS Appl Bio Mater. 2024 Dec 16;7(12):8517-8527. doi: 10.1021/acsabm.4c01323. Epub 2024 Nov 19.
For developing a successful cancer therapeutic modality, the early precise detection of cancer cells in patient biopsies in oral squamous cell carcinoma (OSCC) is crucial. This could help researchers create new diagnostic and therapeutic tools and assist clinicians in recommending more effective treatment plans and improving patient survival. We have developed an SMPD, cyclooxygenase-2 (COX-2) targeting pH-activable fluorophore named , combining a potent COX-2 inhibitor, celecoxib, linked to a naphthalimide fluorophore with an acidic microenvironment-responsive piperazine moiety for specific optical imaging of OSCC in cells and patient tissues. Compared to reference probe lacking celecoxib, selectively enters the COX-2 overexpressing oral cancer cells. Its acidity-responsive imaging response enhances selectivity over cancers with lower COX-2 expression levels and normal cells. Further, is demonstrated in imaging OSCC cells in patient-derived biopsies. Thus, multifunctional shows potential in exploring more reagents for fluorescence-based detection of OSCC cells in patient tissues with translational applications.
对于开发一种成功的癌症治疗方法,在口腔鳞状细胞癌(OSCC)患者活检中早期精确检测癌细胞至关重要。这有助于研究人员创建新的诊断和治疗工具,并协助临床医生推荐更有效的治疗方案,提高患者生存率。我们开发了一种名为 的鞘磷脂磷酸二酯酶(SMPD),靶向环氧化酶-2(COX-2)的pH可激活荧光团,它结合了一种强效COX-2抑制剂塞来昔布,与萘二甲酰亚胺荧光团相连,并带有一个酸性微环境响应性哌嗪部分,用于在细胞和患者组织中对OSCC进行特异性光学成像。与缺乏塞来昔布的参考探针相比, 选择性地进入COX-2过表达的口腔癌细胞。其酸度响应成像反应增强了对COX-2表达水平较低的癌症和正常细胞的选择性。此外, 在患者来源的活检中对OSCC细胞进行成像得到了证实。因此,多功能 在探索更多用于基于荧光检测患者组织中OSCC细胞的试剂方面具有潜力,并具有转化应用价值。