Buríková Monika, Bilčík Boris, Máčajová Mariana, Výboh Pavel, Bizik Jozef, Mateašík Anton, Miškovský Pavol, Čavarga Ivan
Institute of Animal Biochemistry and Genetics, SAS, Ivanka pri Dunaji, Slovak Republic.
Gen Physiol Biophys. 2016 Oct;35(4):459-468. doi: 10.4149/gpb_2016014. Epub 2016 Jul 22.
There has been increasing interest in fluorescence-based imaging techniques in clinical practice, with the aim to detect and visualize the tumour configuration and the border with healthy tissue. Strong photodynamic activity of hypericin (Hyp) can be improved by various molecular transport systems (e.g. LDL). Our aim was to examine pharmacokinetics of Hyp in the presence of LDL particles on ex ovo chorioallantoic membrane (CAM) of Japanese quail with implanted TE1 tumour spheroids (human squamocellular carcinoma). Spheroids were implanted on CAM surface on embryonal day 7 and after 24 hours formulations of free Hyp and Hyp:LDL 100:1 and 200:1 were topically applied. All experimental formulations in the fluorescent image very well visualized the tumour spheroid position, with gradual increase of fluorescence intensity in 6-h observation period. LDL transportation system exhibited clear superiority in fluorescence pharmacokinetics than free Hyp formulation by increasing tumour-normal difference. Our experimental results confirm that Hyp and Hyp:LDL complex is potent fluorophore for photodynamic diagnosis of squamocellular carcinoma.
在临床实践中,基于荧光的成像技术越来越受到关注,其目的是检测并可视化肿瘤形态以及肿瘤与健康组织的边界。金丝桃素(Hyp)的强光动力活性可通过各种分子转运系统(如低密度脂蛋白)得到增强。我们的目的是在植入TE1肿瘤球体(人鳞状细胞癌)的日本鹌鹑的卵外绒毛尿囊膜(CAM)上,研究在低密度脂蛋白颗粒存在的情况下Hyp的药代动力学。在胚胎第7天将球体植入CAM表面,24小时后局部应用游离Hyp以及Hyp:LDL 100:1和200:1的制剂。在荧光图像中,所有实验制剂都很好地显示了肿瘤球体的位置,在6小时的观察期内荧光强度逐渐增加。通过增加肿瘤与正常组织的差异,低密度脂蛋白转运系统在荧光药代动力学方面表现出明显优于游离Hyp制剂的优势。我们的实验结果证实,Hyp和Hyp:LDL复合物是鳞状细胞癌光动力诊断的有效荧光团。