Chung P S, Saxton R E, Paiva M B, Rhee C K, Soudant J, Mathey A, Foote C, Castro D J
Department of Otolaryngology-Head and Neck Surgery, Dankook University, College of Medicine, Cheonan, Korea.
Laryngoscope. 1994 Dec;104(12):1471-6. doi: 10.1288/00005537-199412000-00008.
Tissue uptake and biodistribution of hypericin was measured in rabbits and in nu/nu mice xenografted with P3 human squamous cell carcinoma to assess the value of this dye as an in vivo sensitizer for laser photoinactivation of solid tumors. Hypericin has absorption maxima at 545 and 590 nm with a fluorescence emission peak at 640 nm in ethanol. Dye uptake after intravenous injection was tested at 4 and 24 hours in rabbit tissues by ethanol extraction and quantitative fluorescence spectrophotometry. Maximum dye levels were seen at 4 hours in most vascular organs with lung having fivefold higher uptake than spleen followed by liver, blood, and kidney. Mice were examined after 2, 4, 6, 8, and 24 hours and after 3 and 7 days for dye uptake. The peak concentration of hypericin in murine organs was reached at 4 hours with uptake per gram of tissue as follows: lung > spleen > liver > blood > kidney > heart > gut > tumor > stomach > skin > muscle > brain. Elimination of hypericin was rapid in most murine organs with residual dye under 10% of maximum by 7 days compared to 25% to 30% retention for the squamous cell tumors and several normal tissues. These results suggest that hypericin may be a useful photosensitizer for KTP/532 laser interstitial therapy of human cancer.
在兔子以及移植了P3人鳞状细胞癌的裸鼠体内测量了金丝桃素的组织摄取和生物分布，以评估这种染料作为实体瘤激光光灭活体内敏化剂的价值。金丝桃素在乙醇中的吸收最大值在545和590nm，荧光发射峰在640nm。通过乙醇萃取和定量荧光分光光度法在4小时和24小时检测兔子组织静脉注射后的染料摄取情况。在大多数血管器官中，4小时时观察到染料水平最高，肺的摄取量比脾高五倍，其次是肝、血液和肾。在2、4、6、8和24小时以及3和7天后检查小鼠的染料摄取情况。金丝桃素在鼠器官中的峰值浓度在4小时时达到，每克组织的摄取量如下：肺>脾>肝>血液>肾>心脏>肠道>肿瘤>胃>皮肤>肌肉>脑。金丝桃素在大多数鼠器官中的消除速度很快，到7天时残留染料低于最大值的10%，而鳞状细胞肿瘤和一些正常组织的保留率为25%至30%。这些结果表明，金丝桃素可能是用于人类癌症KTP/532激光间质治疗的一种有用的光敏剂。
