Wang Z J, He Y Y, Huang C G, Huang J S, Huang Y C, An J Y, Gu Y, Jiang L J
Department of Gastrointestinology, PLA 305 Hospital, Beijing, China.
Photochem Photobiol. 1999 Nov;70(5):773-80.
Hypocrellin A, from Hypocrella bambusae, is a novel photosensitizer of high singlet oxygen quantum yield for photodynamic therapy (PDT). Tissue distributions were studied in tumor-bearing mice as a function of time following administration. The tumor model was S-180 sarcoma transplanted into one hind leg of male Kunming mice; hypocrellin A (HA) was delivered to the mice by intravenous injection of 5 mg/kg of body weight as a suspension either as a unilamellar liposome or in dimethyl sulfoxide (DMSO)-solubilized saline. The HA was isolated from several tissues and organs, as well as tumors and peritumoral muscles and skin. Quantitation was performed by a high-performance liquid chromatographic technique with detection that utilizes the native fluorescence of HA. Independent of the delivery system, the dye was retained in tumors at higher concentrations than in normal tissues, except for kidney, liver, lung and spleen. The dye retention in tumors was high and was vehicle dependent. For the liposomal system, the maximal accumulation in tumor and maximal ratios of dye in tumor versus peritumoral muscle and skin occurred 12 h postinjection; for the DMSO saline system, the maximal ratio occurred earlier, 6 h postadministration. Liposomal delivery improved the selective accumulation of the dye in tumor with higher maximal levels in tumor and higher ratios of tumor-to-muscle and tumor-to-skin. Levels of dye were very low or not detectable in the brain. The PDT efficacy of HA in the liposome and DMSO saline systems was determined by evaluating the tumor volume regression percent. The PDT efficacy of HA in liposomes was highest when light treatment was performed at 12 h postinjection, consistent with the highest retention of HA in tumors. Similarly, the maximal PDT efficacy in DMSO saline was attained at 6 h postinjection, the highest HA retention point in tumor. Moreover, the peak PDT efficacy of HA in liposomes was much higher than that of HA in DMSO saline and even hematoporphyrin monomethylether.
竹红菌甲素（Hypocrellin A）来源于竹红菌（Hypocrella bambusae），是一种新型的用于光动力疗法（PDT）的单线态氧量子产率高的光敏剂。研究了荷瘤小鼠给药后不同时间的组织分布情况。肿瘤模型为移植到雄性昆明小鼠一侧后腿的S-180肉瘤；通过静脉注射5 mg/kg体重的竹红菌甲素（HA）悬浮液（以单层脂质体形式或溶于二甲基亚砜（DMSO）的盐溶液形式）给药。从多个组织和器官以及肿瘤、瘤周肌肉和皮肤中分离出HA。采用利用HA天然荧光进行检测的高效液相色谱技术进行定量分析。与给药系统无关，除肾脏、肝脏、肺和脾脏外，该染料在肿瘤中的浓度高于正常组织。染料在肿瘤中的滞留量较高且与载体有关。对于脂质体系统，注射后12 h肿瘤中出现最大积累量以及染料在肿瘤与瘤周肌肉和皮肤中的最大比率；对于DMSO盐溶液系统，最大比率出现得更早，给药后6 h。脂质体给药改善了染料在肿瘤中的选择性积累，肿瘤中的最大水平更高，肿瘤与肌肉以及肿瘤与皮肤的比率更高。脑中的染料水平非常低或无法检测到。通过评估肿瘤体积缩小百分比来确定HA在脂质体和DMSO盐溶液系统中的光动力疗法疗效。当在注射后12 h进行光治疗时，HA在脂质体中的光动力疗法疗效最高，这与HA在肿瘤中的最高滞留量一致。同样，DMSO盐溶液中的最大光动力疗法疗效在注射后6 h达到，这是肿瘤中HA滞留的最高时间点。此外，HA在脂质体中的光动力疗法疗效峰值远高于HA在DMSO盐溶液中的疗效峰值，甚至高于血卟啉单甲醚。
