Graduate-Program of Medical System Engineering, Gwangju Institute of Science and Technology, Gwangju, Republic of Korea.
Bioorg Med Chem. 2011 Sep 15;19(18):5383-91. doi: 10.1016/j.bmc.2011.07.058. Epub 2011 Aug 2.
Pheophorbide-a, a chlorine based photosensitizer known to be selectively accumulated in cancer cells, was conjugated with anticancer drugs, doxorubicin and paclitaxel in the purpose of selective cancer diagnosis and therapy. Pheophorbide-a was conjugated with anticancer drugs via directly and by the use of selective cleavage linkers in cancer cell. The fluorescence of pheophorbide-a and doxorubicin conjugate by excitation at 420 or 440 nm was greatly diminished possibly by the energy transfer mechanism between two fluorescent groups. However, upon treatment in cancer cells, the conjugate showed to be cleaved to restore each fluorescence of pheophorbide-a and doxorubicin after 48 h of incubation. Also, pheophorbide-a conjugates either with doxorubicin and paclitaxel inhibited the growth of various cancer cells more potently than pheophorbide-a, which displayed very weak inhibitory activity. The results indicated that the pheophorbide-a conjugates with anticancer drugs could be utilized for selective cancer therapy as well as for the fluorescence detection of cancer.
叶绿酸-a 是一种含氯的光敏剂，已知其能选择性地在癌细胞中积累，因此被用来与抗癌药物阿霉素和紫杉醇偶联，用于癌症的选择性诊断和治疗。叶绿酸-a 通过直接偶联和使用在癌细胞中选择性切割的连接子与抗癌药物偶联。通过在 420 或 440nm 处激发，叶绿酸-a 和阿霉素偶联物的荧光大大减弱，可能是由于两个荧光团之间的能量转移机制。然而，在癌细胞中处理后，该偶联物在孵育 48 小时后显示出被切割，从而恢复了叶绿酸-a 和阿霉素各自的荧光。此外，叶绿酸-a 与阿霉素和紫杉醇的偶联物对各种癌细胞的生长抑制作用比叶绿酸-a 更强，而叶绿酸-a 显示出非常弱的抑制活性。结果表明，叶绿酸-a 与抗癌药物的偶联物可用于癌症的选择性治疗以及癌症的荧光检测。
