Rodal G H, Rodal S K, Moan J, Berg K
Institute for Cancer Research, Department of Biophysics, Oslo, Norway.
J Photochem Photobiol B. 1998 Sep;45(2-3):150-9. doi: 10.1016/s1011-1344(98)00175-4.
In the present study, cellular uptake of a liposomal formulation of ZnPc (CGP 55847) has been studied in human cervix carcinoma cells of the line NHIK 3025. The cellular uptake of ZnPc is found to be completed after 4-8 h of incubation. The maximum level of ZnPc in the cells after incubation with 1 microgram/ml ZnPc in E2a medium containing 3% serum is 60 ng/mg protein. The cellular uptake is attenuated by the presence of serum and at low temperature of the incubation medium, but the activation energy (30 kJ/mol) and fluorescence microscopic analysis of cells incubated with ZnPc at 0 degree C indicate that ZnPc is taken up into cells by a diffusion-mediated pathway. Measurements of subcellular marker enzymes have been performed immediately after light exposure of ZnPc-treated cells. The mitochondrial marker enzyme (cytochrome c oxidase) and the marker enzyme for the Golgi apparatus (UDP galactosyl transferase), but not those for lysosomes (beta-N-acetyl-D-glucosaminidase) and endoplasmic reticulum (NADPH cytochrome c reductase), are inactivated upon photodynamic treatment. These results indicate that ZnPc is mainly located in the Golgi apparatus and the mitochondria of NHIK 3025 cells. In contrast, photoactivated Photofrin is found to reduce the activity of UDP galactosyl transferase, but not that of NADPH cytochrome c reductase. The tetraphenylporphine TPPS2a and light reduce the activity of NADPH cytochrome c reductase, without influencing the activity of UDP galactosyl transferase. TPPS4 and light do not attenuate the activities of UDP galactosyl transferase and NADPH cytochrome c reductase.
在本研究中，已对锌酞菁（CGP 55847）脂质体制剂在NHIK 3025人宫颈癌细胞系中的细胞摄取情况进行了研究。发现锌酞菁的细胞摄取在孵育4 - 8小时后完成。在含有3%血清的E2a培养基中用1微克/毫升锌酞菁孵育后，细胞中锌酞菁的最大水平为60纳克/毫克蛋白质。血清的存在和孵育培养基的低温会减弱细胞摄取，但活化能（30千焦/摩尔）以及在0℃下用锌酞菁孵育的细胞的荧光显微镜分析表明，锌酞菁是通过扩散介导的途径被细胞摄取的。在用锌酞菁处理的细胞光照后立即进行了亚细胞标记酶的测量。光动力处理后，线粒体标记酶（细胞色素c氧化酶）和高尔基体标记酶（UDP半乳糖基转移酶）失活，但溶酶体（β-N-乙酰-D-氨基葡萄糖苷酶）和内质网（NADPH细胞色素c还原酶）的标记酶未失活。这些结果表明锌酞菁主要位于NHIK 3025细胞的高尔基体和线粒体中。相比之下，发现光激活的血卟啉会降低UDP半乳糖基转移酶的活性，但不会降低NADPH细胞色素c还原酶的活性。四苯基卟啉TPPS2a和光照会降低NADPH细胞色素c还原酶的活性，而不影响UDP半乳糖基转移酶的活性。TPPS4和光照不会减弱UDP半乳糖基转移酶和NADPH细胞色素c还原酶的活性。
