Cozzani I, Jori G, Reddi E, Fortunato A, Granati B, Felice M, Tomio L, Zorat P
Chem Biol Interact. 1981 Oct;37(1-2):67-75. doi: 10.1016/0009-2797(81)90166-6.
Different doses (0.5-20 mg/kg) of hematoporphyrin (HP) have been injected intraperitoneally into normal rats and rats affected by Yoshida ascites hepatoma. About 80% of HP reaching the liver was recovered in the extracellular compartment after liver perfusion, the ratio of extra- to intracellular HP being essentially independent of the administered dose. Similar data were obtained at different times after injection of 20 mg/kg HP. Intracellular HP largely accumulates in the mitochondria and in the membrane components of the nuclear fraction of isolated hepatocytes. Kinetic studies suggest that the cell receptors of highest affinity for HP are present in the external membrane. The latter result obtains for ascites hepatoma cells in an even more evident way, although the latter cells exhibit secondary HP binding sites probably constituted by cytoplasmatic proteins. Moreover, the clearance of intracellular HP from malignant cells occurs at a remarkably lower rate as compared with HP clearance from liver cells.
已将不同剂量（0.5 - 20毫克/千克）的血卟啉（HP）腹腔注射到正常大鼠和吉田腹水肝癌大鼠体内。肝脏灌注后，到达肝脏的HP约80%在细胞外区室中回收，细胞外与细胞内HP的比例基本与给药剂量无关。注射20毫克/千克HP后在不同时间也获得了类似的数据。细胞内HP大量积聚在线粒体和分离的肝细胞核部分的膜成分中。动力学研究表明，对HP亲和力最高的细胞受体存在于外膜中。后一结果在腹水肝癌细胞中表现得更为明显，尽管后者细胞表现出可能由细胞质蛋白构成的二级HP结合位点。此外，与肝细胞中HP的清除相比，恶性细胞中细胞内HP的清除速率明显更低。
