Two tetrapyridine porphyrins, cationic porphyrin P4 (TMPyP4) and its amphiphilic derivative porphyrin P1 with carboxyl groups, and their zinc-containing analogs ZnP4 and ZnP1 were examined in order to obtain the photosensitizers with a narrower specificity for target tissue. The two classes of molecules were compared with respect to physicochemical properties of and the effect on Caki-1 clear cell renal cell carcinoma cells in vitro. Micromolar concentrations of the compounds did not cause morphological changes in cells in the absence of light irradiation. Cell treatment with porphyrin porphyrin P4 under blue light led to a rapid cytotoxic effect. The cells began to detach from the substrate, and swellings (blebs) became detectable in their membranes. The rate of the changes was consistent with direct membrane damage by porphyrin P4. Compound ZnP1 did not cause any visible changes in Caki-1 cell morphology in similar conditions. The results were explained by different lipophilicities and, therefore, different intracellular localization of the compounds. Membrane localization was assumed to prevail in the case of porphyrin P4, which is more lipophilic then ZnP1, and to mediate its fast cytopathic effect.

检测了两种四吡啶卟啉、阳离子卟啉 P4 (TMPyP4) 及其具有羧基的两亲衍生物卟啉 P1 及其含锌类似物 ZnP4 和 ZnP1，以获得对靶组织具有更窄特异性的光敏剂。就体外Caki-1透明细胞肾细胞癌细胞的理化性质和对这两种分子的作用进行了比较。在没有光照射的情况下，微摩尔浓度的化合物不会引起细胞的形态变化。在蓝光下用卟啉卟啉 P4 处理细胞会产生快速的细胞毒性作用。细胞开始从基质上分离，并且在它们的膜中可以检测到肿胀（气泡）。变化率与卟啉 P4 对膜的直接损伤一致。在类似条件下，化合物 ZnP1 不会引起 Caki-1 细胞形态的任何可见变化。结果由不同的亲脂性和因此不同的化合物的细胞内定位来解释。假设膜定位在卟啉 P4 的情况下占主导地位，它比 ZnP1 更亲脂，并介导其快速的细胞病变效应。