Vandenbogaerde A L, Cuveele J F, Proot P, Himpens B E, Merlevede W J, de Witte P A
Laboratorium voor Farmaceutische Biologie en Fytofarmacologie, Faculteit Farmacie, Katholieke Universiteit Leuven, Belgium.
J Photochem Photobiol B. 1997 Apr;38(2-3):136-42. doi: 10.1016/s1011-1344(96)07446-5.
The cytotoxic effects of the natural photosensitizing agent hypericin were evaluated. A dramatic difference in the sensitivity of several different human and mouse cell lines towards photoactivated hypericin (4 J cm-2) was demonstrated using a neutral red assay (e.g. A431, IC50 = 0.14 +/- 0.02 microM; HeLa, IC50 = 0.32 +/- 0.05 microM, MCF7, IC50 = 1.84 +/- 0.22 microM). Dark cytotoxicity was absent, even at high hypericin concentration (25 microM). The differential phototoxicity of hypericin did not correlate with the expression of the epidermal growth factor (EGF) receptor nor with the expression of the P170 glycoprotein in the cell. The reduction of the intracellular glutathione content did not enhance further the cytotoxic effects of photoactivated hypericin, as investigated with the A431, HeLa and MCF7 cells. Conversely, using confocal laser microscopy, it was shown that the phototoxicity correlated well with the hypericin cellular uptake.
对天然光敏剂金丝桃素的细胞毒性作用进行了评估。使用中性红试验证明了几种不同的人和小鼠细胞系对光活化金丝桃素(4 J/cm²)的敏感性存在显著差异(例如,A431细胞,IC50 = 0.14 ± 0.02 μM;HeLa细胞,IC50 = 0.32 ± 0.05 μM,MCF7细胞,IC50 = 1.84 ± 0.22 μM)。即使在高浓度金丝桃素(25 μM)下也不存在暗细胞毒性。金丝桃素的差异光毒性与表皮生长因子(EGF)受体的表达以及细胞中P170糖蛋白的表达均无关。如用A431、HeLa和MCF7细胞所研究的那样,细胞内谷胱甘肽含量的降低并未进一步增强光活化金丝桃素的细胞毒性作用。相反,使用共聚焦激光显微镜显示,光毒性与金丝桃素的细胞摄取密切相关。