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首页> 外文期刊>Photodiagnosis and Photodynamic Therapy >Photodynamic efficiency of hypericin compared with chlorin and hematoporphyrin derivatives in HEp-2 and Vero epithelial cell lines
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Photodynamic efficiency of hypericin compared with chlorin and hematoporphyrin derivatives in HEp-2 and Vero epithelial cell lines

机译：金丝桃素与二氢卟酚和血卟啉衍生物在HEp-2和Vero上皮细胞系中的光动力学效率

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Hypericin (HY) is a photoactive aromatic dianthraquinone that is considered a potent photodynamic agent. In this study, hypericin and two other photosensitizers, a hematoporphyrin derivative (Photogem (R); PG) and a chlorin derivative (Photodithazine (R); PZ), were compared in terms of their phototoxicity toward two cell lines, HEp-2 and Vero. The median inhibitory concentration (IC50) of each of the photosensitizers was obtained after a 16.2J cm(-2) dose of irradiation at 630 +/- 10 nm. The IC50 values were 0.07 +/- 0.01 (HY), 1.0 +/- 0.2 (PZ), and 9 +/- 1 mu g mL(-1) (PG) in HEp-2 cells and 0.3 +/- 0.1 (HY), 1.6 +/- 0.2 (PZ) and 11 +/- 1 mu g mL(-1) (PG) in Vero cells, showing that HY is more phototoxic than the others when irradiated at 630 nm. If these results are analyzed, simultaneously, with the first-order constant for BSA tryptophan photooxidation, obtained by fluorescence decay (lambda(excitation) = 280 nm), which are 11 x 10(-3) min(-1) +/- 1. 10(-3) min(-1) (HY), 10 x 10(-3) min(-1) +/- 1 x 10(-3) min(-1) (PZ), and 6x 10(3) min 1 x 10(-3) min(-1) (PG), it is possible to infer that the photodynamic efficiency alone is not sufficient to explain the higher HY phototoxicity. The lipophilicity is also an important factor for an efficient target cell accumulation and was assessed for all sensitizers through the octanol-water partition coefficient (log P): 1.20 +/- 0.02 (HY), -0.62 +/- 0.03 (PZ), and -0.9 +/- 0.2 (PG). The higher value for HY correlates well with its observed superior efficiency to promote damage at low concentrations and doses. As HY is used for the long-term treatment of mild depression, it is considered safe for humans. This fact and the present results reinforce the great potential of this photosensitizer to replace porphyrin derivatives, with the advantages that mean it could be used as photosensitizer in clinical photodynamic therapy. (c) 2015 Elsevier B.V. All rights reserved.
机译：金丝桃素（HY）是一种光活性芳香族二蒽醌，被认为是一种有效的光动力剂。在这项研究中，比较了金丝桃素和其他两种光敏剂，即血卟啉衍生物（Photogem（R）； PG）和二氢卟酚衍生物（Photodithazine（R）； PZ）对两种细胞系HEp-2和HEp的光毒性。维罗每种光敏剂的中值抑制浓度（IC50）在630 +/- 10 nm的剂量下以16.2J cm（-2）的剂量照射后获得。在HEp-2细胞中，IC50值为0.07 +/- 0.01（HY），1.0 +/- 0.2（PZ）和9 +/- 1μgmL（-1）（PG），而在0.3 +/- 0.1（ HY），Vero细胞中的1.6 +/- 0.2（PZ）和11 +/- 1μgmL（-1）（PG），表明当在630 nm处照射时，HY的光毒性比其他高。如果同时分析这些结果，则通过荧光衰减（λ（激发）= 280 nm）获得的BSA色氨酸光氧化的一阶常数为11 x 10（-3）min（-1）+/- 1. 10（-3）min（-1）（HY），10 x 10（-3）min（-1）+/- 1 x 10（-3）min（-1）（PZ）和6x 10 （3）min 1 x 10（-3）min（-1）（PG），有可能推断出光动力学效率不足以解释较高的HY光毒性。亲脂性也是有效靶细胞蓄积的重要因素，并且通过辛醇-水分配系数（log P）对所有敏化剂进行了评估：亲脂性：1.20 +/- 0.02（HY），-0.62 +/- 0.03（PZ），和-0.9 +/- 0.2（PG）。 HY的较高值与其在低浓度和低剂量下促进损伤的优越效率密切相关。由于HY用于长期治疗轻度抑郁症，因此被认为对人类安全。这一事实和目前的结果增强了这种光敏剂替代卟啉衍生物的巨大潜力，其优点是可以在临床光动力疗法中用作光敏剂。 （c）2015 Elsevier B.V.保留所有权利。

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