Zhang W, Anker L, Law R E, Hinton D R, Gopalakrishna R, Pu Q, Gundimeda U, Weiss M H, Couldwell W T
Departments of Neurological Surgery, robiolology, and Radiation Oncology, University of Southern California School of Medicine, Los Angeles, California 90033, USA.
Clin Cancer Res. 1996 May;2(5):843-6.
Hypericin, an antidepressant and antiviral agent being evaluated in phase I and II trials for patients with HIV infection, is known to be a potent protein kinase C inhibitor. We have investigated its effects on cellular response to radiation via a tetrazolium-formazan cell growth rate assay using 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide and clonogenic assay in three human glioblastoma cell lines, U87-MG, A-172, and T98G, and a low-passage malignant glioma culture, 93-492. At a concentration of 5 microM, hypericin inhibited these cells slightly but caused significant radiosensitization (e.g., the cell survival rate after the radiation treatment was 50.2 and 26.0% in cells treated with 6 Gy and 6 Gy plus 5 microM hypericin in U87-MG cells, respectively; P = 0.0285). Hypericin also enhanced the radiosensitivity significantly in the low-passage glioma 93-492 cells. These findings suggest that hypericin represents a potential new agent in combination with radiation therapy of malignant gliomas.
金丝桃素是一种正在针对HIV感染患者进行I期和II期试验评估的抗抑郁和抗病毒药物，已知它是一种有效的蛋白激酶C抑制剂。我们通过使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐的四氮唑-甲臜细胞生长速率测定法以及克隆形成测定法，在三种人胶质母细胞瘤细胞系U87-MG、A-172和T98G以及一种低传代恶性胶质瘤培养物93-492中研究了其对细胞辐射反应的影响。在5微摩尔浓度下，金丝桃素对这些细胞有轻微抑制作用，但会引起显著的放射增敏作用（例如，在U87-MG细胞中，用6 Gy辐射处理的细胞和用6 Gy加5微摩尔金丝桃素处理的细胞，辐射处理后的细胞存活率分别为50.2%和26.0%；P = 0.0285）。金丝桃素在低传代胶质瘤93-492细胞中也显著增强了放射敏感性。这些发现表明，金丝桃素是一种与恶性胶质瘤放射治疗联合使用的潜在新药。
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