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Cancer Cell Int. 2016 Feb 9;16:3. doi: 10.1186/s12935-016-0279-4. eCollection 2015.

Cytotoxic and apoptogenic effect of hypericin, the bioactive component of Hypericum perforatum on the MCF-7 human breast cancer cell line.

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Department of Surgery, Islamic Azad University, Tehran Medical Sciences Branch, Tehran, Iran.
Students' Research Committee, Islamic Azad University, Tehran Medical Sciences Branch, Tehran, Iran.
Young Researchers and Elite Club, Islamic Azad University, Tehran Medical Sciences Branch, Tehran, Iran.
Department of Molecular Genetics, Faculty of Biological Sciences, Tarbiat Modares University, Tehran, Iran.
Young Researchers and Elite Club, Islamic Azad University, Tehran Medical Sciences Branch, Tehran, Iran ; Medical Research Center, Azad University, Tehran Medical Branch, Attarimoqaddam Ave, Haqani Ave, Dr. Shariati St, Tehran, P. O. BOX : 19395-1495, Iran.
Students Research Committee, School of Public Health, Shahroud University of Medical Sciences, Shahroud, Iran.
Molecular and Cell Biology Research Center, Mazandaran University of Medical Sciences, Sari, Iran.



Breast cancer is the most prevalent malignancies among the women that have a high mortality. Previous studies demonstrated that hypericin, a bioactive component of Hypericum perforatum have a cytotoxic effect on the malignant cell lines. However, an anti-carcinogenic activity of hypericin on MCF-7 is uncertain. To investigate the cytotoxic effect of hypericin on MCF-7 cells, a human breast adenocarcinoma cell-line, that resistance to chemotherapy.


The MCF-7 and fibroblast (as normal cell line) were treated with various concentrations of hypericin, and Cisplatin as a positive control for 24 and 48 h. Cytotoxicity activity was measured and confirmed by MTT assay and Trypan blue staining, respectively. In addition, Apoptosis were determined by Annexin V/Propidium Iodide assay. Immunocytochemistry (ICC) analysis for bcl2 and p53 proteins performed to further investigate different expression of these genes in different samples.


Both cisplatin and the hypericin exhibited a dose-dependent cytotoxic effect in the MCF-7 cell line. Although the LD50 of the hypericin was significantly lower when compared to cispaltin (5 vs. 20 μg/ml), it continued to decrease the growth rate of the MCF-7 cells when tested at higher concentration than LD50. In contrast, cisplatine, at higher concentration than LD50, completely inhibited the growth of the MCF-7 in 48 h. Regarding Annexin V/Propidium results, treatment of MCF-7 cells with LD50 concentration of cisplatin and hypericin showed 60 and 52 % apoptosis in 24 h, respectively. ICC analysis for bcl2 and p53 also confirmed our results; in treated samples for the dose of LD50 in 24 and 48 h of cisplatin and hypercin, more cells expressed p53 (guardian of cells in front of tumor formation/progression) and less expressed bcl2 (which has anti apoptotic activity) compared to untreated samples.


Considering that hypericin showed to be cytotoxic, it seems to be a chemopreventive agent and a good candidate for antineoplastic drug development.


Apoptosis; Breast Cancer; Cytotoxic; Hypericin; Hypericum perforatum; MCF-7

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