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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.

Author information

1
Department of Surgery, Islamic Azad University, Tehran Medical Sciences Branch, Tehran, Iran.
2
Students' Research Committee, Islamic Azad University, Tehran Medical Sciences Branch, Tehran, Iran.
3
Young Researchers and Elite Club, Islamic Azad University, Tehran Medical Sciences Branch, Tehran, Iran.
4
Department of Molecular Genetics, Faculty of Biological Sciences, Tarbiat Modares University, Tehran, Iran.
5
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.
6
Students Research Committee, School of Public Health, Shahroud University of Medical Sciences, Shahroud, Iran.
7
Molecular and Cell Biology Research Center, Mazandaran University of Medical Sciences, Sari, Iran.

Abstract

BACKGROUND:

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.

METHODS:

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.

RESULTS:

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.

CONCLUSIONS:

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

KEYWORDS:

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

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