BRAZILEIN INCREASES THE SENSITIVITY OF DOXORUBICIN ON MCF-7 RESISTANT DOXORUBICIN (MCF-7/DOX) CELLS THROUGH INHIBITION OF HER-2 ACTIVATION


N. P. Linda Laksmiani, R. Asmah Susidarti, Edy Meiyanto

Abstract


Objective: Brazilein is a compound obtained in a large amount from the dried heartwood of Secang (Caesalpinia sappan L.). Brazilein has strong cytotoxic effect in several cancer cell lines. This study was designed to evaluate the cytotoxic effect of combination brazilein with a chemotherapy agent, doxorubicin on MCF-7/DOX breast cancer cell lines and evaluate the molecular mechanism of brazilein by in silico using molecular docking to HER-2.

Methods: In the cytotoxicity assay, MCF-7/DOX cells were cultured in the presence of brazilein and doxorubicin for 24 hours and cell viability was evaluated by using MTT assay. Interactions between brazilein and the target protein, HER-2 (3PP0) was evaluated and calculated in silico by molecular docking using PLANTS.

Results: Brazilein increased doxorubicin’s cytotoxic activity on MCF-7/DOX cells. Both of single treatment with different concentration brazilein 12.5 and 25 mM or doxorubicin 0.8 and 1 mM gave cell viability percentage above 80%, but combination of them led to decrease the cell viability percentage significantly. The score docking of brazilein was -77.73 kcal/mol and lapatinib value -71.34 kcal/mol.

Conclusion: Interaction between brazilein and HER-2 (3PP0) as protein target in breast cancer higher affinity than lapatinib as HER-2 drug. Brazilein performed as a potent co-chemotherapy agent for breast cancer treatment.

 


Keywords


Brazilein, Doxorubicin, Cytotoxic, HER-2 (3PP0), MCF-7/DOX (Resistant MCF-7 Cells to Doxorubicin)

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About this article

Title

BRAZILEIN INCREASES THE SENSITIVITY OF DOXORUBICIN ON MCF-7 RESISTANT DOXORUBICIN (MCF-7/DOX) CELLS THROUGH INHIBITION OF HER-2 ACTIVATION

Keywords

Brazilein, Doxorubicin, Cytotoxic, HER-2 (3PP0), MCF-7/DOX (Resistant MCF-7 Cells to Doxorubicin)

Date

02-01-2015

Additional Links

Manuscript Submission

Journal

International Journal of Pharmacy and Pharmaceutical Sciences
Vol 7, Issue 2, 2015 Page: 525-528

Online ISSN

0975-1491

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262 Views | 139 Downloads

Authors & Affiliations

N. P. Linda Laksmiani
Udayana University
Indonesia

R. Asmah Susidarti
Gadjah Mada University
Indonesia

Edy Meiyanto
Gadjah Mada University
Indonesia


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