CYTOTOXIC ACTIVITY OF BRAZILEIN ISOLATED FROM SECANG (CAESALPINIA SAPPAN L.) AGAINST MCF7/DOX CELLS BY INHIBITION OF P-GLYCOPROTEIN


N. P. Linda Laksmiani, E. D. Y. Meiyanto, R. Asmah Susidarti

Abstract


Objective: This study was focused on isolation of brazilein from the dried heartwood of Secang (Caesalpinia sappan L.) followed by its characterization using Infrared (IR) spectroscopy, liquid chromatography-mass spectrometry (LC-MS) with electrospray ionization (ESI), proton (1H), carbon-13 (13C) nuclear magnetic resonance (NMR) and two dimensional (2D)-NMR, evaluation the cytotoxic activity of brazilein in MCF-7 resistant doxorubicin (MCF-7/DOX) cells and evaluate the interaction between brazilein and ATP with P-glycoprotein (Pgp) in silico using molecular docking.

Methods: Brazilein was isolated and purified from ethyl acetate fraction by flash silica gel column chromatography, eluting with chloroform, ethyl acetate and methanol in gradient concentration. In the cytotoxicity assay, MCF-7/DOX cells were cultured in the presence of brazilein for 24 hour (h) and cell viability was evaluated by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Interactions between brazilein and the target proteins were evaluated and calculated in silico by molecular docking using PLANTS.

Results: The infrared, mass spectra with a molecular weight of 284 and NMR signal confirmed that was brazilein. MTT assay showed a dose-dependent inhibition of MCF-7/DOX cell proliferation with brazilein IC50 value of 43 µM. The docking score of brazilein was-71,45 kcal/mol and ATP value-96,23 kcal/mol.

Conclusion: Brazilein has a potent cytotoxic value on MCF-7/DOX and high affinity in Pgp protein target. Brazilein can be developed as anticancer especially in cancer resistance incidence. Further study must be established to evaluate the molecular mechanism of brazilein inhibit MCF-7/DOX cell proliferation in vitro.


Keywords


Isolation, Brazilein, Cytotoxic, MCF-7/DOX, Pgp

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About this article

Title

CYTOTOXIC ACTIVITY OF BRAZILEIN ISOLATED FROM SECANG (CAESALPINIA SAPPAN L.) AGAINST MCF7/DOX CELLS BY INHIBITION OF P-GLYCOPROTEIN

Keywords

Isolation, Brazilein, Cytotoxic, MCF-7/DOX, Pgp

DOI

10.22159/ijpps.2017v9i12.19861

Date

01-12-2017

Additional Links

Manuscript Submission

Journal

International Journal of Pharmacy and Pharmaceutical Sciences
Vol 9, Issue 12, 2017 Page: 124-130

Online ISSN

0975-1491

Statistics

15 Views | 4 Downloads

Authors & Affiliations

N. P. Linda Laksmiani
Department of Pharmacy, Faculty of Mathematics and Science, Universitas Udayana, Bali
Indonesia

E. D. Y. Meiyanto
Cancer Chemoprevention Research Center, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta
Indonesia

R. Asmah Susidarti
Cancer Chemoprevention Research Center, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta
Indonesia


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