Potential Anticancer Activity of Caesalpinia sappan Linn., in Silico and In Vitro Studies
Abstract
The bark of Caesalpinia sappan Linn. has been used in Indonesian traditional medicine for long time. Current studies on plant chemistry reveal the compound of the bark of CS. Among other compounds, Brazillin is the major flavonoid constituent of Caesalpinia sappan Linn. This paper aimed to report a in silico study of Brazillin molecule for its capacity to activate Adenosine Monophosphate Activated Kinase (AMPK) and a in vitro
study to examine anticancer potential of methanolic extract of the bark of Caesalpinia sappan Linn against breast adenocarcinoma cell line MCF-7. Molecular docking was conducted using AutoDockVina software. The antiproliferative activity was examined with MTT assay. Furthermore, the activity of MeOH extract to induce apoptosis was examined using PI-Annexin V assay. The docking result showed that ’ activates the γ subunit of AMPK with the docking score on Asp89, Asp244, Asp316 were -7.5 Kal/mol, -8.3 Kal/mol, and -8.6 Kal/mol, respectively. Activation of AMPK exerts antiproliferative effect toward actively dividing cells through inhibition of mTOR complex molecule. The IC50 of the extract toward MCF-7 cells growth was 48 μg/ml. The flowcytometry
analysis showed that MeOH extract of Caesalpinia sappan Linn induced apoptosis of MCF-7 cell. In conclusion, MeOH extract of Caesalpinia sappan Linn showed a potential inhibition activity toward MCF-7 proliferation. Further study to justify the anticancer mechanism of methanolic extract of Caesalpinia sappan Linn. is required.
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