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[Akar Kuning (Arcangelisia Flava) Sebagai Inhibitor EGFR : Kajian in Silico] (Akar Kuning (Arcangelisia Flava) As EGFR Inhibitor : In Silico Study)

Jurnal Farmagazine, Vol. 3, No. 1 (February 2016)

11 Pages Posted: 23 Aug 2017  

Mohammad Rizki Fadhil Pratama

Muhammadiyah University of Palangkaraya

Date Written: February 1, 2016

Abstract

Indonesian Abstract: [Akar kuning (Arcangelisa flava) diketahui memiliki berbagai aktivitas farmakologi seperti antikanker. Beberapa metabolit sekunder akar kuning menunjukkan aktivitas antiproliferasi sel kanker. Overproliferasi pada sel kanker salah satunya disebabkan oleh kelainan pada EGFR, kelompok reseptor yang berperan pada saat inisiasi proliferasi sel. Inhibisi pada EGFR dapat menghambat proses proliferasi sel kanker. Penelitian ini bertujuan mengetahui metabolit sekunder dari akar kuning dengan potensi paling besar sebagai inhibitor berbagai EGFR. Metode yang digunakan adalah molecular docking beberapa metabolit sekunder akar kuning terhadap EGFR-1, EGFR-2, EGFR-3, dan EGFR-4. Hasil docking menunjukkan berberin memberikan energi bebas ikatan paling negatif dan konstanta inhibisi paling kecil pada seluruh EGFR, dengan afinitas paling tinggi ditunjukkan pada EGFR-2 dengan ΔG dan ki secara berturut-turut sebesar -9,34 kcal/mol dan 141,81 nM. Over-ekspresi aktivitas dari EGFR-2 sendiri seringkali terjadi pada kanker payudara, terutama kanker payudara HER2-positif. Hasil tersebut memberikan prediksi bahwa berberin memiliki aktivitas sebagai inhibitor EGFR terutama EGFR-2 dan berpotensi untuk dikembangkan pada terapi kanker payudara HER2-positif.]

English Abstract: Akar kuning (Arcangelisia flava) was known for having several pharmacologic activities including as anticancer. Several secondary metabolites of akar kuning shown antiproliferative activity towards cancer cells. Cancer cells over-proliferation was caused by abnormalities of EGFRs, a group of receptors that playing roles in the initiation of cell proliferation. EGFRs inhibition could inhibit cancer cells proliferation process. The present study aims to determine the most potent secondary metabolites of akar kuning as several EGFRs inhibitors. Molecular docking was performed on several secondary metabolites against EGFR-1, EGFR-2, EGFR-3, and EGFR-4. Docking results show that berberine provided most negative free energy of binding and lowest inhibition constant towards all EGFRs, with the highest affinity was shown toward EGFR-2 with ΔG and ki -9.34 kcal/mol and 141.81 nM, respectively. Over-expression activity of EGFR-2 often occurrs in breast cancer, especially HER2-positive breast cancer. This results predicted that berberine has activity as EGFR inhibitor especially EGFR-2 and should be potential to be developed as HER2-positive breast cancer therapy.

Notes: Downloadable document is available in Indonesian.

Keywords: Akar Kuning, EGFR, Anticancer, Docking

Suggested Citation

Pratama, Mohammad Rizki Fadhil, [Akar Kuning (Arcangelisia Flava) Sebagai Inhibitor EGFR : Kajian in Silico] (Akar Kuning (Arcangelisia Flava) As EGFR Inhibitor : In Silico Study) (February 1, 2016). Jurnal Farmagazine, Vol. 3, No. 1 (February 2016). Available at SSRN: https://ssrn.com/abstract=3023163

Mohammad Rizki Fadhil Pratama (Contact Author)

Muhammadiyah University of Palangkaraya ( email )

RTA Milono Street Km. 1.5
Palangka Raya, Central Borneo 73111
Indonesia

HOME PAGE: http://www.umpalangkaraya.ac.id

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