AKAR KUNING (Arcangelisia flava) SEBAGAI INHIBITOR EGFR : KAJIAN IN SILICO

Mohammad Rizki Fadhil Pratama

Sari


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.
Keyword : Akar Kuning, EGFR, Antikanker, Docking

Teks Lengkap:

PDF (English)

Referensi


Bissantz, C., Folkers, G., Rognan, D. 2000. Protein-base Virtual Screening of Chemical Databases : Evaluation of Different Docking/Scoring Combinations. J. Med. Chem. 43, 4759-4767.

Ciardiello, F., Tortora, G. 2001. Review : A Novel Approach in The Treatment of Cancer : Targeting the Epidermal Growth Factor Receptor. Clin. Cancer Res. 7, 2958-2970.

Cosconati, S., Forli, S., Perryman, A.L., Harris, R., Goodsell, D.S., Olson, A.J. 2010. Virtual Screening with AutoDock : Theory and Practice. Exp. Op. Drug. Disc. 5(6). 597-607.

Hanahan, D., Weinberg, R.A. 2011. Review : The Hallmark of Cancer : The Next Generation. Cell. 144, 646-674.

Incorvati, J.A., Shah, S., Mu, Y., Lu, J. 2013. Targeted Therapy for HER2 Positive Breast Cancer. J. Hematol. Oncol. 6(38), 1-9.

Jorissen, R.N., Walker, F., Pouliot, N., Garrett, T.P.J., Ward, C.W., Burgess, A.W. 2003. Epidermal Growth Factor Receptor : Mechanisms of Activation and Signalling. Exp. Cell. Res. 284, 31-53.

Kaharap, A.D., Mambo, C., Nangoy, E. 2016. Uji Efek Antibakteri Ekstrak Batang Akar Kuning (Arcangelisia flava Merr) terhadap Bakteri Staphylococcus aureus dan Escherichia coli. Jurnal e-Biomedik. 4(1).

Keawpradub, N., Dej-adisai, S., Yuenyongsawad, S. 2005. Antioxidant and cytotoxic activities of Thai medicinal plants named Khaminkhruea : Arcangelisia flava, Coscinium blumeanum and Fibraurea tinctoria. Songklanakarin J. Sci. Technol. 27, 455-467.

Kim, R., Skolnick, J. 2008. Assesment of Programs for Ligand Binding Affinity Prediction. J. Comput. Chem. 29(8), 1316-1331.

Kontoyianni, M., McClellan, L.M., Sokol, G.S. 2004. Evaluation of Docking Performance : Comparative Data on Docking Algorithms. J. Med. Chem. 47(3), 558-565.

Kunii, T., Kagei, K., Kawakami, Y., Nagai, Y., Nezu, Y., Sato, T. 1985. Indonesian Medicinal Plants. I. New Furanoditerpenes from Arcangelisa flava MERR. (1). Chem. Pharm. Bull. 33(2), 479-487.

Larisu, M.A., Sudarsono, Iravati, S., Nurrochmad, A. 2010. Kajian Ilmiah Air Rebusan Katola (Arcangelisia flava L Merr) Obat Diare Berdarah Masyarakat Kabupaten Muna Sulawesi Tenggara. Indonesian J. Pharm. 21(4), 283-289.

Lovin, E.R., Arwati, H., Ramadhani, R.B. 2012. In Vitro Intraerythrocytic Antimalarial Activity of Akar Kuning (Arcangelisia flava (L) Merr) Stem Aqueous Extract in Plasmodium falciparum. Folia Medica Indonesiana. 48(3), 90-95.

Maryani, Marsoedi, Nursyam, H., Maftuch. 2013. The Phytochemistry and The Anti-bacterial Activity of Yellow Root (Arcangelisia flava Merr) against Aeromonas hydrophila. Journal of Biology and Life Science. 4(2), 180-190.

Mohammad Rizki Fadhil Pratama 2016

Farmagazine Vol. 3 No. 1 Februari 2016 16

Morris, G.M., Huey, R., Lindstrom, W., Sanner, M.F., Belew, R.K., Goodsell, D.S., Olson, A.J. 2009. Autodock 4 and AutoDockTools 4 : Automated Docking with Selective Receptor Flexibility. J. Comput. Chem. 30(16), 2785-2791.

O’Boyle, N., Banck, M., James, C.A., Morley, C., Vandermeersch, T., Hutchison, G.R. 2011. Open Babel : An Open Chemical Toolbox. J. Cheminform. 3(33).

Pratama, M.R.F. 2015. Molecular Docking of Anticancer Agents : Artemisinins and Derivatives as HER2 inhibitor. In Prociding 1st Sari Mulia International Conference on Health and Science 2015. SMICHS 2015. Stikes Sari Mulia. Banjarmasin. 155-168.

Puspitasari, E., Pangaribowo, D.A., Isparnaning, I.Y., Utami, Y. 2015. Ethanolic Extract of Arcangelisia flava Leaves is and Selective against Breast and Colon Cancer Cell Lines. In Prociding The 1st University of Muhammadiyah Purwokerto – Pharmacy International Conference 2015. University of Muhammadiyah Purwokerto. Purwokerto. 82-86.

Rothschild, S.I. 2015. Review : Targeted Therapies in Non-Small Cell Lung Cancer – Beyond EGFR and ALK. Cancer. 7(2), 930-949.

Tiara, A., Arief, R.H., Sudarsono. 2014. The Antidepressant Effects of (Arcangelisia flava Merr) Water-Soluble Extract in Balb-C Mice Reviewed from Immobility Time by Forced. Biology, Medicine, & Natural Product Chemistry. 3(2), 65-57.

Setyowati, R., Sudarsono, Setyowati, E.P. 2014. The Effect of Water-soluble Stem Extract “Kayu Kuning” (Arcangelisia flava L Merr) on The Growth Inhibition of Candida albicans ATCC 10231 and Trichophyton mentagrophytes In Vitro. Biology, Medicine, & Natural Product Chemistry. 3(1), 17-22.

Subiandono, E., Heriyanto, N.M. 2009. Kajian Tumbuhan Obat Akar Kuning (Arcangelisia flava Merr) di Kelompok Hutan Gelawan, Kabupaten Kampar, Riau. Buletin Plasma Nutfah. 15, 43-44.

Sun, Y., Xun, K., Wang, Y., Chen, X. 2009. A Systematic Review of The Anticancer Properties of Berberine, a Natural Product from Chinese Herbs. Anticancer Drugs. 20, 757-769.

Wahyudi, L.D., Ratnadewi, A.A.I., Siswoyo, T.A., 2016. Potential Antioxidant and Antidiabetic Activities of Kayu Kuning (Arcangelisia flava). In Prociding International Conference on Food, Agriculture and Natural Resources, IC-FANRes 2015. Universitas Jember. Jember. 396-402.

Widi, R., Indriati, T. 2007. Penjaringan dan Identifikasi Senyawa Alkaloid dalam Batang Kayu Kuning (Arcangelisia flava Merr). Jurnal Ilmu Dasar. 8(1), 24-29.

Wongbutdee, J. 2009. Review Article : Physiological Effects of Berberine. The Pharmaceutical and Health Science Journal. 4(1). 78-83.


Refbacks

  • Saat ini tidak ada refbacks.