Perbandingan Afinitas Kurkumin-enol dan Kurkumin-keto terhadap Reseptor COX-2 (Comparisons of Affinity between Curcumin-Enol and Curcumin-Keto Towards COX-2 Receptor)

Proceedings of the National Seminar of Health Sciences SNIK 2016

6 Pages Posted: 9 Aug 2017 Last revised: 7 Dec 2017

Date Written: September 1, 2016

Abstract

Indonesian Abstract: Kurkumin selain dikenal memiliki aktivitas sebagai hepatoprotektor juga diketahui memiliki aktivitas sebagai analgetik. Aktivitas analgetik kurkumin dihubungkan dengan potensi sebagai inhibitor jalur metabolisme asam arakidonat. Salah satu komponen penting pada jalur asam arakidonat adalah enzim siklooksigenase (COX), dimana inhibisi pada COX-2 diketahui memiliki efek lebih signifikan terhadap aktivitas analgetik suatu senyawa. Kurkumin merupakan rasemat dengan dua bentuk aktif yaitu bentuk –enol dan –keto. Penelitian ini bertujuan untuk membandingkan afinitas masing-masing bentuk aktif kurkumin terhadap COX-2. Metode yang digunakan adalah docking dengan kurkumin-keto memberikan energi bebas ikatan paling negatif dan konstanta inhibisi paling kecil, secara berturut-turut yaitu -8,45 kcal/mol dan 642,19 nM. Bentuk –keto pada kurkumin memberikan afinitas hampir 2 kali lipat lebih tinggi dibandingkan bentuk –enol pada kurkumin. Hasil tersebut memberikan prediksi bahwa untuk meningkatkan aktivitas analgetik kurkumin sebagai inhibitor COX-2 dapat dilakukan dengan meningkatkan perbandingan bentuk –keto dari kurkumin.

English Abstract: Curcumin other than known to have activity as a hepatoprotector is also known to have activity as an analgesic. Curcumin analgesic activity is associated with potential as an inhibitor of arachidonic acid metabolism pathway. One important component of the arachidonic acid pathway is the cyclooxygenase enzyme (COX), in which COX-2 inhibition is known to have a more significant effect on the analgesic activity of a compound. Curcumin is a racemate with two active forms of the -enol and -keto forms. This study aimed to compare the affinity of each of the active forms of curcumin to COX-2. The method used is docking with curcumin-keto provides the most negative free energy of binding and the smallest inhibitory constant, respectively -8.45 kcal/mol and 642.19 nM. The -keto form of curcumin gives an affinity almost 2 times higher than that of the -enol form Curcumin. These results provide predictions that to increase curcumin analgesic activity as COX-2 inhibitors can be done by increasing comparison of the -keto form of curcumin

Note: Downloadable document is in Indonesian.

Keywords: COX-2, Docking, Curcumin-Enol, Curcumin-Keto

Suggested Citation

Pratama, Mohammad Rizki Fadhil, Perbandingan Afinitas Kurkumin-enol dan Kurkumin-keto terhadap Reseptor COX-2 (Comparisons of Affinity between Curcumin-Enol and Curcumin-Keto Towards COX-2 Receptor) (September 1, 2016). Proceedings of the National Seminar of Health Sciences SNIK 2016. Available at SSRN: https://ssrn.com/abstract=3007728

Mohammad Rizki Fadhil Pratama (Contact Author)

Universitas Muhammadiyah Palangkaraya ( email )

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

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

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