Synthesis of Artemether by Bifungtional Catalyst in One Pot Reaction System and Cytotoxocity Test Against L1210 Leukemia Cells
Artemisinin has been known as herbal medicine from China, which was isolated from the Artemisia annua L. plant. Artemisinin was originally known as antipyretic and antimalarial drug. Artemisinin and its derivatives also have potential as anticancer, due to the sesquiterpene lactone containing a unique peroxide group. This study aimed to modify the structure of artemisinin into artemether using solid catalyst Ni/TiO2-SO4 through the hydrogenation and methylation of the alcohol group in one pot reaction system. The product was then investigated for its cytotoxic activity against L1210 leukemia cells. The solid catalyst in this study was composed of metalic Ni as the active center, TiO2 as a catalyst support and sulphate as the promoter. The modification of artemisinin produced 1.29% artemether white crystalls as a minor product, and 19% dihidroartemisinin as an intermediate compound. The synthesized artemether showed an anticancer activity against L1210 leukimia cells with IC50 value of 3.07 µg / mL. The result suggests that the synthesized artemether has a potency as an anticancer.
2. Tang W and Eisenbrand. Chinese drug of plant origin: Chemistry pharmacology and use in traditional and modern medicine: Artemisia annua. Springer Verlag; 1992. 159-71.
3. Purwantiningsih. Artemisinin dari Artemisia saccarum, Ledep dan Turunannya Sebagai Komponen Bioaktif Antimalaria. FMIPA Kimia IPB. [karya utama doktor kimia]. 2003.
4. Lai H and Singh NP. Selective cancer cell cytotoxicity from exposure to dihydroartemi sinin and holotransferrin. Cancer Letter. 1995. 91:41-6.
5. Klayman DL, Lin AJ, Acton N, et al. Isolation of artemisinin (Qinghaosu) fromArtemisia annua growing in the United States. J Natural Products. 1984. 47(4):715-7.
6. Klayman DL. Qinghaosu (Artemisinin): an antimalarial drug from China. Science Direct. 1985. 228:1054-94.
7. Li Y, Yuan-Ming Zhu, Hong-Jian Jiang, Jian Ping Pan, Guang Shao Wu, and Jin-Ming Wu. Studies on artemisinine analogs. I. synthesis of ether, Carboxylates and carbonates of dyhidroartemisinine. Acta Pharm Sin. 1981. 16:429-39.
8. Lin AJ, Klayman DL, Milhous WK. (1987). Antimalarial activity of new water soluble dyhidroartemisinin derivatives. J Med Chem. 1987. 30:2147-50
9. Lin AJ, Lee M, Klayman DL. Antimalarial Activity of New Water Soluble Dihydroarte misinin Derivatives and stereospecificity of the ether side chain. J Med Chem. 1989. 32:1249-52
10. Jenie SA. Sintesa nanomaterial katalis super asam untuk sistem satu reaktor (One Pot System) siklisasi dan hidrogenasi. Laporan Penelitian LIPI-Serpong. 2009.
11. Laksono AJ. Sintesa Nano Material Katalis Super Asam untuk Sistem Satu-Reaktor (One Pot System) Siklisasi dan Hidrogenasi. Laporan Penelitian LIPI-Serpong. 2008.
12. Lin AJ . Antimalarial activity of new dihydro artemisinin derivatives. 6. a alkylbenzylic ethers. J Med Chem. 1995. 38:764-70.
13. Meyer BN, Ferrigni NR, Putnam JE, Jacobsen LB, Nichols DE, McLaughlin JL. Brine shrimp: a convenient general bioassay for active plant constituents. Planta Medica. 1982. 45:31-4.
14. Sumatra M. Bioassai in vitro dengan sel leukimia L1210, sebuah metode skrining zat anti tumor dari bahan alam. Prosiding Seminar Bioteknologi Kelautan Indonesia. Jakarta. 1998. 183-4.
15. Wang, et al. Analysis of artemisinin in Artemisia annua L. by LC MS With selected ion monitoring. J Agric Food Chem. 2005. 53: 7010-3.
Copyright @2017. This is an open-access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License (http://creativecommons.org/licenses/by-nc-sa/4.0/) which permits unrestricted non-commercial used, distribution and reproduction in any medium
This work is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License.