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Sintesis Artemeter dengan Katalis Bifungsional dalam Satu Sistem Reaksi dan Uji Aktivitas Sitotoksik Terhadap Sel Leukimia L1210 LIA NURLIANA; HARMITA HARMITA; SILVESTER S. TURSILOADI; L.B. S KARDONO
JURNAL ILMU KEFARMASIAN INDONESIA Vol 10 No 1 (2012): JIFI
Publisher : Fakultas Farmasi Universitas Pancasila

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Abstract

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.
Fraksinasi Ekstrak Butanolik Kaldu Fermentasi Isolat Kapang Tanah Banjarmasin Biomcc-F.T.3762 Berbasis Uji Aktivitas Penghambatan Dihidroorotat Dehidrogenase Plasmodium falciparum AMILA PRAMISANDI; HARMITA HARMITA; ANIS HERLIYATI MAHSUNAH
JURNAL ILMU KEFARMASIAN INDONESIA Vol 15 No 1 (2017): JIFI
Publisher : Fakultas Farmasi Universitas Pancasila

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Abstract

Butanolic extract of soil fungus BioMCC-F.T.3762 fermentation broth exhibited inhibitory activity against Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH), a fl avin dependent mitochondrial electron transport chain, an essential enzyme in de novo pyrimidine biosynthesis pathway of the parasite. The crude butanolic extract exhibited PfDHODH inhibition of 97% at a concentration of 413 μg/mL, and showed no inhibitory activity against its human homolog. Bioassayguided fractionation was performed on butanolic extract of microbial fermentation broth to isolate the active compounds. The active fraction was isolated using liquid–liquid partition, silica gel column chromatography, octadecylsilane (ODS) column chromatography and was purifi ed by preparative high performance liquid chromatography (HPLC). Major peak of active fractions, FS10-2-12 and FS10-2- 13, were detected by PDA HPLC, which showed a retention time of 12.6 minute and 13.9 minute at 254 nm, respectively. The active fractions exhibited 75% and 40% inhibitory activity against PfDHODH, respectively, at a concentration of 100 μg/mL. In comparison, atpenin A5, a known potent mitochondrial complex II inhibitor exhibited 75% inhibitory activity againts PfDHODH at 366 μg/mL.