Open AccessSintesis dan Evaluasi Antimalaria In Vitro Turunan Kinin Terhadap Plasmodium falciparum
Author(s) -
Salahuddin Salahuddin,
Rahmana Emran K,
Muhammad Farhan Hanafi,
Andini Sundowo,
Puspa Dewi Nl,
Nadia Adipratiwi,
Titin Ariyani,
Erwahyuni Endang Prabandari,
Danang Waluyo
Publication year - 2021
Publication title -
jurnal kefarmasian indonesia
Language(s) - English
Resource type - Journals
eISSN - 2354-8770
pISSN - 2085-675X
DOI - 10.22435/jki.v11i2.3923
Subject(s) - plasmodium falciparum , quinine , chemistry , hydrogen peroxide , ic50 , in vitro , pharmacology , organic chemistry , malaria , biochemistry , biology , immunology
Nowadays kinin is the most effective antimalarial drug and its used as an alternative in malaria treatment. However, toxicity of quinine restrict its use as an antimalarial drug. Lipophilicity and long half-life (t½) of quinine that reach 10-20 hours are responsible for its toxicity. The aim of this research is to obtain more polar quinine derivatives by means of hydrogen peroxide reactions to reduce the toxicity. The reactions using hydrogen peroxyde is performed analogously to the procedures reported in the literature. Extract of pure anhydrous kinin is purified in coloumn chromatography followed by structure elucidation. Synthetic product is tested in vitro against Plasmodium falciparum. The characterization of reaction products is performed with proton (1H) and carbon 13 (13C) nuclear magnetic resonance (NMR) spectroscopy. It showed that the reaction using reagents led to epoxidation of vinyl substituents of chinuclidine ring with 61,08% yields. Antimalarial test against Plasmodium falciparum obtained 1.250-2.500 μg/mL of IC50 value. The IC50 values indicated that the synthesis products were not potential for malaria treatment.