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All Journal Jurnal Kefarmasian Indonesia Jurnal Bioteknologi & Biosains Indonesia (JBBI) Jurnal Bioteknologi & Biosains Indonesia
Ariyani, Titin
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Agriculture, Biological Sciences & Forestry Biochemistry, Genetics & Molecular Biology Chemistry Environmental Science Health Professions Medicine & Pharmacology

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Sintesis dan Evaluasi Antimalaria In Vitro Turunan Kinin Terhadap Plasmodium falciparum Salahuddin, Salahuddin; K, Rahmana Emran; Hanafi, Muhammad; Sundowo, Andini; NL, Puspa Dewi; Adipratiwi, Nadia; Ariyani, Titin; Prabandari, Erwahyuni Endang; Waluyo, Danang
Jurnal Kefarmasian Indonesia VOLUME 11, NOMOR 2, AGUSTUS 2021
Publisher : Pusat Penelitian dan Pengembangan Biomedis dan Teknologi Dasar Kesehatan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.22435/jki.v11i2.3923

Abstract

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.
TEMPERATURE EFFECTS ON THE STABILITY OF MYCOBACTERIUM TUBERCULO-SIS SHIKIMATE KINASE (MtSK): STRATEGIES FOR SECURE TRANSPORT Wibowo, Aji; Komariyah, Tinta; Prabandari, Erwahyuni Endang; Ariyani, Titin; Siska, Eka
Jurnal Bioteknologi & Biosains Indonesia (JBBI) Vol. 11 No. 1 (2024)
Publisher : BRIN - Badan Riset dan Inovasi Nasional

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.55981/jbbi.2024.5751

Abstract

Mycobacterium tuberculosis Shikimate Kinase (MtSK) has a crucial role in the shikimic pathway, which is essential for this bacteria but is absent in humans, making it a potential target for novel anti-tuberculosis drugs. This study used enzyme-coupled fluorescence to examine the stability of MtSK stored in 50% glycerol at -30 ℃, 4 ℃, and ±28 ℃ for six days. Results showed stable enzyme activity values (α=0.05) at all temperatures. This research underscores that MtSK’s stability depends on its molecular properties, including GC content, hydrophobic residues, Mg2+ binding, and intra-helical salt bridge. Despite some activity decline over time due to glycerol-induced aggregation, MtSK can be safely transported at ±28 ℃ for up to six days without special cooling compartment. Understanding MtSK stability ensures its active conformation remains consistent, reducing off-target effects on drug design and enhancing drug efficacy. This insight ultimately leads to high-quality and commercially viable tuberculosis treatment development. Future research should explore MtSK stability at higher temperatures and assess the optimal glycerol content for cryopreservation.
TEMPERATURE EFFECTS ON THE STABILITY OF MYCOBACTERIUM TUBERCULO-SIS SHIKIMATE KINASE (MtSK): STRATEGIES FOR SECURE TRANSPORT Wibowo, Aji; Komariyah, Tinta; Prabandari, Erwahyuni Endang; Ariyani, Titin; Siska, Eka
Jurnal Bioteknologi & Biosains Indonesia (JBBI) Vol. 11 No. 1 (2024)
Publisher : BRIN - Badan Riset dan Inovasi Nasional

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.55981/jbbi.2024.5751

Abstract

Mycobacterium tuberculosis Shikimate Kinase (MtSK) has a crucial role in the shikimic pathway, which is essential for this bacteria but is absent in humans, making it a potential target for novel anti-tuberculosis drugs. This study used enzyme-coupled fluorescence to examine the stability of MtSK stored in 50% glycerol at -30 ℃, 4 ℃, and ±28 ℃ for six days. Results showed stable enzyme activity values (α=0.05) at all temperatures. This research underscores that MtSK’s stability depends on its molecular properties, including GC content, hydrophobic residues, Mg2+ binding, and intra-helical salt bridge. Despite some activity decline over time due to glycerol-induced aggregation, MtSK can be safely transported at ±28 ℃ for up to six days without special cooling compartment. Understanding MtSK stability ensures its active conformation remains consistent, reducing off-target effects on drug design and enhancing drug efficacy. This insight ultimately leads to high-quality and commercially viable tuberculosis treatment development. Future research should explore MtSK stability at higher temperatures and assess the optimal glycerol content for cryopreservation.
Co-Authors Adipratiwi, Nadia Aji Wibowo Andini Sundowo ERWAHYUNI ENDANG PRABANDARI K, Rahmana Emran Komariyah, Tinta Muhammad Hanafi NL, Puspa Dewi Salahuddin Salahuddin Siska, Eka Waluyo, Danang