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All Journal Jurnal Kefarmasian Indonesia Jurnal Bioteknologi & Biosains Indonesia
Waluyo, Danang
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Biochemistry, Genetics & Molecular Biology Chemistry 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.
EVALUATION AND INHIBITORY MECHANISM ANALYSIS OF NATURAL COMPOUNDS AGAINTS DIHYDROOROTATE DEHYDROGENASE AS ANTI-CANCER AGENTS Wibowo, Aji; Waluyo, Danang; Tejo, Bimo Ario; Komariyah, Tinta; Besari, Ariza Yandwiputra; Prabandari, Erwahyuni Endang
Jurnal Bioteknologi & Biosains Indonesia (JBBI) Vol. 10 No. 2 (2023)
Publisher : BRIN - Badan Riset dan Inovasi Nasional

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.55981/jbbi.2023.2842

Abstract

Cancer remains one of the deadliest diseases worldwide, and currently cancer treatment is facing several problems related to adverse effects and drug resistance. To address these problems, new prospective anticancer medications are required. Natural compounds, which have been extensively used in the drug research, including for the treatment of cancer, are emerging as viable candidates. This study aimed to evaluate 33 in-house natural compounds against dihydroorotate dehydrogenase (DHODH) enzyme, a viable target to develop anticancer agent, and to analyze the hit inhibitory mechanism against protein target. In the activity assay, atovaquone was the sole substance to have activity against DHODH, with an inhibition rate of 47.44% at 10 µM. However, discrepancies were shown in the molecular docking result, where atovaquone were identified as hits. Molecular dynamic analysis revealed that atovaquone initially bound to the active site before being forced to the outside due to cleavage of hydrogen bond between the ligand and responsible residue. This study clearly demonstrated the importance of molecular dynamic analysis to study inhibitory mechanism of compound against target protein that may be useful for further development.
INHIBITORY ACTIVITY OF INDONESIAN MICROBIAL EXTRACTS AGAINST PROLIFERATION OF DLD-1 COLORECTAL CANCER CELL LINE Besari, Ariza Yandwiputra; Waluyo, Danang; Komariyah, Tinta; Prabandari, Erwahyuni Endang
Jurnal Bioteknologi & Biosains Indonesia (JBBI) Vol. 10 No. 1 (2023)
Publisher : BRIN - Badan Riset dan Inovasi Nasional

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.55981/jbbi.2023.2851

Abstract

Colorectal cancer (CRC) is the second deadliest cancer in the world. Several anti-cancer agents are currently used for the clinical treatment of CRC. However, toxicity and drug resistance pose significant challenges in CRC chemotherapy. On the other hand, microbe-derived natural products have been explored as a source for the development of anti-cancer therapeutic agents. This study aimed to examine the potential of the microbial library in BioMCC (Biotech Center-BPPT Microbial Culture Collection) as a source for anti-cancer drug discovery. Among the 720 fungal extracts tested, 60 extracts (8.3%) showed inhibitory activity against the proliferation of the colorectal carcinoma DLD-1 cell line, while not affecting Vero cells (African green monkey kidney normal cell line). One of these active extracts was derived from the fungus Sporothrix sp. BioMCC-f.T.7716. Although the inhibitory mechanism of this extract against the proliferation of the DLD-1 cell line could not be determined, this study clearly demonstrated the potential use of Indonesian microbial extracts as a source for the discovery of anti-cancer agents.
Co-Authors Adipratiwi, Nadia Aji Wibowo Andini Sundowo Ariyani, Titin Ariza Yandwiputra Besari, Ariza Yandwiputra ERWAHYUNI ENDANG PRABANDARI K, Rahmana Emran Komariyah, Tinta Muhammad Hanafi NL, Puspa Dewi Salahuddin Salahuddin Tejo, Bimo Ario