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In Silico Screening and Designing Synthesis of Cinchona Alkaloids Derivatives as Potential Anticancer Hanafi, Muhammad; Rosmalena, Rosmalena; Prasasty, Vivitri Dewi; Udin, Linar Zalinar; Primahana, Gian
Journal of Tropical Life Science Vol 7, No 2 (2017)
Publisher : Journal of Tropical Life Science

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.11594/jtls.07.02.06

Abstract

P-glycoprotein (P-gp) resistance in cancer cells decreases intracellular accumulation of various anticancer drugs. This multidrug resistance (MDR) protein can be modulated by a number of non-cytotoxic drugs. We have screened 30 chincona alkaloids derivatives as a potent P-gp inhibitor agent in silico. Hereby, we report the highest potential inhibitions of P-gp is Cinchonidine isobutanoate through molecular docking approach. with affinity energy -8.6 kcal/mol and inhibition constant, Ki is 4.89 x 10-7 M. Cinchonidine isobutanoate is also known has molecular weight below 500, Log P value 3.5, which is indicated violation free of Lipinski`s rule of five. Thus, Cinchonidine isobutanoate is the most potent compound as anticancer compare to other Cinchona alkaloids. Ultimately, we design Cinchonidine isobutanoate for further lead synthesis by using DBSA, act as a combined Brønsted acid-surfactant-catalyst (BASC) to obtain high concentration of organic product by forming micellar aggregates which is very powerful catalytic application in water environment.
Cholestan Steroids from The Stem Bark of Aglaia angustifolia Miq and Their Cytotoxic Activity against MCF-7 Breast Cancer Cell Lines Hutagaol, Ricson Pemimpin; Mozef, Tjandrawati; Fajriah, Sofa; Primahana, Gian; Supratman, Unang; Harneti, Desi; Hidayat, Ace Tatang; Awang, Khalijah; Shiono, Yoshihito
Molekul Vol 18 No 2 (2023)
Publisher : Universitas Jenderal Soedirman

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.20884/1.jm.2023.18.2.6205

Abstract

With about 120 species, Aglaia is one of the largest genera of the plant family Meliaceae (the mahogany plants). Various Aglaia species have been investigated since the 1960s for their phytochemical constituents and biological properties. This research objective was to find secondary metabolites that have activity as anti-breast cancer compounds from endemic Indonesian Aglaia, such as Aglaia angustifolia Miq. Two cholestan type steroids, stigmast-5en-3α-acetat (1), as a new steroid with α-sterochemistry of acetyl moiety at C-3 and 23a-homostigmast-5en-3β-ol (2), with unusual side chain were isolated for the first time from the stem bark of Aglaia angustifolia Miq or known as segara tree in Kalimantan. The chemical structures of two steroids were identified with spectroscopic data, including IR, NMR (1H, 13C, DEPT 135°, HMQC, HMBC, NOESY, 1H-1H COSY) and HRTOF-MS, as well as by comparing with previously reported spectral data. These two steroids were isolated for the first time from this genus. Steroids 1 and 2 were evaluated for cytotoxic activity against MCF-7 breast cancer cells and showed weak activity with IC50 values of 829.0 and 903.0 µg/mL, respectively.
Cytotoxic of Usnic Acid Isolated from Ramalina sp.: Cytotoxic of Usnic Acid Isolated from Ramalina sp. Darmawan, Akhmad; Maulidiyah; Megawati; Ariani, Novita; Aisya, Sitti; Sukirno; Randy, Ahmad; Primahana, Gian; Hendra, Medi; Nurdin, Muhammad
Journal of Tropical Life Science Vol. 14 No. 2 (2024)
Publisher : Journal of Tropical Life Science

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.11594/jtls.14.02.14

Abstract

Ramalina sp. (Ramalinaceae) is a type of lichen known to contain many active secondary metabolite compounds that have the potential to be used as medicine or medicinal raw materials. One of the biological activities possessed by Ramalina sp. lichen is its anticancer activity. This research aims to isolate and identify active secondary metabolite compounds from the methanol extract of the Ramalina sp. lichen and to find out the cytotoxic activity of the isolated compound against MCF7 breast cancer cells. Compound 1 (usnic acid) was successfully isolated from fraction A. The isolation and purification process was carried out starting with a maceration process using acetone solvent, followed by silica gel column chromatography using a gradient solvent system consisting of n-hexane, n-hexane:EtOAc, EtOAc, EtOAc:MeOH, and MeOH with 5% increment of polarity to obtain 17 fractions (F-1 to F-17). From the 17 fractions obtained, fraction 3 (F-3) and fraction 4 (F-4) (eluted with n-hexane:EtOAc 30%), which had the same TLC profile, were combined and named as fraction A. Compound 1 (50 mg) is a yellow needle crystal that was formed in a bottle of fraction A, which was obtained after the process of combining fractions F-3 and F-4 and solvent evaporation process. The crystals were then separated and purified with CHCl3 and MeOH. Compound 1 was then characterized based on spectroscopic data. Various spectroscopic analysis data, including FTIR, 1D- and 2D-NMR, and LC-ESI-MS, show that Compound 1 is a dibenzofuran derivative compound with 18 carbons (3 from carbonyl groups (C=O) and 3 from methyl groups) and 2 hydroxyl (-OH). Cytotoxicity assay showed that at a low concentration of 18.75 ug/mL, Compound 1 caused a 67.06% decrease in MCF7 viability
Antioxidant and Cytotoxic Properties of Extract from Soil Bacteria Isolated from Muna Island, Southeast Sulawesi Priyanto, Jepri Agung; Hening, Egiyanti Nur Widhia; Permatasari, Vera; Prastya, Muhammad Eka; Hasidu, La Ode Abdul Fajar; Primahana, Gian
Jurnal ILMU DASAR Vol 25 No 1 (2024)
Publisher : Fakultas Matematika dan Ilmu Pengetahuan Alam Universitas Jember

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.19184/jid.v25i1.39244

Abstract

Soil bacteria could be the promising source of secondary metabolites with diverse pharmacological activities. Bacteria coded as P1 and M7 were isolated from soil obtained from Muna Island, Southeast Sulawesi. This research aimed to evaluate the antioxidant activity, cytotoxic property, and identify the chemical profile of the extract derived from soil bacteria P1 and M7. Based on 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, extract derived from P1 isolate was moderately active against ABTS free radical with IC50 of 126.22±10.82 µg/mL, and less active on DPPH (IC50: 721.95±16.59 µg/mL), while M7 extract was less active towards DPPH and ABTS. Interestingly, these extracts in the concentration of 100 µg/mL were cytotoxic to breast cancer cell (MCF-7), as tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. MCF-7 viability was decreased up to 69.83±1.46 % and 61.49±0.76 % after treated with P1 and M7 extract, respectively. The extracts were also induced membrane disruption and apoptosis of MCF-7 cells. The extracts contained phenol (9.52±0.22 and 10.41±0.09 mg EAG/g extract, for P1 and M7, respectively) and flavonoids (9.16±0.16 and 9.29±0.24 mg EQ/g extract, for P1 and M7, respectively). According to Gas Chromatography Mass Spectrometry (GC-MS) analysis, Pyrrolo[1,2-a] pyrazine-1,4-dione, hexahydro-3-(2-methylpropyl) that previously well known as antioxidant and cytotoxic compounds, were found in the M7 and P1 extract. This compound may play a vital role in the radical scavenging and cytotoxic properties of P1 and M7 extracts. The results of this study indicate that P1 and M7 extracts could be the potential source of antioxidant and cytotoxic compounds and need to be further developed for pharmaceutical use.
Uji Aktivitas Antibakteri dan Antioksidan dari Metabolit Ekstraseluler Bakteri Endofit Tumbuhan Mahang (Macaranga bancana): Antibacterial and Antioxidant Activity Test of Extracellular Metabolites of Endophytic Bacteria of Mahang Plants (Macaranga bancana) Chang, Helen; Pujiyanto, Sri; Prastya, Muhammad Eka; Primahana, Gian; Yuswan, Apriza; Retnowati, Dwi; Permatasari, Vera
Jurnal Sumberdaya Hayati Vol. 10 No. 4 (2024): 2024
Publisher : Departemen Biologi, Institut Pertanian Bogor

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.29244/jsdh.10.4.190-197

Abstract

The increasing pollution which promotes accumulation of free radicals and a significant number of bacterial resistances to antibiotics have prompted various efforts to search for new sources of bioactive compounds. The aim of this study was to investigate the antibacterial and antioxidant properties of bioactive compounds produced by endophyte bacteria from M. bancana. The most potential bacterial isolate was extracted its active constituents until obatined crude extract and tested using disc diffusion technique and detemined MIC and MBC values. Antioxidant properties using DPPH radicals were performed followed by GC-MS analysis of its crude extract. We obtained that MB3.1 isolate exhibited antibacterial activity against all four tested bacteria including Escherichia coli strain ATCC 8739, Pseudomonas aeruginosa strain ATCC 9027, Staphylococcus aureus strain ATCC 25923, and Bacillus subtilis strain ATCC 6633. The best MIC values of this extract were shown against B. subtilis with an MIC value of 39.06 μg/ml. Further, MB3.1 extract showed a moderate antioxidant activity with an IC50 value of 248.19 μg/ml. GC-MS analysis of MB3.1 extract revealed 10 dominant compounds, including phenylethyl alcohol, benzeneethanol, 4-hydroxy, and tryptophol, which might be responsible for the antibacterial and antioxidant properties.
Evaluation of Antibacterial and Antibiofilm Effects from Soil Streptomyces spp. against Multidrug-Resistant Bacteria Prastya, Muhammad Eka; Simbolon, Sumihartati; Priyanto, Jepri Agung; Hasidu, La Ode Abdul Fajar; Permatasari, Vera; Primahana, Gian; Dewi, Rizna Triana; Kristiana, Rhesi; Suryanti, Erma
HAYATI Journal of Biosciences Vol. 32 No. 1 (2025): January 2025
Publisher : Bogor Agricultural University, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.4308/hjb.32.1.12-26

Abstract

The global increase in multidrug-resistant (MDR) bacterial infection has rapidly gained concern globally. This study aimed to investigate antibacterial and antibiofilm potential of 25 soil actinomycete strains against MDR strains including Escherichia coli strain M4, Pseudomonas aeruginosa strain M19, Klebsiella pneumoniae strain M19, Bacillus subtilis strain M18, and Methicillin Resistant Staphylococcus aureus (MRSA). In this study, three actinomycete isolates encoded APM-7, APM-11, and APM-21 showed a strong and broad antibacterial spectrum. The minimum inhibitory concentration (MIC) of extracts derived from these isolates was ranged from 78 μg/ml to 10,000 μg/ml. In addition, The extracts also displayed significant biofilm inhibition values ranging from 6.06 to 72.4%. Based on the results, APM-21 extract had the best antibacterial and antibiofilm activities with the strongest values against MRSA. According to the nucleotide sequencing of the 16S rRNA gene, APM-7, APM-11, and APM-21 strains possessed similar identities with Streptomyces cyaneus, Streptomyces coerulescens, and Streptomyces panayensis, respectively. Based on Liquid Chromatography Tandem-Mass Spectrometry (LC-MS/MS) analysis, two antibacterial compounds, namely rancimanycin III, and enteromycin were detected in all those three extracts. Interestingly, APM-21 extract also contained two prominent antibacterial substances including paramagnetoquinone C, and caerulomycin I, suggesting their contribution to the most potential activities. Moreover, new insights were provided into a promising candidate for use in an active compound combating strategy to control MDR bacterial strain infection.
Antioxidant Activity and Phenolics of Kabau (Archidendron bubalinum) Pod Peel Extract from East Lampung on Blood Cell Male Mice Induced by Cadmium Riana, Elisa Nurma; Prastya, Muhammad Eka; Primahana, Gian; Anisa, Hida Arliani Nur; Khairani, Iffa Afiqa; Imaniar, Lisana Husna
Jurnal Ilmu Pertanian Indonesia Vol. 30 No. 2 (2025): Jurnal Ilmu Pertanian Indonesia
Publisher : Institut Pertanian Bogor

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.18343/jipi.30.2.353

Abstract

Cadmium (Cd) increases oxidative stress, which increases the likelihood of health problems. To protect the body from oxidative stress, natural antioxidants obtained from plants are required. The kabau plant (Archidendron bubalinum) is thought to have antioxidant phytochemicals. The purpose of this study was to assess the antioxidant activity and total phenolic component content of kabau pod peels, as well as their effect on the quantity of erythrocytes and leukocytes in male mice exposed to cadmium. This study used a completely randomized design, with 24 mice divided into six groups: three control groups and three treatment groups. The findings of assessing the antioxidant activity of peel extract revealed that the IC50 was 93.6 ppm, which is considered strong. The phenolic content of peel extract was 72.26 mg GAE/g. Giving pod peel extract to mice increased the number of erythrocytes and leukocytes, however the impact was not significant (p = 0.028 and P = 0.239). Mice with 380 mg/kg BW produced better outcomes. Keywords: antioxidant, Archidendron, blood cell, kabau, phenolics
Parameter kemunduran mutu sebagai indikator pembeda asal formaldehida pada ikan opah selama penyimpanan suhu chilling: Quality deterioration parameters as a differentiating indicator of formaldehyde origin in moonfish during chilling temperature storage Fikriyah, Annisaa Nurul; Nurjanah, Nurjanah; Nurhayati, Tati; Primahana, Gian; Barokah, Giri Rohmad
Jurnal Pengolahan Hasil Perikanan Indonesia Vol 27 No 10 (2024): Jurnal Pengolahan Hasil Perikanan Indonesia 27(10)
Publisher : Department of Aquatic Product Technology IPB University in collaboration with Masyarakat Pengolahan Hasil Perikanan Indonesia (MPHPI)

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.17844/jphpi.v27i10.56765

Abstract

Ikan opah (Lampris guttatus) merupakan salah satu jenis ikan laut yang mengandung kadar formaldehida alami cukup tinggi. Hal tersebut menjadi hambatan utama karena disebabkan oleh pendeteksian formaldehida alami dan formaldehida artifisial yang ditambahkan. Pembusukan pada ikan dapat mengakibatkan pembentukan formaldehida secara alami melalui reduksi enzimatik trimetilamina oksida (TMAO), yang mengarah pada pembentukan produk sampingan, yaitu formaldehida dan dimetilamina (DMA). Penelitian ini bertujuan menentukan indikator pembeda antara formaldehida alami dan artifisial berdasarkan parameter kemunduran mutu pada ikan opah selama 14 hari penyimpanan suhu chilling. Penelitian ini menggunakan rancangan acak lengkap faktorial (RALF) dengan perlakuan penambahan konsentrasi formaldehida 0, 2 dan 4% serta waktu penyimpanan selama 14 hari. Parameter yang diamati, yaitu pH, total volatile base (TVB), formaldehida (FA), dan dimetilamina (DMA). Hasil penelitian menunjukkan bahwa konsentrasi formaldehida 0% memiliki nilai yang berbeda nyata dengan konsentrasi lainnya. Formaldehida (FA) dapat menjadi indikator kuat sebagai pembeda asal formaldehida pada ikan. Parameter lain, yaitu pH, TVB dan DMA tidak dapat dijadikan sebagai indikator tunggal, tetapi kombinasi keempat parameter kemunduran mutu dapat digunakan sebagai indikator kuat pembeda asal formaldehida pada ikan opah.
Antiplasmodial and Metabolite Profiling of Hyrtios sp. Sponge Extract from Southeast Sulawesi Marine Using LC-HRMS, Molecular Docking, Pharmacokinetic, Drug-likeness, Toxicity, and Molecular Dynamics Simulation Pulung, Maria Ludya; Swasono, Respati Tri; Sholikhah, Eti Nurwening; Yogaswara, Radite; Primahana, Gian; Raharjo, Tri Joko
Journal of Multidisciplinary Applied Natural Science Vol. 5 No. 2 (2025): Journal of Multidisciplinary Applied Natural Science
Publisher : Pandawa Institute

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.47352/jmans.2774-3047.259

Abstract

Hyrtios sponge is known to possess alkaloid compounds that may exhibit in vitro activity against Plasmodium falciparum. The aim of this study was therefore to isolate and characterise the antiplasmodial active compounds of Hyrtios sp. Sponges collected from the island of Podang-Podang, South Sulawesi, Indonesia. In addition, the LC-HRMS analysis was performed on the active fractions of methanol and ethyl acetate extract to evaluate their antiplasmodial activity. We also validated the in silico antiplasmodial activity of PfDHFR-TS with molecular docking, pharmacokinetics, drug likeness, toxicity, and molecular dynamics analysis. The molecular docking studies showed that the synthesized extremes would have high binding affinity to PfDHFR-TS, thus confirming their potential as powerful enzyme inhibitors. Moreover, the pharmacokinetic and drug-likeness calculations showed that all compounds met the requirements for sufficient resistance and bioavailability, indicating potential as therapeutic candidates. The results of the toxicity analysis indicated that the compounds had a relatively good safety profile, but some potential adverse reactions in the renal and cardiac vasculature could not be excluded. Molecular dynamics simulations confirmed that the complexes formed between the ligand and the target were stable, and the low RMSD value indicated that the active site interactions were also quite stable. These observations reinforce the notion that the extract from Hyrtios sp. not only shows remarkable antimalarial activity but also exhibits pharmacological properties of a prospective drug candidate, which encourages further work in the development of malaria combination therapy both in clinical assessment and comprehensive mechanism of action investigation.
Potensi Aktivitas Antibakteri dan Antioksidan dari Senyawa Bioaktif Bakteri Tanah Asal Samarinda, Kalimantan Timur: The Antibacterial and Antioxidant Potential of Bioactive Metabolites from Soil-Derived Bacteria in Samarinda, East Kalimantan Atwita, Syelziva Yonda; Malau, Jekmal; Permatasari, Vera; Primahana, Gian; Dewijanti, Indah D.; Yuswan, Apriza; Prastya, Muhammad Eka
Jurnal Sumberdaya Hayati Vol. 11 No. 2 (2025): 2025
Publisher : Departemen Biologi, Institut Pertanian Bogor

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.29244/jsdh.11.2.63-73

Abstract

Antibiotic resistance is a global challenge, especially in the treatment of bacterial infections. This study aims to explore the antibacterial and antioxidant potential of bioactive compounds isolated from soil bacteria in Samarinda, East Kalimantan. Of the 30 isolates tested, 1 potential isolate was obtained, namely isolate code T1.16. This potential bacterial isolate was further cultured and fermented in Tryptic Soybean and Luria Bertani Broth medium to obtain its crude secondary metabolite. Interestingly, its crude extract showed antibacterial activity with MIC values of 100.4-3,211 µg/ml against Escherichia coli strain ATCC 8739, Pseudomonas aeruginosa strain ATCC 9027, Bacillus subtilis strain ATCC 6633, and Staphylococcus aureus strain ATCC 25923. Based on 1,1-diphenyl-2-picrylhydrazyl (DPPH) method was used to identify antioxidant activity, IC50 values obtained ranged from 990-1730 µg/ml. Ultimately, by using Gas Chromatography Mass Spectrometry (GC-MS) analysis, bioactive compounds in the form of Cyclo(L-prolyl-L-valine), 2-methylpropyl and phenylmethyl in bacterial extract T1.16 have potential antioxidant and antibacterial bioactivities. These results support the potential development of new antibacterial and antioxidant compounds from soil bacteria, as well as the importance of further exploration for pharmacological applications.