In Vivo Antimalarial Test of Artocarpin and in vitro Antimalarial Test of Artonin M Isolated from Artocarpus

Suhartati, Tati; Epriyanti, Eka; Borisha, Inggit; Yandri,; Suwandi, Jhons Fatriyadi; Yuwono, Suripto Dwi; Qudus, Hardoko Insan; Hadi, Sutopo

doi:10.37358/rc.20.5.8150

Cited by 9 publications

(6 citation statements)

References 12 publications

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“…The results of fractionation with the VLC process showed that a separation was present between semi-polar components and non-polar components, resulting in seven combined fractions, namely E21 (fr.1-10; 23 mg), E22 (fr.11; 439.5 mg), E23 (fr.12; 1,336 mg), E24 (fr.13), E25 (fr.14-15), E26 (fr. [16][17][18][19], E27 (fr.20-23; 1,675 mg). All these fractions were screened for antibacterial activity using the agar diffusion method, and the results obtained were tabulated in Table 3.…”

Section: Resultsmentioning

confidence: 99%

“…According to their chemicals profile analyzed by TLC and their proton NMR spectrum, these fractions were grouped and combined into seven primary fractions, E21 (fr.1-10), E22 (fr.11), E23 (fr.12), E24 (fr.13), E25 (fr.14-15), E26 (fr. [16][17][18][19], E27 (fr.20-23) (Figure 2). All fractions E21-E27 were tested for their antibacterial property separately using disc diffusion and microdilution methods.…”

Section: Bioassay-guided Separation Of Ethyl Acetate Extractmentioning

confidence: 99%

“…The search for antibiotic sources from natural ingredients is still the main trend for researchers. The ability of bioactive compounds of natural materials as a healing medium is estimated because of the content of secondary metabolites, including terpenoids, steroids, coumarin, flavonoids, and alkaloids (10)(11)(12)(13)(14)(15)(16)(17)(18).…”

Section: Introductionmentioning

confidence: 99%

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Bioassay-Guided Separation Approach for Characterization of New Antibacterial Fractions from the Stem Roots Extracts of Archidendron jiringa

Noviany

Dicky

Andi

et al. 2021

Journal of the Turkish Chemical Society Section A: Chemistry

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Infectious diseases caused by bacteria has become a global health issue, especially antibacterial drug resistance. The most serious concern with antibacterial resistance is that some bacteria became resistant to almost all antibacterial drugs, which makes them less effective. Archidendron jiringa is one of the most potent medicinal plants to be developed as a new source of antibacterial components. In current study, based on the antibacterial assay-guided approach, the separation of bioactive fractions of A. jiringa stem roots was carried out through several stages including isolation, fractionation, and characterization. The stages of isolation of secondary metabolites were conducted by gradually extraction followed by fractionation using chromatographic methods. The antibacterial potential of extracts was evaluated by the disc diffusion and microdilution methods employing the resazurin assay against one Gram-negative resistant bacteria, Escherichia coli, and one Gram-positive bacteria, Bacillus subtilis. Among three extracts obtained, ethyl acetate and methanol extracts demonstrated to be the most significant antibacterial effects, while no antibacterial activity was shown on the n-hexane extract. The fractionation of ethyl acetate extract led to the isolation of the most bioactive fractions (E2815 and E2816) with the MIC's values ranging of 12.5-25 µg/mL for both resistant bacteria. Due to the low amount, only the fraction E2816 was subjected to analysis by 1 H-NMR spectroscopy. The results exhibited that the bioactive fraction was obtained as a mixture of at least three major constituents. However, the purification of the bioactive fraction is required, to further clarify the antibacterial compound that can be utilized as a new promising antibacterial agent. The bioassay-guided separation approach and the dye resazurin as an indicator of the growth of bacteria are applied for the first time for the phytopharmacological investigation from this plant. The present study represented the most effective method for subsequent finding and isolation of potential novel antibacterial constituents from A. jiringa stem roots, in particular against the multi-drug resistant strains.

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Section: Resultsmentioning

confidence: 99%

Section: Bioassay-guided Separation Of Ethyl Acetate Extractmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Bioassay-Guided Separation Approach for Characterization of New Antibacterial Fractions from the Stem Roots Extracts of Archidendron jiringa

Noviany

Dicky

Andi

et al. 2021

Journal of the Turkish Chemical Society Section A: Chemistry

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“…antibacterial [12], antiplatelet [13], antifungal [14], antimalarial [15], anti-aging [16], and cytotoxic [17].…”

Section: Introductionmentioning

confidence: 99%

Activity Screening and Structure Modification of Artocarpin Against Ace2 and Main Protease Through in Silico Method

et al. 2021

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Objective: SARS-CoV-2 is a type of coronavirus that causes COVID-19 disease. Currently, the right and effective drug for the treatment of COVID-19 has not been found. Artocarpin in the breadfruit plant (Artocarpus altilis), which was tested, has been shown to have antiviral activity. However, artocarpin has a hydroxyl group that can undergo oxidation within a certain time, thereby reducing the stability of the compound and non-specific antiviral activity. Methods: In this study, the structural modification of artocarpin was carried out to obtain compounds with anticoronavirus activity with good physicochemical properties. This research was conducted in silico, including molecular docking simulation, bioavailability prediction, and preADMET. Results: The top 20 modified compounds were selected from each target's top 3 compounds, which had better bond energies compared to the positive control. These 3 compounds have the potential to inhibit ACE2 and Mpro receptors and 1 compound are better at inhibiting both. Conclusion: From the results of the research conducted, we conclude that the 3 best compounds can be potential candidates that can be developed as COVID-19 therapy.

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“…The therapeutic effect is associated with the abundance of phenolics, such as flavonoids, stilbenoids, dihydrochalcones, dihydrobenzoxanthones and prenylated flavonoids [12]. Single metabolites reported in vivo antimalarial [13], inhibition of LPS-induced inflammation [14], α-glucosidase inhibitory [15], TRAILresistance overcoming with antiviral [16], and anticancer [17] activities. Alkylated flavonoid Artonin E from A. elasticus also revealed considerable cytotoxic effect in MCF-7 human breast cancer cells by ROS mediated mitochondrial pathway [18,19].…”

Section: Introductionmentioning

confidence: 99%

Human neutrophil elastase inhibitory dihydrobenzoxanthones and alkylated flavones from the Artocarpus elasticus root barks

et al. 2020

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Neutrophil elastases are deposited in azurophilic granules interspace of neutrophils and tightly associated with inflammatory ailments. The root barks of Artocarpus elasticus had a strong inhibitory potential against human neutrophil elastase (HNE). The responsible components for HNE inhibition were confirmed as alkylated flavones (2–4, IC50 = 14.8 ~ 18.1 μM) and dihydrobenzoxanthones (5–8, IC50 = 9.8 ~ 28.7 μM). Alkyl groups on flavone were found to be crucial functionalities for HNE inhibition. For instance, alkylated flavone 2 (IC50 = 14.8 μM) was 20-fold potent than mother compound norartocarpetin (1, IC50 > 300 μM). The kinetic analysis showed that alkylated flavones (2–4) were noncompetitive inhibition, while dihydrobenzoxanthones (5–8) were a mixed type I (KI < KIS) inhibitors, which usually binds with free enzyme better than to complex of enzyme–substrate. Inhibitors and HNE enzyme binding affinities were examined by fluorescence quenching effect. In the result, the binding affinity constants (KSV) had a significant correlation with inhibitory potencies (IC50).

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In Vivo Antimalarial Test of Artocarpin and in vitro Antimalarial Test of Artonin M Isolated from Artocarpus

Cited by 9 publications

References 12 publications

Bioassay-Guided Separation Approach for Characterization of New Antibacterial Fractions from the Stem Roots Extracts of Archidendron jiringa

Bioassay-Guided Separation Approach for Characterization of New Antibacterial Fractions from the Stem Roots Extracts of Archidendron jiringa

Activity Screening and Structure Modification of Artocarpin Against Ace2 and Main Protease Through in Silico Method

Human neutrophil elastase inhibitory dihydrobenzoxanthones and alkylated flavones from the Artocarpus elasticus root barks

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