Backgrounds: Bacteriocin has been used widely in industry as a biopreservative agent. The objective of the present study was to investigate the potency of Bacteriocin isolated from tiger prawnPenaeus monodonand freshwater shrimpMacrobrachium rosenbergiias an anti-bacterial on fish. Methods: A total of ten candidates of probiotic bacteria consisted of five isolates from tiger shrimps (H1, H2, H3, H4, H5) and five isolates from freshwater prawns (W1, W2, W3, W4, W5) were evaluated. Bacteriocin wasBacteriocin was produced by centrifugation at a speed of 150 rpm and at 37 °C for 24 hours. The bacteriocin extract was purified by adding sulphate ammonium salt {(NH4) 2SO4} at 80% of the saturation level. Bacteriocin activity was determined using a diffusion method against pathogenic bacteriaVibrio alginolyticus,Aeromonas hydrophillaAeromonas hydrophillaandPseudomonas stutzeri. Bacteriocins were analyzed usinganalyzedusing High Performance Liquid Chromatography (HPLC) and Fourier Transform Infra-Red (FTIR). The data were subjected to analysis of variance (ANOVA) and followed with Duncans multiple range test. Results: Bacteriocins produced by bacteria isolate H4 from tiger prawn indicated the highest bacteriocin activity againstbacteriocin activity againstPseudomonas stutzeriatstutzeriat the diameter of inhibition zone of 887.10 ± 409.24 mm2/mL. While isolate W2 from freshwater shrimp indicated inhibition zone of 1466.96 ± 127.62 mm2/mL. Both bacteriocins were purified by chromatography column using Sephadex LH-20. Conclusion s: This finding showed that bacterial isolates H4 and W2 have the potential to produce bacteriocins which inhibit the pathogenic bacteria. FTIR analysis showed an amide group at wave number 1652cm-1contained in the bacteriocins of isolates H4 and W2.
1 November 2022 in Advances in Pharmacological and Pharmaceutical Sciences
Stenochlaena palustris (Burm.f.) Bedd. (Blechnaceae) or Kelakai is a traditional medicinal plant found in the Indonesian islands of Borneo and Sumatra. It has been used to treat wound healing, infection, and diabetes. This study looked into the free radical scavenging activity, antiplasmodial activity, toxicity, and antibacterial activity against pathogenic bacteria. The species aerial part was extracted with methanol, followed by a liquid-liquid extraction against (n-hexane, dichloromethane, and ethyl acetate). The extracts free radical scavenging activities were determined using DPPH and NO radicals. The antiplasmodial and toxicity assays were conducted using two Plasmodium falciparum strains (3D7 and W2) and the brine shrimp lethality test. In addition, antibacterial activity was determined using the well diffusion method. The results revealed that ethyl acetate depicted potential activities toward the assay. The ethyl acetate showed potential free radical scavenging activities with an IC50 value of 51.63±0.46μg/mL (DPPH) and 60.03±0.65μg/mL (NO). The antiplasmodial activities showed that the ethyl acetate had potential activities among the extracts with an IC50 value of 11.06±0.45μg/mL. However, all the extracts demonstrated nontoxic toward Artemia salina with LC50>1000μg/mL. Furthermore, the ethyl acetate demonstrated intermediate susceptibility against B. cereus ATCC 10876, V. parahaemolyticus ATCC 17802, L. monocytogenes ATCC 7644, and S. Typhimurium ATCC 14028 at a concentration of 500μg/disc. According to these findings, the ethyl acetate extract of S. palustris (Burm.f.) Bedd is a promising source of natural antioxidants and antiplasmodial agents.
Considering the escalating resistance to conventional antifungal medications, it is critical to identify novel compounds that can efficiently counteract this challenge. The purpose of this research was to elucidate the fungicidal properties of secondary metabolites derived from Arcangelisia flava, with a specific focus on their efficacy against Candida species. This study utilized a combination approach comprising laboratory simulations and experiments to discern and evaluate the biologically active constituents present in the dichloromethane extract of A. flava. The in vitro experiments demonstrated that compounds 1 (palmatine) and 2 (fibraurin) exhibited antifungal properties. The compounds exhibited minimum inhibitory concentrations (MICs) ranging from 15.62 to 62.5 µg/mL against Candida sp. Moreover, compound 1 demonstrated a minimum fungicidal concentration (MFC) of 62.5 µg/mL against Candida glabrata and C. krusei. In contrast, compound 2 exhibited an MFC of 125 µg/mL against both Candida species. Based on a molecular docking study, it was shown that compounds 1 and 2 have a binding free energy of −6.6377 and −6.7075 kcal/mol, respectively, which indicates a strong affinity and specificity for fungal enzymatic targets. This study utilized pharmacophore modeling and Density Functional Theory (DFT) simulations to better understand the interaction dynamics and structural properties crucial for antifungal activity. The findings underscore the potential of secondary metabolites derived from A. flava to act as a foundation for creating novel and highly efficient antifungal treatments, specifically targeting fungal diseases resistant to existing treatment methods. Thus, the results regarding these compounds can provide references for the next stage in antifungal drug design. Further investigation is necessary to thoroughly evaluate these natural substances’ clinical feasibility and safety characteristics, which show great potential as antifungal agents.
Background: The roots of tunjuk langit (Helminthostacshys zeylanica) have been used traditionally in some villages in Indonesia, particularly in Riau Province. Objective: In this study we reported two flavonoids and their antidiabetic activity. Material and methods: Isolation of the metabolites was based on polarity fractionation method. Purification processes were conducted by vacuum liquid chromatography (VLC). Chemical structures were elucidated based on spectroscopy characteristics, including FTIR and 1D/2D NMR. Results: The isolated compounds were identified as ugonin J and K. The antidiabetic activity was measured by α-glucosidase inhibitor assay. The antidiabetic activity of ugonin J was found at IC 50 273,13±0,402 ppm and Ugonin K was found at IC 50 138,21±0,263 ppm (moderately active). Conclusion: Therefore this plant can be used traditionally as antidiabetic medicine.
1 April 2020 in Pharmacology and Clinical Pharmacy Research
Curcumin is a secondary metabolite compound that has diverse biological activities. However, it is easily hydrolyzed at physiological pH due to the presence of the β-diketone group. Therefore, the replacement of the β-diketone group with mono ketone is expected to overcome this issue. We hereby report the synthesis of mono ketone curcumin derivatives from piperidone by two-steps reactions. The synthesis of curcumin derivate 3 was carried out by Claisen-Schmidt condensation between 4-piperidone and 4-methoxybenzaldehyde using alkaline catalyst. The synthesized curcumin derivate 3 was then reacted with the 1-bromo-3-chloropropane to produce curcumin derivate 5, 1-(3-chloropropyl)-3.5-bis((E)-4-methoxybenzylidene)piperidin-4-one, with 72% yield. The calculated docking scores, the curcumin derivate 5 possessed a better affinity for receptors than the standard panduratin A. The curcumin derivate 5 has a lower docking score of -6.40 kcal/mol compared to panduratin A with value of -5.18 kcal/mol and also had strong binding interactions to DEN2 NS2B/NS3 protease. Thus, this compound is promising candidate as a new anti-dengue agent.
Some 2’-hydroxychalcone analogues have been widely used as an intermediate to synthesize various heterocyclic compounds, such as flavanones, flavanonols, flavones, flavonols and others. The heterocyclic compounds are also known to have a variety of interesting bioactivities in the medicinal chemistry and also have potency to be applied in material chemistry including in industry. Therefore, 2’-hydroxychalcone analogues are often synthesized by researchers as intermediate, both in research associated with drug discovery and material synthesis. The aim of this study is to investigate the effect of microwave irradiation power variations on the selectivity of reaction of 2’-hydroxychalcone analogue synthesis. The variations of power that have been used in this study were 100, 180, 300 and 450 W with using a domestic microwave. Based on the study, we conclude that the power variation of microwave irradiationwere proven to effect the selectivity of synthesis reaction. In this study, the most suitable irradiation power to be applied on this synthesis is 180 W.