Synthesis and antimicrobial evaluation of fatty chain substituted 2,5-dimethyl pyrrole and 1,3-benzoxazin-4-one derivatives

AbstractFatty acids themselves have a number of biological properties and its easy intake by the human body will focus to the synthesis of many heterocyclic moiety substituted with fatty acid residue, to make more gradual intake of heterocycles in the human body. 2,5-Dimethyl pyrrole 2(a–e) and 1,3-benzoxazin-4-one 4(b–e) derivatives were synthesized, from cyclization of fatty acid hydrazide 1(a–e) with acetonyl acetone and from the reaction of fatty esters 3(b–e) with anthranilic acid in the presence of POCl3, respectively. All these compounds were characterized with the help of IR, 1H NMR, 13C NMR and mass spectra. The synthesized compounds were screened for antimicrobial evaluation against gram-positive (Staphylococcus aureus SA 22, Bacillus subtilis MTCC 121), gram-negative (Escherichia coli K12, Klebsiella pneumoniae) and fungal strains (Candida albicans IOA-109) and were found to be good antimicrobial agents

Biosynthesized Silver Nanoparticle (AgNP) From Pandanus odorifer Leaf Extract Exhibits Anti-metastasis and Anti-biofilm Potentials

Cancer and the associated secondary bacterial infections are leading cause of mortality, due to the paucity of effective drugs. Here, we have synthesized silver nanoparticles (AgNPs) from organic resource and confirmed their anti-cancer and anti-microbial potentials. Microwave irradiation method was employed to synthesize AgNPs using Pandanus odorifer leaf extract. Anti-cancer potential of AgNPs was evaluated by scratch assay on the monolayer of rat basophilic leukemia (RBL) cells, indicating that the synthesized AgNPs inhibit the migration of RBL cells. The synthesized AgNPs showed MIC value of 4–16 µg/mL against both Gram +ve and Gram -ve bacterial strains, exhibiting the anti-microbial potential. Biofilm inhibition was recorded at sub- MIC values against Gram +ve and Gram -ve bacterial strains. Violacein and alginate productions were reduced by 89.6 and 75.6%, respectively at 4 and 8 µg/mL of AgNPs, suggesting anti-quorum sensing activity. Exopolysaccharide production was decreased by 61–79 and 84% for Gram +ve and Gram -ve pathogens respectively. Flagellar driven swarming mobility was also reduced significantly. Furthermore, In vivo study confirmed their tolerability in mice, indicating their clinical perspective. Collective, we claim that the synthesized AgNPs have anti-metastasis as well as anti-microbial activities. Hence, this can be further tested for therapeutic options to treat cancer and secondary bacterial infections

Biosynthesized Silver Nanoparticle (AgNP) From Pandanus odorifer Leaf Extract Exhibits Anti-metastasis and Anti-biofilm Potentials

Cancer and the associated secondary bacterial infections are leading cause of mortality, due to the paucity of effective drugs. Here, we have synthesized silver nanoparticles (AgNPs) from organic resource and confirmed their anti-cancer and anti-microbial potentials. Microwave irradiation method was employed to synthesize AgNPs using Pandanus odorifer leaf extract. Anti-cancer potential of AgNPs was evaluated by scratch assay on the monolayer of rat basophilic leukemia (RBL) cells, indicating that the synthesized AgNPs inhibit the migration of RBL cells. The synthesized AgNPs showed MIC value of 4–16 µg/mL against both Gram +ve and Gram -ve bacterial strains, exhibiting the anti-microbial potential. Biofilm inhibition was recorded at sub- MIC values against Gram +ve and Gram -ve bacterial strains. Violacein and alginate productions were reduced by 89.6 and 75.6%, respectively at 4 and 8 µg/mL of AgNPs, suggesting anti-quorum sensing activity. Exopolysaccharide production was decreased by 61–79 and 84% for Gram +ve and Gram -ve pathogens respectively. Flagellar driven swarming mobility was also reduced significantly. Furthermore, In vivo study confirmed their tolerability in mice, indicating their clinical perspective. Collective, we claim that the synthesized AgNPs have anti-metastasis as well as anti-microbial activities. Hence, this can be further tested for therapeutic options to treat cancer and secondary bacterial infections

Antibacterial and antibiofilm activity of Abroma augusta stabilized silver (Ag) nanoparticles against drug-resistant clinical pathogens

Infectious diseases remain among the most pressing concerns for human health. This issue has grown even more complex with the emergence of multidrug-resistant (MDR) bacteria. To address bacterial infections, nanoparticles have emerged as a promising avenue, offering the potential to target bacteria at multiple levels and effectively eliminate them. In this study, silver nanoparticles (AA-AgNPs) were synthesized using the leaf extract of a medicinal plant, Abroma augusta. The synthesis method is straightforward, safe, cost-effective, and environment friendly, utilizing the leaf extract of this Ayurvedic herb. The UV-vis absorbance peak at 424 nm indicated the formation of AA-AgNPs, with the involvement of numerous functional groups in the synthesis and stabilization of the particles. AA-AgNPs exhibited robust antibacterial and antibiofilm activities against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). The MIC values of AA-AgNPs ranged from 8 to 32 μg/mL. Electron microscopic examination of the interaction of AA-AgNPs with the test bacterial pathogens showed a deleterious impact on bacterial morphology, resulting from membrane rupture and leakage of intracellular components. AA-AgNPs also demonstrated a dose-dependent effect in curtailing biofilm formation below inhibitory doses. Overall, this study highlights the potential of AA-AgNPs in the successful inhibition of both the growth and biofilms of MRSA and VRE bacteria. Following studies on toxicity and dose optimization, such AgNPs could be developed into effective medical remedies against infections

Leaf Extracts of Mangifera indica L. Inhibit Quorum Sensing – Regulated Production of Virulence Factors and Biofilm in Test Bacteria

Quorum sensing (QS) is a global gene regulatory mechanism in bacteria for various traits including virulence factors. Disabling QS system with anti-infective agent is considered as a potential strategy to prevent bacterial infection. Mangifera indica L. (mango) has been shown to possess various biological activities including anti-QS. This study investigates the efficacy of leaf extracts on QS-regulated virulence factors and biofilm formation in Gram negative pathogens. Mango leaf (ML) extract was tested for QS inhibition and QS-regulated virulence factors using various indicator strains. It was further correlated with the biofilm inhibition and confirmed by electron microscopy. Phytochemical analysis was carried out using ultra performance liquid chromatography (UPLC) and gas chromatography–mass spectrometry (GC-MS) analysis. In vitro evaluation of anti-QS activity of ML extracts against Chromobacterium violaceum revealed promising dose-dependent interference in violacein production, by methanol extract. QS inhibitory activity is also demonstrated by reduction in elastase (76%), total protease (56%), pyocyanin (89%), chitinase (55%), exopolysaccharide production (58%) and swarming motility (74%) in Pseudomonas aeruginosa PAO1 at 800 μg/ml concentration. Biofilm formation by P. aeruginosa PAO1 and Aeromonas hydrophila WAF38 was reduced considerably (36–82%) over control. The inhibition of biofilm was also observed by scanning electron microscopy. Moreover, ML extracts significantly reduced mortality of Caenorhabditis elegans pre-infected with PAO1 at the tested concentration. Phytochemical analysis of active extracts revealed very high content of phenolics in methanol extract and a total of 14 compounds were detected by GC-MS and UPLC. These findings suggest that phytochemicals from the ML could provide bioactive anti-infective and needs further investigation to isolate and uncover their therapeutic efficacy

Comparative efficacy of ternary Cu (II) complex and Zn (II)-complex in amelioration of carbon tetrachloride-induced hepatotoxicity in vivo

Cu (II) and Zn (II) are two of the most favored metals in synthesis chemistry, encompassing their therapeutic potentials. The present study aims to evaluate the comparative ameliorative potential of a group B carcinogen, CCl4-induced hepatotoxicity, by our recently synthesized and characterized ternary Cu and Zn-based complexes in vivo. Three groups of rats were treated with CCl4 alone and with the combination of Cu (II) complex and Zn (II) complex beside the control negative group without any treatment. After completion of the treatment, the samples were subjected to biochemical and histological analysis. The analysis demonstrated extensive alteration in redox status, liver markers, and hepatotoxicity markers in the CCl4, treated group compared to the control group. However, the Cu (II) complex showed significant improvement in most of the parameters under the study. Also, histopathological evaluation and comet assay further consolidated the findings. Hence, this investigation reveals that Cu (II) complex has more substantial ameliorative potential in ceasing CCl4-induced hepatotoxic insults. Therefore, the ternary Cu (II) complex act as a more potent chemotherapeutic agent in cancer treatment with milder side effects than the Zn (II) complex

Attenuation of quorum sensing regulated virulence functions and biofilm of pathogenic bacteria by medicinal plant Artemisia annua and its phytoconstituent 1, 8-cineole

The emergence of multidrug resistance (MDR) in bacterial pathogens is a serious public health concern. A significant therapeutic target for MDR infections is the quorum sensing-regulated bacterial pathogenicity. Determining the anti-quorum sensing abilities of certain medicinal plants against bacterial pathogens as well as the in-silico interactions of particular bioactive phytocompounds with QS and biofilm-associated proteins were the objectives of the present study. In this study, 6 medicinal plants were selected based on their ethnopharmacological usage, screened for Anti-QS activity and Artemisia annua leaf extract (AALE) demonstrated pigment inhibitory activity against Chromobacterium violaceum CV12472. Further, the methanol active fraction significantly inhibited the virulence factors (pyocyanin, pyoverdine, rhamnolipid and swarming motility) of Pseudomonas aeruginosa PAO1 and Serratia marcescens MTCC 97 at respective sub-MICs. The inhibition of biofilm was determined using a microtiter plate test and scanning electron microscopy. Biofilm formation was impaired by 70%, 72% and 74% in P. aeruginosa, C. violaceum and S. marcescens, respectively at 0.5xMIC of the extract. The phytochemical content of the extract was studied using GC–MS and 1, 8-cineole was identified as major bioactive compound. Furthermore, 1, 8-cineole was docked with quorum sensing (QS) proteins (LasI, LasR, CviR, and rhlR) and biofilm proteins (PilY1 and PilT). In silico docking and dynamics simulations studies suggested interactions with QS-receptors CviR’, LasI, LasR, and biofilm proteins PilY1, PilT for anti-QS activity. Further, 1, 8-cineole demonstrated 66% and 51% reduction in violacein production and biofilm formation, respectively to validate the findings of computational analysis. Findings of the present investigation suggests that 1, 8-cineole plays a crucial role in the QS and biofilm inhibitory activity demonstrated by Artemisia annua extract. Research Highlights: Artemisia annua leaf extract (AALE) methanol fraction demonstrated broad-spectrum QS and biofilm inhibition Scanning electron microscopy (SEM) confirmed biofilm inhibition Molecular docking and simulation studies suggested positive interactions of 1,8-cineol with QS-receptors and biofilm proteins

Broad-spectrum antibacterial and antibiofilm activity of biogenic silver nanoparticles synthesized from leaf extract of Phyllanthus niruri

Multidrug resistance (MDR) among pathogenic bacteria is a global health concern as it has rendered the current antibiotic therapy ineffective. A recent and rapidly developing research area in the biomedical sector is the use of biogenic nanoparticles as antibacterial agents. In the current investigation, aqueous leaf extract of Phyllanthus niruri (Pn-AgNPs) were employed for the biogenic synthesis of silver nanoparticles, further characterized by SEM, EDX, FTIR, TEM, UV–Vis and XRD techniques. Electron microscopy images of the green-synthesized Pn-AgNPs showed them as evenly dispersed spherical particles having an average size of about ∼ 20 nm. The Pn-AgNPs were further tested for potential antibacterial activity against isolated drug-resistant pathogenic bacteria such as Burkholderia cepacia complex, carbapenem-resistant Enterobacterales (CRE), Citrobacter freundii, Enterococcus faecalis, Escherichia coli, Enterobacter clocae, MRSA, Salmonella typhi, Streptococcus spp, and vancomycin-resistant Enterococci (VRE).The Pn-AgNPs significantly inhibited growth all of the studied bacterial isolates, including antibiotic-resistant isolates such as MRSA, VRE, and CRE. Electron micrographs clearly showed the enhanced penetration of AgNPs leading to disruption of cell membrane causing death of the cell. Further, Pn-AgNPs dramatically reduced the ability of P. aeruginosa, Bacillus cereus, E. coli, and S. aureus to form biofilms. Leakage of protein from bacterial cells could be main reason for the effective bactericidal action of synthesized AgNPs. This antibacterial and antibiofilm potential of Phyllanthus niruri biosynthesized AgNPs against clinically significant drug-resistant bacteria is impressive and can be developed as a novel antimicrobial agent to combat the threat of drug-resistant bacterial infections