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Schiff bases of existing antimicrobial drugs are an area, which is still to be comprehensively explored to improve drug efficiency against consistently resisting bacterial species. In this study, we have targeted a new and eco-friendly method of condensation reaction that allows the "green synthesis" as well as improved biological efficacy. The transition metal complexes of cefpodoxime with well-enhanced biological activities were synthesized. The condensation reaction product of cefpodoxime and vanillin was further reacted with suitable metal salts of [Mn (II), Cu (II), Fe (II), Zn (II), and Ni (II)] with 1:2 molar ratio (metal: ligand). The characterization of all the products were carried out by using UV-Visible, elemental analyzer, FTIR, 1H-NMR, ICP-OES, and LC-MS. Electronic data obtained by UV-Visible proved the octahedral geometry of metal complexes. The biological activities Schiff base ligand and its transition metal complexes were tested by using in-vitro anti-bacterial analysis against various Gram-negative, as well as Gram-positive bacterial strains. Proteinase and protein denaturation inhibition assays were utilized to evaluate the products in-vitro anti-inflammatory activities. The in vitro antioxidant activity of the ligand and its complexes was evaluated by utilizing the 2,2-diphenyl-1-picrylhydrazyl (DPPH) in-vitro method. The final results proved metal complexes to be more effective against bacterial microorganisms as compared to respective parent drug as well as their free ligands. Patch Dock, a molecular docking tool, was used to dock complexes 1a-5e with the crystal structure of GlcN-6-P synthase (ID: 1MOQ). According to the docking results, complex 2b exhibited a highest score (8,882; ACE = -580.43 kcal/mol) that is well correlated with a high inhibition as compared to other complexes which corresponds to the antibacterial screening outcomes.
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This study focuses on the investigation of the significance of polymers in drug delivery approaches. The carboxymethyl cellulose (CMC), polyvinyl alcohol (PVA) and dextrin-based hydrogel membrane were prepared and employed for the sustained release of third-generation oral antibiotic (cefixime). Different proportions of CMC, PVA and dextrin were blended and hydrogel membranes were fabricated via solvent casting method. The prepared membrane was characterized by FTIR, SEM, UV-visible, TGA and swelling analysis. Cefixime drug was incorporated in the CMC/PVA/dextrin matrix and drug release was investigated. The sustained release of the tested drug (cefixime) was investigated and the drug was released in 120 min in the phosphate-buffered saline (PBS) solution. The antibacterial activity of the prepared membrane was promising against Proteus vulgaris, salmonella typhi, Escherichia coli and Bacillus subtilis strains. The swelling capabilities, thermal stability and non-toxic nature of the prepared CMC/PVA/dextrin membrane could have potential applications for cefixime drug in delivery in a controlled way for the treatment of infectious diseases.
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Novel spiropyrazoline-indolinones (4a-t) have been synthesized successfully in neutral deep eutectic solvents by reacting 5-Cl/Br-isatin (1a-b) with aromatic ketones (2a-b) and a variety of substituted hydrazines (3a-e) in good to excellent yields. This eco-friendly straightforward synthetic protocol discloses good functional group compatibility. The conventional synthetic approach was compared with the greener route of microwave-assisted synthesis of spiropyrazolines using ethanol. This approach utilized mild reaction conditions which furnished high yields in short reaction time employing one pot two-step multicomponent. All new compounds were structurally confirmed by detailed spectroscopic analysis and density functional theory calculations. This method provides efficient access to spiropyrazole derivatives using biodegradable and green solvent.
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Antibacterial, durable and smart cotton fabrics was developed using chitosan-based formulation. The cellulose was covalently cross-linked with chitosan using TEOF. The antibacterial activity of prepared smart fabrics and CS was studied against S. aureus and E. coli strains. The FTIR, SEM and XRD were employed to confirm the linkage of CS molecules with cellulose in cotton fabrics. The CS of 160 KDa extracted from shrimp shell showed the optimum antibacterial activity. The prominent asymmetric, symmetric alkyl CH peaks of CS were shifted to 2930 and 2845 (cm-1), respectively. Moreover, the shifted peaks at 1590 and 1400 (cm-1) indicate the CO stretching and NH2 bending bands of CS, respectively. This confirm the existence of new imine functional group that was generated after cross-linking of NH2 groups of CS. The SEM results showed more uniform morphology of TEOF cross-linked fabrics versus CS coated fabrics, which revealed a promising microbial growth inhibition activity. The TEOF as a cross-linker has been unveiled, showcasing the effectiveness of this innovative crosslinking approach. The fabric treated with cross-linked CS exhibited remarkable antibacterial properties that endured even after undergoing 30 washing cycles. These antibacterial textiles possess substantial commercial potential across a diverse range of industries.
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Quitosana , Fibra de Algodão , Celulose , Escherichia coli , Staphylococcus aureus , Têxteis , Antibacterianos/farmacologiaRESUMO
Myrtenol (C10H16O) is a volatile compound belonging to the terpenoid family of monocyclic monoterpenes. It is one of the essential oils constituents of several aromatic plants, including the genera Myrtus, Tanacetum, Artemisia, Hyssopus, and Rhodiola. The oxidation of α-pinene can produce it. Several reports demonstrated the pharmacological properties of myrtenol, including its antioxidant, antibacterial, antifungal, antidiabetic, anxiolytic, and gastroprotective activities. In this review, we discussed and highlighted in depth the pharmacological activities, cellular and molecular, providing insight into the mechanisms of myrtenol. In light of this finding, the interesting biological activities and abundance of myrtenol in nature suggests its potential applications in medicinal settings in the fight against various diseases.
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Óleos Voláteis , Extratos Vegetais , Humanos , Extratos Vegetais/farmacologia , Óleos Voláteis/farmacologia , Monoterpenos/farmacologia , Antioxidantes/farmacologiaRESUMO
In this work, ZnO, CrZnO, RuZnO, and BaZnO nanomaterials were synthesized and characterized in order to study their antibacterial activity. The agar well diffusion, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) assays were used to determine the antibacterial activity of the fabricated nanomaterials against Staphylococcus aureus ATCC 29213, Escherichia coli ATCC35218, Klebsiella pneumoniae ATCC 7000603, and Pseudomonas aeruginosa ATCC 278533. The well-diffusion test revealed significant antibacterial activity against all investigated bacteria when compared to vancomycin at a concentration of 1 mg/mL. The most susceptible bacteria to BaZnO, RuZnO, and CrZnO were Staphylococcus aureus (15.5 ± 0.5 mm), Pseudomonas aeruginosa (19.2 ± 0.5 mm), and Pseudomonas aeruginosa (19.7 ± 0.5), respectively. The MIC values indicated that they were in the range of 0.02 to 0.2 mg/mL. The MBC values showed that the tested bacteria's growth could be inhibited at concentrations ranging from 0.2 to 2.0 mg/mL. According to the MBC/MIC ratio, BaZnO, RuZnO, and CrZnO exhibit bacteriostatic effects and may target bacterial protein synthesis based on the results of the tolerance test. This study shows the efficacy of the above-mentioned nanoparticles on bacterial growth. Further biotechnological and toxicological studies on the nanoparticles fabricated here are recommended to benefit from these findings.
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Infecções Estafilocócicas , Staphylococcus aureus , Humanos , Testes de Sensibilidade Microbiana , Pseudomonas aeruginosa , Klebsiella pneumoniae , Antibacterianos/farmacologia , Escherichia coli , BactériasRESUMO
The volatiles chemical composition and biological attributes of coriander (Coriandrum sativum L.) leaves essential oil obtained by two extraction techniques namely supercritical fluid extraction and hydro-distillation is appraised. The coriander essential oil yield (.12%) by hydro-distillation was slightly higher than that of supercritical fluid extraction (.09%). The physico-chemical variables of the essential oil obtained from both the techniques varied in significantly (P < .05). GC-MS analysis identified 23 different components in supercritical fluid extracted oil and 18 components in hydro-distilled essential oil having linalool as major component (51.32% and 61.78%, respectively) followed by phytol (12.71%). The oil recovered by supercritical fluid extraction exhibited greater DPPH radical scavenging activity as well as reducing power as compared to the essential oil obtained by hydro-distillation technique along with a stronger biofilm inhibition and least hemolysis. The results of antimicrobial activity revealed that super critical fluid extracted essential oil has potent antifungal and antibacterial activity against P. multocida and A alternata, whereas hydro-distilled essential oil displayed better antimicrobial potential against E coli and A niger. Overall, these results depict that supercritical fluid extraction is superior than hydro-distillation with regard to isolation of better-quality coriander essential oil for nutra-pharmaceutical developments.
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Present research work evaluates variation in volatile chemicals profile and biological activities of essential oil (EO) obtained from the leaves of eucalyptus (Eucalyptus camaldulensis Dehnh.) using hydro-distillation (HD) and supercritical fluid extraction (SFE). The yield (1.32%) of volatile oil by HD was higher than the yield (.52%) of the SFE method (P < .05). The results of physical factors like density, color, refractive index, and solubility of the EOs produced by both the methods showed insignificant variations. Gas chromatography - mass spectrometry (GC-MS) compositional analysis showed that eucalyptol (31.10% and 30.43%) and α-pinene (11.02% and 10.35%) were the main constituents detected in SFE and HD extracted Eucalyptus camaldulensis EO, respectively. Antioxidant activity-related parameters, such as reducing ability and DPPH free radical scavenging capability exhibited by EO obtained via SFE were noted to be better than hydro-distilled EO. Supercritical fluid extracted and hydro-distilled essential oils demonstrated a considerable but variable antimicrobial potential against selected bacterial and fungal strains. Interestingly, oil extracted by SFE showed relatively higher hemolytic activity and biofilm inhibition potential. The variation in biological activities of tested EOs can be linked to the difference in the volatile bioactives composition due to different isolation techniques. In conclusion, the EO obtained from Eucalyptus leaves by the SFE method can be explored as a potential antioxidant and antimicrobial agent in the functional food and nutra-pharmaceutical sector.
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PURPOSE: The secondary metabolites in plants are the basis of defense and stress balance, which is an important aspect in plant growth. The UV-B treatment (a biotic stress) and salt stress on bitter melon (Momordica charantia L.) were studied, and the impact of pre-sowing seed treatment was evaluated on the basis of biochemical and enzymatic biomarkers, antioxidants, and wound-healing potential during early growth stages. METHODS: The UV-B treatment for 5 and 10 min and salt stress 250 mM and 500 mM treatments were applied, and 21-day seedling tissue were collected for total phenolic contents (TPC), total flavonoid contents (TFC), antioxidant, chlorophyll contents, hydrogen peroxide, total soluble sugar, enzymes activities, and wound-healing potential studies. RESULTS: The TPC, TFC, diphenyl picrylhydrazyl (DPPH), chlorophyll contents, and total soluble sugar were recorded higher at 5 min treatment with UV-B and salt stress at 250 mM concentration. Antioxidant enzymes activities were recorded higher for 10 min UV-B treatment and 500 mM salt treatment. Wound-healing potential was found significant at 5 min treatment with UV-B radiation, which was studied in vivo in rabbits. The LC-MS analysis revealed a variety of phenolic compounds in the seedlings. CONCLUSION: The study concluded that treatments significantly affect the biological activities of bitter melon seeds at the seedling stage, and the seeds contain important phenolic compounds responsible for its antioxidant potential and enzymatic activities. Future studies could be focused on the later stages of growth, development, and yield characteristics subjected to salt stress along with UV-B radiation treatment.
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The present study demonstrated that chitin-based nanofibers (CNFs) trigger the chitinase genes (PGIP1 and CaChi2), while elevating salicylic acid that can protect plants against pathogens. Cross-talk between this genetic induction and salicylic-acid-mediated immune response was also observed, which may arm a plant against multiple pathovars. Crab and mushroom based CNFs were synthesized by electrospinning and ball milling techniques. Plants (mung bean, Vigna radiata) (pepper, Capsicum annuum) were pre-inoculated with CNFs and treated with the pathogens Scrolotium rolfsii for pepper and Macrophomina phaseolina for mung bean and shrimp-based CNFs were used as a control. Treated plants had elevated levels of chitinase genes in response to CNFs at inoculation concentrations <10 mg/mL both in soil and media, to protect them against the pathogenic fungal disease. After 24 h of exposure to the pathogens, qRT-PCR showed genes class II chitinase gene (CaChi2) and polygalacturonase inhibitor protein 1 (PGIP1) to be up-regulated in both root and shoot at 0.1 and 1 mg/mL of inoculation, respectively. The ball milled mushroom CNFs were sufficient to trigger the membrane based enzymes with less diameter (≥15 nm) to be most efficient versus others. In vitro analysis showed IC50 of ball milled mushroom CNFs to be most efficient in limiting the growth of fungal biomass. Further trigger-like effects were prominent in reducing pathogenic fungal spread in both species.
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Ascomicetos/imunologia , Capsicum , Membrana Celular , Quitina , Nanofibras/química , Doenças das Plantas , Imunidade Vegetal/efeitos dos fármacos , Vigna , Capsicum/imunologia , Capsicum/microbiologia , Membrana Celular/imunologia , Membrana Celular/microbiologia , Quitina/química , Quitina/farmacologia , Doenças das Plantas/imunologia , Doenças das Plantas/microbiologia , Vigna/imunologia , Vigna/microbiologiaRESUMO
Forty-three bacterial isolates in five genera were recovered from naturally infected green pepper fruits (38 samples) showing dark brown, irregular-shaped splotches. The pathogenicity test was performed on healthy green pepper fruits and red colonies were from inoculated fruits showing the same symptoms and the infected area developed into soft rot. Their identification was based on phenotypic characters and sequence of the gene fragment coding 16S rRNA. Of 43 isolates, 10 showing splotches on green pepper fruits belonged to genus Serratia on the basis of phenotypic characters. One representative isolate of the genus Serratia has been identified by partial 16S rRNA gene sequencing and phylogenetic analysis as belonging to the Serratia rubidaea and has the potential to cause spot on green pepper. Eleven phytopathogenic bacterial isolates were also obtained at the same time but did not induce any splotch symptoms on artificially infected green pepper. Five out of 11 bacterial isolates were identified as Ralstonia on the basis of biochemical tests. Partial sequencing of 16S ribosomal gene of representative isolate revealed that the isolate is Ralstonia solanacearum. The six remaining isolates were related to Xanthomonas vesicatoria on the basis of biochemical tests. Twenty-two of opportunistic human pathogens were isolated at the same time and related to Proteus and Klebsiella. Opportunistic human pathogens did not produce any symptoms on artificially infected green pepper. One representative isolate for each genus was identified as Klebsiella oxytoca and Proteus mirabilis based on their partial 16S rRNA gene sequences. The virulence of the S. rubidaea, the causal agent of green pepper fruits splotches was attributed to the production and secretion of a large variety of enzymes capable of degrading the complex polysaccharides of the plant cell wall and membrane constituents.