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BackgroundGlaucoma is the leading cause of permanent blindness. Primary angle closure glaucoma (PACG) is diagnosed only after the onset of symptoms and can result in irreversible blindness despite the standard intraocular pressure (IOP) reduction therapy. The identification of potential biomarkers associated with prognosis will help improve disease management. This study aimed to identify mechanisms associated with disease progression, potential biomarkers, and therapeutic targets of PACG.MethodsThe clinical data assessment of IOP, cup/disc ratio (CDR), Retinal Nerve Fiber Layer (RNFL) thickness of control, and PACG group were collected and analyzed for significant differences. The ATP levels were estimated, and targeted metabolomic analysis was performed on aqueous humor and cytokines in plasma. The pathways obtained from the metabolomics data set were compared with those obtained for data sets from the literature. Clinical parameters were correlated with cytokine levels. Targeted metabolomic analysis of cell culture supernatant from TNFα-treated N9 microglia was carried out, and overlap analysis was performed with data obtained from PACG patients.ResultsElevated IOP, CDR, ATP, cytokines, and reduced RNFL thickness were found in PACG compared to controls. Analysis of PACG and TNFα-treated N9 microglial cell culture supernatant shows activation of immuno-metabolites. The metabolic pathways of PACG, TNFα, and ATP-treated microglia from the literature show considerable overlap. Biomarker analysis identified clinical parameters, ATP, cytokines, and immuno-metabolites.ConclusionThis study shows an association between elevated levels of ATP, cytokines, immuno-metabolism, and potential microglial inflammation with disease progression, rendering these levels potential biomarkers. P2 receptors, cytokines, and IDO1/2 could be potential therapeutic targets.

Infections and pests affecting plants pose significant threats to global food security. Over the top utilize of chemical pesticides is frequently utilized to diminish the impacts of plant illnesses caused by bacterial and parasitic pathogens. The greatest concern as we work towards more feasible horticulture is expanding agrarian efficiency for a developing populace. Microbial biocontrol operators (MBCAs) have illustrated their viability as a green procedure to oversee plant illnesses, invigorate edit development and execution, and increment yields. Other than their growth-promoting part, plant growth-promoting bacteria/fungi (PGPR/PGPF) can stifle plant illnesses by creating inhibitory chemicals and actuating a plant resistant reaction against plant pathogens. As biofertilizers and biopesticides, PGPR and PGPF are considered financially practical and appealing strategies for economical horticulture; This leads to a “win–win” circumstance. A few strains of PGPR and PGPF have been distinguished as compelling BCAs beneath controlled natural conditions. In common, any MBCA must overcome certain challenges some time recently it can be enrolled or broadly utilized for disease/pest control. Viable MBCA gives a down to earth arrangement to progress nursery edit execution with decreased fertilizer inputs and chemical pesticide utilization. This current audit points to fill the current crevice in information on plant growth-promoting microorganisms (PGPM), drawing consideration to the logical premise for arrangement, improvement proposals and extra investigate related to commercial utilize of PGPM.

Background:The most frequent lesion in the blood vessels feeding the myocardium is vascular stenosis, a condition that develops slowly but can prove to be deadly in a long run. Non-invasive biomarkers could play a significant role in timely diagnosis, detection and management for vascular stenosis events associated with cardiovascular disorders.Aims:The study aimed to investigate high sensitivity troponin I (hs-TnI), cardiac troponin I (c-TnI) and high sensitivity C-reactive protein (hs-CRP) that may be used solely or in combination in detecting the extent of vascular stenosis in CVD patients.Methodology:274 patients with dyspnea/orthopnea complaints visiting the cardiologists were enrolled in this study. Angiographic study was conducted on the enrolled patients to examine the extent of stenosis in the five prominent vessels (LDA, LCX, PDA/PLV, RCA, and OM) connected to the myocardium. Samples from all the cases suspected to be having coronary artery stenosis were collected, and subjected to biochemical evaluation of certain cardiac inflammatory biomarkers (c-TnI, hsTn-I and hs-CRP) to check their sensitivity with the level of vascular stenosis. The extent of mild and culprit stenosis was detected during angiographic examination and the same was reported in the form significant (≥50% stenosis in the vessels) and non-significant (

The present research work describes the phyto-synthesis of Manganese dioxide nanoparticles (MnO2NPs) from the reduction of potassium permanganate using Martynia annua (M.annua) plant extract. From the literature review, we clearly understood the M.annua plant has anti-inflammatory activity. Manganese dioxides are important materials due to their wide range of applications. Their increased surface area gives them distinct capabilities, as it increases their mechanical, magnetic, optical, and catalytic qualities, allowing them to be used in more pharmaceutical applications. A detailed review of literature highlighting the issues related to this present work and its knowledge gap that none of the inflammatory activities had been done by MnO2 NPs synthesized from M.annua plant extract. So we selected this study. The product MnO2 NPs showed the wavelength centre at 370 nm and was monitored by UV–Vis spectra. The wave number around 600 cm−1 has to the occurrence of O–Mn–O bonds of pure MnO2 confirmed by FTIR spectroscopy. Transmission electron microscopy images showed the morphology of MnO2 NPs as spherical-shaped particles with average sizes at 7.5 nm. The selected area electron diffraction analysis exhibits the crystalline nature of MnO2 NPs. The obtained MnO2 NPs showed potential antioxidant and anti-inflammatory activity was compared to the plant extract. The synthesized MnO2 NPs have a large number of potential applications in the field of pharmaceutical industries. In the future, we isolate the phytocompounds present in the M.annua plant extract and conduct a study against corona virus. MnO2 produces manganese (III) oxide and oxygen, which increases fire hazard. But further research is required to understand their environmental behaviour and safety.

The (E)-4-((4-hydroxy-3-methoxy-5-nitrobenzylidene) amino) pyrimidin-2(1H)-one (C5NV) was synthesized from cytosine and 5-nitrovanilline by simple straightforward condensation reaction. The structural characteristics of the compound was determined and optimized by WB97XD/cc-pVDZ basis set. The vibrational frequencies were computed and subsequently compared to the experimental frequencies. We investiated the electronic properties of the synthesized compound in gas and solvent phases using the time-dependent density functional theory (TD-DFT) approach, and compared them to experimental values. The fluorescence study showed three different wavelengths indicating the nature of the optical material properties. Frontier molecular orbital (FMO) and molecular electrostatic potential (MEP) analyses were conducted for the title compound, and electron localized functions (ELF) and localized orbital locators (LOL) were used to identify the orbital positions of localized and delocalized atoms. Non-covalent interactions (H-bond interactions) were investigated using reduced density gradients (RDGs). The objective of the study was to determine the physical, chemical, and biological properties of the C5NV. The molecular docking study was conducted between C5NV and 2XNF protein, its lowest binding energy score is −7.92 kcal/mol.

This study deals with the facile synthesis of a single-pot chemical technique for chitosan–curcumin (CUR)-based hybrid nanocomposites with nanostructured graphene oxide (GO) and copper oxide (CuO) as the antibacterial and cytotoxic drugs. The physicochemical properties of synthesized hybrid nanocomposites such as CS-GO, CS-CuO, CS-CUR-GO, and CS-CUR-GO/CuO were confirmed with various advanced tools. Moreover, the in vitro drug release profile of the CS-CUR-GO/CuO nanocomposite exhibited sustained and controlled release during different time intervals. Also, the antibacterial activity of the CS-CUR-GO/CuO hybrid nanocomposite presented the maximum bactericidal effect against Staphylococcus aureus and Escherichia coli pathogens. The hybrid nanocomposites revealed improved cytotoxicity behaviour against cultured mouse fibroblast cells (L929) via cell adhesion, DNA damage, and proliferation. Thus, the chitosan-based hybrid nanocomposites offer rich surface area, biocompatibility, high oxidative stress, and bacterial cell disruption functionalities as a potential candidate for antibacterial and cytotoxicity applications.

The electronic and geometrical structure of the well-known photosensitizer verteporfin VD (1), as well as its guanidine and dicarboxylic acid derivatives VD(Gua)1 (2), VD(COOH)2 (3), and VD(Gua)3 (4) are analyzed using density functional theory (DFT) calculations. The investigation of compound’s thermal and kinetic stability supports their potential use as photodynamic therapeutics. Though there are reports about the biological applications of verteporfin and its derivatives, the basic structural futures at molecular level which play a crucial role in their potential applications, are not well-explored. The results of electronic and spectral analyses by DFT calculation in this work reveal important points underlying the applications of these compounds.

A novel spiroheterocyclic hybrid comprising several privileged structures comprising pyrrolidine, quinoxaline, indole and ferrocene moieties were synthesized in good yields in sustainable fashion using [Bmim]Br augmented four component cycloaddition process. A relatively less explored ylide prepared from quinoxalinone and L-tryptophan with diverse ferrocenyl derivatives in ionic liquids afforded spiropyrrolidinoindole tethered ferrocene hybrids. The reaction provides highly regioselective fashion thus created five new bonds and four adjoining stereocenter in single synthetic transformation, thus created with complete diastereomeric control. The cholinesterase inhibitory potency was performed for synthesized compounds against AChE/BChE enzymes. Among them, compound bearing with fluorine substituted heterocycles showed significant activity which is comparable activity with reference standard, galantamine.

In this study we have reported sodium tartrate (ST) and Zn2+ as the potential mixed corrosion inhibitors for copper corrosion in drinking water, by using electrochemical impedance and polarization techniques. The results of potentio-dynamic polarization indicated that sodium tartrate could be used as mixed type inhibitor with Zn2+. ST was found to be 92% effective for slowing down both the anodic and cathodic reaction rates. It was additionally found that ST could coat the surface of copper to prevent it from conducting electricity. As the inhibitor concentration increased, the stability of the formed protective layer was also improved. The results obtained from studies like SEM, EDAX, AFM, and water contact angle clearly indicated the development of a barrier by inducing the lotus effect on copper surface. The water contact angle measurement results suggested that the coating formed in the presence of inhibitor was superhydrophobic, and the surface was homogeneous.

The Schiff base was synthesized using the m-bromosalicylaldehyde and ethylenediamine in 1:1 mole ratio. Using the infrared, UV, fluorescence and 1H-13CNMR spectral analysis the m-bromosalicylaldehyde derivative structure was confirmed. Using DFT study the compound structure was optimized. Local energy decomposition (LED) analysis calculated binding energy is -9.19 kcal/mol. The molecule 5BRSET is a optical material, its wavelength is 512 nm and 784 nm respectively. We used three different solvents to calculate the non-linear optical, HOMO-LUMO and molecular electrostatic potential studies, when compared to other solvent the water is showed good activity. Using topological analysis we confirms the localization and delocalization electrons from the synthesized compound. The non-covalent interaction study confirms the intermolecular and intermolecular hydrogen bondings. The natural bond orbital analysis calculation showed the interactions between and within the molecule. A docking study was done on the molecule, and the results show that 5BRSET interacts well with the crystal structure of hypothetical protein (PDB ID: 2EA9). The molecule is moderate activity, which is confirmed by antimicrobial activity.

The titled compound TA structure was optimized in B3LYP/cc-pVDZ basis set using Gaussian software. In natural bond orbital analysis the highest stabilization energy is 82.3 kcal/mol, which is confirmed by LP(1)-C19 to antibonding π*(C13-C14). Electron localization and delocalization areas are confirmed by wavefunction studies. The Gaussian-16w software establishes thermodynamic properties for a titled compound which is confirmed by various solvents. The HOMO and LUMO analysis ethanol have the highest energy gap value, which is 5.88 eV. In molecular electrostatic potential study nitrogen is the nucleophilic attack (blue color) and oxygen is the electrophilic attack (red color). In non-linear optical (NLO) study water solvent shows the highest dipole moment activity. The docking study showed the greatest binding affinity score of −4.08 kcal/mol.

The consistent increase in multidrug resistance among pathogens and increased cancer incidence are serious public health concerns and threaten humans by killing countless lives. In the present study, Talaromyces pinophilus CJ15 was characterized and evaluated for its antibacterial, candidicidal and cytotoxic activities. The selected isolate Talaromyces pinophilus CJ15 with 18S rRNA gene sequence of 1021 base pairs exhibited antifungal activity on plant pathogens via dual culture. The GC-MS profiling of crude extract illustrated the existence of many bioactive macromolecules which include squalene belonging to the terpenoids family. The biological macromolecules in the bioactive fraction of CJ15 exhibited increasing antibacterial activity with an increase in concentration such that the highest activity was recorded against Shigella flexneri with 15, 18, 20, and 24 mm inhibition zones at 25, 50, 75 and 100 μl concentrations, respectively. The squalene, having a molecular weight of 410.718 g/mol, displayed candidicidal activity with a right-side shifted log phase in the growth curve of all the treated Candida species, indicating delayed exponential growth. In cytotoxic activity, the extracted squalene exhibited an IC50 concentration of 26.22 μg/ml against JURKAT cells and induced apoptosis-induced cell death. This study's outcomes encourage the researchers to explore further the development of new and improved bioactive macromolecules that could help to prevent infections and human blood cancer.

Incessant utilization of chemical fertilizers leads to the accumulation of minerals in the soil, rendering them unavailable to plants. Unaware of the mineral reserves present in the soil, farming communities employ chemical fertilizers once during each cultivation, a practice that causes elevated levels of insoluble minerals within the soil. The use of biofertilizers on the other hand, reduces the impact of chemical fertilizers through the action of microorganisms in the product, which dissolves minerals and makes them readily available for plant uptake, helping to create a sustainable environment for continuous agricultural production. In the current investigation, a field trial employing Arachis hypogaea L was conducted to evaluate the ability of Pseudomonas aeruginosa to enhance plant growth and development by solubilizing minerals present in the soil (such as zinc and phosphorus). A Randomized Complete Block Design (RCBD) included five different treatments as T1: Un inoculated Control; T2: Seeds treated with a liquid formulation of P. aeruginosa; T3: Seeds treated with a liquid formulation of P. aeruginosa and the soil amended with organic manure (farmyard); T4: Soil amended with organic manure (farmyard) alone; T5: Seeds treated with lignite (solid) based formulation of P. aeruginosa were used for the study. Efficacy was determined based on the plant's morphological characters and mineral contents (Zn and P) of plants and soil. Survival of P. aeruginosa in the field was validated using Antibiotic Intrinsic patterns (AIP). The results indicated that the combination treatment of P. aeruginosa liquid formulation and organic fertilizer (farmyard) (T3) produced the highest biometric parameters and mineral (Zn and P) content of the groundnut plants and the soil. This outcome is likely attributed to the mineral solubilizing capability of P. aeruginosa. Furthermore, the presence of farmyard manure increased the metabolic activity of P. aeruginosa by inducing its heterotrophic activity, leading to higher mineral content in T3 soil compared to other soil treatments. The AIP data confirmed the presence of the applied liquid inoculant by exhibiting a similar intrinsic pattern between the in vitro isolate and the isolate obtained from the fields. In summary, the Zn and P solubilization ability of P. aeruginosa facilitates the conversion of soil-unavailable mineral form into a form accessible to plants. It further proposes the utilization of the liquid formulation of P. aeruginosa as a viable solution to mitigate the challenges linked to solid-based biofertilizers and the reliance on mineral-based chemical fertilizers.

Objectives: Failure of chemical control methods in conferring protection against Cercospora leaf spot (CLS) disease in mung bean crop led to the investigation of biocontrol agents for effective management of the CLS. The current study was focused on increased defense response (histochemical and biochemical) in mung bean plants by alginate pellet formulation of endophytic Amycolatopsis sp. SND-1 (SND-1) against CLS disease. Methods: The sodium alginate bioformulation of SND-1 was prepared by standard method using CaCl2 and evaluated for viability and contamination. Greenhouse study of prepared SND-1 formulation was performed on mung bean plants against CLS infection. Further, the acceleration of histochemical depositions (lignin, H2O2 and phenol) by differential staining methods and biochemical defense enzymes like PAL, GLU, and POX, phenolic, flavonoid and chlorophyll contents and cell death analysis were evaluated through microscopic and spectroscopic studies. Results: The viability assay of the prepared formulation exhibited a negligible reduction in SND-1 spores (99.5% to 86.55%) throughout the six months of storage period. In-vivo (Greenhouse) study exhibited increased growth parameters in alginate pellet formulation of SND-1challenged with Cercospora pathogen (SND-1+Pathogen) treated mung bean plants in comparison with Control (SDW) and only pathogen infested plants. Consequently, the plants with SND-1+Pathogen treatment showed significant reduction in disease severity up to 56%. Furthermore, the microscopic evaluation of histochemical defense markers depicted increased deposition of lignin (82.43±0.31%), H2O2 (47.97±0.66%), and phenol (76.74±0.79%) and cell death analysis through microscopic observation exhibited lesser dead cells of 31% in SND-1+Pathogen treatment in comparison with other treatments. Defense patterns at biochemical level hinted the elevation in activities of defense enzymes like PAL, GLU and POX at 12 and 24 h post pathogen inoculation (hpi) in SND-1+Pathogen treatment. The formulation treatment with pathogen (SND-1+Pathogen) also substantiated that enhanced total phenolic, flavonoid, and chlorophyll contents at different time intervals. Conclusions: Overall the present investigation showed that Amycolatopsis sp. SND-1 formulation confers the protection in mung bean upon Cercospora infection and it might be an effective eco-friendly approach towards sustainable agriculture.

Objectives: The ecological niche of soil for microorganisms that produce beneficial naturally occurring and biologically active products suitable for pharmaceutical industries is widely recognized. The purpose of the current study is to isolate fungus from soil samples of Dandeli, Karnataka and its metabolic profiling and investigating biological activities. Methods: Soil fungal isolates were screened for their antimicrobial potency against pathogens. The selected fungal isolate was morphologically characterized and ascertained by 18S rRNA gene sequencing, and the extract was investigated by gas chromatography-mass spectrometry (GC–MS) to identify the bio-molecules. Later the fungal extract was evaluated for antioxidant, antimicrobial, anti-mycobacterial and anti-proliferative activity against Human acute leukemia (K562) cell line. Results: The potential fungal isolate, Alternaria sp. KUDB15 showed a number of bioactive compounds through GC–MS analysis. A significant antioxidant activity (IC50 = 37.60 µg/ml) was also reported for this organism. A significant inhibitory activity against tested pathogens was shown by Alternaria sp. KUDB15 along with a strong anti-mycobacterial activity with an IC50 value of 3.12 μg/ml. During anticancer assay, this organism showed a concentration dependent reduction in cell viability having IC50 of 112.09 µg/ml. Further purification of the crude extract with column chromatography and thin layer chromatography (TLC) recorded several bands and the particular band having antibacterial activity was determined by bioautography. Conclusions: In the present research, the in vitro evaluation of biological activities of the fungal extract suggested that it might serve as a useful foundation for the discovery of compounds that have potential for medical applications. Additional research is required to identify and understand the structure of bio-molecules.

Using natural dyes in dyeing industries becomes an alternative to synthetic dyes, which are known to contain harmful chemicals that can pose risks to the environment and human health. This study involves the extraction of yellow dye from Cassia alata flower petals, optimization of the extraction process using an ultrasonic bath (40 KHz and an input power of 500), ultrasonic probe (390 W, 455 W, 520 W, 585 W, and 650 W), and conventional heating (heating mantle with 30 °C, 40 °C, 50 °C, 60 °C, and 70 °C), characterization of the dye, as well as dyeing (cotton, silk, and leather) without using a mordant. The extracted yellow dye was further evaluated to determine its antibacterial activity against skin bacteria. Dye extraction optimization using UV–Visible spectrophotometric analysis revealed that the maximum yellow color in methanol extract (287 and 479 nm) was obtained at 50 °C for 45 min using ultrasonic water bath extraction, followed by the ultrasonic probe and direct heating. Based on the FTIR spectra, it is evident that OH is present at approximately 3300 cm−1, while CH stretches at around 2900 cm−1. A characteristic peak at 1608 cm−1 bears a striking similarity to anthraquinonoid-based compounds. Also, using the ultrasonic water bath dyeing technique at 50 °C for 45 min, the yellow color of cotton, silk, and leather was dyed optimally. Due to effective color removal after two washings with boiling soap liquid, the dyed cotton and silk fabric displayed good washing and rubbing fastness. Regarding antibacterial activity, the dye was highly active against all pathogens after extraction in methanol. The maximum inhibition was observed against Pseudomonas sp. with a MIC value of 1.56 mg/ml.

New class of highly functionalized dispiropyrrolidine tethered indandione heterocycles in good yield were obtained through stereo- and regioselective single-pot three component cycloaddition methodology between benzylidene-indandione and non-stabilized azomethine ylide. The ylide generated from active diketone and aminophenylpropanoic acid via dehydration/decarboxylative pathway. The synthesized dispiropyrroldine comprising indandiones were elucidated through 1H and 13C NMR spectroscopic analysis, the stereo and regioselective formation of the dispiropyrrolidine were unequivocally assigned by X-ray diffraction analysis. Compound thus synthesized were assayed as potential inhibitor for the treatment of AD. Spiropyrrolidine 4h that bearing methoxy group on the phenyl ring showed significant activity, IC50 of 3.24 ± 0.25 and 10.25 ± 0.16 μM against acetyl and butyryl cholinesterase enzyme, respectively. The lead compound 4h executed to investigate for their docking simulation that showed strong binding affinity with binding site of the cholinesterase protein.

Employing naturally extracted dyes and their derivatives as photosensitizers towards the construction of dye-sensitized solar cells (DSSCs) has been recently emerging for establishing sustainable energy conversion devices. In this present work, Rhodobacter Sphaeroides Photobacteria (Rh. Sphaeroides) was used as a natural source from which Bacteriopheophytine-a (Bhcl) dye was extracted. Further, two cationic derivatives of Bhcl, viz., Guanidino-bacteriopheophorbide-a (Gua-Bhcl) and (2-aminoethyl)triphenylphosphono-bacteriopheophorbide-a (2AETPPh-Bhcl) were synthesized. The thus obtained Bhcl, Gua-Bhcl and 2AETPPh-Bhcl were characterized using liquid chromatography–mass spectrometry (LC–MS) and their photophysical properties were investigated using excitation and emission studies. All three near-infrared (NIR) responsive dyes were employed as natural sensitizers towards the construction of DSSC devices, using platinum as a photocathode, dye-sensitized P25-TiO2 as a photoanode and I−/I3− as an electrolyte. DSSCs fabricated using all three dyes have shown reasonably good photovoltaic performance, among which 2AETPPh-Bhcl dye has shown a relatively higher power conversion efficiency (η) of 0.38% with a short circuit photocurrent density (JSC) of 1.03 mA cm−2. This could be attributed to the dye’s natural optimal light absorption in the visible and NIR region and uniform dispersion through the electrostatic interaction of the cationic derivatives on the TiO2 photoanode. Furthermore, the atomic force microscopy studies and electrochemical investigations using cyclic voltammetry, electrochemical impedance spectroscopy and Bode’s plot also supported the enhancement in performance attained with 2AETPPh-Bhcl dye.

Marine actinomycetes represent a highly favorable source of bioactive compounds and have been the mainstay of much research in recent years. Recent reports have shown that marine Streptomyces sp. can produce compounds with diverse and potent biological activities. Therefore, the key objective of the study was to isolate and screen a potential actinomycete from marine ecosystems of Devbagh and Tilmati beaches, Karwar. Streptomyces sp. KS20 was characterized and the ethyl acetate extract (EtOAc-Ex) was screened for biomedical applications. Streptomyces sp. KS20 produced grayish-white aerial and pale-yellow substrate mycelia and revealed an ancestral relationship with Streptomyces violaceusniger. Optimum growth of the organism was recorded at 30 °C and pH 7.0. The metabolite profiling of EtOAc-Ex expressed the existence of several bioactive metabolites, whereas the functional groups were indicated by Fourier transform infrared (FTIR) spectroscopy. A considerable antioxidant activity was shown for EtOAc-Ex with IC50 of 92.56 μg/mL. In addition to this, Streptomyces sp. KS20 exhibited significant antimicrobial properties, particularly against Escherichia coli, where a zone of inhibition measuring 36 ± 0.83 mm and a minimum inhibitory concentration (MIC) of 3.12 µg/mL were observed. The EtOAc-Ex even revealed significant antimycobacterial potency with IC50 of 6.25 μg/mL. Finally, the antiproliferative potentiality of EtOAc-Ex against A549 and PC-3 cell lines revealed a constant decline in cell viability while raising the concentration of EtOAc-Ex from 12.5 to 200 μg/mL. The IC50 values were determined as 94.73 μg/mL and 121.12 μg/mL for A549 and PC-3 cell lines, respectively. Overall, the exploration of secondary metabolites from marine Streptomyces sp. KS20 represents an exciting area of further research with the potential to discover novel bioactive compounds that could be developed into therapeutics for various medical applications.

Background: Aggressive antimicrobial infections together with an increasing in resistance to antimicrobial medications cause a threat to immunocompromised individual. In this context, spiro compounds play an important role in drug discovery research due to their diverse biological activities including antimicrobial activity which is well documented in literature, because of their unique structural properties allow for easy interaction with the target enzyme of the biological system. This biological precedent encouraged us to design and synthesis of novel dispirooxindolopyrrolidine hybrid heterocycles via multicomponent cycloaddition protocol. Materials and methods: Novel class of dispirooxindolopyrrolidine hybrid heterocycles has been synthesized by multicomponent 1,3-dipolar cycloaddition methodology and the structure of the products was determined through spectroscopic analysis. The synthesized organic compounds were evaluated for their antimicrobial activities using sensitivity test with standard agar well diffusion method. Results: The synthesized new class of dispiropyrrolidine embedded indandione hybrids showed significant antimicrobial activity against carbapenemase producing Klebsiella pneumoniae (CKPs) isolated from hospital patients. Compound that possessing chlorine substituted on the aryl ring exhibited more potent antimicrobial activities and the zone of inhibitions was observed between 7.00 ± 0.09 and 18.40 ± 0.70 mm. The MIC value of compound 4b was 0.030 mg/mL against tested CKP. Conclusion: A new class of dispiropyrrolidine heterocyclic hybrids were synthesized in good to excellent yield employing multicomponent 1,3-dipolar cycloaddition strategy. Among them, compounds bearing 4-chloro substituted on the aryl ring exhibited notable activity just equal to the standard drug, ciprofloxacin. Future studies are needed to elucidate the pharmacological properties of new compounds that were synthesized in our laboratory for the novel therapeutic development.

Background: Microbial infections together with rising drug resistance pose a threat to immunocompromised individual. In this perspective, compounds with spirooxindolopyrrolidine play a significant role in research on antimicrobial drug delivery research owing to their various pharmaceutical activities. Spiroheterocyclic compounds are present in number of medications as active motif due to their exceptional structural properties which enable for easy interaction with the protein of the biological target. Inspired by this biological precedent encouraged to synthesize a new class of dispirooxindole fused pyrrolidine heterocycles via a three-component cycloaddition strategy. Materials and Methods: The new class of structurally intriguing spirooxindolopyrrolidines were synthesized through three component cycloaddition process and the structure of products were assigned through spectroscopic analysis. The newly synthesized compounds were assessed for their antimicrobial sensitivity test with standard Kirby Bauer method with common drugs. Results: The structurally unexplored hybrid heterocycles fused spirooxindolopyrrolidine exhibited excellent antimicrobial activity against the common nosocomial microbial pathogens. Of four compounds, the compound bearing a chlorine atom on the aryl ring (4a) exhibited significant antimicrobial activity (zone of inhibition: 9.00 ± 1.00–17.00 ± 0.35 mm and MIC: 16.00–256.00 μg/mL) against selected nosocomial infection causing microbial pathogens. Hence, the compound 4a has been considered as an effective drug of interest in therapeutic field for compacting infectious diseases causing pathogens. Conclusion: With an aim of developing more effective and economically more affordable antimicrobial leads with a unique mechanism of action, we have designed and synthesized structurally diverse spirooxindolopyrrolidine tethered hybrids that has been assayed against multidrug resistant nosocomial pathogens. The regioisomer having chloro substituted on the phenyl ring showed potent activity when compared to standard drug. Future studies are required to explicate the pharmacological properties of new hybrid heterocycles that have been synthesized in our laboratory for the novel therapeutic development.

Structurally interesting chromeno-quinolines were constructed via the cyclization reaction of O-propargylated naphthaldehyde and substituted anilines in good yields. We explored compound methyl-chromenoquinoline (MCQ) in detail for its optical properties using Time-dependent density-functional theory (TD-DFT) and experimental studies. The conjugated-polymer (CP) Poly[(9,9-dioctylfluorenyl-2,7-diyl)-co-(2,5-p-xylene)] or [(ADS145UV or PFOPX)] was studied as donor. The TD-DFT implied that MCQ is a fluorescent compound with well-defined highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) structure at −5.327 eV and −1.836 eV, respectively, with an energy gap of 3.49 eV in toluene captivity. The TD-DFT-based model and experimental study showed an energy gap of 3.326 eV and 3.351 eV, respectively, and the deviation was 0.025 eV. The experimental studies of MCQ showed solvent-dependent fluorescence peak shifted from 445 ± 2 nm to 538 ± 2 nm for dielectric constant ranging from 0.01 (hexane) to 10.2 (water). Despite the good optical properties, MCQ produced a weak laser-induced fluorescence (LIF) and not produce amplified spontaneous emission (ASE) to any pump energy of 3rd harmonic from Nd:YAG laser (5 ns, 355 nm). When PFOPX of concentration 500 nM (500 μL) was added to MCQ of 506 mM (3.5 mL) concentration, the LIF suddenly improved tenfold due to efficient Fluorescence resonance energy transfer (FRET) process. At the optimal concentration of PFOPX (670 nM) in MCQ solution, the spectrum changed dramatically. The spectrum has five peaks with a LIF in the background, where peaks around 393.5 nm and 417.3 nm attribute to the oligomer; 438.7 nm attributed to a combined fluorescence of PFOPX and MCQ; 466.4 nm, and 493.1 nm corresponding to MCQ. Analysis shows that the peaks at 440 nm (partly) and 493 nm were ASE from MCQ.

Green nanoparticle (NPs) synthesis is eco-friendly, non-toxic, and the NPs have demonstrated improved biocompatibility for use in healthcare. This study evaluated the biogenic synthesis of AgNPs from the leaves of Cardamine hirsuta L. and their biological properties. The UV-Vis. spectra at 411 nm exhibited a distinct resonance spectrum for C-AgNPs produced from C. hirsuta L. FT-IR analysis exhibited the presence of functional groups of phyto-compounds of C. hirsuta responsible of silver salt reduction and capping agents of C-AgNPs. The microscopic-based study, such as HR-TEM analysis, showed that the particles were uniformly distributed, spherical, and ranged in size from 5.36 to 87.65 nm. EDX analysis confirmed a silver (Ag) content of 36.3% by weight, and XRD analysis exhibited the face-centred cubic (FCC) crystalline nature of C-AgNPs. DLS measured the mean particle size of 76.5 nm. The zeta potential was significant at −27.9 mV, and TGA analysis revealed that C-AgNPs had higher thermal stability. C-AgNPs demonstrated moderate antimicrobial activity against the tested pathogens. In addition, the anti-proliferative activity measured by the MTT assay on the Caco-2 cell line demonstrated decreased cell viability with increasing C-AgNPs dosage, with an IC50 concentration of 49.14 µg/mL. In addition, an Annexin-V/Propidium iodide flow cytometric study was utilized to evaluate the induction of apoptosis in cancer cells. Early and late apoptosis cell populations increased significantly compared to the untreated control. Therefore, green-synthesized C-AgNPs have significant antimicrobial and anti-proliferative abilities, making them intriguing options for future biomedical applications.

The actinomycete strain HSN-02 was isolated from the soil of a mining field in the Sandur region, Bellary, Karnataka, India. According to the morphological, cultural, physiological, and biochemical characteristics and the 16S rDNA sequence analysis, the strain HSN-02 was identified as Amycolatopsis sp. The antimicrobial activity strain HSN-02 presented stable and moderate inhibitory activity against human pathogens. In pot experiments in the greenhouse, the development of Cercospora leaf spot was markedly suppressed by treatment with the purified compound from the strain HSN-02, and the control efficacy was 45.04 ± 1.30% in Septoria lycopersici-infected tomato plants. A prominent compound was obtained from the fermentation broth of the strain HSN-02 using column chromatography and HPLC. The chemical structural analyses using UV, FTIR, HR-ESI-MS, and NMR confirmed that the compound produced by the strain HSN-02 is 7-hydroxyflavone. This investigation showed the role which the actinomycete strain can play in controlling leaf spots caused by S. lycopersici to reduce treatments with chemical fungicides.

The present study demonstrated the isolation, characterization, and antimicrobial and anticancer activity of active metabolite produced from mining-soil-derived actinomycetes. Among the 21 actinomycete isolates, the isolate HSN-01 exhibited significant antimicrobial activity in primary screening and was identified as Streptomyces sp. through 16S rRNA gene sequencing. The active metabolite was separated, purified, and confirmed through UV–Vis spectroscopy, FTIR, HR-ESI-MS, and NMR analysis and identified as pyraclostrobin. Further, the active metabolite pyraclostrobin was tested for antimicrobial and anticancer activity against the hepatocellular carcinoma (HepG2) cell line. The metabolite exhibited maximum antimicrobial potential with 17.0, 13.33, 17.66, 15.66, 14.66, and 14.0 mm of inhibition against B. cereus, S. aureus, E. coli, P. aeruginosa, S. flexneri, and C. glabrata. The active metabolite exhibited dose-dependent anticancer potential against the hepatocellular carcinoma (HepG2) cell line with the IC50 56.76 µg/mL. This study suggests that Streptomyces sp. HSN-01 is an excellent source of active secondary metabolites with various biological activities.

Biosynthesized nano-composites, such as silver nanoparticles (AgNPs), can be engineered to function as smart nano-biomedicine platforms for the detection and management of diverse ailments, such as infectious diseases and cancer. This study determined the eco-friendly fabrication of silver nanoparticles using Lagerstroemia speciosa (L.) Pers. flower buds and their efficacy against antimicrobial and anticancer activities. The UV-Visible spectrum was found at 413 nm showing a typical resonance spectrum for L. speciosa flower bud extract-assisted silver nanoparticles (Ls-AgNPs). Fourier transform infrared analysis revealed the presence of amines, halides, and halogen compounds, which were involved in the reduction and capping agent of AgNP formation. X-ray diffraction analysis revealed the face-centered cubic crystals of NPs. Energy dispersive X-ray verified the weight of 39.80% of silver (Ag), TEM analysis revealed the particles were spherical with a 10.27 to 62.5 nm range, and dynamic light scattering recorded the average particle size around 58.5 nm. Zeta potential showed a significant value at −39.4 mV, and finally, thermo-gravimetric analysis reported higher thermal stability of Ls-AgNPs. Further, the obtained Ls-AgNPs displayed good antimicrobial activity against clinical pathogens. In addition, a dose-dependent decrease in the anticancer activity by MTT assay on the osteosarcoma (MG-63) cell line showed a decrease in the cell viability with increasing in the concentration of Ls-AgNPs with an IC50 value of 37.57 µg/mL. Subsequently, an apoptotic/necrosis study was conducted with the help of Annexin-V/PI assay, and the results indicated a significant rise in early and late apoptosis cell populations. Therefore, green synthesized Ls-AgNPs were found to have potent antimicrobial and anticancer properties making them fascinating choices for future bio-medical implementations.

Stem cells serve as an ideal source of tissue regeneration therapy because of their high stemness properties and regenerative activities. Mesenchymal stem cells (MSCs) are considered an excellent source of stem cell therapy because MSCs can be easily obtained without ethical concern and can differentiate into most types of cells in the human body. We prepared cell culture materials combined with synthetic polymeric materials of poly-N-isopropylacrylamide-co-butyl acrylate (PN) and extracellular matrix proteins to investigate the effect of cell culture biomaterials on the differentiation of dental pulp stem cells (DPSCs) into neuronal cells. The DPSCs cultured on poly-L-ornithine (PLO)-coated (TPS-PLO) plates and PLO and PN-coated (TPS-PLO-PN) plates showed excellent neuronal marker (βIII-tubulin and nestin) expression and the highest expansion rate among the culture plates investigated in this study. This result suggests that the TPS-PLO and TPS-PN-PLO plates maintained stable DPSCs proliferation and had good capabilities of differentiating into neuronal cells. TPS-PLO and TPS-PN-PLO plates may have high potentials as cell culture biomaterials for the differentiation of MSCs into several neural cells, such as cells in the central nervous system, retinal cells, retinal organoids and oligodendrocytes, which will expand the sources of cells for stem cell therapies in the future.

Preparing electrode materials plays an essential role in the fabrication of high-performance supercapacitors. In general, heteroatom doping in carbon-based electrode materials enhances the electrochemical properties. Herein, nitrogen, oxygen, and sulfur co-doped porous carbon (PC) materials were prepared by direct pyrolysis of Anacardium occidentale (AO) nut-skin waste for high-performance supercapacitor applications. The as-prepared AO-PC material possessed interconnected micropore/mesopore structures and exhibited a high specific surface area of 615 m2 g−1. The Raman spectrum revealed a moderate degree of graphitization of AO-PC materials. These superior properties of the as-prepared AO-PC material help to deliver high specific capacitance. After fabricating the working electrode, the electrochemical performances including cyclic voltammetry, galvanostatic charge–discharge, and electrochemical impedance spectroscopy measurements were conducted in 1 M H2SO4 aqueous solution using a three-electrode configuration for supercapacitor applications. The AO-PC material delivered a high specific capacitance of 193 F g−1 at a current density of 0.5 A g−1. The AO-PC material demonstrated −1. All the above outcomes confirmed that the as-prepared AO-PC from AO nut-skin waste via simple pyrolysis is an ideal electrode material for fabricating high-performance supercapacitors. Moreover, this work provides a cost-effective and environmentally friendly strategy for adding value to biomass waste by a simple pyrolysis route.

Amyotrophic lateral sclerosis (ALS) is a multi-systemic, incurable, amyloid disease affecting the motor neurons, resulting in the death of patients. The disease is either sporadic or familial with SOD1, C9orf72, FUS, and TDP-43 constituting the majority of familial ALS. Multi-omics studies on patients and model systems like mice and yeast have helped in understanding the association of various signaling and metabolic pathways with the disease. The yeast model system has played a pivotal role in elucidating the gene amyloid interactions. We carried out an integrated transcriptomic and metabolomic analysis of the TDP-43 expressing yeast model to elucidate deregulated pathways associated with the disease. The analysis shows the deregulation of the TCA cycle, single carbon metabolism, glutathione metabolism, and fatty acid metabolism. Transcriptomic analysis of GEO datasets of TDP-43 expressing motor neurons from mice models of ALS and ALS patients shows considerable overlap with experimental results. Furthermore, a yeast model was used to validate the obtained results using metabolite addition and gene knock-out experiments. Taken together, our result shows a potential role for the TCA cycle, cellular redox pathway, NAD metabolism, and fatty acid metabolism in disease. Supplementation of reduced glutathione, nicotinate, and the keto diet might help to manage the disease.

Currently, the exploration of fungal organisms for novel metabolite production and its pharmacological applications is much appreciated in the biomedical field. In the present study, the fungal strains were isolated from soil of unexplored Yellapura regions. The potent isolate NP5 was selected based on preliminary screening and identified as Penicillium brasilianum NP5 through morphological, microscopic, and molecular characterizations. Synthesis of silver nanoparticles from P. brasilianum was confirmed by the color change of the reaction mixture and UV-visible surface plasmon resonance (SPR) spectra of 420 nm. Fourier transform infrared (FTIR) analysis revealed the functional groups involved in synthesis. Atomic force microscopy (AFM) and transmission electron microscope (TEM) analysis showed aggregation of the NPs, with sizes ranged from 10 to 60 nm, an average particle size of 25.32 nm, and a polydispersity index (PDI) of 0.40. The crystalline nature and silver as the major element in NP5-AgNPs was confirmed by X-ray diffraction (XRD) and energy dispersive X-ray (EDX) analysis. The negative value −15.3 mV in Zeta potential exhibited good stability, and thermostability was recorded by thermogravimetric analysis (TGA). NP5-AgNPs showed good antimicrobial activity on selected human pathogens in a concentration-dependent manner. The MTT assay showed concentration-dependent anticancer activity with an IC50 of 41.93 µg/mL on the MDA-MB-231 cell line. Further, apoptotic study was carried out by flow cytometry to observe the rate of apoptosis. The calculated sun protection factor (SPF) value confirms good photoprotection capacity. From the results obtained, NP5-AgNPs can be used in the pharmaceutical field after successful in vitro clinical studies.

A Novel class of 1,4-disubstituted 1,2,3-triazoles have been synthesized in good to excellent yields via Cu(I) accelerated azide-alkyne click chemistry reaction strategy. The newly synthesized compounds were assessed for their in vitro antimicrobial activity against five Gram-positive, seven Gram-negative bacteria and three fungi. Most of the synthesized compounds displayed significant activity against the tested Gram-positive and Gram-negative bacteria. Molecular docking study revealed that all docked compounds are bound efficiently with the active site of Topoisomerase IV (4EMV) receptor with the observed the free energy of binding from −7.79 to −9.44 kcal/mol. Interestingly, compound 13a forms four hydrogen bonds and displayed high binding energy (−9.44 kcal/mol) with the Topoisomerase IV (4EMV) receptor which correlated with their in vitro antimicrobial assays.

Background: Healthcare-associated infections (HAI) are prime health task worldwide and issue of patient safety besides intensifying antimicrobial drug resistance. It is essential to formulate structurally fascinating novel, active and cost-effective anti-microbial drugs possessing a peculiar way of action and capable of overcoming the resistance to effectively combat this disease. Materials and methods: The synthesized spiro-heterocyclic hybrids (SHHs) were elucidated through spectroscopic analysis and were assessed for their in vitro antimicrobial activity by agar diffusion method and minimal inhibitory concentration (MIC) value was also determined. In addition, antioxidant potential was also evaluated through DPPH radical scavenging assays. Results: The novel class of SHHs 4a and 4b displayed significant antibacterial activity against selected healthcare associated microbial pathogens (HAMPs). In addition, SHH 4b showed potent antioxidant properties. Conclusion: Antibacterial and antifungal activity of dispirooxindolopyrrolidine fused acenaphthenone heterocyclic hybrids were examined. Interestingly, SHH 4b exhibited potent antimicrobial activity against selected HAMPs. Further, these compounds were also showed potent antioxidant properties. These results revealed that SHH 4b is a promising lead for the development of new antimicrobial drugs.

An expedient regioselectivesynthesis of novel mono, C2-symmetric bis-triazole and acridinedione bridged macromolecules has been achieved in good yields employing intermolecular Cu(I) catalyzed azide and alkyne click reaction. Synthesis of O-propargyl acridinedione was achieved in three good yielding steps starting from dimedone, while the symmetrical aliphatic and aryl bis-azides were derived from appropriate dibromides in the presence of sodium azide in dry DMF. The synthesized mono and C2-symmetric bis-macromolecules have been elucidated by 1H, 13C, elemental and mass spectroscopic analysis. The antioxidant activity of synthesized compounds has also been investigated.

A small library of hitherto unexplored novel 5-fluorobenzoisoxazolyl-piperidinyl-1, 2, 3-triazole derivatives has been synthesized from 2-azido-fluorobenzoisoxazolyl piperidinyl ethanone and various alkynes in good to excellent yields through a click chemistry approach. Compounds thus synthesized were evaluated for their cytotoxicity against HepG-2 and A549 cancer cells. Interestingly, compounds 4c, 4d, 4e and 4h displayed significant cytotoxicity against HepG-2 and A549 cancer cells. Toxicity study of active compounds was compared with human normal lung IMR-90 cells. Molecular docking has also been investigated for 4a-i with Chk1 protein and the compounds 4c and 4h displayed reasonable molecular interactions with good docking scores.

An efficient, eco-friendly and sustainable approach for the synthesis of novel spiroindeno[1,2-b]quinoxaline-3-phenylspiro[4,3″]benzylidenepiperidone ring system has been developed by a one-pot four component [3 + 2] cycloaddition strategy. The 1,3-dipole generated in situ from quinoxalinone and l-phenylalanine reacts with the highly functionalized dipolarophiles, bisarylidene piperidones affording spirohybrid heterocycles in good yields. The unexplored novel class of dispirohybrid heterocycles obtained possess three CN and two CC bonds with four adjacent stereogenic carbons, out of which two is spirocarbons. The structure of compounds was elucidated using 1H, 13C and mass spectroscopic studies.

A versatile green chemical procedure for the highly selective construction of 2-aryl substituted benz-/naphthimidazoles starting from the reaction of aromatic 1,2-diamines with a series of substituted arylthioprolines with three to five drops of water under simple grinding at ambient temperature in good yields is described. The short reaction time, simplified experimental procedure, the absence of extraction and chromatographic purification steps in addition to the environment affability makes this green strategy highly attractive in view of green chemistry. The expected reaction to furnish the thiazole grafted benz-/naphthimidazole did not occur. Perhaps the arylthioprolines could be in zwitterionic form, which could react with 1,2-diamine giving dihyrobenzimidazole, which undergoes air oxidation to furnish the 2-aryl benzimidazole rather than the expected thiazole grafted imidazoles.

A novel polycyclic cage-like heterocyclic hybrid comprising several privileged structures such as pyrroloisoquinoline, 4-pyridinone and a α,β -unsaturated ketone moiety has been synthesized in good yield employing a microwave mediated [3 + 2]-cycloaddition/annulation strategy in 1-butyl-3-methylimidazolium bromide ([bmim]Br). The compound thus synthesized was analyzed for in vitro anticancer activity employing MCF-7, Jurkat, HCT 116 and NCI-H460 cell lines. The effect of polycyclic cage-like heterocyclic hybrid on cells viability was analyzed by MTT assay and its DNA damage efficiency was confirmed by several examinations like apoptosis study, cell cycle analysis, caspase-3 expression analysis and TUNEL assay. Mitochondrial membrane potential was determined by JC-1 staining. The polycyclic cage-like heterocyclic hybrid bearing diverse functionalities played a major role in DNA damage of cancerous cells and in consequence inhibited the DNA cells proliferation.

Spiropyrrolidine engrafted ferrocene heterocycles were synthesized in excellent yields in a sustainable fashion employing an ionic liquid, 1-butyl-3-methylimidazoliumbromide accelerated one-pot multicomponent cycloaddition strategy. The in situ 1,3-dipole component derived from indenoquinoxalinone and L-phenylalanine that reacts with various substituted ferrocenyl chalcone in [bmim]Br affording spirocycloadduct.

Methyl orange dye-doped K2SO4 single crystal has been synthesized by a slow evaporation method, and its properties have been investigated. The powder X-ray diffraction (PXRD) studies on the single crystal confirmed the crystalline property, noncentrosymmetric system, and the space group P63/mmc (D64th) of crystal. The reaction involved in the functional group of the grown crystal has been confirmed from the FTIR analysis. The optical properties of absorbance and band gap were calculated from the UV-Vis analysis. The obtained materials were identified from the EDX analysis. The electron transformation and optical distortion were identified at 270 nm in the photoluminescence study. The transmission electron microscopy method analyzed the morphology of the grown crystal. The dielectrics of the grown crystal were studied. The effect of temperature on the grown crystal was studied using the TG/DTA analysis. The bacterial susceptibility of the grown crystal was evaluated from Gram-positive and Gram-negative bacteria. All the results demonstrated that the grown crystal is suitable for optical, electronic, and bacterial applications.

Objective: The bio-synthesis of silver nanoparticles (AgNPs) is regarded as environment friendly and cost effective method compared to physical and chemical synthesis methods. Silver (Ag) is an important noble metal due to its tremendous use in research and medical fields throughout the world. This research work was aimed at green synthesis and characterizations of AgNPs from G. glauca leaf extract and evaluation of their bioactive potential. Methods: In the current research work, synthesis of AgNPs from G. glauca aqueous leaf extracts was performed and was characterized by UV–Visible (UV–Vis.), Fourier transform infrared (FTIR), Atomic force microscopy (AFM), Scanning electron microscopy (SEM), Energy dispersive spectroscopy (EDS), High-resolution transmission electron microscopy (HR-TEM), X-ray diffraction (XRD), Thermo gravimetric analysis (TGA) and Zeta potential exploration. Later, antioxidant, antimicrobial activity was examined against various pathogenic organisms and anticancer activities of AgNPs were carried out against SK-HEP1 cell line. Results: The first indication of synthesis of nanoparticles was the change in color from yellowish to brown. UV–Vis. band exhibited surface plasmon resonance (SPR) at 402 nm. FTIR analysis revealed the probable bio-molecules including alkanes, alkenes, aromatics, aromatic phosphates, imine or oxime, etc. subjected to reduction of silver ions to metallic silver. The AFM, SEM and TEM analysis reported the particles were spherical shaped, poly-dispersed, 17 to 40 nm in size. The zeta potential analysis expressed a peak at –32.0 ± 0.5 mV and suggested the particles with significant long term stability. The TGA analysis revealed the stability of AgNPs at high temperature (179 ℃). The antioxidant assay of AgNPs unveiled an effective dose dependent increase in scavenging activity. Antimicrobial activity showed efficient inhibitory activity against P. aeruginosa and C. glabrata. Lastly, the AgNPs revealed a strong anticancer activity against SK-HEP1 liver cancer cell line with an IC50 value of 19.12 μg/mL. Conclusions: Therefore, it could be concluded that a substantial in-vivo investigations are needed for antioxidant, antibacterial and anticancer activities, so that it will be useful in medical field in future.

The aqueous extract of Alternanthera sessilis (As) acts as the precursors for the quick reduction of silver ions, which leads to the formation of silver nanoparticles. In the agar, well diffusion method of the Klebsiella pneumoniae shows the minimal inhibitory concentration of 12 mm against A. sessilis mediated silver nanoparticles (As-AgNPs) at 60 µg/mL concentration. Fabric treated with novel AS-AgNPs is tested against the K. pneumoniae and shows an inhibitory action of 12 mm with mixed cotton that determines the antimicrobial efficacy of the fabrics. Uv- visible spectrophotometer was performed, showing a surface plasmon resonance peak at 450 nm cm−1. FTIR shows the vibration and the infrared radiation at a specific wavelength of 500–4000 cm−1. The HR-TEM analysis showed the presence of black-white crystalline, spherical-shaped As-AgNPs embedded on the fabrics range of 15 nm–40 nm. In the scanning electron microscope, the presence of small ball-shaped As-AgNPs embedded on the fabrics at a voltage of 30 KV was found with a magnification of 578X. EDAX was performed in which the nanoparticles show a peak of 2.6–3.9 KeV, and it also reveals the presence of the composition, distribution, and elemental mapping of the nanoparticles. The cytotoxic activity of synthesized nanosilver was carried out against L929 cell lines, which show cell viability at a concentration of 2.5 µg mL−1. Cell proliferation assay shows no cytotoxicity against L929 cell lines for 24 h. In this study, the green synthesis of silver nanoparticles from A. sessilis appears to be a cheap, eco-friendly, and alternative approach for curing infectious ulcers on the floor of the stratum corneum. Nanotechnology conjoined with herbal therapeutics provides a promising solution for wound management.

The present investigation was aimed at the evaluation of synthesis, characterization and antimicrobial activity of Ixora brachypoda DC. leaf extract mediated silver nanoparticles (AgNPs). The AgNPs were characterized by UV–Visible (UV–Vis) spectrophotometer, Fourier transform infrared spectroscopy (FTIR), Atomic force microscopy (AFM), Scanning electron microscopy (SEM) with Energy dispersive X-ray spectrometry (EDS), Transmission electron microscopy (TEM), Zeta potential and X-ray diffractometry (XRD). Finally, the antimicrobial activity of synthesized AgNPs was investigated against pathogenic microorganisms. The absorption peak, obtained at 423 nm in UV–Vis analysis, confirmed the synthesis of AgNPs and the presence of biological functional groups involved in the capping and stabilization were determined by FTIR analysis. The other characterizations revealed the details about the AgNPs as spherical, poly-dispersed and size ranging from 18 to 50 nm with an average diameter of 27.76 nm. The zeta potential was calculated to be −30.4 mV and the typical Bragg’s planes in the metallic silver range indicated the confirmation of AgNPs formation. The in-vitro analysis confirmed the antimicrobial potential of I. brachypoda leaf aqueous extract synthesized AgNPs, which effectively inhibited the growth of pathogens and it can be concluded that the I. brachypoda AgNPs can be used as broad-spectrum antimicrobials against multi-drug resistant microbial pathogens.

A stereo- and regioselective synthesis of hitherto unexplored novel class of β-lactam embedded spirooxindolopyrrolidine hybrid heterocycles have been accomplished via ionic liquid accelerated [3 + 2]-cycloaddition reaction process. The expected unusual lactonization/lactamization product could not be observed even in traces. The in vitro antimycobacterium tubercular activity of the synthesized spiroheterocyclic hybrids were assessed against Mycobacterium tuberculosis H37Rv. Among them, the compounds with no substitution and chlorosubstitution on the oxindole ring showed the most potent activity with a MIC 0.78 μg/mL and 1.56 μg/mL, respectively which were two-fold and equal activity than the standard drug, ethambutol (MIC = 1.56 μg/mL).

With an aim to construct novel anticancer drugs, a series of polycyclic heterocycles comprising diverse structural sub-units based on molecular hybridization strategy have been designed and synthesized through a three-component [3 + 2]-cycloaddition/annulation strategy. Anticancer evaluation of these compounds against MCF-7 and NCI-H460 cell lines revealed dose dependent reduction with noteworthy anticancer activity. Compound 4b inhibited MCF-7 and NCI-H460 cell lines with IC50 values 10.86 ± 0.94 and 9.17 ± 0.63 µM respectively. Further, apoptosis and cell cycle analysis revealed that this compound was able to prompt apoptosis at an early stage in MCF-7 cell line besides increasing the threshold of MMP and % of cells expressing FITC-dUTP. These results suggest that compound 4b is a potential molecule for the further exploration.

Novel spiro acenaphthylene pyrrolo[1,2-b]isoquinoline/pyrrolidine hybrids have been achieved through Pictet-Spengler/Eschweiler-Clarke reactions depending on the substitution in the benzyl ring. The in vitro biological efficacy of N-methyl spiropyrrolidine derivatives toward different cancer and non-cancer cell lines revealed that these novel spiro heterocyclic hybrids induced cancer cell death at moderate concentrations, while slight reduction in non-cancer cell viability at the higher concentrations. The analysis of cancer cells proved that the major pathway of cell death is apoptosis and in addition, the role of caspases is confirmed by the appearance of fluorescent cells in microscopic images. Therefore, this study indicates a sustainable way of treating cancer cells by inducing apoptotic pathways and associated caspases, while simultaneously protecting the non-cancer cells.

The one-pot four-component reaction of 3-(1H-indol-3-yl)-3-oxopropanenitriles, aromatic aldehydes, cycloalkanones and ammonium acetate occurred via a six-step tandem Knoevenagel condensation–nucleophilic addition to carbonyl–Michael addition–N-cyclization–elimination–air oxidation sequence to afford structurally intriguing indole–cycloalkyl[b]pyridine-3-carbonitrile hybrid heterocycles in excellent yields.

Abstract Background Spiropyrrolidine tethered piperidone heterocyclic hybrids were synthesized with complete regio- and stereoselectively in excellent yield via a tandem three-component 1,3-dipolar cycloaddition and subsequent enamine reaction in [bmim]Br. The synthesized compounds were evaluated for their anticancer activity against FaDu hypopharyngeal tumor cells. Findings Interestingly, most compounds displayed cytotoxicities similar to the standard anticancer agent bleomycin, with two of them (5a and 5g) being slightly more active than the reference drug. Conclusion Synthesized compounds have also been evaluated for their apoptosis-inducing properties in a cancer cell model, finding that treatment with compounds 5a–e led to apoptotic cell death.

Quinoline Schiff bases display potential applications in optoelectronics and laser fields because of their unique optical properties that arise from extensive delocalization of the electron cloud, and a high order of non-linearity. In this context, a new class of conjugated quinoline-derivative viz. N-(quinolin-3-ylmethylene)anilines were synthesized from 2-hydroxyquinoline-3-carbaldehyde in two good yielding steps. The ability of these imines to accept an electron from a donor is denoted by their electron acceptor number and sites, which is calculated using density functional theory (DFT). The optical properties such as FT-IR, Raman, UV-VIS, and EDS spectra were calculated using TD-DFT, which also provided the energy gap, HOMO-LUMO structure. The optical properties of the synthesized imino quinolines were experimentally studied using photoluminescence and absorption spectroscopy. The properties such as Stokes shift and quantum yield were calculated using experimental data. Furthermore, the compound bearing a methyl group on the aryl ring and ZnO nanoparticles (hydrothermally synthesized) were dissolved in toluene, and optically excited with a 355 nm nanosecond laser, which produced a random laser.

Cancer stem cells (CSCs) or cancer-initiating cells (CICs) are key factors for tumor generation and metastasis. We investigated a filtration method to enhance CSCs (CICs) from colon carcinoma HT-29 cells and primary colon carcinoma cells derived from patient colon tumors using poly(lactide-co-glycolic acid)/silk screen (PLGA/SK) filters. The colon carcinoma cell solutions were permeated via porous filters to obtain a permeation solution. Then, the cell cultivation media were permeated via the filters to obtain the recovered solution, where the colon carcinoma cells that adhered to the filters were washed off into the recovered solution. Subsequently, the filters were incubated in the culture media to obtain the migrated cells via the filters. Colon carcinoma HT-29 cells with high tumorigenicity, which might be CSCs (CICs), were enhanced in the cells in the recovered solution and in the migrated cells based on the CSC (CIC) marker expression, colony-forming unit assay, and carcinoembryonic antigen (CEA) production. Although primary colon carcinoma cells isolated from colon tumor tissues contained fibroblast-like cells, the primary colon carcinoma cells were purified from fibroblast-like cells by filtration through PLGA/SK filters, indicating that the filtration method is effective in purifying primary colon carcinoma cells.

With an aim to develop more effective and affordable anticancer agents possessing a unique mechanism of action, we designed and synthesized derivatives of spirooxindole-pyrrolidine heterocyclic hybrids in good yields through a one-pot three-component (3+2) cycloaddition strategy. The synthesized compounds were characterized thoroughly for the physicochemical properties by making use of FT-IR, NMR spectroscopy, and mass spectrometry. Further, these compounds have been evaluated for the influence of anticancer activity against HepG2 cells up to 200 µg/mL concentration. The highly active molecular scaffold was tested for the in-depth mechanistic studies, and it was found that the major pathway of cell death is apoptosis which occurs through the induction of reactive oxygen species followed by the involvement of caspases.