RESUMEN
Herein, luminous blue carbon quantum dots (CDs) employing Anisomeles indica (Catmint) were reported with imaging, self-targeting, and therapeutic effects on triple-negative breast cancer (TNBC, MDA-MB-231) cells. The salient features of CDs generated from catmint are as follows: i) optical studies confirm CDs with excitation-dependent emission; ii) high-throughput characterization authenticates the formation of CDs with near-spherical shape with diameter ranging between 5 and 15 nm; iii) CDs induce cytotoxicity (3.22 ± 0.64 µg/ml) in triple-negative breast cancer (TNBC, MDA-MB-231) cells; iv) fluorescence microscopy demonstrates that CDs promote apoptosis by increasing reactive oxygen species (ROS) and decreasing mitochondrial membrane potential; v) CDs significantly up-regulate pro-apoptotic gene expression levels such as caspases-8/9/3. Finally, our work demonstrates that catmint-derived CDs are prospective nanotheranostics that augment cancer targeting and imaging.
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Apoptosis , Carbono , Puntos Cuánticos , Transducción de Señal , Neoplasias de la Mama Triple Negativas , Puntos Cuánticos/química , Humanos , Apoptosis/efectos de los fármacos , Neoplasias de la Mama Triple Negativas/metabolismo , Neoplasias de la Mama Triple Negativas/patología , Neoplasias de la Mama Triple Negativas/tratamiento farmacológico , Carbono/química , Carbono/farmacología , Transducción de Señal/efectos de los fármacos , Especies Reactivas de Oxígeno/metabolismo , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Lamiaceae/química , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Antineoplásicos/farmacología , Antineoplásicos/químicaRESUMEN
Plant-derived phytocompounds are effective in treating a variety of ailments and disorders, the most common of which are bacterial infections in humans, which are a major public health concern. Flavonoids, one of the groups of phytocompounds, are known to have significant antimicrobial and anti-infective properties. Hence, the current study investigates the efficacy of the citrus flavonoid hesperidin methylchalcone (HMC) in addressing this major issue. The results of this study indicate that the anti-quorum sensing (anti-QS) action against Aeromonas hydrophila infections is exhibited with a decrease in biofilm development and virulence factors production through in vitro and in silico analyses. In addition, the qPCR findings indicate that HMC has antivirulence action on A. hydrophila by reducing the expression of QS-related virulence genes, including ahyR, ahyB, ahh1, aerA, and lip. Interestingly, HMC significantly rescued the A. hydrophila-infected zebrafish by reducing the internal colonization, demonstrating the in vivo anti-infective potential of HMC against A. hydrophila infection. Based on these results, this study recommends that HMC could be employed as a possible therapeutic agent to treat A. hydrophila-related infections in humans.
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Chalconas , Hesperidina , Animales , Humanos , Chalconas/farmacología , Hesperidina/farmacología , Hesperidina/metabolismo , Aeromonas hydrophila , Pez Cebra , Flavonoides/farmacología , Flavonoides/metabolismo , Biopelículas , Factores de Virulencia/genética , Proteínas Bacterianas/genética , Proteínas Bacterianas/metabolismoRESUMEN
Saudi Arabia has a rich culture of folk medicines and three such common herbs used by Saudi people for therapy of breast cancer are Turmeric (Kurkum) Curcuma longa, Chamomile (Babunaj) Matricaria chamomilla, and Aswaghantha (Aswaghadh) Withania somnifera. Hence, the present study aims to develop a polyherbal phytosome formulation by thin film hydration technique with a synergistic anti-cancer effect for the treatment of breast cancer. The phytosomes were standardized for their phytoconstituents by HPTLC and showed the best optimal properties with a mean vesicle diameter of less than 200 nm, zeta potential in the range of -24.43 to -35.70 mV, and relatively integrated structure with fairly uniform size on TEM. The in vitro MTT assay on MCF-7 breast cancer cell lines and MDA MB 231 breast adenocarcinoma cell lines was carried out. MTT assay on MCF-7 breast cancer cell lines indicated that plant extract-loaded phytosomes exhibited enhanced cytotoxic effects at IC50 values. of 55, 50, 45, 52, 42, 44, and 20 µg/mL compared to the extracts of C. longa, M. chamomilla, W. somnifera, and their combined extracts (80, 82, 74, 60, 70, 60, and 35 µg/mL respectively). Moreover, intracellular reactive oxygen species production was found to be higher for phytosomes treated cells at respective IC50 concentrations when compared to extracts. Overall, the developed polyherbal phytosomes were found to be effective and afford synergistic effects for breast cancer therapy.
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Antineoplásicos , Neoplasias de la Mama , Humanos , Femenino , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/metabolismo , Detección Precoz del Cáncer , Extractos Vegetales/farmacología , Extractos Vegetales/química , Células MCF-7 , Antineoplásicos/químicaRESUMEN
The present study reveals the plant growth-promoting (PGP) potentials and characterizes the antifungal metabolites of Kutzneria sp. strain TSII isolated from mangrove sediment soil through in vitro and in silico studies. In this study, Kutzneria sp. strain TSII was screened for PGP activities and the antifungal activities against Pithomyces atro-olivaceous, a leaf spot-associated pathogen in groundnut plants. The ethyl acetate extract of Kutzneria sp. strain TSII was purified using column chromatography, and the presence of various antimicrobial compounds was studied by gas chromatography-mass spectrometry (GC-MS) analysis. In silico modeling and docking were carried out to evaluate the antifungal potent of bioactive compound. Kutzneria sp. strain TSII produced proteases, phosphatases, ammonia, siderophores, cellulases, indole acetic acid (IAA), lipases, and amylases, indicating its ability to enhance the growth of plants. The ethyl acetate extract of Kutzneria sp strain TSII was found to be a potent inhibitor of fungal mycelial growth in the potato dextrose agar (PDA) plates. The GC-MS spectral study showed 24 antimicrobial compounds belonging to five chemical groups: phenolics, phthalates, fatty acid methyl esters (FAME), spiro, and fatty alcohols. In silico docking studies showed that phenol, 2,4-bis(1,1-dimethylethyl)-effectively attaches with the active site of mitochondrial F1F0 Adenosine triphosphate synthase enzymes of Pithomyces atro-olivaceous. Hence, it is clear that these antifungal compounds shall be formulated shortly to treat many plant fungal diseases in an eco-friendly manner.
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Actinobacteria , Antifúngicos , Ascomicetos , Simulación del Acoplamiento Molecular , Fenoles , Actinobacteria/química , Antifúngicos/química , Antifúngicos/farmacología , Ascomicetos/efectos de los fármacos , Sedimentos Geológicos/microbiología , Fenoles/química , Fenoles/farmacologíaRESUMEN
Biomass-derived carbon quantum dots have drawn special interest owing to their admirable photostability, biocompatibility, fluorescence, high solubility, sensitivity and environmentally friendly properties. In the present work, the Carbon Quantum Dots (CQDs) was synthesized from the Plectranthus amboinicus (Mexican Mint) leaves via the microwave-assisted reflux method. The strong absorption peaks observed from UV-vis spectra at 291 and 330 nm corresponds to the π-π* and n-π* transitions, respectively, reveal the formation of CQDs. The synthesized CQDs showed bright blue fluorescence under UV irradiation with a fluorescence quantum yield of 17% and a maximum emission of 436 nm in the blue region at an excitation wavelength of 340 nm. The HRTEM analysis elucidates that the synthesized CQDs were crystalline and spherical in shape with a particle size of 2.43 ± 0.02 nm. The FT-IR spectroscopy confirms the presence of the different functional groups such as -OH, -CH, CO and C-O. The chemical composition of CQD was revealed through XPS analysis. The synthesized CQDs were used as a fluorescent probe to detect different metal ions, where high selectivity was obtained for Fe3+ ions through quenching phenomenon. The emission intensity of CQD showed a good linear relationship with R2 = 0.9111 with the concentration of Fe3+ ions in the range of 0-15 µM. The fluorescence emission of CQD was turned OFF upon the binding of Fe3+ ions and turned - ON with the addition of ascorbic acid. With this fluorescent turn ON-OFF behaviour of CQD, the NOT and IMPLICATION logic gates were constructed and studied for different input conditions. The biocompatibility of CQD was tested via MTT assay using MCF7 breast cancer cell line, which revealed that CQD synthesized from the Mexican Mint leaves possess less cytotoxicity. Further, the prepared CQD was applied effectively as fluorescent probes in a cell imaging application.
Asunto(s)
Mentha , Puntos Cuánticos , Carbono , Microondas , Extractos Vegetales , Puntos Cuánticos/toxicidad , Espectroscopía Infrarroja por Transformada de FourierRESUMEN
Herein, we demonstrated a sustainable green approach for the preparation of fluorescent biocompatible carbon quantum dots by microwave-assisted reflux synthesis from Aloe barbadensis Miller (Aloe vera) extract. The Transmission Electron Microscopic images reveal that the as-prepared CQDs are spherical with less than 5 nm in size. The CQDs are amorphous, showed an excitation-independent behaviour, emitted blue fluorescence and have a fluorescence quantum yield of 31%. The presence of -OH groups contributed to the blue emission and helped CQDs to disperse uniformly in an aqueous solution. The prepared CQDs were employed as a photocatalyst for the environmental remediation to degrade the anionic dye, eosin yellow under visible light irradiation. The results showed that the CQDs exhibited excellent photocatalytic efficiency of 98.55% within 80 min and a 100% efficiency within 100 min. Further, the cytotoxic properties of as-prepared CQDs are investigated in the MCF-7 breast cancer cell line using MTT assay. The results demonstrated a notable reduction in cell viability in a dose-subjected manner, and the cell viability decreased to 50% (IC50) at a concentration of 52.2 ± 1.35 µg/mL. Furthermore, cellular internalization of CQDs in breast cancer cells is studied. As expected, CQDs are found to internalize by the cancer cells with blue emission as revealed by fluorescence microscope. In the end, CQDs in human breast cancer cells demonstrate the anti-proliferative effect and are found to be an impressive fluorescent probe for live-cell imaging, paving a path for its potential biomedical applications.
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Aloe , Puntos Cuánticos , Carbono , Colorantes Fluorescentes , Humanos , Microscopía Electrónica de Transmisión , Puntos Cuánticos/toxicidadRESUMEN
The present investigation reports a simple, rapid, inexpensive, and eco-friendly approach for synthesizing Amphiroa rigida-mediated silver nanoparticles (AR-AgNPs) for the first time. The biomimetic synthesized AR-AgNPs were characterized by both spectral and microscopic analysis. The UV-visible spectrum showed the surface plasmon peak at 420 nm, which indicated the formation of AR-AgNPs. X-ray diffraction characterization of AR-AgNPs showed a face-centered cubic crystal (25 nm) and the transmission electron microscope micrograph showed spherical shape. The functional group of polysaccharide that plays a major role as a stabilizing and reducing agent is confirmed by Fourier-transform infrared spectroscopy. The biomimetic synthesized AR-AgNPs showed antibacterial activity against Staphylococcus aureus (21 ± 0.2 mm) and Pseudomonas aeruginosa (15 ± 0.2 mm). Further, the cytotoxic effects of AR-AgNPs against MCF-7 human breast cancer cells were observed through acridine orange-ethidium bromide and Hoechst staining. Besides, AR-AgNPs are found to be inhibit the growth of 3rd and 4th instar larvae of Aedes aegypti in a dose-dependent manner.
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Aedes/crecimiento & desarrollo , Antibacterianos , Materiales Biomiméticos , Citotoxinas , Insecticidas , Nanopartículas del Metal , Pseudomonas aeruginosa/crecimiento & desarrollo , Rhodophyta/química , Plata , Staphylococcus aureus/crecimiento & desarrollo , Animales , Antibacterianos/síntesis química , Antibacterianos/química , Antibacterianos/farmacología , Materiales Biomiméticos/síntesis química , Materiales Biomiméticos/química , Materiales Biomiméticos/farmacología , Citotoxinas/síntesis química , Citotoxinas/química , Citotoxinas/farmacología , Tecnología Química Verde , Humanos , Insecticidas/síntesis química , Insecticidas/química , Insecticidas/farmacología , Larva/crecimiento & desarrollo , Células MCF-7 , Nanopartículas del Metal/química , Nanopartículas del Metal/uso terapéutico , Plata/química , Plata/farmacologíaRESUMEN
The main objective of this study was to identify the antifungal metabolites from Achromobacter kerstersii JKP9, a rhizosphere bacterium isolated from tomato cultivations, inhibiting the melanin biosynthetic pathways in vascular wilt pathogen Fusarium oxysporum f. sp. lycopersici (Fol). To achieve this objective, all the rhizobacterial morphotypes were screened for plant-growth-promoting and antagonistic activities. Ethyl acetate extract of Achromobacter kerstersii JKP9 was purified in HPLC and predicted for antifungals in GC-MS equipped with Wiley library. After identification, molecular docking of useful ligands with modeled Short-chain Dehydrogenase/ Reductase (SDR) of Fol (Locus: FOXG_00472). Results were indicated that the potential strain Achromobacter kerstersii JKP9 exclusively secreted five pyrrole analogs notable for their antifungal role with no extracellular antifungal enzyme production as seen in other rhizobacterial isolates. In silico docking studies identified, Pyrrolo[1, 2-a]pyrazine-1,4-dione, hexahydro- as effective for SDR in Fol. From these results, we conclude that bacterial pyrroles can be used as an effective fungicide to control Fusarium wilt in tomatoes. In the future, these pyrrole derivatives can directly be employed as eco-friendly fungicides or may be used as antifungal supplements in agrochemical products for the sustainable production of tomatoes.
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Achromobacter/metabolismo , Antifúngicos/farmacología , Fungicidas Industriales/farmacología , Fusarium/efectos de los fármacos , Pirroles/farmacología , Achromobacter/genética , Antifúngicos/metabolismo , Solanum lycopersicum/microbiología , Simulación del Acoplamiento Molecular , Enfermedades de las Plantas/microbiología , Enfermedades de las Plantas/prevención & control , Pirroles/metabolismoRESUMEN
In this study, we report a green synthesis of pharmaceutically active gold nanoparticles from marine red alga Acanthophora spicifera by the reduction of chloroauric acid. The formation of A. spicifera-mediated gold nanoparticles (As-AuNPs) was characterized by several analytical techniques. The crystalline and face-centered cubic (fcc) structure were confirmed by X-ray diffraction (XRD) analysis. Electron microscopy results confirmed that As-AuNPs were spherical and the average size of particles was < 20 nm. As-AuNPs hold a significant level of antioxidant activities than A. spicifera extract. As-AuNPs exhibited the highest antibacterial activity against Vibrio harveyi than Staphylococcus aureus at 100 µg/ml. Furthermore, As-AuNPs exhibited the utmost cytotoxicity against human colon adenocarcinoma (HT-29) cells and registered the half-maximal inhibitory concentration (IC50) at 21.86 µg/ml. These findings authenticated that the synthesized As-AuNPs possess a broad spectrum of biological activities, and it can be effectively applied in the field of aquaculture and biomedical application.
Asunto(s)
Antibacterianos/farmacología , Antineoplásicos/farmacología , Antioxidantes/farmacología , Oro/química , Nanopartículas del Metal/química , Algas Marinas/metabolismo , Bioensayo , Compuestos de Bifenilo/química , Supervivencia Celular , Depuradores de Radicales Libres , Tecnología Química Verde/métodos , Células HT29 , Humanos , Concentración 50 Inhibidora , Microscopía Electrónica , Óxido Nítrico/química , Tamaño de la Partícula , Picratos/química , Plata/química , Staphylococcus aureus/metabolismo , Vibrio , Difracción de Rayos XRESUMEN
The present study deals with the proteomics analysis of crude squid ink isolated from Sepia esculenta for their antibacterial, antifungal, antibiofilm and cytotoxic properties. To achieve this, SDS-PAGE was used to separate proteins as bands, In-gel trypsin digested and analyzed by MALDI-TOF mass spectrometry. A total of 4 bands were identified by MASCOT search analysis namely astacin-like squid metalloprotease type I (ASMT-I), 70â¯kDa neurofilament protein (NP), uncharacterized protein LOC106181966 isoform X1 (UP-Iso-X1) and Ommochrome-binding protein (Oc-BP). Further, the obtained crude squid proteins were subjected to antimicrobial and antibiofilm activities against pathogenic bacterial and fungal strains respectively. Further, MTT assay was also carried out to deliberately explain the cytotoxic ability of crude squid ink protein against MCF-7 breast cancer cell lines. The results from the study revealed that, the proteins are shown to be toxic against pathogenic strains and breast cancer cell lines in a dose-dependent manner. More importantly, the proteins are well enough to eradicate biofilms substantiated by light and confocal laser scanning microscopic observations. Altogether, the crude squid ink proteins hampered the growth of breast cancer cells with an IC50 value of 65.3⯱â¯0.46⯵gâ¯mL-1. In conclusion, it is believed that the proteins from crude squid ink will provide new insights in hampering bacterial biofilms and cancer in near future.
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Antiinfecciosos/química , Antiinfecciosos/farmacología , Antineoplásicos/química , Antineoplásicos/farmacología , Pigmentos Biológicos/química , Proteoma/análisis , Sepia/metabolismo , Animales , Antiinfecciosos/aislamiento & purificación , Antineoplásicos/aislamiento & purificación , Bacterias/efectos de los fármacos , Biopelículas/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Hongos/efectos de los fármacos , Humanos , Células MCF-7 , Pigmentos Biológicos/aislamiento & purificación , Proteómica , Espectrometría de Masa por Láser de Matriz Asistida de Ionización DesorciónRESUMEN
Acinetobacter baumannii, a virulent uropathogen with widespread antibiotic resistance, has arisen as a critical scientific challenge, necessitating the development of innovative therapeutic agents. This is the first study reveal the proteomic changes in A. baumannii upon pyrogallol treatment for understanding the mechanisms using nano-LC-MS/MS-based quantitative proteomics and qPCR analysis. The obtained results found that pyrogallol treatment dramatically downregulated the expression level of several key proteins such as GroEL, DnaK, ClpB, SodB, KatE, Bap, CsuA/B, PgaA, PgaC, BfmR, OmpA, and SecA in A. baumannii, which are involved in chaperone-mediated oxidative stress responses, antioxidant defence system, biofilm formation, virulence enzyme production, bacterial adhesion, capsule formation, and antibiotic resistance. Accordingly, the pyrogallol dramatically enhanced the lifespan of A. baumannii-infected zebrafish by inhibiting bacterial colonization, demonstrating the anti-infective potential of pyrogallol against A. baumannii. Further, the histopathological results also demonstrated the disease protection efficacy of pyrogallol against the pathognomonic sign of A. baumannii infection. In addition, the pyrogallol treatment effectively improved the immune parameters such as serum myeloperoxidase activity, leukocyte respiratory burst activity, and serum lysozyme activity in zebrafish against A. baumannii infection. Based on the results, the present study strongly proposes pyrogallol as a promising therapeutic agent for treating A. baumannii infection.
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Acinetobacter baumannii , Antiinfecciosos , Animales , Virulencia , Pez Cebra/metabolismo , Acinetobacter baumannii/metabolismo , Pirogalol/farmacología , Pirogalol/metabolismo , Proteómica , Espectrometría de Masas en Tándem , Biopelículas , Antibacterianos/farmacología , Antibacterianos/metabolismo , Antiinfecciosos/metabolismo , Proteínas Bacterianas/genética , Proteínas Bacterianas/metabolismo , InmunidadRESUMEN
Polycyclic aromatic hydrocarbons (PAHs) are highly carcinogenic substances and accumulate in water bodies through various industries. Due to their harmful effects on humans, it is very important to monitor PAHs in various water resources. In the present work, we report an electrochemical sensor based on silver nanoparticles synthesized using mushroom-derived carbon dots for the simultaneous determination of anthracene and naphthalene, for the first time. Pleurotus species mushroom was used to synthesize the carbon dots (C-dots) via the hydrothermal method and these C-dots were used as a reducing agent for the synthesis of silver nanoparticles (AgNPs). The synthesized AgNPs have been characterized through UV-Visible and FTIR spectroscopy, DLS, XRD, XPS, FE-SEM, and HR-TEM. Well-characterized AgNPs were used to modify glassy carbon electrodes (GCEs) by the drop-casting method. Ag-NPs/GCE has shown strong electrochemical activity towards the oxidation of anthracene and naphthalene at well-separated potentials in phosphate buffer saline (PBS) at pH 7.0. The sensor exhibited a wide linear working range of 250 nM to 1.15 mM for anthracene and 500 nM to 842 µM for naphthalene with the corresponding lowest detection limits (LODs) of 112 nM and 383 nM respectively with extraordinary anti-interference ability against many possible interferents. The fabricated sensor showed high stability and reproducibility. The usefulness of the sensor for the monitoring of anthracene and naphthalene in a seashore soil sample has been demonstrated by the standard addition method. The sensor gave better results with a high recovery percentage indicating the first-ever device to detect two PAHs at the single electrode with the best analytical results.
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Agaricales , Contaminantes Ambientales , Nanopartículas del Metal , Humanos , Carbono/química , Nanopartículas del Metal/química , Plata/química , Reproducibilidad de los Resultados , Antracenos , NaftalenosRESUMEN
Although gold nanoparticles based photodynamic therapy (PDT) were reported to improve efficacy and specificity, the impact of surface charge in targeting cancer is still a challenge. Herein, we report gold nanotriangles (AuNTs) tuned with anionic and cationic surface charge conjugating triphenylphosphonium (TPP) targeting breast cancer cells with 5-aminoleuvinic acid (5-ALA) based PDT, in vitro. Optimized surface charge of AuNTs with and without TPP kill breast cancer cells. By combining, 5-ALA and PDT, the surface charge augmented AuNTs deliver improved cellular toxicity as revealed by MTT, fluorescent probes and flow cytometry. Further, the 5-ALA and PDT treatment in the presence of AuNTs impairs cell survival Pi3K/AKT signaling pathway causing mitochondrial dependent apoptosis. The cumulative findings demonstrate that, cationic AuNTs with TPP excel selective targeting of breast cancer cells in the presence of 5-ALA and PDT.
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Neoplasias de la Mama , Nanopartículas del Metal , Fotoquimioterapia , Humanos , Femenino , Proteínas Proto-Oncogénicas c-akt , Oro/farmacología , Fosfatidilinositol 3-Quinasas , Neoplasias de la Mama/tratamiento farmacológico , Nanopartículas del Metal/uso terapéutico , Ácido Aminolevulínico/farmacología , Apoptosis , Fármacos Fotosensibilizantes/farmacología , Fármacos Fotosensibilizantes/uso terapéutico , Línea Celular TumoralRESUMEN
Herein, the impact of surface charge tailored of gold nanorods (GNRs) on breast cancer cells (MCF-7 and MDA-MB-231) upon conjugation with triphenylphosphonium (TPP) for improved photodynamic therapy (PDT) targeting mitochondria was studied. The salient features of the study are as follows: (i) positive (CTAB@GNRs) and negative (PSS-CTAB@GNRs) surface-charged gold nanorods were developed and characterized; (ii) the mitochondrial targeting efficiency of gold nanorods was improved by conjugating TPP molecules; (iii) the conjugated nanoprobes (TPP-CTAB@GNRs and TPP-PSS-CTAB@GNRs) were evaluated for PDT in the presence of photosensitizer (PS), 5-aminolevulinic acid (5-ALA) in breast cancer cells; (iv) both nanoprobes (TPP-CTAB@GNRs and TPP-PSS-CTAB@GNRs) induce apoptosis, damage DNA, generate reactive oxygen species, and decrease mitochondrial membrane potential upon 5-ALA-based PDT; and (v) 5-ALA-PDT of two nanoprobes (TPP-CTAB@GNRs and TPP-PSS-CTAB@GNRs) impact cell signaling (PI3K/AKT) pathway by upregulating proapoptotic genes and proteins. Based on the results, we confirm that the positively charged (rapid) nanoprobes are more advantageous than their negatively (slow) charged nanoprobes. However, depending on the kind and degree of cancer, both nanoprobes can serve as efficient agents for delivering anticancer therapy.
RESUMEN
The increased incidence of healthcare-related Candida infection has necessitated the use of effective disinfectants/antiseptics in healthcare settings as a preventive measure to decontaminate the hospital environment and stop the persistent colonization of the offending pathogens. Quanternary ammonium surfactants (QASs), with their promising antimicrobial efficacy, are considered as intriguing and appealing candidates for disinfectants. From this perspective, the present study investigated the antifungal efficacy and action mechanism of the QAS cetyltrimethylammonium chloride (CTAC) against three clinically important Candida species: C. albicans, C. tropicalis, and C. glabrata. CTAC exhibited phenomenal antifungal activity against all tested Candida spp., with minimum inhibitory concentrations (MIC) and minimum fungicidal concentrations (MFC) between 2 and 8 µg/mL. The time−kill kinetics of CTAC (at 2XMIC) demonstrated that an exposure time of 2 h was required to kill 99.9% of the inoculums in all tested strains. An important observation was that CTAC treatment did not influence intracellular reactive oxygen species (ROS), signifying that its phenomenal anticandidal efficacy was not mediated via oxidative stress. In addition, sorbitol supplementation increased CTAC's MIC values against all tested Candida strains by three times (8−32 µg/mL), indicating that CTAC's possible antifungal activity involves fungus cell membrane destruction. Interestingly, the increased fluorescence intensity of CTAC-treated cells in both propidium iodide (PI) and DAPI staining assays indicated the impairment of cell plasma membrane and nuclear membrane integrity by CTAC, respectively. Additionally, CTAC at MIC and 2XMIC was sufficient (>80%) to disrupt the mature biofilms of all tested spp., and it inhibited the yeast-to-hyphae transition at sub-MIC in C. albicans. Finally, the non-hemolytic activity of CTAC (upto 32 µg/mL) in human blood cells and HBECs signified its non-toxic nature at the investigated concentrations. Furthermore, thymol and citral, two phytocompounds, together with CTAC, showed synergistic fungicidal effectiveness against C. albicans planktonic cells. Altogether, the data of the present study appreciably broaden our understanding of the antifungal action mechanism of CTAC and support its future translation as a potential disinfectant against Candida-associated healthcare infections.
Asunto(s)
Candida , Desinfectantes , Humanos , Candida/fisiología , Antifúngicos/farmacología , Cetrimonio/farmacología , Permeabilidad de la Membrana Celular , Candida albicans , Desinfectantes/farmacología , Muerte Celular , Pruebas de Sensibilidad MicrobianaRESUMEN
Carbon quantum dots (CQDs) have gained significant growing attention in the recent past due to their peculiar characteristics including smaller size, high surface area, photoluminescence, chemical stability, facile synthesis and functionalization possibilities. They are carbon nanostructures having less than 10 nm size with fluorescent properties. In recent years, the scientific community is curiously adopting biomass precursors for the preparation of CQDs over the chemical compounds. These biomass sources are sustainable, eco-friendly, inexpensive, widely available and convert waste into valuable materials. Hence in our work the fundamental understating of diverse fabrication methodologies of CQDs, and the types of raw materials employed in recent times, are all examined and correlated comprehensively. Their unique combination of remarkable properties, together with the ease with which they can be fabricated, makes CQDs as promising materials for applications in diverse biomedical fields, in particular for bio-imaging, targeted drug delivery and phototherapy for cancer treatment. The mechanism for luminescence is of considerable significance for leading the synthesis of CQDs with tunable fluorescence emission. Therefore, it is aimed to explore and provide an updated review on (i) the recent progress on the different synthesis methods of biomass-derived CQDs, (ii) the contribution of surface states or functional groups on the luminescence origin and (iii) its potential application for cancer theranostics, concentrating on their fluorescence properties. Finally, we explored the challenges in modification for the synthesis of CQDs from biomass derivatives and the future scope of CQDs in phototherapy for cancer theranostics.
Asunto(s)
Neoplasias , Puntos Cuánticos , Carbono/química , Fluorescencia , Humanos , Luminiscencia , Neoplasias/diagnóstico , Medicina de Precisión , Puntos Cuánticos/químicaRESUMEN
Prostate cancer (PC) is one of the major impediments affecting men, which leads approximately 31,620 deaths in both developing and developed countries. Although some chemotherapy drugs have been reported for prostate cancer, they are not effective due to the lack of safety, efficacy and low selectivity. Hence, the novel alternative anticancer agents with remarkable effect are highly appreciable. Natural plants contain several bio-active compounds which have been traditionally used for the various medical treatments. Particularly, naringin is a natural bio-active compound commonly found in the citrus fruits, which have shown numerous biological activities. Phosphatase and tensin homolog (PTEN) is a tumor suppressor gene, which activates both lipid phosphates and protein phosphates. The PTEN gene is negative regulator of PI3K/AKT/mTOR pathways, since, this signaling pathway play an essential role in the cell survival, proliferation and migration. In the present in silico investigation, structure based virtual screening, molecular docking, molecular dynamics simulation and Adsorption, Distribution, Metabolism, Excretion (ADME) prediction were employed to determine the binding affinity, stability and drug likeness properties of top ranked screened compounds and naringin, respectively. The results revealed that the complex has good molecular interactions, binding stability (peak between 0.3 and 0.4 nm) and no violations in the Lipinski Rule of 5 in naringin, but the screened compounds violated the drug likeness properties. From the in silico analyses, it is identified that naringin compound might assist in the development of novel therapeutic candidate against prostate cancer. Communicated by Ramaswamy H. Sarma.
Asunto(s)
Activadores de Enzimas/farmacología , Flavanonas/farmacología , Fosfohidrolasa PTEN , Neoplasias de la Próstata , Humanos , Masculino , Simulación del Acoplamiento Molecular , Neoplasias de la Próstata/tratamiento farmacológicoRESUMEN
Microplastics in personal care and food products are given much importance globally due to the adverse impact of microplastics on living beings. In the present study, microplastics from ten different commercially sold toothpaste in India were extracted by vacuum filtration and characterized with microscopic and Fourier-transform infrared spectroscopic analyses. Results revealed that colorless fragments and fibers were the microparticle types of common occurrence which ranged from 0.2 to 0.9% weight in the toothpaste with an abundance range of 32.7-83.2%. Fifty percent of the toothpaste samples showed more than 50% microplastic particle abundance indicating that the microplastic plastic particles were added by the manufacturers. The minimum size of microplastics recorded in the present study was 3.5 µm with a maximum size exceeding 400 µm. The maximum number of microplastics in the toothpaste was 167, 508 and 193 respectively, distributed in the size range of <100 µm, 100-400 µm, and >400 µm. The present study recorded four major polymer types, viz., cellophane, polypropylene, polyvinyl chloride, and polyamide in the toothpaste samples. Surprisingly, polyethylene-a common polymer reported in toothpaste was not traced in the present samples. Regarding the Indian context, the current study is a new addition to the knowledge of the occurrence of microplastics in toothpaste. The average annual addition of microplastics into the environment through toothpaste was calculated as 1.4 billion g/year for India, posing a significant threat to the environment.
Asunto(s)
Microplásticos , Contaminantes Químicos del Agua , Monitoreo del Ambiente , Plásticos/química , Polímeros , Medición de Riesgo , Pastas de Dientes , Contaminantes Químicos del Agua/análisisRESUMEN
The present study has investigated the distribution of microplastics in sediment and its impact on histological, ultrastructural, and oxidative stress mechanisms in Perna viridis (P. viridis) from Kasimedu, Chennai, India. The results confirmed that fibers were the predominant type of microplastics observed, followed by spheres, flakes, sheets, and fragments. The observed microplastics were confirmed as polyester, polypropylene, polyethylene, cellophane, and rayon using µ-FT-IR. Microplastic particles entangled in gills caused abrasion of ciliated structure and hemocyte infiltration in the hemolymph vessels. The digestive gland showed a shrunken nucleus, dark inclusions, and damage in the nucleoid core structure. Enlarged vacuoles and the presence of clusters of vesicles presumably represented the transformed golgi cisternae. Further, the results confirmed that oxidative stress markers were significantly high in gills and digestive diverticula of P. viridis. Overall, the results indicated that microplastics induced different toxic physiological and structural alterations in gills and digestive diverticula of P. viridis. These findings highlighted the necessity to focus on exposure studies to understand the absolute magnitude of the problem due to microplastic pollution in the urban estuarine ecosystems of Chennai, Tamil Nadu, India.
Asunto(s)
Perna , Contaminantes Químicos del Agua , Animales , Biomarcadores/metabolismo , Ingestión de Alimentos , Ecosistema , Monitoreo del Ambiente , India , Microplásticos , Estrés Oxidativo , Perna/metabolismo , Plásticos/toxicidad , Espectroscopía Infrarroja por Transformada de Fourier , Contaminantes Químicos del Agua/toxicidadRESUMEN
The present study was deliberately focused to explore the antivirulence efficacy of a plant allelochemical-catechol against Candida albicans, and attempts were made to elucidate the underlying mechanisms as well. Catechol at its sub-MIC concentrations (2-256 µg/mL) exhibited a dose dependent biofilm as well as hyphal inhibitory efficacies, which were ascertained through both light and fluorescence microscopic analyses. Further, sub-MICs of catechol displayed remarkable antivirulence efficacy, as it substantially inhibited C. albicans' virulence enzymes i.e. secreted hydrolases. Notably, FTIR analysis divulged the potency of catechol in effective loosening of C. albicans' exopolymeric matrix, which was further reinforced using EPS quantification assay. Although, catechol at BIC (256 µg/mL) did not disrupt the mature biofilms of C. albicans, their initial adherence was significantly impeded by reducing their hydrophobic nature. Besides, FTIR analysis also unveiled the ability of catechol in enhancing the production of farnesol-a metabolite of C. albicans, whose accumulation naturally blocks yeast-hyphal transition. The qPCR data showed significant down-regulation of candidate genes viz., RAS1, HWP1 and ALS3 which are the key targets of Ras-cAMP-PKA pathway -the pathway that contribute for C. albicans' pathogenesis. Interestingly, the up-regulation of TUP1 (a gene responsible for farnesol-mediated hyphal inhibition) during catechol exposure strengthen the speculation of catechol triggered farnesol-mediated hyphal inhibition. Furthermore, catechol profusely enhanced the fungicidal efficacy of certain known antifungal agent's viz., azoles (ketoconazole and miconazole) and polyenes (amphotericin-B and nystatin).