A549 Cells Research Articles

New quinoxaline-oxadiazole hybrids as tubulin inhibitors: Synthesis, cytotoxicity, and molecular dynamics simulations

This study describes the synthesis and biological evaluation of a series of novel quinoxaline-oxadiazole hybrid compounds. These compounds were designed to enhance anticancer activity through the incorporation of specific pharmacophoric groups. Structural characterization using NMR and HRMS spectroscopy confirmed the successful synthesis of the hybrids. Cytotoxicity assays revealed that several compounds exhibited significant activity against various cancer cell lines. Compounds 8a and 8f demonstrated potent activity against A549 cells, while 8a, 8b, and 8c were effective against HaCaT cells. Additionally, compounds 8i and 8a showed activity against HepG2 cells. Molecular docking and dynamics simulations suggested that compounds 8c and 8d bind strongly to the tubulin protein, a target for anticancer drugs. These compounds exhibited binding affinities comparable to known anticancer compounds. The results of this study highlight the potential of quinoxaline-oxadiazole hybrids, especially those with halogen substitutions, as promising candidates for the development of novel anticancer therapeutics.

Tanshinone T1/T2A inhibits non-small cell lung cancer through Lin28B-let-7-BORA/MYC regulatory network

BackgroundLung cancer is the leading cause of cancer-related deaths worldwide. Tanshinones are a group of compounds in Salvia miltiorrhiza. Although the effects of tanshinone I (T1) and tanshinone IIA (T2A) are widely concerned, the mechanisms of T1 and T2A in lung cancer is rarely studied. Experimental procedureXenograft tumor growth was performed to detect the role of T1/T2A in vivo. Next-generation sequencing of miRNA expression profiles in T1/T2A-treated A549 cells showed that T1/T2A upregulated the expression of the let-7 family. Then, let-7a-5p and its downstream target gene BORA were identified as the research objects in this paper. Mechanistically, we examined the interplay between miR-let-7 and BORA through the dual-luciferase reporter assay. Finally, the potential regulatory role of T1/T2A on Lin28B and MYC was explored. ResultsThis study found that the let-7 family was significantly up-regulated via “Next-generation” sequencing (NGS) in the T1/T2A-treated A549 cell line, while BORA was downregulated. BORA was confirmed as a direct target of let-7. LncRNA MYCLo-5 was up-regulated after treatment with tanshinones. Knockdown of MYCLo-5 promoted the cell cycle and proliferation of non-small cell lung cancer (NSCLC) cells. ConclusionsThis study explored the effects of tanshinone T1 and T2A on NSCLC in vitro and in vivo, revealing the T1/T2A-let-7/BORA/MYCLo-5 regulatory pathway, which provided new insights for lung cancer treatment.

Study on the activity and mechanism of herbal formula anti-infection powder (AIP) against influenza-virus-induced pneumonia through genetic susceptibility genes

Anti-infection powder (AIP), a patented Chinese herbal formulation, is used traditionally in the treatment of upper respiratory tract infections. In this study, an ethanol extract of AIP was demonstrated to inhibit influenza A virus (IAV) infection and IAV-induced pneumonia (IVP), both in vitro and in vivo, highlighting its potential mechanism of action. To determine the anti-IAV activity of AIP and to explore the possible mechanisms of inhibiting IAV-induced pneumonia. An ethanol extract was extracted from AIP and its major ingredients were determined by high-performance liquid chromatography (HPLC). An IAV-infected A549 cell model and an IAV-induced mouse pneumonia model were established to evaluate the therapeutic effects of AIP on IVP in vivo and in vitro. The mice were respectively administered AIP at high- and low-dose in different groups. The anti-IAV activity of AIP was evaluated by detecting viral load, lung lesion, lung index, suvival time, inflammatory cytokines and transcriptomic analysis in the lung tissue. The potential pathways and targets that involved in AIP against IVP were predicted by network pharmacology. Mendelian randomization (MR), colocalization analysis, and molecular docking were employed to identify novel therapeutic targets for IVP. Polymerase chain reaction (PCR) and Western blot (WB) techniques were used to confirm the effect of AIP on the expression of risk target genes in the lungs of IVP mice. In A549 cell line, AIP effectively inhibited IAV infection with IC50 values of 65.49 μg/mL. The anti-IAV activity of AIP was mainly determined by chlorogenic acid, forsythiarin, puerarin, paeoniflorin and prim-o-glucosylcimigin. Moreover, AIP inhibited the neuraminidase activity and the M gene expression in vitro. In vivo, oral administration of AIP significantly reduced viral load and improved lung tissue lesions. AIP decreased the concentration of pro-inflammatory factors such as IL-1β, TNF-α, and IFN-γ, and significantly increased the concentration of the anti-inflammatory factor IL-4. According to network pharmacology analysis, toll-like receptor signaling pathway, chemokine signaling pathway, and TNF signaling pathway may be the possible mechanisms by which AIP inhibits IVP and regulates excessive inflammatory response.Two new genes, LRG1 and PSMA4, associated with genetic susceptibility to influenza and pneumonia, predicted as potential IVP drug target genes by MR and colocalization analysis. The antiviral mechanism of AIP may be to inhibit the expression levels of LRG1 and PSMA4 in lungs of mouse IVP. AIP exhibited anti-IAV activities both in vitro and in vivo. AIP had a protective effect against pneumonia caused by influenza virus and can inhibit the progression of inflammation. This effect may be associated with its ability to inhibit the expression levels of genetic susceptibility genes (LRG1 and PSMA4) in lungs of mouse IVP. The findings of this study enhance our understanding of the role and mechanisms of AIP in the treatment of IVP.

Biogenic silver nanoparticles from Simarouba glauca DC leaf extract: Synthesis, characterization, and anticancer efficacy in lung cancer cells with protective effects in Caenorhabditis elegans

This study explores the synthesis, characterization, and biomedical applications of silver nanoparticles (AgNPs) synthesized using Simarouba glauca leaf extract. The biogenic AgNPs were characterized through UV–visible spectroscopy, X-ray diffraction (XRD), particle size analysis, zeta potential analysis, energy dispersive X-ray spectroscopy (EDX), Fourier-transform infrared spectroscopy (FTIR), atomic force microscopy (AFM), and high-resolution transmission electron microscopy (HR-TEM). The nanoparticles exhibited a distinct absorbance peak at 413.5 nm, confirming their synthesis and surface plasmon resonance. XRD and HR-TEM analyses revealed a face-centered cubic structure with an average size of 12.45 nm, while AFM indicated a mean particle size of 18.34 nm. The particles demonstrated moderate stability with a zeta potential of −41.4 mV and exhibited various elemental compositions as confirmed by EDX. In the biomedical evaluation, the anticancer potential of SG-AgNPs was tested on L-132 and A549 cell lines using MTT, live/dead, and DNA damage assays. Results showed dose-dependent cytotoxicity, with significant effects observed at higher concentrations, particularly against A549 cells. Additionally, the protective effects of SG-AgNPs were assessed in Caenorhabditis elegans using survival and paralysis assays. The nanoparticles significantly improved survival rates and reduced paralysis in worms infected with Pseudomonas aeruginosa PAO1 and Staphylococcus aureus. These findings highlight the potential of biogenic SG-AgNPs as effective agents with both anticancer and antimicrobial properties. Future research should focus on elucidating the mechanisms underlying these effects and optimizing their therapeutic applications.

A bibliometric analysis of the application of the PI3K-AKT-mTOR signaling pathway in cancer.

PI3K-AKT-mTOR plays as important role in the growth, metabolism, proliferation, and migration of cancer cells, and in apoptosis, autophagy, inflammation, and angiogenesis in cancer. In this study, the aim was to comprehensively review the current research landscape regarding the PI3K-AKT-mTOR pathway in cancer, using bibliometrics to analyze research hotspots, and provide ideas for future research directions. Literature published on the topic between January 2006 and May 2023 was retrieved from the Web of Science core database, and key information and a visualization map were analyzed using CiteSpace and VOSviewer. A total of 5800 articles from 95 countries/regions were collected, including from China and the USA. The number of publications on the topic increased year on year. The major research institution was the University of Texas MD Anderson Cancer Center. Oncotarget and Clinical Cancer Research were the most prevalent journals in the field. Of 26,621 authors, R Kurzrock published the most articles, and J Engelman was cited most frequently. "A549 cell," "first line treatment," "first in human phase I," and "inhibitor" were the keywords of emerging research hotspots. Inhibitors of the PI3K-AKT-mTOR pathway and their use in clinical therapeutic strategies for cancer were the main topics in the field, and future research should also focus on PI3K-AKT-mTOR pathway inhibitors. This study is the first to comprehensively summarize trends and development s in research into the PI3K-AKT-mTOR pathway in cancer. The information that was obtained clarified recent research frontiers and directions, providing references for scholars of cancer management.

Unveiling the Dynamic Mechanism of SARS-CoV-2 Entry Host Cells at the Single-Particle Level.

Understanding the dynamic features of severe acute respiratory coronavirus 2 (SARS-CoV-2) binding to the cell membrane and entry cells is crucial for comprehending viral pathogenesis and transmission and facilitating the development of effective drugs against COVID-19. Herein, we employed atomic force microscopy (AFM)-based single-molecule force spectroscopy (SMFS) to study the binding dynamics between the virus and cell membrane. Our findings revealed that the Omicron variant of SARS-CoV-2 virus-like particles (VLPs) exhibited a slightly stronger affinity for the angiotensin-converting enzyme-2 (ACE2) receptor compared with the Delta variant and was significantly higher than the wild-type (WT). Using a real-time force-tracing technique, we quantified the dynamic parameters for a single SARS-CoV-2 VLP entry into cells, showing that approximately 200 ms and 60 pN are required. The parameters aligned with the analysis obtained from coarse-grained molecular dynamics (CGMD) simulations. Additionally, the Omicron variant invades cells at a higher entry cell speed, smaller force, and higher probability. Furthermore, single-particle fluorescence tracking visually demonstrated clathrin-dependent endocytosis for SARS-CoV-2 entry into A549 cells. The dynamic features of endocytosis provide valuable insights into the SARS-CoV-2 entry mechanism and possible intervention strategies targeting the viral infection process.

Anticancer behavior of cyclometallated iridium(III)-tributyltin(IV) carboxylate schiff base complexes with aggregation-induced emission

Cyclometallated iridium(III) and organotin(IV) carboxylate complexes have shown potential application value in the field of anticancer. However, the widespread aggregation-caused quenching (ACQ) effect of these complexes is not conducive to the exploration of their targeting and anticancer mechanism, and the idea of aggregation-induced emission (AIE) effect can effectively solve this problem. Then, AIE-activated cyclometallated iridium(III)-tributyltin(IV) carboxylate Schiff base complexes were designed and prepared in this study. Complexes exhibited AIE effect in highly concentrated solution or aggregative state, which facilitated the investigation of subcellular tissue targeting (mitochondria) and cell morphology. Compared with cyclometallated iridium(III) complex and tributyltin(IV) carboxylate monomers, these complexes showed the better in-vitro anti-proliferative activity toward A549 cells, confirming the favorable synergistic anticancer activity. Even for A549/DDP (cisplatin-resistance) cells, these complexes also exhibited the better activity. In addition, complexes showed a mitochondrial apoptotic pathway. Therefore, cyclometallated iridium(III)-tributyltin(IV) carboxylate Schiff base complexes can be used as the potential substitutes for platinum-based drugs and gain further application.

MERS-CoV Infection and Its Impact on the Expression of TSLP Cytokine and IgG Antibodies: An In Vivo and In Vitro Study.

Thymic stromal lymphopoietin (TSLP) is a proinflammatory cytokine produced by epithelial cells that is involved in the activation of allergic disorders. To date, no study has examined TSLP induction during Middle East respiratory syndrome coronavirus (MERS-CoV) infection. Herein, we aimed to study the effects of the recombinant spike protein of MERS-CoV on TSLP production. Additionally, the effects of recombinant human TSLP (rhTSLP) on B cell survival and antibody production were investigated. B cells were separated using the Human B Cell Enrichment Kit, and B cell survival was measured using the WST-1 Assay Kit. Enzyme-linked immunosorbent assay (ELISA) was used to measure TSLP levels in the sera of both MERS-CoV-infected (n=4; median age, 53 years) and healthy individuals (n=5; median age, 35 years). We showed that the group of infected patients had significantly higher levels of TSLP than healthy controls (37.6 pg/mL vs 19.8 pg/mL, *p<0.05). The levels of TSLP in A549 cells were remarkably increased after 48h of stimulation with recombinant full-length spike protein (rSP) (32.2 pg/mL, p=0.01). B cell survival was greatly enhanced by rhTSLP alone or in combination with rSP (0.02 vs 0.046, and 0.045; **p<0.01, respectively). Our data also showed a significant synergistic effect of rhTSLP and rSP on the augmented response of IgG antibodies against the spike protein of MERS-CoV compared with unstimulated cells (0.156 vs 0.22; *p<0.05). TSLP production is induced in vivo after MERS-CoV infection and in vitro after treatment with the rSP of MERS-CoV, which has a significant effect on the survival of B cells. Our data suggest that TSLP can be used as a strong mucosal adjuvant for vaccine development against MERS-CoV infection. However, further investigation is required to study the functional role of TSLP in MERS-CoV infection.

Role of miR-455-3p in the alleviation of LPS-induced acute lung injury by allicin

Acute lung injury (ALI) is a type of diffuse lung injury that seriously affects the survival of critically ill patients. MicroRNAs (miRNAs) can serve as promising therapeutic targets or offer insights for the development of potential therapeutic strategies against ALI. In our previous study, we demonstrated the protective effect of allicin in ALI, but the role of miRNAs in the alleviation of ALI by allicin remains unclear. This study aimed to investigate whether miRNAs mediate the effects of allicin on ALI. Cell viability and proliferation were determined using CCK-8 and EdU assays, respectively, while cellular apoptosis was analyzed by flow cytometry. The claudin-4 protein was detected by quantitative real-time reverse-transcription polymerase chain reaction (qRT-PCR) and western blotting. The binding of miR-455 with claudin-4 was determined by bioinformatics analysis and validated by dual luciferase reporter assays. The lung wet/dry ratio of lipopolysaccharide (LPS)-treated rats was determined by hematoxylin and eosin (HE) and TUNEL staining of the pulmonary tissues. The levels of myeloperoxidase (MPO), interleukin (IL)-2, IL-6, and tumor necrosis factor (TNF)-α were determined by enzyme-linked immunosorbent assay (ELISA). We observed that allicin alleviated LPS-induced injury in A549 cells, and claudin-4 knockdown reversed the protective effect of allicin in ALI. Claudin-4 is a direct target of miR-455-3p, and miR-455-3p overexpression partially reversed the protective effect of allicin in LPS-treated A549 cells. Subsequent in vivo experiments confirmed that allicin protects against LPS-induced ALI by regulating the miR-455-3p/claudin-4 axis. The study revealed that the protective effect of allicin in ALI is mediated via miR-455-3p, which suppresses the expression of claudin-4.

Inhibition of Candida albicans virulence by moscatin from Dendrobium nobile lindl.

Candida albicans infection poses a significant global health threat. It is imperative to exploit new antifungal agents against C. albicans infections without leading to drug resistance, so that these potential agents can complement or combine with current medications to effectively treat diseases caused by C. albicans. We screened moscatin, and assessed the inhibitory effectiveness against C. albicans SC5314 on hyphae production and biofilm formation. It was revealed that moscatin exhibited significant effects on morphological transition and biofilm formation in C. albicans SC5314. It also lowered the pathogenicity of C. albicans SC5314 in a concentration-dependent way in both A549 cells and mice fungal infection models, but had no cytotoxicity to A549 cells. In addition, moscatin attenuated the virulence of clinical fluconazole-resistant C. albicans and exhibited synergistic activity with fluconazole. It could also restore the composition and richness of the intestinal microbiota in mice infected by C. albicans. These findings indicate that these moscatin has great potential to be developed as a new therapeutic drug against C. albicans infection.

Biobased hydrogel bioinks of pectin, nanocellulose and lysozyme nanofibrils for the bioprinting of A375 melanoma cell-laden 3D in vitro platforms

Melanoma is one of the most aggressive types of skin cancer, and the need for advanced platforms to study this disease and to develop new treatments is rising. 3D bioprinted tumor models are emerging as advanced tools to tackle these needs, with the design of adequate bioinks being a fundamental step to address this challenging process. Thus, this work explores the synergy between two biobased nanofibers, nanofibrillated cellulose (NFC) and lysozyme nanofibrils (LNFs), to create pectin nanocomposite hydrogel bioinks for the 3D bioprinting of A375 melanoma cell-laden living constructs. The incorporation of LNFs (5, 10 or 15 wt%) on a Pectin-NFC suspension originates inks with enhanced rheological properties (shear viscosity and yield point) and proper shear-thinning behavior. The crosslinked hydrogels mimic the stiffness of melanoma, being stable under physiological and cell-culture conditions, and non-cytotoxic towards A375 melanoma cells. P-NFC-LNFs (10 %) reveals good printability (Pr = 0.89) and printing accuracy (51 ± 2 %), and when loaded with A375 cells (3 × 106 cells mL−1) the bioink originates 3D-constructs with high cell viability (92 ± 1 %) after 14 days. The potential of the constructs as in vitro models is corroborated by a drug-screening test with doxorubicin, where cells within the model displayed high sensitivity to the drug.

Rational design, synthesis and anticancer screening of 1,2,4-oxadiazole incorporated thieno[2,3-d]thiazole-isoxazole-pyridine derivatives

We have design and synthesized a new series of 1,2,4-oxadiazole incorporated thieno[2,3-d]thiazole-isoxazole-pyridine analogues (13a-j) and were confirmed by 1H NMR, 13C NMR and mass spectral data. Further, the newly synthesized compounds (13a–j) were evaluated for their preliminary anticancer activity against a panel of four human cancer cell lines such as MCF-7 (breast cancer), A549 (lung cancer), Colo-205 (colon cancer) & A2780 (ovarian cancer) by using of MTT method, the known chemotherapeutic agent as etoposide used as positive control. Most of the tested compounds were displayed good to moderate activities on all cell lines. The IC50 values showed compound ranges from 0.01 ± 0.009 µM to 8.41 ± 5.48 µM. Where positive control showed values range from 3.34 ± 0.152 µM to 0.17 ± 0.034 µM. Among them, compound 13a, 13b, 13c, 13d, 13e and 13f were showed more potent activity than etoposide. Predominantly, The compound 13a showed potent anticancer activity against MCF-7, A549, Colo-205, and A2780 cancer cell lines with IC50 values of 0.02 ± 0.007 µM, 0.01 ± 0.009 µM, 0.13 ± 0.052 µM, and 0.11 ± 0.083 µM.

ERK5 mediates pro-tumorigenic phenotype in non-small lung cancer cells induced by PGE2

Lung cancer is the leading cause of cancer-related deaths worldwide, with non-small cell lung cancer (NSCLC) constituting approximately 84 % of all lung cancer cases. The role of inflammation in the initiation and progression of NSCLC tumors has been the focus of extensive research. Among the various inflammatory mediators, prostaglandin E2 (PGE2) plays a pivotal role in promoting the aggressiveness of epithelial tumors through multiple mechanisms, including the stimulation of growth, evasion of apoptosis, invasion, and induction of angiogenesis. The Extracellular signal-Regulated Kinase 5 (ERK5), the last discovered member among conventional mitogen-activated protein kinases (MAPK), is implicated in cancer-associated inflammation. In this study, we explored whether ERK5 is involved in the process of tumorigenesis induced by PGE2. Using A549 and PC9 NSCLC cell lines, we found that PGE2 triggers the activation of ERK5 via the EP1 receptor. Moreover, both genetic and pharmacological inhibition of ERK5 reduced PGE2-induced proliferation, migration, invasion and stemness of A549 and PC9 cells, indicating that ERK5 plays a critical role in PGE2-induced tumorigenesis. In summary, our study underscores the pivotal role of the PGE2/EP1/ERK5 axis in driving the malignancy of NSCLC cells in vitro. Targeting this axis holds promise as a potential avenue for developing novel therapeutic strategies aimed at controlling the advancement of NSCLC.

A Human GSDMD Protein-Derived Cell-Penetrating Peptide Enhances the Antitumor Effects of the Proapoptotic Peptide KLA

Cell-penetrating peptides (CPPs) possess significant potential for the transportation of cell-impermeable biological molecules into tumor cells. However, the nonhuman origins of CPPs can cause cytotoxicity and immunogenicity, limiting their clinical applicability. In this study, using in silico approaches combined with in vitro experiments, we identified and characterized a novel CPP named RYK derived from the human gasdermin D (GSDMD) protein. Compared with the R8 peptide, which served as a positive control, RYK exhibited superior penetration efficiency into A549 and HepG2 cells without inducing cytotoxic effects. Confocal laser scanning microscopy further demonstrated that RYK penetrated the nuclei of tumor cells more rapidly than did the R8 peptide. The subsequent experimental results demonstrated that RYK facilitates the cellular internalization of KLA without modifying its cytotoxic mechanism. To summarize, RYK has emerged as a promising CPP for the efficient delivery of exogenous biological agents into tumor cells.

Alpinia galanga induces caspase-dependent apoptotic cell death in human lung and cervical cancer cells

Introduction: Alpinia galanga (L.) Willd is a rhizomatous, recurrent herb used to treat numerous diseases, including cancer. This study examines the efficiency of the different parts of A. galanga for their phytochemical, antioxidant, and anti-cancer properties. Methods: The powdered leaf, stem, and rhizome of A. galanga were extracted using hexane, ethyl acetate and methanol; the phytochemical compositions of the extracts were characterized using high performance liquid chromatography (HPLC) and gas chromatography-mass spectroscopy (GC-MS). Their antioxidant potentials were evaluated using different assays, including 2,2-Diphenyl-1picrylhydrazil (DPPH), 2-Azino-bis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS), Superoxide anion (O2-), Hydroxyl radical (OH), and Phosphomolybdenum assays. The in vitro anticancer activity was studied using the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay. Comet assay was used to determine the level of DNA damage. Inductions of morphological alterations were studied using the AO/Et-Br dual staining method. The ELISA kits were used to measure caspase activities. Results: The cytotoxicity results showed that the various extracts had inhibitory and cytotoxic effects on cancer cell lines. The leaf hexane (LH) extract of A. galanga induced DNA damage with prominent increased tail length and tail moment followed by the induction of apoptotic cells and up-regulation of the caspase activities. HPLC and GC-MS analysis allowed the identification of bioactive compounds, recognized as apoptotic inducers in human cancer cells by activating caspase-dependent pathways. Conclusion: This work reports for the first time the effect of LH extract of A. galanga in triggering apoptosis in A-549 and HeLa cells through the upregulation of caspase-8 and caspase-3 activities.

A novel normonoterpene glycoside and a new benzophenone derivative from Hypericum cerastioides and their in vitro cytotoxic activities

Phytochemical investigations on the aerial parts of Hypericum cerastioides led to the isolation and identification of a novel normonoterpene (1) and a previously undescribed benzophenone glycoside (3) along with eleven known secondary metabolites (2, 4–13). Their structures were deduced based on extensive 1D and 2D NMR analyses as well as HRESIMS. Compound 1 is a rare type of normonoterpene derivative with eight carbon atoms. The chemotaxonomic significance of the isolates was also discussed. Compounds were evaluated for their in vitro cytotoxic activities against SW480, A375, DU145 and MCF7 cancer cell lines using doxorubicin as a reference drug. Compounds 1 and 7 demonstrated weak cytotoxicity.

Novel nanoformulation for enhanced amphotericin B efficacy and sustained release using vetiver root cellulose nanofibers against Candida albicans

The formidable antifungal agent, Amphotericin B, is well-known for its potency; however, its clinical application has been significantly limited due to toxicity and poor solubility. This study aims to address these challenges by developing and evaluating a novel nano-cellulose-based formulation of Amphotericin B to enhance its efficacy. Amphotericin B was encapsulated within cellulose nanofibers at varying ratios to optimize formulation parameters, including drug concentration, particle size, zeta potential, and entrapment efficiency. Notably, a composition ratio of 10:1 of cellulose nanofibers to Amphotericin B achieved an impressive encapsulation efficiency of 96.64 %. Subsequent physicochemical characterizations employing techniques such as FTIR, DLS, XRD, and SEM provided insights into structural attributes and interactions within formulation. Controlled and extended-release profiles were observed at various physiological pH levels, with the Korsmeyer-Peppas model showing the highest correlation, indicating predominant drug diffusion. Importantly, nanoformulation demonstrated non-toxicity to A431 cells and human erythrocytes up to a maximum concentration of 20 μg/ml, as corroborated by MTT and hemolysis assays. Furthermore, antimicrobial susceptibility and efficacy assessments, conducted using agar diffusion and broth micro-dilution methods, revealed enhanced inhibition of Candida albicans growth. The nanoformulation produced a larger zone of inhibition (DIZ) of 19.66 mm compared to a DIZ of 16.33 mm for Amphotericin B alone. Impressively, the nanoformulation exhibited a minimum inhibitory concentration (MIC) of 25 μg/ml against Candida albicans, underscoring its heightened efficacy. Additionally, the formulation's ability to improve the targetability and bioavailability of Amphotericin B holds promise for enhancing its antifungal effectiveness while reducing associated toxicity.

Minting Progress: Multifunctional Bismuth Oxide Nanoparticles via Mentha arvensis extract for Biomedical Advancements

AbstractTo surpass the constraints associated with conventional therapeutic methods in clinical therapy, nanoparticles have been rapidly prepared and developed as a separate treatment method for diseases. In this study, we have synthesized bismuth oxide nanoparticles (BiNPs) using aqueous leaf extract of Mentha arvensis (M. arvensis) as a biogenic approach. The formation of BiNPs was confirmed by the characteristic peak observed at 276 nm in the UV–vis spectrum and PXRD analysis exhibited the crystalline nature with monoclinic phase. The TEM images revealed the quasi‐spherical shape of BiNPs with an average particle size of 12 nm. For biomedical studies, BiNPs exhibited significant cytotoxicity against A431 cell line (lung cancer) with IC50 value of 92.45 µg/mL. Further studies revealed significantly higher apoptosis, antibacterial, anti‐inflammatory, antidiabetic, and antioxidant activities of the biosynthesized BiNPs. The collective results from the study suggest that the M. arvensis mediated synthesis of multifunctional BiNPs enhances their biological potential, positioning it as a potential candidate for the multimodal therapeutic applications.

Nano-synthesis, characterization, theoretical, biological and catalytic studies of Mn(II), Cu(II), Cd(II), and Th(IV) complexes based on antipyrine azo dye ligand

The design and detailed characterization of the azo dye ligand obtained from the reaction of 4-aminoantipyrine diazonium salt with 3-hydroxybenzaldehyde (HL) and its novel metal chelates with Mn2+, Cu2+, Cd2+ and Th4+ ions have been presented. Utilizing modern spectroscopic and analytical techniques, these complexes were found to adopt an octahedral geometry, demonstrate inner sphere d2sp3 hybridization for Th(IV) complex and outer sphere sp3d2 hybridization for other complexes. Particle sizes calculated using the Debye-Scherrer equation on XRD patterns were 32.05 nm for Mn(II), 34.07 nm for Cu(II), 30.90 nm for Cd(II), and 22.05 nm for Th(IV). These substances' anticancer activity was assessed on human lung cancer cells (A-549) and pancreatic carcinoma cell lines (PANC-1). Cd(II) complex exhibited higher cytotoxicity against the A-549 cell line than the reference drug vinblastine sulfate which revealing its potential application as a new anticancer agent. Quantum chemical computations using the DMOL3 module's density functional theory (DFT) and molecular docking studies with the Schrödinger suite demonstrated significant inhibitory effects of the free organic compound and Cu(II) chelate on the FGFR1 protein, crucial for cell development and differentiation. Additionally, the study examined the catalytic activity of HL and its metal chelates in the oxidative degradation of methyl violet 2B dye in presence of H2O2. The order was followed by the pseudo-first-order rate constants: Th(IV) chelate (0.9556 min⁻¹) > HL (0.4911 min⁻¹) > Cu(II) chelate (0.5979 min⁻¹) > Mn(II) chelate (0.2645 min⁻¹) > Cd(II) chelate (0.2280 min⁻¹).

Pimozide-loaded nanostructured lipid carriers: Repurposing strategy against lung cancer.

This study aimed to repurpose pimozide (PMZ) by incorporating it into nanostructured lipid carriers (NLC) using a modified melting emulsion ultrasonication method. We employed stearic and oleic acids in a 1:1 ratio as lipids, with Tween 80 and PEG 4000 as surfactants. The formulation was analyzed for particle size, zeta potential, and encapsulation efficiency. Transmission electron microscopy (TEM) was used to confirm the spherical shape of the particles. The release profile of PMZ-NLC was evaluated under different pH conditions, and anticancer activity was tested on A549 cell lines. The PMZ-NLC exhibited an average particle size of 136 ± 2.9 nm, a zeta potential of -25.1 ± 0.9 mV, and an encapsulation efficiency of 86% ± 11. TEM confirmed the spherical shape of the NLCs. PMZ release from PMZ-NLC was pH-sensitive, enhancing tumor targeting. IC50 values were 16.5 μM for free PMZ and 12.9 μM for PMZ-NLC after 72 h. PMZ-NLC demonstrated improved anticancer activity compared to free PMZ, suggesting that encapsulation enhances the drug's effectiveness. The pH-sensitive release profile supports its potential for targeted therapy in lung cancer. PMZ-NLC showed potential as a safe and effective strategy for lung cancer treatment. Further investigation is warranted to evaluate its in vivo efficacy, long-term safety, and clinical application.