Background: Colon cancer remains a major global health concern, and conventional chemotherapy is often associated with systemic toxicity and therapeutic resistance. Nanocarrier-based drug delivery systems are being investigated as potential approaches to improve the delivery of anticancer agents. Objectives: This study aimed to develop magnetic bovine serum albumin nanoparticles co-loaded with curcumin (CUR) and paclitaxel (PTX) and to evaluate their physicochemical characteristics and in vitro cytotoxic effects against Ls174T colorectal cancer cells. This formulation combines the drug-carrying properties of BSA with the magnetic responsiveness of cobalt ferrite (CoFe2O4); however, magnetic field-guided targeting was not evaluated. Methods: Nanoparticles were prepared using the desolvation method with incorporation of a CoFe2O4 magnetic core. Their physicochemical characteristics were evaluated using scanning electron microscopy and Fourier-transform infrared spectroscopy. Cytotoxicity was assessed using methylthiazolyl tetrazolium assays in Ls174T human colorectal cancer cells after 24, 48, and 72 h of treatment. Results: The dual-loaded nanoparticles exhibited greater in vitro cytotoxic activity against Ls174T cells than did the corresponding single-drug formulations and free drugs under the tested conditions. Curcumin alone showed relatively limited cytotoxic activity, whereas its combination with paclitaxel was associated with enhanced cytotoxic effects. These findings demonstrate the in vitro activity of the dual-loaded formulation; however, its effects on systemic toxicity and tumor-specific targeting remain undetermined. Conclusions: bovine serum albumin-CoFe2O4 nanoparticles co-loaded with CUR and PTX demonstrated in vitro cytotoxic activity against Ls174T colorectal cancer cells. These findings support further investigation of this formulation as a potential platform for combined anticancer drug delivery. Additional studies using normal cell models and in vivo tumor models are required to evaluate cytotoxic selectivity, biodistribution, tumor targeting, systemic toxicity, and therapeutic efficacy.
Background: The global rise in cancer incidence underscores the urgent need for novel and more effective therapeutic strategies. Among emerging modalities, gene therapy offers a powerful and precise approach by directly modulating genetic pathways involved in tumor growth. However, the success of gene therapy depends critically on the development of safe, efficient, and target-specific carriers capable of condensing, protecting, and delivering nucleic acids to cancer cells with minimal toxicity. Objectives: This study aimed to develop and characterize a novel, biocompatible nanocarrier system based on graphene oxide quantum dots (GOQDs) functionalized with polyethylenimine (PEI) and hyaluronic acid (HA) for potential CD44-targeted gene delivery applications. Methods: The GOQD/PEI/HA nanocarrier was synthesized by covalent conjugation using EDC/NHS chemistry and characterized by Fourier transform infrared spectroscopy (FT-IR) and thermogravimetric analysis (TGA), which confirmed successful functionalization. DNA-binding and condensation were assessed by agarose gel retardation, and field-emission scanning electron microscopy (FE-SEM) was used to determine the size and surface morphology of the prepared complexes. Finally, hemocompatibility and cytocompatibility were evaluated using hemolysis test and MTT assay in HeLa cells. Results: TGA and FT-IR analyses confirmed the successful preparation of functionalized GOQD/PEI/HA NPs. The gel retardation assay demonstrated complete plasmid DNA (pDNA) condensation at a 1:2 pDNA-to-carrier ratio, confirming a strong electrostatic interaction between the DNA and the carrier. Hemolysis rates remained below 2% at all tested concentrations, demonstrating the high hemocompatibility of the carriers. Moreover, MTT assay results showed that HA conjugation significantly increased cell viability from approximately 76% for GOQD/PEI to above 90% for GOQD/PEI/HA, indicating a substantial reduction in GOQD/PEI-associated cytotoxicity. Conclusions: Collectively, these findings confirm that the covalently HA-modified GOQD/PEI nanocarrier effectively integrates strong gene-condensation capability with excellent biocompatibility and hemocompatibility. This system represents a promising and safe nonviral platform with the potential for targeted gene delivery to CD44-positive HeLa cancer cells. Future studies should assess its therapeutic efficacy in more physiologically relevant models, including 3D tumor spheroids, organoid cultures, and in vivo systems, to validate its potential for advanced cancer gene therapy applications.
Context: Breast cancer is a lethal multifactorial illness among women. Recent studies have highlighted the importance of the neural network in breast tumor progression. Objectives: This review aimed to consider the potential contributions of neurotransmitters to breast cancer growth, migration, angiogenesis, and metastasis, as well as to discuss the function of neurotransmitter inhibitors in preventing tumor growth. Results: Neurons infiltrate the tumor microenvironment by secreting neurotransmitters and actively stimulate tumor progression. In breast cancer cells, neurotransmitters induce migration, growth, angiogenesis, and metastasis by regulating intracellular signaling pathways downstream of neurotransmitter receptors. Neurotransmitter inhibitors may therefore represent an alternative approach for breast cancer management. Conclusions: Neurotransmitter inhibitors might be crucial for targeting breast cancer treatment.
Background and Objective: Despite the urgent demand for the discovery of novel anticancer agents, anticancer discovery and development remain limited. Azo-containing compounds have emerged as attractive candidates in the field of anticancer drug discovery due to their distinctive reductive metabolism, which may be exploited to enhance anticancer efficacy and selectivity. Accordingly, increasing attention has been directed toward exploring the therapeutic potential of azo-aromatic scaffolds. Methods: In the present study, condensation reactions between benzoyl acetone and various aromatic diazonium salts were carried out to afford four azo derivatives, namely E-2-4-bromophenyldiazenyl-1-phenylbutane-1,3-dione KAioi, E-1-phenyl-2-phenyldiazenylbutane-1,3-dione KA102, E-2-4-methoxyphenyldiazenyl-1-phenylbutane-1,3-dione KA103, and E-2-4-nitrophenyldiazenyl-1-phenylbutane-1,3-dione KA104. Subsequent cyclization of these azo precursors provided the corresponding phenyl pyrazole derivatives, designated KA5, KA6, KA7, and KA8, respectively Results: Previously, KA5 exhibited promising anticancer activity against the human hepatocellular carcinoma cell line HepG2. The biological evaluation demonstrated that the newly synthesized KA7 is more potent than KA5, indicating that compounds exhibiting a higher propensity to exist in the hydrazone tautomeric form, particularly KA5 and KA7, showed enhanced cytotoxic activity against HepG2 cells compared with other analogues. Conclusions: These findings demonstrate that both pyrazole ring formation and tautomeric preference significantly influence anticancer activity, supporting azo-pyrazole scaffolds as promising leads for further optimization in anticancer drug development.
Background: Getting genetic material safely and efficiently into the nucleus of a cell is a monumental hurdle in gene therapy. While viruses are efficient carriers, their potential risks have pushed us to engineer smarter, non-viral alternatives. Our inspiration came from cell-penetrating peptides (CPPs), but we know that a single-function peptide is not enough; it needs to be a multi-tool capable of navigating every step of the complex delivery. Objectives: This study aimed to rationally design and optimize a modular CPP that integrates distinct functional domains to coordinate all critical stages of gene delivery: DNA binding, cellular uptake, endosomal escape, and nuclear import. Methods: In the present study, we designed a library of 30 chimeric peptides by combining functional motifs including an Hi histone-derived DNA-binding domain, the TAT membrane-translocating sequence, endosomal escape motifs such as gp4iFP and H5WYG, and the SV4o nuclear localization signal (NLS) connected by flexible linkers. Candidates were screened computationally for key properties. The lead peptide was expressed in Escherichia coli, purified, and evaluated for DNA-binding activity via gel retardation assays. Results: Computational screening identified seven top-ranked candidates, among which Peptide_24 exhibited favorable predicted stability, solubility, and pH-responsive charge characteristics. Successful recombinant expression and DNA-binding ability of Peptide_24 were confirmed experimentally for further investigations. Conclusions: This study demonstrates a rational, modular integration rather than de novo motif discovery to create a unified, multi-domain CPP architecture. Our lead candidate, Peptide_24, embodies this synergistic design, mimicking a coordinated, viral-like delivery pathway. Although computational analyses and preliminary experimental results support the potential of Peptide_24, further biological evaluation is required to assess its delivery performance in cellular systems.
