Ligand-conjugated multiwalled carbon nanotubes for cancer targeted drug delivery.

Multiwalled carbon nanotubes (MWCNTs) are at the forefront of nanotechnology-based advancements in cancer therapy, particularly in the field of targeted drug delivery. The nanotubes are characterized by their concentric graphene layers, which give them outstanding structural strength. They can deliver substantial doses of therapeutic agents, potentially reducing treatment frequency and improving patient compliance.

In silico-guided discovery and in vitro validation of novel sugar-tethered lysinated carbon nanotubes for targeted drug delivery of doxorubicin.

Context: Multiwalled carbon nanotubes (MWCNTs) functionalized with lysine via 1,3-dipolar cycloaddition and conjugated to galactose or mannose are potential nanocarriers that can effectively bind to the lectin receptor in MDA-MB-231 or MCF-7 breast cancer cells. In this work, a method based on molecular dynamics (MD) simulation was used to predict the interaction of these functionalized MWCNTs with doxorubicin and obtain structural evidence that allows a better understanding of the drug loading and release process. The MD simulations showed that while doxorubicin only interacted with pristine MWCNTs through π-π stacking interactions, functionalized MWCNTs were also able to establish hydrogen bonds, suggesting that the functionalized groups improve doxorubicin loading.

Curcumin coating: a novel solution to mitigate inherent carbon nanotube toxicity.

Multi-walled Carbon Nanotubes (MWCNTs) are inert structures with high aspect ratios that are widely used as vehicles for targeted drug delivery in cancer and many other diseases. They are largely non-toxic in nature however, when cells are exposed to these nanotubes for prolonged durations or at high concentrations, they show certain adverse effects. These include cytotoxicity, inflammation, generation of oxidative stress, and genotoxicity among others.

Virulence traits and novel drug delivery strategies for mucormycosis post-COVID-19: a comprehensive review.

The outbreak of a fatal black fungus infection after the resurgence of the cadaverous COVID-19 has exhorted scientists worldwide to develop a nutshell by repurposing or designing new formulations to address the crisis. Patients expressing COVID-19 are more susceptible to Mucormycosis (MCR) and thus fall easy prey to decease accounting for this global threat. Their mortality rates range around 32-70% depending on the organs affected and grow even higher despite the treatment.

Medicinal Aspects of PTP1B Inhibitors as Anti-Breast Cancer Agents: An Overview.

Protein tyrosine phosphatase 1B (PTP1B) has gained interest as a therapeutic target for type 2 diabetes and obesity. Besides metabolic signalling, PTP1B is a positive regulator of signalling pathways linked to ErbB2-induced breast tumorigenesis. Substantial evidence proves that its overexpression is involved in breast cancer, which suggests that selective PTP1B inhibition might be effective in breast cancer treatment.

Multifunctional GQDs for receptor targeting, drug delivery, and bioimaging in pancreatic cancer.

Pancreatic cancer is a devastating disease with a low survival rate and limited treatment options. Graphene quantum dots (GQDs) have recently become popular as a promising platform for cancer diagnosis and treatment due to their exceptional physicochemical properties, such as biocompatibility, stability, and fluorescence. This review discusses the potential of multifunctional GQDs as a platform for receptor targeting, drug delivery, and bioimaging in pancreatic cancer.

Design, synthesis, and anticancer activity of some novel 1H-benzo[d]imidazole-5-carboxamide derivatives as fatty acid synthase inhibitors.

Multiple malignancies exhibit aberrant FASN expression, associated with enhanced de novo lipogenesis to meet the metabolic demands of rapidly proliferating tumour cells. Furthermore, elevated FASN expression has been linked to tumour aggressiveness and poor prognosis in a variety of malignant tumours, making FASN is an attractive target for anticancer drug discovery. Herein, we report the de novo design and synthesis of (2-(2-hydroxyphenyl)-1H-benzo[d]imidazol-5-yl)(piperazin-1-yl)methanone derivatives as novel FASN inhibitors with potential therapeutic applications in breast and colorectal cancers.

Hybrid nanomaterial composed of chitosan, curcumin, ZnO and TiO for antibacterial therapies.

Metal nanoparticles have been tremendously utilised, such as; antibacterial and anticancer agents. Although metal nanoparticles exhibits antibacterial and anticancer activity, but the drawback of toxicity on normal cells limits their clinical applications. Therefore, improving the bioactivity of hybrid nanomaterial (HNM) and minimizing toxicity is of paramount importance for biomedical applications.

Microwave-Assisted Functionalization of Multi-Walled Carbon Nanotubes for Biosensor and Drug Delivery Applications.

Microwave-assisted synthetic methods have emerged as a popular technique for surface modification and the functionalization of multi-walled carbon nanotubes (MWCNTs) for diverse drug delivery applications. Microwave-induced functionalization of MWCNTs provides a high functionalization and requires less time than conventional techniques. Microwave methods are simple, fast, and effective for the covalent and noncovalent conjugation of MWCNTs with various biomolecules and polymers.

Recent advances in green synthesized nanoparticles for bactericidal and wound healing applications.

Nanotechnology has become an exciting area of research in diverse fields, such as: healthcare, food, agriculture, cosmetics, paints, lubricants, fuel additives and other fields. This review is a novel effort to update the practioneers about the most current developments in the widespread use of green synthesized nanoparticles in medicine. Biosynthesis is widely preferred among different modes of nanoparticle synthesis since they do not require toxic chemical usage and they are environment-friendly.

Synthesis, properties and antibacterial activity of Ca doped ZnSnO nanoparticles by microwave assisted method.

A major problem in world health care is the development of antibiotic resistance in bacteria. In light of this, pure and calcium-doped zinc tin oxide (ZTO) nanoparticles, ZnSnO (S), ZnSnCaO (S), ZnSnCaO (S), and ZnSnCaO (S), were synthesized via simple and cost effective microwave assisted method. The doping effect on antibacterial activity was studied in detail.

Fatty Acid Synthase (FASN): A Patent Review Since 2016-Present.

Introduction: Fatty acid synthase (FASN), is a key metabolic enzyme involved in fatty acid biosynthesis and is an essential target for multiple disease progressions like cancer, obesity, NAFLD, etc. Aberrant expression of FASN is associated with deregulated energy metabolism of cells in these diseases.

Area Covered: This article provides a summary of the most recent developments in the discovery of novel FASN inhibitors with potential therapeutic uses in cancer, obesity, and other metabolic disorders such as nonalcoholic fatty liver disease from 2016 to the present.

Nanorod-like Structure of ZnO Nanoparticles and ZnO Clusters Using 4-Dimethylamino Benzaldehyde Liquid to Study the Physicochemical and Antimicrobial Properties of Pathogenic Bacteria.

To study their physicochemical and antimicrobial properties, zinc oxide nanoparticles were synthesized using a simple chemical route and 4-dimethylaminobenzaldehyde (4DB) as an organic additive. ZnO nanoparticles were characterized with XRD analysis, which confirmed the presence of a hexagonal wurtzite structure with different crystalline sizes. The SEM morphology of the synthesized nanoparticles confirmed the presence of nanorods in both modifications of ZnO nanoparticles.

IND-2, a Quinoline Derivative, Inhibits the Proliferation of Prostate Cancer Cells by Inducing Oxidative Stress, Apoptosis and Inhibiting Topoisomerase II.

In men, prostate cancer (PC) is the most frequently diagnosed cancer, causing an estimated 375,000 deaths globally. Currently, existing therapies for the treatment of PC, notably metastatic cases, have limited efficacy due to drug resistance and problematic adverse effects. Therefore, it is imperative to discover and develop novel drugs for treating PC that are efficacious and do not produce intolerable adverse or toxic effects.

Lysinated Multiwalled Carbon Nanotubes with Carbohydrate Ligands as an Effective Nanocarrier for Targeted Doxorubicin Delivery to Breast Cancer Cells.

Multiwalled carbon nanotubes (MWCNTs) are elongated, hollow cylindrical nanotubes made of sp2 carbon. MWCNTs have attracted significant attention in the area of drug delivery due to their high drug-loading capacity and large surface area. Furthermore, they can be linked to bioactive ligands molecules via covalent and noncovalent bonds that allow for the targeted delivery of anticancer drugs such as doxorubicin.

Classification analysis of fatty acid synthase inhibitors using multialgorithms on topological descriptors and structural fingerprints.

Fatty acid synthase (FASN) is one of the enzymes required for fatty acid biosynthesis and is expressed as low or absent in most normal cells/tissues. However, this enzyme is upregulated in various cancer cells; hence, it can act as an important target to design and develop novel FASN inhibitors for cancer therapy. In the present investigation, a series of structurally diverse compounds that possessed FASN inhibitory activities were subjected to classification analysis using different algorithms such as support vector machine, decision tree, Naïve Bayes and random forest.

Substituent Orchestration in Dimethylquinoxaline Derivatives: A Tool for Fishing Out Appropriate CDK5 Inhibitors as Potential Therapeutics for Alzheimer's.

A set of new heterocyclic analogs (Compounds I-IX), comprising of 6,7 dimethyl Quinoxalines were found to be active against the receptor GSK3β (Compounds IV-V) (Chem. Biodiversity 2021, 18, e2100364). In an effort to modulate effective CDK5 inhibitors herein our hypothesis underpinned to fish out an appropriate derivative from the same quinoxaline series, as these two targets GSK3β and CDK5 shared structural resemblance with each other.

The significance of biomacromolecule alginate for the 3D printing of hydrogels for biomedical applications.

Natural biopolymers have been widely employed as biomaterial ink hydrogels for three-dimensional (3D) extrusion bioprinting in the preparation of the next generation of bioengineering materials for healthcare applications. Alginate is a linear anionic polysaccharide with favourable properties, such as: typical rheological (gelling, viscosifying, and stabilizing dispersions) characteristics, biodegradability and biocompatibility properties. However, in order to improve alginate applicability for practical biomaterial/bio ink for advanced medical applications, it is often modified and functionalized with several polymers and nanomaterials in order to obtain better printability of alginate-based biomaterial/bio ink hydrogels.

Biocidal activity of Ba-doped CeO NPs against and bacterial strains.

Mishandling of antibiotics often leads to the development of multiple drug resistance (MDR) among microbes, resulting in the failure of infection treatments and putting human health at great risk. As a response, unique nanomaterials with superior bioactivity must be developed to combat bacterial infections. Herein, CeO-based nanomaterials (NMs) were synthesized by employing cerium(iii) nitrate and selective alkaline ions.

A newly emerging alphasatellite affects banana bunchy top virus replication, transcription, siRNA production and transmission by aphids.

Banana bunchy top virus (BBTV) is a six-component ssDNA virus (genus Babuvirus, family Nanoviridae) transmitted by aphids, infecting monocots (mainly species in the family Musaceae) and likely originating from South-East Asia where it is frequently associated with self-replicating alphasatellites. Illumina sequencing analysis of banana aphids and leaf samples from Africa revealed an alphasatellite that should be classified in a new genus, phylogenetically related to alphasatellites of nanoviruses infecting dicots. Alphasatellite DNA was encapsidated by BBTV coat protein and accumulated at high levels in plants and aphids, thereby reducing helper virus loads, altering relative abundance (formula) of viral genome components and interfering with virus transmission by aphids.

Lead optimization of novel quinolone chalcone compounds by a structure-activity relationship (SAR) study to increase efficacy and metabolic stability.

Many agents targeting the colchicine binding site in tubulin have been developed as potential anticancer agents. However, none has successfully made it to the clinic, due mainly to dose limiting toxicities and the emergence of multi-drug resistance. Chalcones targeting tubulin have been proposed as a safe and effective alternative.

Biocidal and biocompatible hybrid nanomaterials from biomolecule chitosan, alginate and ZnO.

Biocidal activity and biocompatibility of nanomaterials (NMs) are crucial for healthcare applications. This study aims to develop biocidal hybrid NMs with high inhibition rates to control multidrug-resistant bacterial infection compared to conventional antibiotics. Herein, ZnO, chitosan-ZnO (CZnO) and alginate-ZnO (AZnO) NMs were synthesized via a simple one-pot technique.

Unravelling the Selectivity of 6,7-Dimethyl Quinoxaline Analogs for Kinase Inhibition: An Insight towards the Development of Alzheimer's Therapeutics.

Untangling the most selective kinase inhibitors via pharmacological intervention remains one of the challenging affairs to date. In accordance to this drift, herein we describe the design and synthesis of a set of new heterocyclic analogs consisting of 6,7-dimethyl Quinoxaline, appended to a connector, employing Schiff base strategy (Compounds I-IX). The compounds were characterized by various spectroscopic techniques and the kinase inhibition assay were performed on few prime members of the CMGC family namely the GSK3β, DYRK1A and CLK1 receptors, respectively, that have been known to be directly involved in hyperphosphorylation of Tau.

Antiproliferative Efficacy of -(3-chloro-4-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine, DW-8, in Colon Cancer Cells Is Mediated by Intrinsic Apoptosis.

A novel series of 4-anilinoquinazoline analogues, , were evaluated for anticancer efficacy in human breast cancer (BT-20) and human colorectal cancer (CRC) cell lines (HCT116, HT29, and SW620). The compound, , had the highest anticancer efficacy and selectivity in the colorectal cancer cell lines, HCT116, HT29, and SW620, with IC values of 8.50 ± 2.