A549 Alveolar Carcinoma Spheroids as a Cytotoxicity Platform for Carboxyl- and Amine-Polyethylene Glycol Gold Nanoparticles.

Gold nanoparticles (AuNPs) present with unique physicochemical features and potential for functionalization as anticancer agents. Three-dimensional spheroid models can be used to afford greater tissue representation due to their heterogeneous phenotype and complex molecular architecture. This study developed an A549 alveolar carcinoma spheroid model for cytotoxicity assessment and mechanistic evaluation of functionalized AuNPs.

Evaluating Blood-Brain Barrier Permeability, Cytotoxicity, and Activity of Potential Acetylcholinesterase Inhibitors: In Vitro and In Silico Study.

Acetylcholinesterase inhibitors (AChEIs) remain the first-line treatment for Alzheimer's disease. However, these drugs are largely symptomatic and often associated with adverse effects. This study aimed to evaluate novel pharmacophores for their in vitro AChEI activity, blood-brain barrier (BBB) permeability, and cytotoxic potential, hypothesizing that a combination of AChEIs could enhance symptom management while minimizing toxicity.

From economics to health outcomes: Delving into the significance of reduced insulin prices.

The recent substantial price reductions in insulin therapy by major manufacturers prompt an examination of their impact on South Africa (SA)'s healthcare. While Eli Lilly, Novo Nordisk, and Sanofi cut prices on long-acting basal insulin, among others, significantly, these insulins are not on SA's Essential Medicines List (EML) for primary healthcare. With a high prevalence of diabetes, especially pre-diabetes, in the country, the EML's neglect of newer long-acting insulin treatments hampers effective disease management.

A simplified workflow with end-point validation of real-time electrical cell-substrate impedance sensing of retinoic acid stimulated neurogenesis in human SH-SY5Y cells in vitro.

Objective: Retinoic acid (RA) is known to transition proliferating SH-SY5Y neuroblastoma cells towards functional neurons. However, the activity of RA is restricted due to its photolability where any findings from prolonged time course observations using microscopy may alter outcomes. The aim of the study was to establish a real-time, long-term (9-day) protocol for the screening of differentiation events using Electrical cell-substrate impedance sensing (ECIS).

Comparative Evaluation of the Cytotoxicity of Doxorubicin in BT-20 Triple-Negative Breast Carcinoma Monolayer and Spheroid Cultures.

Three-dimensional cell culture models are increasingly adopted as preferred pre-clinical drug testing platforms, as they circumvent limitations associated with traditional monolayer cell cultures. However, many of these models are not fully characterized. This study aimed to characterize a BT-20 triple-negative breast carcinoma spheroid model and assess its susceptibility to doxorubicin in comparison to a monolayer model.

Cytostatic and cytotoxic effects of a hot water and methanol extract of Acokanthera oppositifolia in HepG2 hepatocarcinoma cells.

Ethnopharmacological Relevance: Herb-induced liver injury is poorly described for African herbal remedies, such as Acokanthera oppositifolia. Although a commonly used treatment for pain, snake bites and anthrax, it is also a well-known arrow poison, thus toxicity is to be expected.

Aim Of The Study: The cytotoxicity and preliminary mechanisms of toxicity in HepG2 hepatocarcinoma cells were assessed.

Utility of Therapeutic Drug Monitoring in Identifying Clinically Significant Interactions Between St. John's Wort and Prescription Drugs.

Background: The general population widely uses herbal medicines, as they are regarded as effective and safe. St. John's wort, which is an effective herbal antidepressant, exhibits both pharmacokinetic and pharmacodynamic interactions with several drugs.

The VEGF/VEGFR Axis Revisited: Implications for Cancer Therapy.

The vascular endothelial growth factor (VEGF)/vascular endothelial growth factor receptor (VEGFR) axis is indispensable in the process of angiogenesis and has been implicated as a key driver of tumor vascularization. Consequently, several strategies that target VEGF and its cognate receptors, VEGFR-1 and VEGFR-2, have been designed to treat cancer. While therapies targeting full-length VEGF have resulted in an improvement in both overall survival and progression-free survival in various cancers, these benefits have been modest.

Mechanisms facilitating the uptake of carboxyl-polythene glycol-functionalized gold nanoparticles into multicellular spheroids.

Objectives: Nanomedicines represent theragnostic alternatives to traditional candidate drugs, with increased targeting and delivery potential due to their size and functional tailorability. Biological activity typically relies on nanomaterials permeating into the intracellular environment, necessitating characterization of uptake and intracellular trafficking pathways. Spheroids' three-dimensional architecture and heterogenous cellular distribution offer an in-vivo-representative platform to assess the biological activity of nanoparticles (NPs).

Hybrid Compounds Containing Carvacrol Scaffold: Antibacterial and Cytotoxicity Evaluation.

Background: The design of hybrid compounds is a distinct approach for developing potent bioactive agents. Carvacrol, an essential oil, exhibits antimicrobial, antifungal, antioxidant, and anticancer activity, making it a good precursor for the development of compounds with potent biological activities. Some patents have reported carvacrol derivatives with promising biological activities.

A Brief Updated Review of Advances to Enhance Resveratrol's Bioavailability.

Resveratrol (RES) has a low bioavailability. This limitation was addressed in an earlier review and several recommendations were offered. A literature search was conducted in order to determine the extent of the research that was conducted in line with these recommendations, along with new developments in this field.

Synthesis, Antibacterial, and Cytotoxicity Evaluation of Oleanolic Acid-4-aminoquinoline Based Hybrid Compounds.

Aim: The study aims to prepare a class of oleanolic-based compounds.

Background: Conventional drugs used to treat infectious diseases suffer from limitations such as drug toxicity and drug resistance. The resistance of microbes to antimicrobial agents is a significant challenge in treating microbial infections.

Underlying mechanisms of cytotoxicity in HepG2 hepatocarcinoma cells exposed to arsenic, cadmium and mercury individually and in combination.

Background: Toxicity data regarding combinational exposure of humans to arsenic, cadmium and mercury is scarce. Although hepatotoxicity has been reported, limited information is available on their mechanistic underpinnings. The cytotoxic mechanisms of these metals were determined in HepG2 hepatocarcinoma cell lines after individual and combinational exposure.

Novel N-benzylpiperidine carboxamide derivatives as potential cholinesterase inhibitors for the treatment of Alzheimer's disease.

A series of fifteen acetylcholinesterase inhibitors were designed and synthesised based upon the previously identified lead compound 5,6-dimethoxy-1-oxo-2,3-dihydro-1H-inden-2-yl 1-benzylpiperidine-4-carboxylate (5) which showed good inhibitory activity (IC 0.03 ± 0.07 μM) against acetylcholinesterase.

Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones.

A series of novel, substituted 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones have been prepared and shown to exhibit promising concentration-dependent activity against human SH-SY5Y cells, Plasmodium falciparum, Mycobacterium tuberculosis and P. aeruginosa. Substituent effects on observed bioactivity have been explored; the para-fluorophenyl derivative 3d exhibited activity across the range of the bioassays employed, indicating the potential of the 2-chloro-3-[(4-arylthiazol-2-yl)amino]-1,4-naphthoquinone scaffold in the development of novel, broad spectrum therapeutics.

Cytotoxic activity of pentachlorophenol and its active metabolites in SH-SY5Y neuroblastoma cells.

As knowledge regarding mechanisms of pentachlorophenol (PCP) toxicity in neuronal cell lines is limited, the aim of the study was to evaluate the effects of PCP and its active metabolites, tetrachloro-1,4-benzoquinone (TCBQ) and tetrachlorohydroquinone (TCHQ) in human neuroblastoma SH-SY5Y cells. All compounds induced cytotoxic effects in time- and dose-dependent manners, and resulted in differential modes of cell death. Reduced mitochondrial membrane potential (ΔᴪM) and oxidative damage lead to apoptosis and necrosis following TCBQ and PCP exposure, respectively.

African Herbal Remedies with Antioxidant Activity: A Potential Resource Base for Wound Treatment.

The use of traditional herbal remedies as alternative medicine plays an important role in Africa since it forms part of primary health care for treatment of various medical conditions, including wounds. Although physiological levels of free radicals are essential to the healing process, they are known to partly contribute to wound chronicity when in excess. Consequently, antioxidant therapy has been shown to facilitate healing of such wounds.

Beneficial effects of folic acid on the kidneys and testes of adult albino rats after exposure to methomyl.

The aim of this study was to evaluate the protective effect of folate against methomyl-induced toxicity on the kidneys and testes of male rats. Adult male albino rats were divided into four groups; Group I served as the control (vehicle), Group II received folic acid (1.1 mg per kg b.

Priority areas for cannabis and cannabinoid product research in South Africa.

No abstract available.

Solamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum induces non-selective cytotoxicity and P-glycoprotein inhibition.

Background: Solanum aculeastrum fruits are used by some cancer sufferers as a form of alternative treatment. Scientific literature is scarce concerning its anticancer activity, and thus the aim of the study was to assess the in vitro anticancer and P-glycoprotein inhibitory potential of extracts of S. aculeastrum fruits.

Attenuation of oxidative stress and artificial wound closure in C2C12 myoblasts induced by sequential extracts of Boerhavia diffusa.

Objectives: Whole plants of Boerhavia diffusa L. are widely used medicine in Ghana and other tropical countries, for the treatment of wounds and other ailments. The aim of the study was to determine the ability of sequential extracts of B.