Silybin Cocrystals with Improved Solubility and Bioavailability.

Silymarin, an extract from milk thistle, is widely recognized for its therapeutic potential in treating liver disorders. However, its clinical utility is limited by the poor solubility and low bioavailability of its key active ingredient, Silybin. In this study, we sought to address this issue through the development of a novel cocrystal of Silyin.

Eco-Friendly Hydrogels Loading Polyphenols-Composed Biomimetic Micelles for Topical Administration of Resveratrol and Rutin.

In this study, we describe the development of hydrogel formulations composed of micelles loading two natural antioxidants-resveratrol and rutin-and the evaluation of the effect of a by-product on the rheological and textural properties of the developed semi-solids. This approach aims to associate the advantages of hydrogels for topical administration of drugs and of lipid micelles that mimic skin composition for the delivery of poorly water-soluble compounds in combination therapy. Biomimetic micelles composed of L-α-phosphatidylcholine loaded with two distinct polyphenols (one non-flavonoid and one flavonoid) were produced using hot shear homogenisation followed by the ultrasonication method.

Optimizing kinase and PARP inhibitor combinations through machine learning and in silico approaches for targeted brain cancer therapy.

The drug combination is an attractive approach for cancer treatment. PARP and kinase inhibitors have recently been explored against cancer cells, but their combination has not been investigated comprehensively. In this study, we used various drug combination databases to build ML models for drug combinations against brain cancer cells.

Dual-mode luminescence and colorimetric sensing for Al and Fe/Fe ions in water using a zinc coordination polymer.

A zinc(II) coordination polymer, [Zn(Hdhtp)(2,2'-bpy)(HO)] (1), has been utilized as a dual-mode luminescence-colorimetric sensor (Hdhtp = 2,5-dihydroxy terephthalate and 2,2'-bpy = 2,2'-bipyridine). The presence of hydroxyl groups in Hdhtp can promote excited-state intra- and intermolecular proton transfer (ESIPT) phenomena. Therefore, compound 1, which displays high stability in aqueous environments, exhibits a strong green-yellow photoluminescence.

Development of Antibacterial Hydrogels Based on Biopolymer Aloe Vera/Gelatin/Sodium Alginate Composited With SM-AgNPs Loaded Curcumin-Nanoliposomes.

To address the rising prevalence of bacterial infections and the need for innovative therapeutic solutions, this study has developed a novel antibacterial hydrogel composite composed of Aloe vera, gelatin, sodium alginate, and Sterculia monosperma-silver nanoparticles (SM-AgNPs) loaded curcumin-nanoliposomes (NLPs). The aloe vera/gelatin/sodium alginate hydrogels (AGS) are prepared using different weight ratios of Aloe vera, gelatin, and sodium alginate, aiming to optimize mechanical properties and biocompatibility for biomedical applications. The incorporation of SM-AgNPs and curcumin-loaded NLPs enhanced the hydrogels' antibacterial properties.

Advances in the selective c-MET kinase inhibitors: Application of fused [5,6]-Bicyclic nitrogen-containing cores for anticancer drug design.

Over the past two decades, small molecules bearing [5,6]-bicyclic nitrogen-containing cores have emerged as one of the most extensively studied structures for the development of selective c-MET kinase inhibitors. Structure-activity relationship (SAR) studies have demonstrated that modifying these cores can significantly impact the biological properties of c-MET inhibitors, including safety/toxicity, potency, and metabolic stability. For example, although c-MET kinase inhibitors containing the [1,2,4]triazolo[4,3-b][1,2,4]triazine scaffold (core P) exhibit high inhibitory potency, they often face challenges due to metabolic stability defects.

New benzimidazole-indole-amide derivatives as potent α-glucosidase and acetylcholinesterase inhibitors.

New derivatives 6a-m with benzimidazole-indole-amide scaffold were developed, synthesized, and assessed for potential inhibitory effects on α-glucosidase and acetylcholinesterase (AChE). These compounds were synthesized by various amine derivatives. With the exception of two compounds, the α-glucosidase inhibitory activities of the title derivatives were more than that of the positive control acarbose.

Combination of chemotherapy and c-MET inhibitors has synergistic effects in c-MET overexpressing pancreatic cancer cells.

Pancreatic ductal adenocarcinoma (PDAC) remains as one of the most lethal malignancies. c-MET is an important oncogenic kinase involved in PDAC progression. We determined the anticancer effect of c-MET inhibitors, crizotinib and cabozantinib, combined with chemotherapeutic agents, doxorubicin, oxaliplatin and gemcitabine, against different PDAC and a lung adenocarcinoma cell line expressing different levels of c-MET.

Green nitrogen and sulfur co-doped carbon dots derived from eggshell as a high performance aptasensing interface for non-invasive detection of metronidazole.

Background: The concentration monitoring of the banned metronidazole (MTZ) drug as the alarmed carcinogenic agent in human biofluids is medically essential. The electrochemical aptasensors are good candidates to overcome some presence challenges in the detection process.

Results: Herein, an electrochemical aptasensor based on nitrogen and sulfur co-doped carbon dots (NcS-CDs) has been developed for the high-sensitive detection of MTZ for the first time.

Development of silk fibroin/collagen film containing GI-20 peptide-loaded PLGA nanoparticles against corneal herpes simplex virus-1.

Herpes simplex virus-1 (HSV-1) is the primary cause of infectious blindness. Despite impressive therapeutic outcomes of conventional treatments, HSV-1 drug resistance can be easily developed. Thus, more constructive strategies should be implemented.

Green preparation of reusable Pd@magnetic lignosulfonate nanocomposite for hydrogen evolution reaction in all pHs.

In this study, palladium nanoparticles (Pd NPs) were successfully synthesized and supported on a cost-effective, eco-friendly magnetic lignosulfonate matrix using Hibiscus Rosasinensis L. leaf extract as a natural reducing and stabilizing agent (Pd@Fe₃O₄-lignosulfonate). The magnetic lignosulfonate prevented the aggregation of Pd NPs, enhanced the active surface area, and improved the hydrophilicity of the modified carbon paste electrode (CPE), thus boosting hydrogen production efficiency.

Unveiling the green synthesis of WO nanoparticles by using beetroot (Beta vulgaris) extract for photocatalytic oxidation of rhodamine B.

Tungsten oxide (WO) nanoparticles (WONPs) were prepared using beetroot (Beta vulgaris) extract. The synthesis was optimized by evaluating the effect of pH during the reduction of the WO precursor and sintering temperature. Physicochemical characterization of the formed nanoparticles was performed using X-ray diffraction (XRD), scanning electron microscopy (SEM), X-ray photoelectron spectroscopy (XPS), and UV-visible diffuse reflectance UV-visible spectroscopy.

c-MET tyrosine kinase inhibitors reverse drug resistance mediated by the ATP-binding cassette transporter B1 (ABCB1) in cancer cells.

This study investigated the potential of MET kinase inhibitors, cabozantinib, crizotinib, and PHA665752, in reversing multidrug resistance (MDR) mediated by ABCB1 in cancer cells. The accumulation of the fluorescent probe, Rhodamine 123, was assessed using flow cytometry and fluorescence microscopy in MDR MES-SA/DX5 and parental cells. The growth inhibitory activity of MET inhibitors as monotherapies and in combination with chemotherapeutic drugs was evaluated by MTT assay.

Removal of chlorpyrifos from aqueous medium using Ca-CuO@clay nanoflakes coated with deep eutectic solvent.

Availability of fresh water for domestic, industrial, and agricultural use has become a huge challenge in different parts of the world due to continuous contamination. The leaching of different pesticides in agricultural lands is one of the major sources of water contamination that needs to be monitored and countered. The current study was designed to synthesize specific material for the removal of pesticides from aqueous medium.

Biodegradable antibacterial food packaging based on carboxymethyl cellulose from sugarcane bagasse/cassava starch/chitosan/gingerol extract stabilized silver nanoparticles (Gin-AgNPs) and vanillin as cross-linking agent.

The increasing issue of plastic waste necessitates improved solutions, and biodegradable food packaging is a promising alternative to traditional plastic. In this study, we prepared packaging films using cassava starch (CV), chitosan (CT) and carboxymethyl cellulose (CMC), with glycerol as a plasticizer. However, these films require modifications to enhance their mechanical properties.

Binding interaction of sodium benzoate, potassium sorbate and sodium dihydrogen citrate with BSA as food preservatives: in Vitro analysis and computational studies.

Advanced glycation end products (AGEs) are obtained intermediate from nonenzymatic reactions between reducing sugars and proteins, lipids, or nucleic acids and it's associated with diabetic complications. Today, potassium sorbate (PS), sodium citrate (CIT) and sodium benzoate (SB) were widespread used as food preservatives that can easily enter biological matrices. Here, the interaction between glycosylation Bovine Serum Albumin (BSA) and food preservatives individually and combination of two and three was studied by biochemical and simulation analysis.

Zeolitic imidazolate framework-67 in chitosan-grafted hydrogel as an effective catalyst for peroxymonosulfate activation to degrade antibiotics and dyes.

Zeolitic imidazolate framework-67 (ZIF-67) was synthesized in the hydrogel of chitosan-grafted poly(acrylic acid) (chitosan--PAA) to activate peroxymonosulfate (PMS) and degrade tetracycline (TC). The catalytic performance of the composite hydrogel for TC degradation was evaluated under different conditions. The results showed rapid degradation, with enhanced degradation efficiency as the catalyst dosage, PMS dosage, and temperature increased.

A Comprehensive Study on the Amino Acids and Tryptophan-Derived Molecules in Iberian Wine Vinegar.

Wine vinegar, valued for its ancient origins and culinary versatility, has garnered scientific interest due to its complex composition and potential health benefits. This study aims to explore the nutritional and bioactive properties of different wine vinegars, focusing on their amino acid content, particularly tryptophan-derived molecules such as serotonin and melatonin. White wine vinegar, red wine vinegar, port wine vinegar, and balsamic vinegar from the Douro and Rioja regions were analyzed using high-performance liquid chromatography and solid-phase extraction (HPLC-SPE).

Design, synthesis, and cytotoxic activity of 2-amino-1,4-naphthoquinone-benzamide derivatives as apoptosis inducers.

A new series of 2-amino-1,4-naphthoquinone-benzamides 5a-n was designed based on previously reported potent cytotoxic agents. These compounds were synthesized from the reaction of 1,4-naphthoquinone, 4-aminobenzoic acid, and appropriate amine derivatives in good yields. Cytotoxic activities of the target compounds 5a-n were evaluated against three cancer cell lines MDA-MB-231, SUIT-2, and HT-29 by MTT assay and the obtained in vitro data.

Multi-functional tyrosinase inhibitors derived from kojic acid and hydroquinone-like diphenols for treatment of hyperpigmentation: Synthesis and in vitro biological evaluation.

A series of multi-functional tyrosinase inhibitors derived from kojic acid (KA) and hydroquinone-like diphenols were designed and synthesized using click chemistry. The in vitro enzymatic assay revealed that all compounds containing a free enolic structure showed excellent activity against tyrosinase (IC = 0.14-3.

A novel electrochemical sensor based on ꞵ-cyclodextrin/bismuth oxybromide/multi-walled carbon nanotubes modified electrode with in situ addition of tetrabutylammonium bromide for the simultaneous detection and degradation of tebuconazole.

A novel electrochemical sensor-based glassy carbon electrode (GCE) was fabricated and applied to simultaneous detection and degradation of tebuconazole (TBZ) for the first time. The GCE was consecutively modified by multi-walled carbon nanotubes (MWCNTs), bismuth oxybromide (BiOBr), ꞵ-cyclodextrin (ꞵ-CD), and in situ addition of tetrabutylammonium bromide (TBABr). The detection was based on the decreasing of Bi signal at its anodic potential (E) of 0.

Scaffold Hopping Method for Design and Development of Potential Allosteric AKT Inhibitors.

Targeting AKT is a practical strategy for cancer therapy in many cancer types. Targeted inhibitors of AKT are attractive solutions for inhibiting the interconnected signaling pathways, like PI3K/Akt/mTOR. Allosteric inhibitors are more desirable among different classes of AKT inhibitors as they could be more specific with fewer off-target proteins.