Phytochemical Profiling and Bioactivity Assessment of L. Essential Oil and Extracts: Experimental and In Silico Insights.

L., a member of the Lamiaceae family, is widely used in traditional medicine for its therapeutic properties. This study aims to analyze the chemical composition of its essential oil and extracts, evaluate their antimicrobial and antioxidant activities, and investigate the interactions of their bioactive compounds with biological targets using in silico methods to better understand their mechanisms of action.

Modelling of Cetylpyridinium Chloride Availability in Complex Mixtures for the Prediction of Anti-Microbial Activity Using Diffusion Ordered Spectroscopy, Saturation Transfer Difference and 1D NMR.

A range of NMR techniques, including diffusion ordered spectroscopy (DOSY) were used to characterise complex micelles formed by the anti-microbial cationic surfactant cetylpyridium chloride and to quantify the degree of interaction between cetylpyridium chloride and hydroxyethyl cellulose in a variety of commercially relevant formulations as a model for the disk retention assay. This NMR-derived binding information was then compared with the results of formulation analysis by traditional disk retention assay (DRA) and anti-microbial activity assays to assess the suitability of these NMR techniques for the rapid identification of formulation components that could augment or retard antimicrobial activity DRA. NMR showed a strong ability to predict anti-microbial activity for a diverse range of formulations containing cetylpyridinium chloride (CPC).

Novel 4-alkoxy Meriolin Congeners Potently Induce Apoptosis in Leukemia and Lymphoma Cells.

(3-(pyrimidin-4-yl)-7-azaindoles) are synthetic hybrids of the naturally occurring alkaloids and and display a strong cytotoxic potential. We have recently shown that the novel derivative is highly cytotoxic in several lymphoma and leukemia cell lines as well as in primary patient-derived lymphoma and leukemia cells and predominantly targets cyclin-dependent kinases (CDKs). Here, we efficiently synthesized nine novel 2-aminopyridyl congeners (-), i.

Regioselective Nucleophilic Aromatic Substitution: Theoretical and Experimental Insights into 4-Aminoquinazoline Synthesis as a Privileged Structure in Medicinal Chemistry.

The 4-aminoquinazoline scaffold is a privileged structure in medicinal chemistry. Regioselective nucleophilic aromatic substitution (SAr) for replacing the chlorine atom at the 4-position of 2,4-dichloroquinazoline precursors is well documented in the scientific literature and has proven useful in synthesizing 2-chloro-4-aminoquinazolines and/or 2,4-diaminoquinazolines for various therapeutic applications. While numerous reports describe reaction conditions involving different nucleophiles, solvents, temperatures, and reaction times, discussions on the regioselectivity of the SAr step remain scarce.

Bis-Iridoid Glycosides and Triterpenoids from and Their Potential as Inhibitors of ACC1 and ACL.

A comprehensive phytochemical investigation of the twigs/leaves and flower buds of , a rare deciduous shrub native to China, led to the isolation of 39 structurally diverse compounds. These compounds include 11 iridoid glycosides (- and -), 20 triterpenoids (, , and -), and 8 phenylpropanoids (-). Among these, amabiliosides A () and B () represent previously undescribed bis-iridoid glycosides, while amabiliosides C () and D () feature a unique bis-iridoid-monoterpenoid indole alkaloid scaffold with a tetrahydro--carboline-5-carboxylic acid moiety.

Natural Antimicrobial Compounds as Promising Preservatives: A Look at an Old Problem from New Perspectives.

Antimicrobial compounds of natural origin are of interest because of the large number of reports regarding the harmfulness of food preservatives. These natural products can be derived from plants, animal sources, microorganisms, algae, or mushrooms. The aim of this review is to consider known antimicrobials of natural origin and the mechanisms of their action, antimicrobial photodynamic technology, and ultrasound for disinfection.

Antimicrobial and Antibiofilm Activity of Extracts Obtained by Supercritical Fluid Extraction Under Various Extraction Conditions.

Sustainable management of agri-food product safety presents a major challenge requiring extensive action to ensure food safety and consumer health. The pursuit of environmentally friendly solutions that will constitute an alternative to the chemical compounds commonly used in agriculture and the food industries is one of the most important problems. One solution is plant extracts containing various biologically active compounds and exhibiting antimicrobial activity.

Photocatalytic Degradation of Lincosamides in the Presence of Commercial Pigments: Kinetics, Intermediates, and Predicted Ecotoxicity.

Lincomycin belongs to the antibiotics commonly used in veterinary medicine. Its residues are easily spread in the environment because of its physicochemical properties, including resistance to biodegradation and good solubility in water. One of the effective methods for the removal of lincomycin from wastewater is the photocatalytic process, but it is not widely used due to the price of photocatalysts.

Anticholinesterase Activity and Bioactive Compound Profiling of Six Hop ( L.) Varieties.

Hops ( L.) are widely recognized for their use in brewing, but they also possess significant pharmacological properties due to their rich bioactive compounds, with many varieties exhibiting diverse characteristics. This study investigates the chemical composition and biological activities of extracts from six hop varieties, focusing on quantifying xanthohumol and lupulone using High-Performance Liquid Chromatography (HPLC) and Total Phenolic Content (TPC) analysis.

Antimicrobial Effectiveness of L. Leaf Extracts Prepared in Natural Deep Eutectic Solvents (NaDESs).

Background: Blackcurrant ( L.) leaves are valuable sources of bioactive compounds, including phenolic acids, flavonoids, and tannins, which contribute to their potent antioxidant, anti-inflammatory, and antimicrobial properties.

Objectives: The overall aim of this study was to investigate the antimicrobial potential of extracts rich in bioactive compounds from blackcurrant leaves prepared in natural deep eutectic solvents (NaDESs).

Chilean Papaya (): A Native Fruit with a High Health-Promoting Functional Potential.

Papaya fruit is commonly known for its nutritional and medicinal value. It is a perennial, herbaceous, and trioecious cross-pollinated species with male, female, and hermaphrodite plants. The Chilean papaya, originating from South America, has been extensively spread throughout the Andean nations, cultivated primarily in the Coquimbo and Valparaíso valleys in Chile, between 34°41' and 36°33' latitude south.

Antioxidant, Phytochemical, and Pharmacological Properties of Algerian Extracts.

Water mint () is used in many formulations worldwide as a functional food and natural remedy to treat gastrointestinal disorders, lung diseases, and certain mental disorders such as epilepsy and depression. This study assessed the bioactivity of its infusion extract (INF) and hydroethanolic extract (HE) to highlight its health benefits. These extracts were analyzed for their chemical composition by HPLC-DAD-ESI-MSn, their antioxidant and antidiabetic properties, and their capacities to protect human erythrocytes against induced hemoglobin oxidation and lipid peroxidation.

Age-associated interplay between zinc deficiency and Golgi stress hinders microtubule-dependent cellular signaling and epigenetic control.

Golgi abnormalities have been linked to aging and age-related diseases, yet the underlying causes and functional consequences remain poorly understood. This study identifies the interaction between age-associated zinc deficiency and Golgi stress as a critical factor in cellular aging. Senescent Golgi bodies from human fibroblasts show a fragmented Golgi structure, associated with a decreased interaction of the zinc-dependent Golgi-stacking protein complex Golgin45-GRASP55.

Development of a mertansine-specific DNA aptamer and novel high-throughput sandwich enzyme-linked oligonucleotide assay for quantification and characterization of trastuzumab emtansine.

We developed a novel DNA aptamer, D8#24S1, which specifically recognizes mertansine (DM1), the cytotoxic payload of the antibody-drug conjugate (ADC) trastuzumab emtansine (T-DM1), and applied it for T-DM1 analysis. D8#24S1 was obtained through SELEX and was shown to specifically recognize DM1 with high affinity (dissociation constant, K = 84.2 nM).

Comparative analysis of hospital laboratory wastewater treatment techniques in Syrian Arab Republic.

Background: Hospital wastewater poses a significant threat to human health due to the presence of difficult-to-degrade organic compounds, active pharmaceutical ingredients and multiple inorganic substances that can pollute water resources and ecosystems.

Aim: To compare the effectiveness of different techniques for removing organic load from hospital laboratory wastewater in Aleppo, Syria.

Methods: We treated wastewater samples from hospital laboratories at Aleppo University Hospital, Syria, using several techniques, including biological treatment with the rotating biological contactor, adsorption with Syrian natural clay, coagulation with aluminium sulphate, advanced oxidation with ultrasound, and a combined treatment using natural clay and ultrasound.

Inhibitory Effect of Human Anti-CA I Autoantibodies and Development of Monoclonal Antibody mAb 2B8 Targeting Carbonic Anhydrase I.

Spontaneous tumor regression is a recognized phenomenon across various cancer types. Recent research emphasizes the alterations in autoantibodies against carbonic anhydrase I (CA I) (anti-CA I) levels as potential prognostic markers for various malignancies. Particularly, autoantibodies targeting CA I and II appear to induce cellular damage by inhibiting their respective protein's catalytic functions.

New Hydrogenated Phenanthrene Glycosides from the Edible Vegetable W.T.Wang with DPP-IV Inhibitory and Hepatoprotective Activity.

Based on molecular networking-guided isolation, 15 previously undescribed hydrogenated phenanthrene glycosides, including eight hexahydro-phenanthrenone glycosides, four tetrahydro-phenanthrenone glycosides, one dihydro-phenanthrenol glycoside, two dimers, and two known dihydrophenanthrene glycosides, were isolated from W.T.Wang, a popular regional edible vegetable at the northwest region of Vietnam.

Exploration of novel triazolo-thiadiazine hybrids of deferasirox as multi-target-directed anti-neuroinflammatory agents with structure-activity relationship (SAR): a new treatment opportunity for Alzheimer's disease.

It is believed that inflammation influences several physiological processes, including the function of the central nervous system. Moreover, the impairment of lipid mechanisms/pathways is associated with neurodegenerative disorders and onset of Alzheimer's disease (AD). AD is a chronic neurodegenerative disease representing the major cause of dementia worldwide.

HepG2 spheroids cultured in alginate microcapsules as a model for exploring mitochondrial and glycolytic metabolism using the Seahorse XFe24 Analyzer.

Mitochondria are affected by chemical substances and play a critical role in drug-induced liver injury (DILI). Chemical substances can have a significant impact on various cellular processes, such as the disruption of oxidative phosphorylation, oxidative stress, and alteration of glucose metabolism. Given the consequences of these effects, it is crucial to understand the molecular pathways of chemical substances in the context of hepatotoxicity to prevent and treat DILI.

Biological Characterization of One Oxadiazole Derivative (5(4-Hydroxyphenyl)-2-(N-Phenyl Amino)-1,3,4-Oxadiazole): In Vitro, In Silico, and Network Pharmacological Approaches.

Oxadiazole compounds are of great interest because they have a range of biological activities ranging from antioxidants to anticancer agents. Against this background, we wanted to demonstrate the antioxidant, enzyme inhibitory, and anticancer effects of 5(4-hydroxyphenyl)-2-(N-phenylamino)-1,3,4-oxadiazole (Hppo). Antioxidant abilities were measured through free radical scavenging and reducing power tests.

Administration of Immune Checkpoint Inhibitors to Patients on Warfarin May Elevate PT-INR.

The relationship between the concomitant use of immune checkpoint inhibitors (ICIs) and elevated prothrombin time-to-international standard ratio (PT-INR) in patients receiving warfarin remains unclear. In the present study, 26 patients treated with ICIs during warfarin therapy were examined for increases in PT-INR within 60 d of ICI administration. Of these patients, 13 developed Grade 2 or higher PT-INR elevations, 5 of which required the immediate administration of vitamin K.

Supramolecular delivery systems for polyphenols: A green approach to predict in vivo permeability through an in vitro setup.

The use of in vitro markers able to reproduce the in vivo permeability and diffusivity of orally administered drugs, could represent an innovative starting point for the formulation of delivery systems, in particular for low soluble and low permeable drugs belonging to BCS class II and IV. Considering the great interest in the green pharmaceutical approaches and the increasing use of natural molecules as novel therapeutic drugs, in this study, rutin, hesperidin and curcumin have been selected as lipophilic model drugs to investigate their possible enhancement of their permeability and bioavailability after oral administration. As the low solubility of the three drugs hinders their application, β-cyclodextrins (CD), amphiphilic natural moieties able to form stable inclusion complexes, have been considered to promote their solubilization.

Progress in Nanotechnology for Treating Ocular Surface Chemical Injuries: Reflecting on Advances in Ophthalmology.

Ocular surface chemical injuries often result in permanent visual impairment and necessitate complex, long-term treatments. Immediate and extensive irrigation serves as the first-line intervention, followed by various therapeutic protocols applied throughout different stages of the condition. To optimize outcomes, conventional regimens increasingly incorporate biological agents and surgical techniques.