Novel Approaches to Monitor Pharmacokinetics and Metabolism of Gemcitabine-Ibandronate Conjugate in Mice and Dogs.

Background: The use of the bone-seeking properties of bisphosphonates (BPs) to target the delivery of therapeutic drugs is a promising approach for the treatment of bone metastases. Currently, the most advanced example of this approach is a gemcitabine-ibandronate conjugate (GEM-IB), where the bone-targeting BP ibandronate (IB) is covalently linked to the antineoplastic agent gemcitabine (GEM) via a spacer phosphate group. In the present study, we describe the development of a new analytical platform to evaluate the metabolism and pharmacokinetics of GEM-IB in mice and dogs and the results of proof-of-concept studies assessing the pharmacokinetics of GEM-IB in dogs and mice.

Characterization and Analysis of 2-(2-Phenylethyl)chromone Derivatives and Sesquiterpenoids from Agarwood of Four "Qi-Nan" Clones () with Different Induction Times.

In recent years, some new "Qi-Nan" clones of with the characteristics of easy induction and high-quality agarwood have been obtained, through the cultivation and propagation of grafted seedlings. These clones are used for the intensive production of high-quality agarwood. The speed of resin formation and yield are crucial for the development of the agarwood industry.

Synthesis and Biological Evaluation of New -Restricted Triazole Analogues of Combretastatin A-4.

The natural products combretastatins A-1 and A-4 are potent antimitotic and vascular-disrupting agents through their binding at the colchicine site in tubulin. However, these compounds suffer from a low water solubility and a tendency to isomerize to the inactive stilbenes. In this study, we have prepared a series of 18 -restricted triazole analogues of combretastatin A-4 (CA-4), maintaining, in all cases, the 3,4,5-trimethoxy phenyl ring A, with the aim of investigating the substitution pattern on the B-ring in a systematic way.

Comparative Analysis of γ-Cyclodextrin, Perilla Oil, and Their Inclusion Complexes on Liver Injury and Dyslipidemia Associated with Elevated Gastrointestinal 12-Hydroxylated Bile Acid Levels.

Our previous study demonstrated that γ-cyclodextrin (γ-CD)-perilla oil inclusion complexes increase plasma α-linolenic acid and eicosapentaenoic acid levels in healthy rats without adverse effects. The present study examined the effects of perilla oil, γ-CD, and their inclusion complexes on rats fed cholic acid (CA) to mimic the elevated gastrointestinal 12-hydroxylated (12OH) bile acid levels in high-fat diet-fed rats. Rats fed CA (CA group) tended to have higher AST, ALT, plasma total cholesterol (T-CHO), and triglyceride (TG) levels compared to controls fed a standard diet without CA.

Autophagy-Enhancing Properties of Extracts in HaCaT Keratinocytes: Potential as an Anti-Photoaging Cosmetic Ingredient.

The decline in autophagy disrupts homeostasis in skin cells, leading to oxidative stress, energy deficiency, and inflammation-all key contributors to skin photoaging. Consequently, activating autophagy has become a focal strategy for delaying skin photoaging. Natural plants are rich in functional molecules and widely used in the development of anti-photoaging cosmetics.

Leaf Essential Oil Compositions and Enantiomeric Distributions of Monoterpenoids in Species: , , , , and .

Members of the genus are well known for their medicinal properties, which can be attributed to their essential oils. In this work, we have examined the leaf essential oils of five understudied species collected from various locations in western North America. The essential oils were obtained by hydrodistillation and analyzed by gas chromatographic methods, including enantioselective gas chromatography.

From Waste to Value: Optimization of Ultrasound-Assisted Extraction of Anthocyanins and Flavonols from L. Oilcakes.

L., commonly known as the mastic tree or lentisk, is a woody Mediterranean plant revered for its ecological relevance as well as for its extensive ethnobotanical heritage. Historically, the fruits and the resin of have been widely utilized in traditional medicine, underscoring its important role in local healing practices.

-Halogenation and -Alkoxylation of Phenylglycine Derivatives by Pd-Mediated C-H Functionalization: Scope and Limitations.

Orthopalladated derivatives from substituted phenylglycines [Pd(μ-Cl)(CHRC(R)(R)N(R)] () react with halogenating reagents (PhICl, Br, I) () to give the corresponding o-halogenated amino acids CH(X)RC(R)(R)N(R) (). The reaction is general and tolerates a variety of functional groups (R to R) at the aryl ring, the Cα, and the N atom. On the other hand, the reaction of [Pd(μ-Cl)(CHRC(R)(R)N(R)] () with PhI(OAc) in the presence of a variety of alcohols ROH () gives the o-alkoxylated phenylglycines CH(OR)RC(R)(R)N(R) (), also as a general process.

Post-Translational Modifications of Proteins Orchestrate All Hallmarks of Cancer.

Post-translational modifications (PTMs) of proteins dynamically build the buffering and adapting interface between oncogenic mutations and environmental stressors, on the one hand, and cancer cell structure, functioning, and behavior. Aberrant PTMs can be considered as enabling characteristics of cancer as long as they orchestrate all malignant modifications and variability in the proteome of cancer cells, cancer-associated cells, and tumor microenvironment (TME). On the other hand, PTMs of proteins can enhance anticancer mechanisms in the tumoral ecosystem or sustain the beneficial effects of oncologic therapies through degradation or inactivation of carcinogenic proteins or/and activation of tumor-suppressor proteins.

Factors Influencing the Choice Between Multi-Target Stool DNA and Colonoscopy for Colorectal Cancer Screening Among Alaska Native Peoples.

The Alaska Tribal Health System is increasing colorectal cancer (CRC) screening among Alaska Native (AN) peoples, who experience the highest CRC rate in the world. Through a clinical trial (NCT04336397), AN people living in rural/remote Alaska were offered either the previously unavailable multi-target stool DNA test (mt-sDNA; Cologuard) or colonoscopy. From April 2022 to August 2024, 113 (59%) people who completed mt-sDNA testing and 51 (39%) who completed a colonoscopy procedure participated in a survey on factors influencing their screening test choice.

MR T2* Map to Predict Worsening Hypertension Control: A Preliminary Study.

Blood pressure measurement is important in monitoring hypertension. However, blood pressure does not provide much information about renal condition in treated hypertension. This study aimed to evaluate renal oxygenation in hypertensive patients using T2* mapping.

Fatty Acid Content and Profile in in Response to Exposure to Variable Growth Conditions in Indoor Photobioreactors.

Seaweed presents a sustainable alternative source of valuable fatty acids (FAs) involving omega-3 (-3) and omega-6 (). As such, there is great potential to reduce pressure on wild fish populations, helping to combat overfishing and its associated global impacts. This study explored the effect of various environmental factors on the FA content and profile of using indoor photobioreactors.

Associations of Voice Metrics with Postural Function in Parkinson's Disease.

Background: This study aimed to explore the potential associations between voice metrics of patients with PD and their motor symptoms.

Methods: Motor and vocal data including the Unified Parkinson's Disease Rating Scale part III (UPDRS-III), Harmonic-Noise Ratio (HNR), jitter, shimmer, and smoothed cepstral peak prominence (CPPS) were analyzed through exploratory correlations followed by univariate linear regression analyses. We employed these four voice metrics as independent variables and the total and sub-scores of the UPDRS-III as dependent variables.

Analysis of Clinically Symptomatic Patients to Differentiate Inflammatory Breast Cancer from Mastitis in Asian Women.

Purpose: To differentiate inflammatory breast cancer (IBC) from mastitis in Asian women presenting with symptoms of inflammation.

Methods: Between January 2012 and June 2024, 101 Asian women with symptoms of inflammation underwent breast ultrasound (US). Clinical and demographic data were extracted from patients' medical records.

Sulfur Analogs of the Core Formose Cycle: A Free Energy Map.

Using computational methods, we examine if the presence of HS can tame the unruly formose reaction by generating a free energy map of the reaction thermodynamics and kinetics of sulfur analogs within the core cycle. With mercaptoaldehyde as the linchpin C species, and feeding the cycle with CHO, selected aldol additions and enolizations are kinetically more favorable. Thione formation is thermodynamically less favored compared to aldehydes and ketones, but all these species can be connected by enolization reactions.

Experimental Investigation on Macroscopic and Microscopic Mechanical Properties of Geopolymer-Stabilized Macadam.

Geopolymer, as a promising inorganic binding material, holds potential for use in constructing base layers for highway pavements. This study aims to evaluate the mechanical properties of geopolymer-stabilized macadam (GSM) at both the micro- and macro-scale by a series of tests, demonstrating that high-Ca GSM is a high-quality material for pavement base layers. The results demonstrated that GSM exhibits outstanding mechanical and fatigue properties, significantly surpassing those of cement-stabilized macadam (CSM).

Sonochemical Functionalization of SiO Nanoparticles with Citric Acid and Monoethanolamine and Its Remarkable Effect on Antibacterial Activity.

Nanoparticles (NPs) are excellent antibacterial agents due to their ability to interact with microorganisms at the cellular level. However, their antimicrobial capacity can be limited by their tendency to agglomerate. Functionalizing NPs with suitable ligands improves their stability and dispersion in different media and enhances their antibacterial activity.

Mechanical Properties and Corrosion Resistance of Thin Ceria and Phosphate Mono- and Multilayers Deposited on Technically Pure Al 1050.

Calcium phosphates are often used for biomedical applications. Hydroxyapatite, for example, has a wide range of applications because it mimics the mineral component of natural bone. Widespread interest in the catalytic properties of ceria is due to its use in automotive catalytic converters.

The Effect of Alumina-Rich Spinel Exsolution on the Mechanical Property of Calcium Aluminate Cement-Bonded Corundum Castables.

This study investigates the effect of the exsolution behavior of alumina-rich spinel on the formation and distribution of CA (CaAlO) in corundum castables bonded with calcium aluminate cement. In this study, alumina-rich spinel is substituted for tabular corundum in the same proportions and grain size. The matrices after curing were analyzed by X-ray diffraction (XRD), scanning electron microscopy (SEM), and energy dispersive spectroscopy (EDS).

Optimization of In-Situ Growth of Superconducting Al/InAs Hybrid Systems on GaAs for the Development of Quantum Electronic Circuits.

Hybrid systems consisting of highly transparent channels of low-dimensional semiconductors between superconducting elements allow the formation of quantum electronic circuits. Therefore, they are among the novel material platforms that could pave the way for scalable quantum computation. To this aim, InAs two-dimensional electron gases are among the ideal semiconductor systems due to their vanishing Schottky barrier; however, their exploitation is limited by the unavailability of commercial lattice-matched substrates.

Finite Element Simulation of Hot Rolling for Large-Scale AISI 430 Ferritic Stainless-Steel Slabs Using Industrial Rolling Schedules-Part 1: Set-Up, Optimization, and Validation of Numerical Model.

A growing need to reduce the environmental impact and cost of manufacturing stainless steels has led to the development of ferritic stainless steel as an alternative to austenitic and duplex steels. The development of new stainless steels involves the optimization of their hot rolling processes, with the aim of minimizing the occurrence of defects and improving productivity. In this context, numerical simulation using the finite element method (FEM) is presented as a key tool to reduce the time and cost associated with traditional trial-and-error optimization methods.

Equation for Calculation of Critical Current Density Using the Bean's Model with Self-Consistent Magnetic Units to Prevent Unit Conversion Errors.

This study analyzes the calculation of the critical current density by means of Bean's critical state model, using the equation formulated by Gyorgy et al. and other similar equations derived from it reported in the literature. While estimations of using Bean's model are widely performed, improper use of different equations with different magnetic units and pre-factors leads to confusion and to significant errors in the reported values of .

Microstructure and Mechanical Properties of High-Pressure Die-Casting Mg-Al-RE Alloys with Minor Ca Addition.

With the increasing demand for magnesium (Mg) alloys with high strength and good ductility, this study explores high-pressure die-cast (HPDC) Mg-6Al-2RE (AE62), Mg-8Al-2RE (AE82) and Mg-8Al-2RE-0.2Ca (AEX820) alloys (wt. %).

The Influence of Alkali Metals on the Sintering Mineralization Process of Iron Ore.

To investigate the influence of alkali metal compounds in different forms on the sintering mineralization process of iron ore, the basic sintering characteristics of iron ore with alkali metal contents ranging from 0 to 4% were measured using the micro-sintering method, and the influence mechanism was analyzed using thermodynamic analysis and first-principles calculations. The results showed that (1) the addition of KCl/NaCl increased the lowest assimilation temperature (LAT) and the index of liquid-phase fluidity (ILF), while that of KCO/NaCO decreased the LAT but increased the ILF of iron ore. (2) The pores formed by the volatilization of KCl/NaCl suppressed the diffusion of Fe and Ca, which inhibited the formation of silico-ferrite of calcium and aluminum (SFCA).

Morphological Comparisons of Adult Worker Bees Developed in Chinese and Italian Honey Bee Combs.

The size of comb cells is a key factor influencing the body size of honey bee workers. Comb cells and the body size of Chinese honey bee workers are smaller than those of Italian honey bee workers. To increase the size of Chinese honey bee workers, this study used newly built combs from Chinese honey bee colonies (control group) and Italian honey bee colonies (treatment group).