Following ICH guidelines, the stability of Belumosudil, a novel protein kinase inhibitor, was tested under different stress conditions (hydrolytic, oxidative, photolytic, and thermal). A selective and efficient separation of Belumosudil and its degradation products was achieved using a Quality by Design approach. In-silico predictions using Zeneth Nexus® software were employed to assess the compound's degradation under various stress scenarios. The methodology developed through experimental design analyzed crucial process parameters connected with chromatographic systems. Reversed-phase high-performance liquid chromatography with a C18 column and a gradient mobile phase of acetonitrile and 25 mM ammonium hydrogen carbonate buffer (pH 5.6) were utilized. For structural characterization and identification of degradation products, UPLC-quadrupole tandem mass spectrometry was employed. Four distinct degradation products were identified under different stress settings. The method was thoroughly validated, assessing accuracy, selectivity, repeatability, system suitability, and linearity range (5.0-120.0 μg/mL). To predict mutagenicity and toxicity, DEREK Nexus® software was used. Two degradation products were predicted to induce skin sensitization, irritation, and hepatotoxicity in humans.
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http://dx.doi.org/10.1016/j.heliyon.2024.e38369 | DOI Listing |
Sci Rep
December 2024
Department of Pharmaceutical Chemistry, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, India.
The emergence of self-propelling magnetic nanobots represents a significant advancement in the field of drug delivery. These magneto-nanobots offer precise control over drug targeting and possess the capability to navigate deep into tumor tissues, thereby addressing multiple challenges associated with conventional cancer therapies. Here, Fe-GSH-Protein-Dox, a novel self-propelling magnetic nanobot conjugated with a biocompatible protein surface and loaded with doxorubicin for the treatment of triple-negative breast cancer (TNBC), is reported.
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December 2024
Department of Biotechnology, Faculty of Agro-industry, Kasetsart University, Bangkok, 10900, Thailand.
Tilapia lake virus (TiLV) disease is highly contagious and causes substantial mortality in tilapia. Currently, no effective treatments or commercial vaccines are available to prevent TiLV infection. In this study, TiLV segment 4 (S4) was cloned into the pET28a(+)vector and transformed into Escherichia coli BL21(DE3).
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December 2024
Department of Endocrinology, Children's Hospital, Zhejiang University School of Medicine, National Children's Regional Medical Center, National Clinical Research Center for Child Health, 3333 Binsheng Road, Hangzhou, 310052, Zhejiang Province, China.
Williams Syndrome (WS) is a rare neurodevelopmental disorder with a prevalence of 1 in 7500 to 1 in 20,000 individuals, caused by a microdeletion in chromosome 7q11.23. Despite its distinctive clinical features, the underlying metabolic alterations remain largely unexplored.
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December 2024
IRCCS SYNLAB SDN, Naples, 80143, Italy.
LAG3 plays a regulatory role in immunity and emerged as an inhibitory immune checkpoint molecule comparable to PD-L1 and CTLA-4 and a potential target for enhancing anti-cancer immune responses. We generated 3D cancer cultures as a model to identify novel molecular biomarkers for the selection of patients suitable for α-LAG3 treatment and simultaneously the possibility to perform an early diagnosis due to its higher presence in breast cancer, also to achieve a theragnostic approach. Our data confirm the extreme dysregulation of LAG3 in breast cancer with significantly higher expression in tumor tissue specimens, compared to non-cancerous tissue controls.
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December 2024
College of Grassland Science, Inner Mongolia Agricultural University, Hohhot, 010019, China.
Hydrothermal biochar has demonstrated potential in enhancing crop growth by improving soil properties and microbial activity; however, its effectiveness varies with application rate, with excessive amounts potentially inhibiting plant growth. This study employed a pot experiment approach to compare varying application rates of hydrothermal biochar (ranging from 0 to 50 t/ha) and to analyze its effects on alfalfa biomass, photosynthetic efficiency, soil nutrient content, and microbial community composition. Biochar application increased alfalfa dry weight by 12.
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