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| http://dx.doi.org/10.1172/JCI104905 | DOI Listing |
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Positively-charged, chalcone-hydroxypyrone hybrid ruthenium(II)-arene complexes functionalized with ethacrynic acid: Synthesis, characterizaion, and antitumor effect.
J Inorg Biochem
February 2025
Key Laboratory of Chemical Biology of Hebei Province; Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education; State Key Laboratory of New Pharmaceutical Preparations and Excipients, College of Chemistry & Materials Science, Hebei University, Baoding 071002, China. Electronic address:
A new family of ethacrynic acid-functionalized, chalcone-hydroxypyrone hybrid ruthenium(II)-arene complexes (4a-4e) have been designed, synthesis and fully characterized by H and C NMR, ESI-MS, elemental analysis, and melting point tests. The molecular structure of 3a, one of the precursor complexes, has been determined by single-crystal X-ray diffraction. The cytotoxicity of the obtained complexes toward human cancer cell lines such as HeLa, MGC803, A549, MDA-MB-231, and MCF-7 cells have been investigated by MTT assay.
View Article and Find Full Text PDFPreparation of Glutathione-Regulated Sorafenib Targeted Nanodrug Delivery System and Its Antihepatocellular Carcinoma Activity.
ACS Appl Mater Interfaces
November 2024
Institute of Microbial Engineering, Laboratory of Bioresource and Applied Microbiology, School of Life Sciences, Henan University, Kaifeng 475004, Henan, China.
Article Synopsis
- Researchers created a targeted nanodrug delivery system, called SMEH nanoparticles, to improve the effectiveness of sorafenib (SOR) for liver cancer treatment by reducing glutathione (GSH) levels in tumor cells.
- The preparation involved synthesizing mesoporous silica nanoparticles, modifying them, loading them with SOR, and coating them with hyaluronic acid, allowing targeted entry into tumor cells.
- Experimental results show that SMEH nanoparticles successfully target liver cancer cells, lower GSH levels, enhance antitumor effects, and demonstrate good safety, indicating their potential for cancer therapy.
Improved intracochlear biopolymeric drug delivery system: an study.
Acta Otolaryngol
December 2024
Department of Otolaryngology - Head and Neck Surgery, University of Miami Ear Institute, University of Miami, Miller School of Medicine, Miami, FL, USA.
Background: The delivery of drugs into the inner ear is a challenging field of study due to the complex cochlear anatomy and physiology. The creation of an intracochlear device that allows for short- and long-term intracochlear delivery of the drugs with a minimal invasive technology is needed to prevent or treat conditions that can potentially prevent the development of permanent hearing loss.
Aim: This study intends to test the efficacy of DXM-infused PLGA microneedles created in our laboratory in an animal model of acute ototoxic injury.
Differential interactions of ethacrynic acid and diethyl maleate with glutathione S-transferases and their glutathione co-factor in the house fly.
Pestic Biochem Physiol
November 2024
Entomology and Nematology Department, University of Florida, Gainesville, FL 32611, USA.
Glutathione S-transferases (GSTs) are an important class of enzymes that facilitate the conjugation of reduced glutathione (GSH) with electrophilic substrates, including some insecticides. Two inhibitors of GSTs, ethacrynic acid (EA) and diethyl maleate (DEM), are often used as diagnostic tools to implicate GST involvement in insecticide resistance, but their modes of action against insect GSTs are largely assumed based on mammalian studies. In mammalian studies, there are two proposed mechanisms of inhibition of GST function by EA and DEM: 1) scavenging or "depleting" cytosolic GSH through non-enzymatic conjugation, and 2) inhibition of GST activity directly by the inhibitor-GSH conjugate (EA-SG and DEM-SG).
View Article and Find Full Text PDFNew Small-Molecule SERCA Inhibitors Enhance Treatment Efficacy in Lenvatinib-Resistant Papillary Thyroid Cancer.
Int J Mol Sci
October 2024
Department of Surgery, Yonsei University College of Medicine, 50-1, Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.
Papillary thyroid cancer (PTC) is one of the most treatable forms of cancer, with many cases being fully curable. However, resistance to anticancer drugs often leads to metastasis or recurrence, contributing to the failure of cancer therapy and, ultimately, patient mortality. The mechanisms underlying molecular differences in patients with metastatic or recurrent PTC, particularly those resistant to anticancer drugs through epigenetic reprogramming, remain poorly understood.
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