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Design, Synthesis, and Antitumor Activity Evaluation of 2-Phenylthiazole-5-Carboxylic Acid Derivatives Targeting Transactivation Response RNA-Binding Protein 2.
J Med Chem
December 2024
Center for Natural Products Research, Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China.
Transactivation response (TAR) RNA-binding protein 2 (TRBP) plays a critical role in microRNA (miRNA) biosynthesis, with aberrant expression linked to various cancers. Previously, we identified , a phenyloxazole derivative that disrupts the TRBP-Dicer interaction in hepatocellular carcinoma (HCC). In this study, we optimized this scaffold and substituent, leading to the discovery of , a 2-phenylthiazole-5-carboxylic acid derivative with nanomolar inhibitory activity (EC = 0.
View Article and Find Full Text PDFPreparation and Evaluation of Tetrandrine Nanocrystals to Improve Bioavailability.
Curr Drug Deliv
December 2024
Institute of Chinese Materia Medica, Chengde Medical University, Hebei Province Key Laboratory of Research and Development for Chinese Materia Medica, Chengde Hebei Province, 067000, P.R. China.
Background: Tetrandrine (TET) has multiple pharmacological activities, but its water solubility is poor, which is the main reason for its low bioavailability.
Objectives: The purpose of this study was to prepare TET nanocrystals (TET-NCs) using a grinding method to enhance the dissolution rate and ultimately improve the bioavailability of TET.
Methods: TET-NCs were synthesized via media milling, employing Poloxam 407 (P407) as surface stabilizer and mannitol as a cryoprotectant during freeze-drying.
Novel Nanoliposomes Synergistically Modulated by Sitogluside and Dioscin: Stability, Bioavailability, and Capacity To Alleviate Hyperuricaemia.
J Agric Food Chem
December 2024
Department of Food Science and Technology, Zhejiang University of Technology, Hangzhou, Zhejiang 310014, People's Republic of China.
Cholesterol (Cho) is commonly used to stabilize nanoliposomes; however, there is controversy on the relationship between Cho and health. In this study, we developed a novel multifunctional nanoliposome utilizing structurally similar sitogluside (SG) and dioscin (Dio) instead of Cho to anchor the phospholipid bilayer and synergistically modulate the membrane properties of the nanoliposome (DPPC or DOPC). The storage and gastrointestinal tract stability experiment demonstrated that the changes of physical and chemical properties, including the significantly reduced size and Dio retention rate of nanoliposomes synergistically modulated by SG and Dio compared to those of SG alone, regulated nanoliposomes.
View Article and Find Full Text PDF[Characteristics and Comprehensive Quality Assessment of Heavy Metals in Soil-crop System of High Geological Background Area].
Huan Jing Ke Xue
January 2025
Chongqing Key Laboratory of Land Quality Geological Survey, Southeast Sichuan Geological Group, Chongqing Bureau of Geology and Minerals Exploration, Chongqing 400038, China.
Heavy metals （HMs） pollution in agricultural soil-rice systems has attracted worldwide attention as it directly threatens regional ecological security and human health. To understand the heavy metal pollution of agriculture soil and rice in the high geological background areas, a total of 200 paddy soil and rice samples were collected in southeast Chongqing. The concentrations of arsenic （As）, cadmium （Cd）, chromium （Cr）, copper （Cu）, mercury （Hg）, nickel （Ni）, lead （Pb）, and zinc （Zn） in paddy soil and rice were analyzed.
View Article and Find Full Text PDFNanomaterials effectively alleviate cadmium hazards in soil-plant systems: A meta-analysis.
Sci Total Environ
December 2024
School of Ecology and Environment, Zhengzhou University, Zhengzhou 450001, China; School of Environmental Science and Engineering, College of Engineering, Southern University of Science and Technology, Shenzhen 518055, China. Electronic address:
Soil cadmium (Cd) contamination is a non-negligible global environmental issue as it may threaten food security and human health through soil-plant interactions. Nanomaterials have a great potential to decrease Cd bioavailability and bioaccumulation, even though the effects have been inconsistent among various studies. Here we compiled data from 137 experiments on the remediation of Cd-contaminated soils by nanomaterials.
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