Alpha6beta2 nicotinic acetylcholine receptors (nAChRs) are potential therapeutic targets for the treatment of several neuropsychiatric diseases, including addiction and Parkinson's disease. Alpha-conotoxin (α-CTx) TxIB is a uniquely selective ligand, which blocks α6/α3β2β3 nAChRs only, but does not block the other subtypes. Therefore, α-CTx TxIB is a valuable therapeutic candidate peptide. Synthesizing enough α-CTx TxIB with high yield production is required for conducting wide-range testing of its potential medicinal applications. The current study optimized the cleavage of synthesized α-CTx TxIB resin-bounded peptide and folding of the cleaved linear peptide. Key parameters influencing cleavage and oxidative folding of α-CTx TxIB were examined, such as buffer, redox agents, pH, salt, co-solvent and temperature. Twelve conditions were used for cleavage optimization. Fifty-four kinds of one-step oxidative solution were used to assess their effects on each α-CTx TxIB isomers' yield. The result indicated that co-solvent choices were particularly important. Completely oxidative folding of globular isomer was achieved when the NH₄HCO₃ or Tris-HCl folding buffer at 4 °C contained 40% of co-solvent DMSO, and GSH:GSSG (2:1) or GSH only with pH 8~8.7.
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http://dx.doi.org/10.3390/md11093537 | DOI Listing |
Green Chem
May 2024
State Key Laboratory of Environmental Criteria and Risk Assessment, National Engineering Laboratory for Lake Pollution Control and Ecological Restoration, State Environmental Protection Key Laboratory for Lake Pollution Control, Chinese Research Academy of Environmental Science, Beijing, China.
The global plasticizer market is projected to increase from $17 billion in 2022 to $22.5 billion in 2027. Various emerging/alternative plasticizers entered the market following the ban on several phthalate plasticizers because of their harmful effects.
View Article and Find Full Text PDFSci Total Environ
March 2024
Research Group "Analytical Chemistry of Contaminants", Department of Chemistry and Physics, Research Centre for Mediterranean Intensive Agrosystems and Agri-Food Biotechnology (CIAIMBITAL), University of Almeria, Agrifood Campus of International Excellence, ceiA3, E-04120 Almeria, Spain. Electronic address:
Non-phthalate plasticizers (NPPs) are a suitable alternative to phthalates, which are harmful compounds for human, animal health, and the environment. In this study, 28 commercial non-phthalate plasticizers (NPPs) from different families, including adipates, citrates, phosphates, sebacates, trimellitates, benzoates and cyclohexanoates, were determined. Two novel methods for determining these alternative compounds in soil were developed using gas chromatography coupled to high-resolution mass spectrometry (GC-HRMS-Q-Orbitrap) and liquid chromatography coupled to high-resolution mass spectrometry (LC-HRMS-Q-Orbitrap).
View Article and Find Full Text PDFInt J Mol Sci
May 2023
School of Medicine, Guangxi University, Nanning 530004, China.
Conotoxins are widely distributed and important for studying ligand-gated ion channels. TxIB, a conotoxin consisting of 16 amino acids derived from , is a unique selective ligand that blocks rat α6/α3β2β3 nAChR (IC = 28 nM) without affecting other rat subtypes. However, when the activity of TxIB against human nAChRs was examined, it was unexpectedly found that TxIB had a significant blocking effect on not only human α6/α3β2β3 nAChR but also human α6/α3β4 nAChR, with an IC of 537 nM.
View Article and Find Full Text PDFJ Toxicol Sci
January 2023
Faculty of Pharmacy, Meijo University.
Transient Receptor Potential Ankyrin 1 (TRPA1), which is expressed in the airways, has causative and exacerbating roles in respiratory diseases. TRPA1 is known as a target of sick building syndrome-related air pollutants, such as formaldehyde. Thus, an in vitro TRPA1 activation assay would be useful for predicting the potential risk of air pollution.
View Article and Find Full Text PDFJ Chem Ecol
June 2022
Division of Applied Life Sciences, Graduate School of Agriculture, Kyoto University, Sakyo, Kyoto, 606-8502, Japan.
TXIB (2,2,4-trimethyl-1,3-pentanediol diisobutyrate), a common plasticizer, inhibits the peach fruit moth, Carposina sasakii from ovipositing on young apple fruits. Using an insect assay and gas chromatography with an electroantennographic detector (GC-EAD) analysis, the stereochemistry of the bioactive compound was identified to be 3R, whereas (3S)-TXIB showed no activity. The inactive enantiomer did not inhibit the activity of commercially available TXIB, which was a racemic mixture.
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