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Four functional genotoxic marker genes (Bax, Btg2, Ccng1, and Cdkn1a) discriminate genotoxic hepatocarcinogens from non-genotoxic hepatocarcinogens and non-genotoxic non-hepatocarcinogens in rat public toxicogenomics data, Open TG-GATEs.
Genes Environ
December 2024
Division of Genome Safety Science, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki-Ku, 210-9501, Japan.
Background: Previously, Japanese Environmental Mutagen and Genome Society/Mammalian Mutagenicity Study Group/Toxicogenomics Study Group (JEMS/MMS toxicogenomic study group) proposed 12 genotoxic marker genes (Aen, Bax, Btg2, Ccnf, Ccng1, Cdkn1a, Gdf15, Lrp1, Mbd1, Phlda3, Plk2, and Tubb4b) to discriminate genotoxic hepatocarcinogens (GTHCs) from non-genotoxic hepatocarcinogens (NGTHCs) and non-genotoxic non-hepatocarcinogens (NGTNHCs) in mouse and rat liver using qPCR and RNA-Seq and confirmed in public rat toxicogenomics data, Open TG-GATEs, by principal component analysis (PCA). On the other hand, the U.S.
View Article and Find Full Text PDFElucidating the molecular mechanism of noncompetitive inhibition of acetylcholinesterase by an antidiabetic drug chlorpropamide: identification of new allosteric sites.
Phys Chem Chem Phys
November 2024
Department of Chemical and Biological Sciences, S. N. Bose National Centre for Basic Sciences, JD Block, Sector III, Salt Lake, Kolkata 700106, India.
Acetylcholinesterase (AChE) has emerged as an important drug target for the treatment of neurodegenerative disorders such as Alzheimer's disease (AD). Recent experimental studies indicate that certain antidiabetic drugs can be repurposed as potent AChE inhibitors. Enzymatic kinetic assays suggest that the antidiabetic drug chlorpropamide (CPM) acts as a noncompetitive inhibitor, but the mechanism of action and the binding site(s) of interaction with AChE are not known.
View Article and Find Full Text PDFEffects of Compound Probiotics on Pharmacokinetics of Cytochrome 450 Probe Drugs in Rats.
Drug Metab Dispos
October 2024
Department of Clinical Pharmacology, Xiangya Hospital, Central South University, Changsha, China (Y.Z., Y.X., T.W., H.Y., Y.L., R.Z., Yal.X., Yan.X., X.Y., J.Z., H.Z., W.Z., Q.L., P.Z.); Institute of Clinical Pharmacology, Central South University, Hunan Key Laboratory of Pharmacogenetics, Changsha, China (Y.Z., Y.X., T.W., H.Y., Y.L., R.Z., Yal.X., Yan.X., X.Y., J.Z., H.Z., W.Z., Q.L., P.Z.); Engineering Research Center of Applied Technology of Pharmacogenomics, Ministry of Education, Changsha, China (Y.Z., Y.X., T.W., H.Y., Y.L., R.Z., Yal.X., Yan.X., X.Y., J.Z., H.Z., W.Z., Q.L., P.Z.); National Clinical Research Center for Geriatric Disorders, Changsha, China (Y.Z., Y.X., T.W., H.Y., Y.L., R.Z., Yal.X., Yan.X., X.Y., J.Z., H.Z., W.Z., Q.L., P.Z.); Department of Hypertension, Xingsha Hospital, Changsha, China (Z.C., F.G., J.Y., S.L.); Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland at Baltimore, Maryland (Y.S.); and Key Specialty of Clinical Pharmacy, The First Affiliated Hospital of Guangdong Pharmaceutical University, Guangzhou, China (X.L.)
Article Synopsis
- The study investigates how the compound probiotic VSL#3 affects the metabolism of various cytochrome P450 enzyme probe drugs in male Wistar rats.
- Results show that VSL#3 alters the gut microbiota, leading to significant increases in the bioavailability of certain drugs, like omeprazole, while decreasing the bioavailability of others like tolbutamide and chlorpropamide.
- Additionally, the administration of VSL#3 impacted gene expression related to drug metabolism and intestinal structure, suggesting that probiotics can influence how drugs are processed in the body.
Metal-Free Synthesis of Pharmaceutically Relevant Sulfonylureas via Direct Reaction of Sulfonamides with Amides.
J Org Chem
September 2024
Department of Chemistry, Central University of Punjab, Bathinda 151401, India.
A metal-free process has been developed for the sustainable synthesis of medicinally important sulfonylureas in one pot via the direct reaction of sulfonamides with amides in green solvent (DMC). The reaction proceeded efficiently at room temperature, and the products were obtained in good to excellent yields. The use of readily accessible, inexpensive, and environmentally benign starting materials and reagents, metal-free mild reaction conditions, wide substrate scope, tolerance to air and moisture, operational simplicity, and good atom economy are the salient features of this reaction protocol.
View Article and Find Full Text PDFSynthon Approach in Crystal Engineering to Modulate Physicochemical Properties in Organic Salts of Chlorpropamide.
Mol Pharm
June 2024
Department of Chemistry, IISER Bhopal, Bhopal Bypass Road, Bhopal, Madhya Pradesh 462066, India.
The formulation of drug with improved bioavailability is always challenging and indispensable in the field of pharmaceutics. The control of intermolecular interactions via crystal engineering approach and solid-state molecular recognition results in the formation of active drug molecules with modulated pharmacological benefits. Therefore, with the aim to improve the solubility and dissolution rate of the drug chlorpropamide (), the mechanochemical liquid-assisted grinding (LAG) of the drug with several pharmaceutically accepted excipients was performed.
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