Drug Metabolism and Bioanalysis Letters - Volume 15, Issue 1, 2022

Background: Herbal products are derived from different natural sources, mainly used as a source of food material and medicine in the health sectors since ancient times. Herbal products have gained popularity in modern medicine due to their beneficial health properties and pharmacological activities. Flavonoids are an important class of secondary metabolites found to be present in medicinal plants and their Read More

Background and Objective: Compound X is a drug candidate for the treatment of neurodegenerative diseases. Its brain distribution was evaluated as part of the lead identification and optimization activities undertaken in early drug discovery. Methods: The brain distribution of compound X was studied in genetic transporter knockout rodent models, in vivo models with a chemical inhibitor, and in vitro transporter cell systems. Re Read More

Background: In this study, we focused primarily on three anti-malarial drugs, namely chloroquine, mefloquine, and proguanil, and these were tested against two malarial targets DHFR and GST. The species Plasmodium falciparum, Plasmodium malariae, Plasmodium ovale, Plasmodium vivax were used for the study. Objective: The purpose of this study was to determine the sequence and structural similarity of the protei Read More

Objective: The study aims to explore the human in vivo metabolism of SEP-227900 (4H-furo[3, 2-b] pyrrole-carboxylic acid, m.w 151.03), a D-amino-acid oxidase (DAAO) inhibitor, by using plasma and urine samples from first-in-human study. Methods: The human plasma and urine samples were from a single dose cohort that consisted of 9 healthy male volunteers each received an 80- mg dose of SEP-227900 orally. The poo Read More

Background: Genetic polymorphism of cytochrome P450 (CYP) contributes to variability in drug metabolism, clearance, and response. This study aimed to investigate the functional and molecular basis for altered ligand binding and catalysis in CYP2D6*14A and CYP2D6*14B, two unique alleles common in the Asian population. Methods: CYP proteins expressed in Escherichia coli were studied using the substrate 3-cyano-7- ethox Read More

Aim: The main aim of the current study was to obtain forward dosimetry assessments of pyrrolizidine alkaloid senkirkine plasma and liver concentrations by setting up a human physiologically based pharmacokinetic (PBPK) model based on the limited information available. Background: The risks associated with plant-derived pyrrolizidine alkaloids as natural toxins have been assessed. Objective: The pyrrolizidine alkaloid Read More