Current Drug Metabolism - Volume 23, Issue 12, 2022

Orphan cytochromes P450 (CYP) are enzymes whose biological functions and substrates are unknown. However, the use of new experimental strategies has allowed obtaining more information about their relevance in the metabolism of endogenous and exogenous compounds. Likewise, the modulation of their expression and activity has been associated with pathogenesis and prognosis in different diseases. In this work, Read More

Background: Salt-processed product of cuscutae semen (SCS), which is documented in Chinese pharmacopoeia (2020 edition), is one of the processed products of cuscustae semen. SCS possesses hepatoprotective effects. However, Pharmacokinetic/Pharmacodynamic (PK-PD) study of SCS with intervening acute liver injury (ALI) has not been reported yet. Effective constituents are still not well addressed. Objective: This Read More

Background: Tangeretin, present in citrus fruits, is a polymethoxy flavone with extensive pharmacological effects. It has been widely used in the clinic, but there were no detailed studies on the in vivo metabolism of tangeretin. Objective: This study aimed to establish a rapid and effective strategy to identify the metabolites of tangeretin and evaluate the biotransformation pathways of tangeretin in rats. Methods: The ultra- Read More

Background: Despite CoQ10 being a powerful antioxidant and its redox state that may characterize the body’s antioxidant system, the latter remains unstudied in patients with cardiovascular diseases. Objective: This prospective case-control study aimed to investigate the concentrations of ubiquinol, ubiquinone, total CoQ10 and its redox state in patients with ischemic heart disease (IHD) and arterial hypertension (AH) duri Read More

Background: Irinotecan is widely used to treat various types of solid and metastatic cancer. It is an ester prodrug and its hydrolytic metabolite (SN-38) exerts potent anticancer activity. Irinotecan is hydrolyzed primarily by carboxylesterase-2 (CES2), a hydrolase abundantly present in the intestine such as the duodenum. We have identified several potent and covalent CES2 inhibitors such as remdesivir and sofosbuvir. Rem Read More