tagitinin and Pulmonary-Arterial-Hypertension

tagitinin has been researched along with Pulmonary-Arterial-Hypertension* in 1 studies

Other Studies

1 other study(ies) available for tagitinin and Pulmonary-Arterial-Hypertension

ArticleYear
Evaluation of Naturally Occurring HIF-1 Inhibitors for Pulmonary Arterial Hypertension.
    Chembiochem : a European journal of chemical biology, 2021, 09-14, Volume: 22, Issue:18

    Pulmonary arterial hypertension (PAH) is a rare and severe progressive disorder characterized by high pulmonary artery pressure. Chronic hypoxia causes a metabolic disorder and the Warburg effect in pulmonary arterial smooth muscle cells (PASMCs). Pyruvate dehydrogenase kinase 1 (PDK1) is a key enzyme in Warburg effect increased by hypoxia-inducible factor (HIF-1). We constructed a cell-based luciferase assay system for HIF-1 inhibitors. Using this system, six HIF-1 inhibitors were identified. Among these inhibitors, the effect of tagitinin C (1) on PASMC was investigated. Tagitinin C (1) clearly decreased the amount of HIF-1β and the HIF-1 target PDK1. This result indicates that HIF-1 inhibitors effectively decrease PDK1 activity, which is a cause of the metabolic disorder and Warburg effect observed in PASMCs. Identifying naturally occurring HIF-1 inhibitors could provide novel insights into the development of PAH medications.

    Topics: Biological Products; Cell Line; Cell Survival; Humans; Hypoxia-Inducible Factor 1, alpha Subunit; Myocytes, Smooth Muscle; Pulmonary Arterial Hypertension; Pyruvate Dehydrogenase Acetyl-Transferring Kinase; Sesquiterpenes

2021