Design and Synthesis of 1,4‐Diformyl‐Piperazine Ferrostatin‐1 Derivatives as Novel Ferroptosis Inhibitors DOI Open Access
Yifan Zhang, Wei Guo, Hui Zheng

и другие.

Chemical Biology & Drug Design, Год журнала: 2024, Номер 104(5)

Опубликована: Окт. 28, 2024

ABSTRACT The present study focuses on the design and synthesis of novel 1,4‐diformyl‐piperazine‐based ferrostatin‐1 (Fer‐1) derivatives, their evaluation against ferroptosis activity. synthesized compounds demonstrated significant anti‐ferroptosis activity in human umbilical vascular endothelial cells (HUVECs), with Compound 24 showing highest potency. Mechanistic studies revealed that effectively reduced intracellular reactive oxygen species (ROS) levels, mitigated mitochondrial damage, enhanced glutathione peroxidase 4 (GPX4) expression. Additionally, exhibited improved solubility plasma stability compared to control compounds, Fer‐1 JHL‐12. These findings suggest derivatives hold promise as therapeutic agents for ferroptosis‐associated cardiovascular diseases.

Язык: Английский

Impairment of Endogenous H2S Pathway due to Aging and Endothelium Denudation in Mouse Isolated Thoracic Aorta DOI Creative Commons

Fatma Aydinoglu,

Eda Erdem,

Tuğba Toyran

и другие.

Physiological Research, Год журнала: 2025, Номер 1/2025, С. 59 - 68

Опубликована: Март 10, 2025

Hydrogen sulfide (H2S) is a gas neurotransmitter that synthesized in various mammalian tissues including vascular and regulates tone. The aim of this study to investigate whether the endogenous L-cysteine/H2S pathway impaired due aging endothelial denudation mouse isolated thoracic aorta. For purpose, young (3-4 months) old (23-25 mice were used experiments. effects endothelium on exogenous H2S-induced vasorelaxation investigated by cumulative L-cysteine-(1 µM-10 mM) NaHS-(1 µM-3 induced vasorelaxations, respectively. L-cysteine-induced relaxations reduced aorta compared mice. Also, vasorelaxant responses L-cysteine (1 rings with denuded-endothelium However, relaxation NaHS not altered age or denudation. loss staining CSE layer was observed Ach-induced (1-30 µM) almost abolished endothelium-denuded from both group. Ach intact tissue In conclusion, but decreased protein expression consistent decrease H2S concentration damage, suggesting may be lead enzyme signaling system damage

Язык: Английский

Процитировано

0

Hydrogen sulfide preserves the function of senescent endothelium through SIRT2 mediated inflammatory inhibition DOI
Xiaoting Qin, Fan Lü,

Jie Wan

и другие.

Journal of Molecular and Cellular Cardiology, Год журнала: 2025, Номер unknown

Опубликована: Апрель 1, 2025

Язык: Английский

Процитировано

0

BMSC-derived exosome overexpressing GATA-4 suppresses H/R-induced cardiomyocyte ferroptosis through miR-330-3p/BAP1/SLC7A11/IP3R axis and mPTP opening DOI Creative Commons
Zhiyuan Xiao,

Si Li,

Xinxin Wu

и другие.

iScience, Год журнала: 2024, Номер 27(10), С. 110784 - 110784

Опубликована: Авг. 23, 2024

Язык: Английский

Процитировано

2

Design and Synthesis of 1,4‐Diformyl‐Piperazine Ferrostatin‐1 Derivatives as Novel Ferroptosis Inhibitors DOI Open Access
Yifan Zhang, Wei Guo, Hui Zheng

и другие.

Chemical Biology & Drug Design, Год журнала: 2024, Номер 104(5)

Опубликована: Окт. 28, 2024

ABSTRACT The present study focuses on the design and synthesis of novel 1,4‐diformyl‐piperazine‐based ferrostatin‐1 (Fer‐1) derivatives, their evaluation against ferroptosis activity. synthesized compounds demonstrated significant anti‐ferroptosis activity in human umbilical vascular endothelial cells (HUVECs), with Compound 24 showing highest potency. Mechanistic studies revealed that effectively reduced intracellular reactive oxygen species (ROS) levels, mitigated mitochondrial damage, enhanced glutathione peroxidase 4 (GPX4) expression. Additionally, exhibited improved solubility plasma stability compared to control compounds, Fer‐1 JHL‐12. These findings suggest derivatives hold promise as therapeutic agents for ferroptosis‐associated cardiovascular diseases.

Язык: Английский

Процитировано

0