Potential drugs which activate nuclear factor E2-related factor 2 signaling to prevent diabetic cardiovascular

Shanshan Zhou1, Jingpeng Jin2, Tao Bai1

  • 1Department of Cardiovascular Diseases, the First Hospital of Jilin University, Changchun 130021, China.

Life Sciences
|June 6, 2015
PubMed

Insights

Certain drugs that activate Nuclear factor E2-related factor 2 (Nrf2) may help prevent cardiovascular issues in diabetic patients. Further research is needed to confirm their safety and effectiveness in humans.

Area of Science:

  • Biomedical Science
  • Cardiovascular Research
  • Metabolic Disorders

Background:

  • Diabetes mellitus poses significant cardiovascular risks, largely due to oxidative stress from reactive oxygen species.
  • The Nuclear factor E2-related factor 2 (Nrf2) pathway is crucial for cellular defense against oxidative damage by regulating antioxidant enzymes.
  • Nrf2 is a key therapeutic target for mitigating diabetic cardiovascular complications.

Purpose of the Study:

  • To review existing clinically-used drugs that up-regulate Nrf2.
  • To explore the potential of these Nrf2-activating drugs for preventing cardiovascular complications in diabetic patients.
  • To examine dimethyl fumarate and related compounds as potential therapeutic agents.

Main Methods:

  • Literature review of Nrf2 activators and their effects on diabetic complications.
  • Analysis of safety and efficacy data for clinically-used drugs.
  • Focus on drugs with demonstrated Nrf2-upregulating properties.

Main Results:

  • Animal studies indicate Nrf2 activators can prevent diabetic complications.
  • Clinical application of Nrf2 activators is limited by insufficient human safety and efficacy data.
  • Several existing drugs possess Nrf2-activating potential.

Conclusions:

  • Clinically-used drugs that up-regulate Nrf2 may offer a new strategy for managing diabetic cardiovascular complications.
  • Dimethyl fumarate and its analogues warrant further investigation for this application.
  • Bridging the gap between preclinical findings and clinical use is essential.

Related Concept Videos

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System01:26

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System

The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
1.5K
Heart Failure V: Medical Management01:30

Heart Failure V: Medical Management

Medical Management of Acute Decompensated Heart Failure (ADHF)The primary goals of therapy for patients hospitalized with acute decompensated heart failure (ADHF) include:Relieving symptomsOptimizing volume statusSupporting oxygenation and ventilationMaintaining cardiac output (CO) and end-organ perfusionIdentifying and addressing the cause of ADHFPreventing complicationsProviding patient education on factors precipitating HF exacerbationPlanning for dischargeOngoing monitoring and assessment...
567
NF-κB-dependent Signaling Pathway02:26

NF-κB-dependent Signaling Pathway

The transcription factor NF-κB was discovered in 1986 in the lab of Nobel laureate Professor David Baltimore, for its interaction with the immunoglobulin light chain enhancer in B-cells. After more than three decades of study, it is now evident that NF-κB regulates the expression of over 100 genes. Most of these genes play an essential role in the innate and adaptive immune responses as well as the inflammatory responses of animals.
NF-κB-dependent Signaling Mechanism
The...
10.7K
Antiarrhythmic Drugs: Class I Agents as Sodium Channel Blockers01:22

Antiarrhythmic Drugs: Class I Agents as Sodium Channel Blockers

Class I antiarrhythmic drugs are used to treat various types of arrhythmias or irregular heart rhythms. These drugs block the sodium (Na+) channels in the cardiac cells, thereby affecting the movement of electrical impulses across the heart. Class I antiarrhythmic drugs are divided into three subgroups: Class IA, Class IB, and Class IC, each with distinct mechanisms of action and effects on the heart.
Class 1A Antiarrhythmic Drugs: These drugs work by moderately blocking sodium channels,...
4.2K
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

Oral Hypoglycemic Agents: Biguanides and Glitazones

Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood...
981
Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively...
981