Resveratrol-Induced Relaxation of the Human Saphenous Vein in Patients with and Without Type 2 Diabetes Mellitus: The Role of Nickel-Sensitive Pathways and Phrixotoxin-Sensitive Vascular Kv4 Channels

Background: Graft stenosis and graft failure remain frequent complications of coronary artery bypass grafting (CABG). People with type 2 diabetes mellitus (T2DM) represent a significant proportion of patients requiring CABG surgery, as T2DM induces vascular damage and impairs vasorelaxation. Resveratrol (RSV), a naturally occurring polyphenol with potent vasorelaxant properties, has emerged as a potential adjuvant for graft preservation solutions. While multiple pathways contribute to its effects, RSV-induced relaxation in endothelium-denuded segments is driven by direct action on vascular smooth muscle tissue, involving various voltage-dependent potassium (Kv) channels and sodium–calcium exchanger type 1 (NCX-1). Therefore, this study aimed to investigate the mechanism of RSV-induced relaxation in the human saphenous vein (HSV) from patients with and without T2DM, focusing on the roles of specific 4-AP-sensitive Kv channels, particularly margatoxin-sensitive (Kv1.2 and Kv1.3) and phrixotoxin-sensitive (Kv4.1-Kv4.3) subtypes, as well as the nickel-sensitive NCX-1. Methods: Samples of HSVs were taken after CABG surgery in two national cardiovascular clinics. Pharmacological experiments were conducted using isolated organ baths. To test the involvement of Kv1.2, Kv1.3, Kv4.1-Kv4.3, and the nickel-sensitive NCX-1 pathway in RSV-induced relaxation, the following blockers were utilized: 4-aminopyridine (4-AP), margatoxin (MgTox), phrixotoxin (PhTox), and nickel. Protein expression was investigated via Western blot. Results: A total of 112 HSV segments obtained from 49 patients (27 with T2DM; 22 non-diabetic controls (NDM)) were analyzed. RSV caused a concentration-dependent relaxation of the HSV, which was significantly less effective in the T2DM group than in the NDM group (pD2 = 4.79 ± 0.05 vs. pD2 = 5.04 ± 0.05, respectively, p = 0.001). 4-AP significantly antagonized RSV-induced relaxation of the HSV in both groups. MgTox did not block the relaxant response in either group, though a distinct variation in maximal efficacy (Emax) was noted in the T2DM group. Notably, PhTox and nickel significantly attenuated RSV-induced relaxation in the NDM group but exerted no significant effect in the T2DM group. Conclusions: RSV induces concentration-dependent relaxation in endothelium-denuded HSV segments from both NDM and T2DM patients. In non-diabetic patients, this relaxation is partially mediated by 4-AP-sensitive and PhTox-sensitive Kv channels, alongside nickel-sensitive pathways, likely corresponding to NCX-1. Conversely, these specific pathways appear compromised and do not contribute to RSV-induced relaxation in patients with T2DM. The involvement of alternative 4-AP-sensitive K channels, including other subtypes of Kv channels, cannot be ruled out in either patient group.

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Journal
Pharmaceuticals
Published
2026-11-09
DOI
https://doi.org/10.3390/ph19111777
Primary Topic
Ion channel regulation and function
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article
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article

Resveratrol-Induced Relaxation of the Human Saphenous Vein in Patients with and Without Type 2 Diabetes Mellitus: The Role of Nickel-Sensitive Pathways and Phrixotoxin-Sensitive Vascular Kv4 Channels

Nevena Mihailovic‐Stanojevic, Ljiljana Bukarica, Igor S. Zivkovic, Jovana Rajković et al.
Pharmaceuticals
Ion channel regulation and function
article

Resveratrol-Induced Relaxation of the Human Saphenous Vein in Patients with and Without Type 2 Diabetes Mellitus: The Role of Nickel-Sensitive Pathways and Phrixotoxin-Sensitive Vascular Kv4 Channels

Nevena Mihailovic‐Stanojevic, Ljiljana Bukarica, Igor S. Zivkovic, Jovana Rajković, Danijela Karanović, Svetozar M. Putnik, Duško Terzić, Miloš Gostimirović, Ana Bukarica, Milovan Bojić
article en

Abstract

Background: Graft stenosis and graft failure remain frequent complications of coronary artery bypass grafting (CABG). People with type 2 diabetes mellitus (T2DM) represent a significant proportion of patients requiring CABG surgery, as T2DM induces vascular damage and impairs vasorelaxation. Resveratrol (RSV), a naturally occurring polyphenol with potent vasorelaxant properties, has emerged as a potential adjuvant for graft preservation solutions. While multiple pathways contribute to its effects, RSV-induced relaxation in endothelium-denuded segments is driven by direct action on vascular smooth muscle tissue, involving various voltage-dependent potassium (Kv) channels and sodium–calcium exchanger type 1 (NCX-1). Therefore, this study aimed to investigate the mechanism of RSV-induced relaxation in the human saphenous vein (HSV) from patients with and without T2DM, focusing on the roles of specific 4-AP-sensitive Kv channels, particularly margatoxin-sensitive (Kv1.2 and Kv1.3) and phrixotoxin-sensitive (Kv4.1-Kv4.3) subtypes, as well as the nickel-sensitive NCX-1. Methods: Samples of HSVs were taken after CABG surgery in two national cardiovascular clinics. Pharmacological experiments were conducted using isolated organ baths. To test the involvement of Kv1.2, Kv1.3, Kv4.1-Kv4.3, and the nickel-sensitive NCX-1 pathway in RSV-induced relaxation, the following blockers were utilized: 4-aminopyridine (4-AP), margatoxin (MgTox), phrixotoxin (PhTox), and nickel. Protein expression was investigated via Western blot. Results: A total of 112 HSV segments obtained from 49 patients (27 with T2DM; 22 non-diabetic controls (NDM)) were analyzed. RSV caused a concentration-dependent relaxation of the HSV, which was significantly less effective in the T2DM group than in the NDM group (pD2 = 4.79 ± 0.05 vs. pD2 = 5.04 ± 0.05, respectively, p = 0.001). 4-AP significantly antagonized RSV-induced relaxation of the HSV in both groups. MgTox did not block the relaxant response in either group, though a distinct variation in maximal efficacy (Emax) was noted in the T2DM group. Notably, PhTox and nickel significantly attenuated RSV-induced relaxation in the NDM group but exerted no significant effect in the T2DM group. Conclusions: RSV induces concentration-dependent relaxation in endothelium-denuded HSV segments from both NDM and T2DM patients. In non-diabetic patients, this relaxation is partially mediated by 4-AP-sensitive and PhTox-sensitive Kv channels, alongside nickel-sensitive pathways, likely corresponding to NCX-1. Conversely, these specific pathways appear compromised and do not contribute to RSV-induced relaxation in patients with T2DM. The involvement of alternative 4-AP-sensitive K channels, including other subtypes of Kv channels, cannot be ruled out in either patient group.

PharmaceuticalsVol. 19(11)
University of Belgrade (RS), Univerzitetski Klinički Centar Srbije (RS), Institute for Medical Research (RS)
Ion channel regulation and function
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