Abstract:Introduction: Hyperinsulinemia occurs in type 2 diabetic patients with insulin resistance. This increase in insulin levels in the blood increases reactive oxygen species production and oxidative stress, resulting in DNA damage. Carvedilol (CRV) is a non-selective beta-blocker, and research has shown that this compound and its metabolites have anti-oxidative properties. Carvedilol can, directly and indirectly, reduce reactive oxygen species (ROS) and has a protective effect on DNA damage from oxidative stress. … Show more
“…In particular, treatment of HUVEC cells with niosome-carvedilol (1) nanoparticles 24 h before insulin administration resulted in a significant decrease in DNA fragmentation related to the insulin-treated group, confirming the better genoprotective effect of the drug loaded in the niosomes compared to the free drug. Treatment of HUVEC cells with niosome carvedilol (1) nanoparticles 24 h before insulin administration decreases DNA fragmentation compared to the insulin-treated group, confirming the greater genoprotective effect of the drug loaded in the niosomes compared to the free drug [7].…”
Section: Carvedilolmentioning
confidence: 70%
“…Data reported in the literature suggest that carbazoles are able to modulate glucose metabolism, block adrenergic hyperactivation, prevent damage to β cells of the pancreas, inhibit inflammatory and oxidative mediators, control the cryptochrome or inhibit α-glucosidase (Table 2). Therefore, carbazole represents a versatile scaffold for the preparation of biologically active derivatives, useful in the treatment of diabetes [6,7,[27][28][29][30][31][32][33][34][35][36][37][38][39][40][41][42][43][44][45][46].…”
Section: Carbazole Derivatives In the Pathogenesis Of Diabetesmentioning
confidence: 99%
“…The adrenergic system, in part through beta-2 adrenergic receptors, regulates glucose and lipid metabolism in the liver, adipose tissue, and skeletal muscle. Taking into consideration all these properties, several studies were focused on the evaluation of the efficacy of carvedilol (1) in preventing heart complications in patients with diabetes [7,[51][52][53]. In an earlier study on the efficacy and tolerability of long-term administration of carvedilol (1), Nodari et al [27] evaluated the drug's effects in patients with chronic heart failure, a number of whom were also diabetic.…”
Section: Carvedilolmentioning
confidence: 99%
“…Therefore, various studies have been conducted in order to formulate the drug in transport systems capable of guaranteeing the desired therapeutic effect without increasing the dose to be administered. Since a high insulin concentration significantly increases DNA fragmentation, Farahani-Zangaraki et al, in 2021 [7], used the Comet test to assess the genoprotective effects of carvediol included into niosomes against supraphysiological insulin levels in human umbilical vein endothelial cells (HUVEC) [62]. As a result, incorporating carvedilol (1) into the nanoparticles increased efficiency by about fivefold.…”
Section: Carvedilolmentioning
confidence: 99%
“…The damages caused by hyperglycemia are related to the alteration of several physiological pathways. Several studies have shown, for example, that high levels of glucose, fatty acids, and insulin in the blood promote the production of reactive oxygen species (ROS), which cause direct DNA damage and promote insulin resistance [7].…”
Carbazole derivatives have gained a lot of attention in medicinal chemistry over the last few decades due to their wide range of biological and pharmacological properties, including antibacterial, antitumor, antioxidant, and anti-inflammatory activities. The therapeutic potential of natural, semi-synthetic or synthetic carbazole-containing molecules has expanded considerably owing to their role in the pathogenesis and development of diabetes. Several studies have demonstrated the ability of carbazole derivatives to reduce oxidative stress, block adrenergic hyperactivation, prevent damage to pancreatic cells and modulate carbohydrate metabolism. In this survey, we summarize the latest advances in the synthetic and natural carbazole-containing compounds involved in diabetes pathways.
“…In particular, treatment of HUVEC cells with niosome-carvedilol (1) nanoparticles 24 h before insulin administration resulted in a significant decrease in DNA fragmentation related to the insulin-treated group, confirming the better genoprotective effect of the drug loaded in the niosomes compared to the free drug. Treatment of HUVEC cells with niosome carvedilol (1) nanoparticles 24 h before insulin administration decreases DNA fragmentation compared to the insulin-treated group, confirming the greater genoprotective effect of the drug loaded in the niosomes compared to the free drug [7].…”
Section: Carvedilolmentioning
confidence: 70%
“…Data reported in the literature suggest that carbazoles are able to modulate glucose metabolism, block adrenergic hyperactivation, prevent damage to β cells of the pancreas, inhibit inflammatory and oxidative mediators, control the cryptochrome or inhibit α-glucosidase (Table 2). Therefore, carbazole represents a versatile scaffold for the preparation of biologically active derivatives, useful in the treatment of diabetes [6,7,[27][28][29][30][31][32][33][34][35][36][37][38][39][40][41][42][43][44][45][46].…”
Section: Carbazole Derivatives In the Pathogenesis Of Diabetesmentioning
confidence: 99%
“…The adrenergic system, in part through beta-2 adrenergic receptors, regulates glucose and lipid metabolism in the liver, adipose tissue, and skeletal muscle. Taking into consideration all these properties, several studies were focused on the evaluation of the efficacy of carvedilol (1) in preventing heart complications in patients with diabetes [7,[51][52][53]. In an earlier study on the efficacy and tolerability of long-term administration of carvedilol (1), Nodari et al [27] evaluated the drug's effects in patients with chronic heart failure, a number of whom were also diabetic.…”
Section: Carvedilolmentioning
confidence: 99%
“…Therefore, various studies have been conducted in order to formulate the drug in transport systems capable of guaranteeing the desired therapeutic effect without increasing the dose to be administered. Since a high insulin concentration significantly increases DNA fragmentation, Farahani-Zangaraki et al, in 2021 [7], used the Comet test to assess the genoprotective effects of carvediol included into niosomes against supraphysiological insulin levels in human umbilical vein endothelial cells (HUVEC) [62]. As a result, incorporating carvedilol (1) into the nanoparticles increased efficiency by about fivefold.…”
Section: Carvedilolmentioning
confidence: 99%
“…The damages caused by hyperglycemia are related to the alteration of several physiological pathways. Several studies have shown, for example, that high levels of glucose, fatty acids, and insulin in the blood promote the production of reactive oxygen species (ROS), which cause direct DNA damage and promote insulin resistance [7].…”
Carbazole derivatives have gained a lot of attention in medicinal chemistry over the last few decades due to their wide range of biological and pharmacological properties, including antibacterial, antitumor, antioxidant, and anti-inflammatory activities. The therapeutic potential of natural, semi-synthetic or synthetic carbazole-containing molecules has expanded considerably owing to their role in the pathogenesis and development of diabetes. Several studies have demonstrated the ability of carbazole derivatives to reduce oxidative stress, block adrenergic hyperactivation, prevent damage to pancreatic cells and modulate carbohydrate metabolism. In this survey, we summarize the latest advances in the synthetic and natural carbazole-containing compounds involved in diabetes pathways.
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