R-enantiomer of α-lipoic acid. Opportunities and prospects for clinical use

The paper presents an analysis of current literature data on the use of the R-enantiomer of α-lipoic acid as an antihypertensive treatment in patients with hypertension and metabolic syndrome. An analysis of the literature was carried out on its use as an antiinflammatory agent in inflammatory diseases. Currently, a very important aspect of researches is the possibility of using R-α-lipoic acid as a micronutrient and therapeutic agent for the treatment of diabetic polyneuropathy and neurodegenerative diseases, especially Alzheimer’s disease, carbohydrate metabolism disorders and metabolic syndrome. Lipoic acid has now become an important ingredient in multivitamin formulas, anti-aging supplements. R-α-lipoic acid is a metabolic antioxidant, its molecule contains a dithiolane ring in oxidized form, this ring has the ability to cleave with formation of dihydrolipoic acid. And since α-lipoic acid, a physiological form of thioctic acid, is a strong antioxidant that relieves the symptoms of diabetic neuropathy, the literature review analyzed data from various authors on the antioxidant effects of the R-enantiomer of α-lipoic acid and found that it had strong antioxidant effects, and its dose of 300 mg is bioequivalent to 600 mg of racemic α-lipoic acid. As presented in a sufficient number of analyzed sources, the biological role of lipoic acid is quite diverse. It is important to determine the exact causal relationship between lipoic acid and its immediate cellular targets. Lipoic acid can have a number of important and diverse physiological effects on the stimulation of neurohormonal function and, thus, indirectly affect multiple cellular signaling pathways in peripheral tissues.

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Update on the Role of Cannabinoid Receptors after Ischemic Stroke

Mediators of Inflammation ◽

10.1155/2012/824093 ◽

2012 ◽

Vol 2012 ◽

pp. 1-8 ◽

Cited By ~ 24

Author(s):

Luciano S. A. Capettini ◽

Silvia Q. Savergnini ◽

Rafaela F. da Silva ◽

Nikos Stergiopulos ◽

Robson A. S. Santos ◽

...

Keyword(s):

Ischemic Stroke ◽

Cannabinoid Receptors ◽

Inflammatory Diseases ◽

Receptor Activation ◽

Protective Effects ◽

Peripheral Tissues ◽

Transmembrane Receptors ◽

Anti Inflammatory

Cannabinoids are considered as key mediators in the pathophysiology of inflammatory diseases, including atherosclerosis. In particular, they have been shown to reduce the ischemic injury after acute cardiovascular events, such as acute myocardial infarction and ischemic stroke. These protective and anti-inflammatory properties on peripheral tissues and circulating inflammatory have been demonstrated to involve their binding with both selective cannabinoid type 1 (CB1) and type 2 (CB2) transmembrane receptors. On the other hands, the recent discoveries of novel different classes of cannabinoids and receptors have increased the complexity of this system in atherosclerosis. Although only preliminary data have been reported on the activities of novel cannabinoid receptors, several studies have already investigated the role ofCB1andCB2receptors in ischemic stroke. WhileCB1receptor activation has been shown to directly reduce atherosclerotic plaque inflammation, controversial data have been shown on neurotransmission and neuroprotection after stroke. Given its potent anti-inflammatory activities on circulating leukocytes, theCB2activation has been proven to produce protective effects against acute poststroke inflammation. In this paper, we will update evidence on different cannabinoid-triggered avenues to reduce inflammation and neuronal injury in acute ischemic stroke.

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The role of lipoic acid residues in the pyruvate dehydrogenase multienzyme complex of Escherichia coli

Biochemical Journal ◽

10.1042/bj1990505 ◽

1981 ◽

Vol 199 (3) ◽

pp. 505-511 ◽

Cited By ~ 13

Author(s):

M J Danson ◽

G Hale ◽

R N Perham

Keyword(s):

Escherichia Coli ◽

Chemical Modification ◽

Lipoic Acid ◽

Pyruvate Dehydrogenase ◽

Enzymic Activity ◽

Multienzyme Complex ◽

Dihydrolipoic Acid ◽

Lipoamide Dehydrogenase

Two lipoic acid residues on each dihydrolipoamide acetyltransferase (E2) chain of the pyruvate dehydrogenase multienzyme complex of Escherichia coli were found to undergo oxidoreduction reactions with NAD+ catalysed by the lipoamide dehydrogenase component. It was observed that: (a) 2 mol of reagent/mol of E2 chain was incorporated when the complex was incubated with N-ethylmaleimide in the presence of acetyl-SCoA and NADH; (b) 4 mol of reagent/mol of E2 chain was incorporated when the complex was incubated with N-ethylmaleimide in the presence of NADH; (c) between 1 and 2 mol of acetyl groups/mol of E2 chain was incorporated when the complex was incubated with acetyl-SCoA plus NADH; (d) 2 mol of acetyl groups/mol of E2 chain was incorporated when the complex was incubated with pyruvate either before or after many catalytic turnovers through the overall reaction. There was no evidence to support the view that only half of the dihydrolipoic acid residues can be reoxidized by NAD+. However, chemical modification of lipoic acid residues with N-ethylmaleimide was shown to proceed faster than the accompanying loss of enzymic activity under all conditions tested, which indicates that not all the lipoyl groups are essential for activity. The most likely explanation for this result is an enzymic mechanism in which one lipoic acid residue can take over the function of another.

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The Role of Lipoic Acid in the Treatment of Diabetic Polyneuropathy

Drug Metabolism Reviews ◽

10.3109/03602539709002242 ◽

1997 ◽

Vol 29 (4) ◽

pp. 1025-1054 ◽

Cited By ~ 25

Author(s):

Gerreke Ph. Biewenga ◽

Guido R. M. M. Haenen ◽

Aalt Bast

Keyword(s):

Lipoic Acid ◽

Diabetic Polyneuropathy

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Lipoic acid and diabetes—Part III: Metabolic role of acetyl dihydrolipoic acid

Journal of Biosciences ◽

10.1007/bf02703474 ◽

1986 ◽

Vol 10 (2) ◽

pp. 171-179 ◽

Cited By ~ 3

Author(s):

S. S. Wagh ◽

V. M. Gandhi ◽

C. V. Natraj ◽

K. K. G. Menon

Keyword(s):

Lipoic Acid ◽

Dihydrolipoic Acid ◽

Metabolic Role

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Role of endocannabinoid system in the pathogenesis of obesity: how can we help a patient? From theory to practice

Russian Medical Inquiry ◽

10.32364/2587-6821-2020-4-6-382-389 ◽

2020 ◽

Vol 4 (6) ◽

pp. 382-389

Author(s):

V.A. Dudareva ◽

◽

M.L. Maksimov ◽

I.G. Djadikova ◽

A.A. Zveginceva ◽

...

Keyword(s):

Metabolic Syndrome ◽

Cannabinoid Receptors ◽

Cannabinoid Receptor ◽

Endocannabinoid System ◽

Medical Society ◽

Cannabinoid Receptor 1 ◽

Peripheral Tissues ◽

Theory To Practice

Obesity that results in various metabolic disorders is one of the central concerns of modern healthcare system. Only 4% to 5% of patients with metabolic syndrome achieve favorable outcomes without any additional pharmacotherapy. Therefore, many patients require weight-loss drugs in addition to non-pharmacological treatments. The endocannabinoid system and the drugs that affect its functions receive a widespread attention of medical society due to its effects on behavioral and cerebral functions and its potential use as a therapeutic “target” in various peripheral and neurological psychiatric disorders. Among known to date cannabinoid receptors, type 1 receptors play a role in the development of obesity. It was demonstrated that the blockade of these receptors in the hypothalamus reduces appetite, inhibits adipocyte activation in peripheral tissues, prevents lipogenesis, and increases the level of adiponectin. The result is the decreased levels of atherogenic lipoproteins and improved insulin resistance. This article addresses the results of fundamental and clinical studies on Dietressa, a drug composed of affine-purified antibodies to cannabinoid receptor 1. Case report of a patient with obesity that analyzes pharmaceutical and non-pharmaceutical treatment approaches is described.KEYWORDS: obesity, metabolic syndrome, diet, endocannabinoid system, cannabinoids, cannabinoid receptors, affine-purified antibodies.FOR CITATION: Dudareva V.A., Maksimov M.L., Djadikova I.G. et al. Role of endocannabinoid system in the pathogenesis of obesity: how can we help a patient? From theory to practice. Russian Medical Inquiry. 2020;4(6):382–389. DOI: 10.32364/2587-6821-2020-4-6-382-389.

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Systemic Role for Vitamin D in the Treatment of Psoriasis and Metabolic Syndrome

Dermatology Research and Practice ◽

10.1155/2011/276079 ◽

2011 ◽

Vol 2011 ◽

pp. 1-4 ◽

Cited By ~ 10

Author(s):

Lisa Wenyang Fu ◽

Ronald Vender

Keyword(s):

Cardiovascular Disease ◽

Metabolic Syndrome ◽

Vitamin D ◽

Inflammatory Diseases ◽

Systemic Disease ◽

The Novel ◽

Oral Vitamin ◽

Potential Use

The novel discovery of the systemic role of vitamin D in the modulation of the immune system especially the Type 1 helper T cell (Th1) pathway reveals its potential for treating Th1 inflammatory diseases. Psoriasis has been recently established to be a systemic disease centered on inflammation and involvement of cytokines of the Th1 pathway. There is an increased prevalence of metabolic syndrome in patients with psoriasis. Metabolic syndrome also involves a proinflammatory state. This paper proposes the idea of the potential use of oral vitamin D to treat psoriasis and metabolic syndrome concurrently. We propose there is merit in more clinical trials investigating the use of vitamin D to treat both psoriasis and metabolic syndrome through its anti-inflammatory effects. On application to psoriasis management and prognosis, the goal is to decrease the risk for cardiovascular disease and decrease disease morbidity and mortality.

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