No abstract available.
Thioctic Acid*

Alpha-lipoic acid, a physiological form of thioctic acid, is a strong antioxidant that relieves diabetic neuropathic symptoms. R(+)-α-lipoic acid shows superior antioxidative effects to its racemate. We compared the pharmacokinetics (PKs) and tolerability of R(+)- and S(-)-α-lipoic acid after a single oral dose of R(+)-α-lipoic acid, Dexid®, and its racemate, thioctic acid in healthy male subjects. We used an open-label, randomized, single-dose, three-treatment, parallel study design to compare the PK exposure of the active form, R(+)-α-lipoic acid. Thirty subjects completed the study with no clinically relevant safety issues. The peak concentrations (C(max), mean±SD) of R(+)-α-lipoic acid after doses of R(+)-α-lipoic acid 200 mg, 300 mg and thioctic acid 600 mg were 4186.8±1956.7, 6985.6±3775.8 and 6498.4±3575.6 µg/L, respectively, and the areas under the plasma concentration-time curve from 0 to the last measurable concentration (AUC(last)) were 1893.6±759.4, 3575.2±1149.2 and 3790.0±1623.0 µg·h⁻¹·L⁻¹, respectively. The geometric mean ratio and 90% confidence intervals of R(+)-α-lipoic acid 200 mg to thioctic acid 600 mg for the C(max) and AUC(last) were 0.71 (0.43–1.15) and 0.51 (0.37–0.70), respectively. The corresponding R(+)-α-lipoic acid 300 mg to thioctic acid 600 mg values were 1.11 (0.68-1.80) and 0.97 (0.71-1.34), respectively. In conclusion, R(+)-α-lipoic acid 300 mg showed PK characteristics similar to those of thioctic acid 600 mg and both formulations were well tolerated.
Humans ; Male* ; Pharmacokinetics ; Plasma ; Thioctic Acid*

No abstract available.
Thioctic Acid ; Thyroid Gland ; Thyroid Neoplasms

No abstract available.
Thioctic Acid ; Thyroid Gland ; Thyroid Neoplasms

In a one-step fermentation system of vitamin C production with Gluconobacter oxydans and Ketogulonicigenium vulgare, a functional module of α-lipoic acid biosynthesis was constructed in G. oxydans. The engineered G. oxydans was co-cultured with K. vulgare to enhance the growth and 2-keto-L-gulonic acid (2-KGA) production of K. vulgare. This one-step fermentation system alleviated the growth inhibition during the mono-culture of K. vulgare and strengthened the interaction between the two bacteria. Moreover, the yield of vitamin C precursor (2-KGA) increased to 73.34 g/L (the control group was 59.09 g/L), and the conversion of D-sorbitol to 2-KGA increased to 86.0%. This study provides a new idea for further optimizing the one-step fermentation system of vitamin C production.
Ascorbic Acid ; Fermentation ; Gluconobacter oxydans ; Rhodobacteraceae ; Thioctic Acid ; biosynthesis

In the present study, the effects of alpha lipoic acid (ALA) supplementation on glycemic control and lipid profile in streptozotocin (STZ)-induced diabetic rats have been evaluated. Sprague Dawley rats were divided into nondiabetic (NDM), diabetic without supplementation (No Suppl) and diabetic with ALA groups. ALA was orally administered once a day for 8 weeks with a dose of 100 mg/kg BW. Supplementation of ALA to STZ-induced rats prevented the severe damage to the islet cells of the pancreas and lowered the plasma glucose and glycated hemoglobin (HbA1c) levels. Supplementation of ALA also suppressed the increased of total cholesterol (TC), triglycerides and low density lipoprotein-cholesterol (LDL-C) levels in the plasma of diabetic rats as well as increased high density lipoproteincholesterol (HDL-C) levels. In conclusion, this study suggest that ALA may be effective in controlling glycemic status and improving dyslipidemia in streptozotocin-induced diabetic rats and has the potential in reducing cardiovascular complications due to diabetes mellitus.
Rattus norvegicus ; Streptozocin ; Aminolevulinic Acid ; Dyslipidemia ; Thioctic Acid

BACKGROUND AND OBJECTIVES: alpha-Lipoic acid (ALA) is known to improve endothelial function in patients with diabetes. However, the effect of ALA on endothelial function in hypertensive patients is unknown. The aim of this study was to investigate whether ALA improves endothelial function in diabetic and hypertensive patients. SUBJECTS AND METHODS: This study included 40 patients who were treated with ALA (Group I: 20 diabetic patients, 54.9+/-10.2 years, Group II: 20 hypertensive patients, 56.5+/-9.0 years). ALA was administered in 600 mg/day doses during the first four weeks, and 1,200 mg/day doses during the second four weeks. Clinical characteristics and endothelial function were assessed at baseline, 4 weeks and 8 weeks after ALA administration. Evaluation of patients included: assessment of the brachial artery for flow mediated vasodilation (FMD) and the inflammatory marker (high sensitive CRP: hsCRP). RESULTS: Clinical characteristics (body mass index, total cholesterol/HDL-cholesterol and hsCRP) were unchanged in each group. However, FMD was significantly improved at 8 weeks after ALA therapy in both groups. Group I-baseline: 4 weeks : 8 weeks = 4.1+/-3.3 : 6.5+/-2.2 : 8.0+/-2.7, Group II-baseline: 4 weeks : 8 weeks = 5.5+/-3.7 : 7.4+/-3.3 : 9.3+/-2.7, p<0.05. The level of fibrinogen was observed to have an inverse correlation with FMD at 8 weeks after ALA therapy in Group I (p<0.05). CONCLUSION: ALA improves endothelial function in both diabetic and hypertensive patients.
Brachial Artery ; Fibrinogen ; Humans ; Hypertension ; Thioctic Acid ; Vasodilation

BACKGROUND AND OBJECTIVES: alpha-Lipoic acid (ALA) is known to improve endothelial function in patients with diabetes. However, the effect of ALA on endothelial function in hypertensive patients is unknown. The aim of this study was to investigate whether ALA improves endothelial function in diabetic and hypertensive patients. SUBJECTS AND METHODS: This study included 40 patients who were treated with ALA (Group I: 20 diabetic patients, 54.9+/-10.2 years, Group II: 20 hypertensive patients, 56.5+/-9.0 years). ALA was administered in 600 mg/day doses during the first four weeks, and 1,200 mg/day doses during the second four weeks. Clinical characteristics and endothelial function were assessed at baseline, 4 weeks and 8 weeks after ALA administration. Evaluation of patients included: assessment of the brachial artery for flow mediated vasodilation (FMD) and the inflammatory marker (high sensitive CRP: hsCRP). RESULTS: Clinical characteristics (body mass index, total cholesterol/HDL-cholesterol and hsCRP) were unchanged in each group. However, FMD was significantly improved at 8 weeks after ALA therapy in both groups. Group I-baseline: 4 weeks : 8 weeks = 4.1+/-3.3 : 6.5+/-2.2 : 8.0+/-2.7, Group II-baseline: 4 weeks : 8 weeks = 5.5+/-3.7 : 7.4+/-3.3 : 9.3+/-2.7, p<0.05. The level of fibrinogen was observed to have an inverse correlation with FMD at 8 weeks after ALA therapy in Group I (p<0.05). CONCLUSION: ALA improves endothelial function in both diabetic and hypertensive patients.
Brachial Artery ; Fibrinogen ; Humans ; Hypertension ; Thioctic Acid ; Vasodilation

OBJECTIVETo establish a method for determining the content of alpha-lipoic acid in New Zealand rabbit plasma.

METHODSAlpha-lipoic acid in the plasma samples was purified by solid-phase extractor and analyzed on an HYPERSIL C18 column with isocratic mobile phase consisting of potassium dihydrogen phosphate-acetonitrile (50:50, v/v) at a flow rate of 1.0 ml/min and detection wavelength of 230 nm.

RESULTSThe standard curve was linear in the range of 5-100 microg/L (r=1) and the average recovery was 77.4%-82.1%. The relative standard deviations of intra-day and inter-day assay were within 1.5%-8.9%.

CONCLUSIONThe method is sensitive, accurate and simple for determining plasma alpha-lipoic acid levels in New Zealand rabbits.

The introduction of intravenous nutritional therapy for cosmetic and health purposes in Korea has been controversial. Because it brings ethical problems of off-label prescribing on the basis of low level of medical evidences for claims of fatigue reduction, detoxification, anti-inflammation effect, skin whitening, antioxidant and anti-aging effects. Despite the lack of clinical studies, the verification of the efficacy and safety of intravenous nutritional therapy and the need to provide objective information to patients are prerequisite for the correct intravenous use. In addition, efforts should be made to prevent the abuse for commercial purposes.
Fatigue ; Fursultiamin ; Glutathione ; Glycyrrhizic Acid ; Humans ; Korea ; Off-Label Use ; Skin ; Thioctic Acid