Enantioselective pharmacokinetics and bioavailability of different racemic α-lipoic acid formulations in healthy volunteers

Hermann, Róbert; Niebch, G.; Borbe, Harald O.; Fieger-Büschges, H.; Ruus, Peter; Nowak, H; Riethmüller-Winzen, H.; Peukert, M.; Blume, Henning

doi:10.1016/0928-0987(95)00045-3

Cited by 103 publications

(100 citation statements)

References 9 publications

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“…In fact, it has been reported that de novo synthesis of ALP originates from octanoic acid (C8:0) and cysteine within the mitochondria [67,68]. Hermann et al [66] report that the hepatic uptake of ALP may be carrier-mediated and selectively inhibited by medium chain fatty acids. Hence, in our study in which ALP and MCTo were fed in combination, there exists the potential for competitive absorption into the liver, which may have affected the results of our combination treatment group (MCTo/ALP), thus negating any benefits like those seen when feeding ALP alone.…”

Section: Discussionmentioning

confidence: 99%

“…The present study outlines the effects elicited from a powerful compound that may have a greater potential for action if provided to the animals in the form of an oral solution, thereby improving the overall absorption into the biological system. Hermann et al [66] also discuss the structural similarity between ALP and MCT. In fact, it has been reported that de novo synthesis of ALP originates from octanoic acid (C8:0) and cysteine within the mitochondria [67,68].…”

Section: Discussionmentioning

confidence: 99%

“…Our study used a powdered synthetic racemic mixture of ALP. With regard to absorption, Hermann et al [66] found that ALP is absorbed more slowly as an oral tablet compared with the rapid absorption of a prepared oral solution. The present study outlines the effects elicited from a powerful compound that may have a greater potential for action if provided to the animals in the form of an oral solution, thereby improving the overall absorption into the biological system.…”

Section: Discussionmentioning

confidence: 99%

“…Studies by Gleiter et al [65] and Hermann et al [66] have examined the influence of dietary components and the bioavailability of ALP. The overall bioavailability of ALP has been reported to range from 20% to 38% depending on the isomer [(R)-lipoic acid or (S)-lipoic acid] and the formulation tested [66].…”

Section: Discussionmentioning

confidence: 99%

“…The overall bioavailability of ALP has been reported to range from 20% to 38% depending on the isomer [(R)-lipoic acid or (S)-lipoic acid] and the formulation tested [66]. Our study used a powdered synthetic racemic mixture of ALP.…”

Section: Discussionmentioning

confidence: 99%

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Effects of a medium chain triglyceride oil mixture and α-lipoic acid diet on body composition, antioxidant status, and plasma lipid levels in the Golden Syrian hamster

Wollin

Wang

Kubow

et al. 2004

The Journal of Nutritional Biochemistry

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The objective of this study was to examine the effects of the antioxidant ␣-lipoic acid (ALP) versus a medium chain triglyceride oil mixture (MCTo), which was designed to increase energy expenditure and to improve lipid profiles containing medium chain triglycerides, phytosterols, and omega-3 fatty acids in the form of flaxseed oil. A total of 48 hamsters were fed a) hypercholesterolemic (HC) control, b) HC MCTo, c) HC ALP, or d) HC MCTo/ALP diet for 4 weeks. No differences were observed on food intake, body weight, total body water, lean and fat mass, and tissue thiobarbituric acid reactive substances (TBARS). ALP alone had no effect on total cholesterol (TC); however, MCTo feeding increased TC with (P Ͻ 0.03) and without (P Ͻ 0.003) ALP when compared with control. ALP increased HDL levels compared with control (P Ͻ 0.04) and MCTo/ALP (P Ͻ 0.007) groups. MCTo, with (P Ͻ 0.0001) or without (P Ͻ 0.006) ALP, increased non-HDL cholesterol levels versus control. The non-HDL:HDL cholesterol ratio was decreased by ALP compared with MCTo (45%) and MCTo/ALP (68%) (P Ͻ 0.0001), a similar trend was seen when compared with the HC control (22%) group (P Ͻ 0.14). Triglyceride levels were not altered by any dietary treatment. Liver and heart tissue reduced glutathione (GSH) was increased (P Ͻ 0.05) by all three treatments when compared with control. Both tissues showed an increase (P Ͻ 0.05) in oxidized glutathione (GSSG) when fed ALP as compared with other treatments. Hamsters fed ALP had a lower (P Ͻ 0.05) GSH/GSSG ratio compared with other treatment groups. In conclusion, MCTo feeding does not elicit beneficial effects on circulating plasma lipids and measures of body composition. In addition, our results do not clearly support an improvement in oxidative status through supplementation of ALP. However, our results do support the existence of beneficial effects of ALP on circulating lipoprotein content in the hamster.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Effects of a medium chain triglyceride oil mixture and α-lipoic acid diet on body composition, antioxidant status, and plasma lipid levels in the Golden Syrian hamster

Wollin

Wang

Kubow

et al. 2004

The Journal of Nutritional Biochemistry

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Enantioselective high-performance liquid chromatography assay of (+)R- and (?)S-?-lipoic acid in human plasma

Niebch¹,

Büchele

Blome³

et al. 1997

Chirality

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A specific plasma level assay for the enantiomers of α‐lipoic acid is described. It makes use of liquid‐liquid extraction, chemical reduction to the dithiol enantiomers, and their precolumn chiral derivatisation with o‐phthalaldehyde in the presence of D‐phenylalanine. The two diastereomeric derivatives are separated by reversed‐phase HPLC with fluorescence detection. The working range of the assay is between 15 ng/ml (lower limit of quantitation) and 1,000 ng/ml for either enantiomer. Chirality 9:32–36, 1997. © 1997 Wiley‐Liss, Inc.

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Combined non-enzymatic and enzymatic reduction favors bioactivation of racemic lipoic acid: an advantage of a racemic drug?

Biewenga¹,

Haenen²,

Groen³

et al. 1997

Chirality

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Enantioselective pharmacokinetics and bioavailability of different racemic α-lipoic acid formulations in healthy volunteers

Cited by 103 publications

References 9 publications

Effects of a medium chain triglyceride oil mixture and α-lipoic acid diet on body composition, antioxidant status, and plasma lipid levels in the Golden Syrian hamster

Effects of a medium chain triglyceride oil mixture and α-lipoic acid diet on body composition, antioxidant status, and plasma lipid levels in the Golden Syrian hamster

Enantioselective high-performance liquid chromatography assay of (+)R- and (?)S-?-lipoic acid in human plasma

Combined non-enzymatic and enzymatic reduction favors bioactivation of racemic lipoic acid: an advantage of a racemic drug?

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