• Nutrition Research and Practice
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• v.6 no.3
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• pp.195-200
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• 2012

The purpose of this study was to investigate the effects of ${\alpha}$-lipoic acid on body weight and lipid profiles in Sprague-Dawley rats fed a high fat diet (HFD). After 4 weeks of feeding, rats on the HFD were divided into three groups by randomized block design; the first group received the high-fat-diet (n = 10), and the second group received the HFD administered with 0.25% ${\alpha}$-lipoic acid (0.25LA), and the third group received the high-fat diet with 0.5% ${\alpha}$-lipoic acid (0.5LA). The high fat diet with ${\alpha}$-lipoic acid supplemented groups had significantly inhibited body weight gain, compared to that in the HFD group (P < 0.05). Organ weights of rats were also significantly reduced in liver, kidney, spleen, and visible fat tissues in rats supplemented with ${\alpha}$-lipoic acid (P < 0.05). Significant differences in plasma lipid profiles, such as total lipids, total cholesterol, triglycerides, low-density lipoprotein, and high-density lipoprotein, were observed between the HFD and 0.5LA groups. The atherogenic index and the plasma high density lipoprotein-cholesterol/total cholesterol ratio improved significantly with ${\alpha}$-lipoic acid supplementation in a dose-dependent manner (P < 0.05). Total hepatic cholesterol and total lipid concentration decreased significantly in high fat fed rats supplemented with ${\alpha}$-lipoic acid in a dose-dependent manner (P < 0.05), whereas liver triglyceride content was not affected. In conclusion, ${\alpha}$-lipoic acid supplementation had a positive effect on weight gain and plasma and liver lipid profiles in rats.

• Polymer(Korea)
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• v.32 no.6
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• pp.561-565
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• 2008

Hyaluronic acid (HA) is a natural glycosaminoglycan and is used widely in the pharmaceutical field. Lipoic acid (LA) helps the regeneration of exogenous and endogenous antioxidants such as Vitamin C and Vitamin E as well as glutathione. It also acts as antioxidant indirectly. Hydrophilic HA as a biodegradable and biocompatible polymer was conjugated with hydrophobic LA as an antioxidant to form the graft copolymer. The carboxyl group of HA was modified by adipic acid dihydrazide (ADH). The synthesis of HA-g-LA graft copolymers was characterized by FT-IR, $^1H$-NMR spectroscopy. The conjugates could form the self-assembled nanoparticles in aqueous solution. The particle size and critical aggregation concentration were verified to use the nanoparticle as a carrier fur the hydrophobic material.

• The Korean Journal of Physiology and Pharmacology
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• v.2 no.4
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• pp.427-433
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• 1998

In brain hypoxic-ischemia, an excess release of glutamate and a marked production of reactive oxygen species (ROS) occur in neuronal and non-neuronal cells. The present study investigated the effect of the biological antioxidants dihydrolipoic acid (DHLA) and lipoic acid (LA) on N-methyl-D-aspartate (NMDA)- and ROS-induced neurotoxicity in cultured rat cortical neurons. DHLA enhanced NMDA-evoked rises in intracellular calcium concentration ($[Ca^{2+}]_i$). In contrast, LA did not alter the NMDA-evoked calcium responses but decreased after a brief treatment of dithiothreitol (DTT), which possesses a strong reducing potential. Despite the modulation of NMDA receptor-mediated rises in $[Ca^{2+}]_i$, neither DHLA nor LA altered the NMDA receptor-mediated neurotoxicity, as assessed by measuring the amount of lactate dehydrogenase released from dead or injured cells. DHLA, but not LA, prevented the neurotoxicity induced by xanthine/xanthine oxidase-generated superoxide radicals. Both DHLA and LA decreased the glutathione depletion-induced neurotoxicity. The present data may indicate that biological antioxidants DHLA and LA protect neurons from ischemic injuries via scavenging oxygen free radicals rather than modulating the redox modulatory site(s) of NMDA receptor.

• Bulletin of the Korean Chemical Society
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• v.28 no.2
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• pp.225-228
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• 2007

Lipoic acid (LA) is a multifunctional antioxidant against a variety of ROS. Nitrone acts as free radical spin trap and exhibits neuroprotective activity. Thus, LA-nitrone derivatives (6, 7, 8, and 9) were synthesized and screened as an antioxidant and inhibitors for cholinesterases. Even though the antioxidant effect of LA-nitrone derivatives was not improved, they turned out to be effective inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) in μM range.

• BMB Reports
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• v.52 no.8
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• pp.508-513
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• 2019

In this study, the anti-inflammatory effects of ${\alpha}-lipoic$ acid (LA) and decursinol (Dec) hybrid compound LA-Dec were evaluated and compared with its prodrugs, LA and Dec. LA-Dec dose-dependently inhibited lipopolysaccharide (LPS)-induced nitric oxide (NO) generation in BV2 mouse microglial cells. On the other hand, no or mild inhibitory effect was shown by the Dec and LA, respectively. LA-Dec demonstrated dose-dependent protection from activation-induced cell death in BV2 cells. LA-Dec, but not LA or Dec individually, inhibited LPS-induced increased expressions of induced NO synthase (iNOS) and cyclooxygenase-2 (COX-2) proteins in a dose-dependent manner in both BV2 and mouse macrophage, RAW264.7 cells. Furthermore, LA-Dec inhibited LPS-induced expressions of iNOS, COX-2, interleukin-6, tumor necrosis $factor-{\alpha}$, and $interleukin-1{\beta}$ mRNA in BV2 cells, whereas the same concentration of LA or Dec was ineffective. Signaling studies demonstrated that LA-Dec inhibited LPS-activated signal transducer and activator of transcription 3 and protein kinase B activation, but not nuclear factor-kappa B or mitogen-activated protein kinase signaling. The data implicate LA-Dec hybrid compound as a potential therapeutic agent for inflammatory diseases of the peripheral and central nervous systems.

• Polymer(Korea)
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• v.36 no.4
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• pp.455-460
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• 2012

Poly(N-isopropylacrylamide) (PNIPAM) hydrogel has been studied as an important drug delivery system due to its volume transition or temperature-responsive swelling properties, whose phase separation temperature is similar to the body temperature. However, because of hydrophilic PNIPAM, hydrophobic drugs are difficult to be uniformly loaded in the networks. Antioxidant alpha-lipoic acid (LA) can be prepared as a polymer(polylipoic acid, PLA) by ring opening polymerization, which is hardly developed as a material due to its low molecular weight and easy depolymerization. To overcome this limitation, a hydrophobic active ingredient, LA was reacted with NIPAM into stable hydrogels. Simple thermal radical reaction successfully resulted in a hydrogel (PNIPAM/PLA), which was confirmed by DSC, FTIR, and Raman spectroscopy. The PNIPAM/PLA showed temperature-responsive properties, and their volume swelling decreased with an increase in lipoic acid content. These hydrogels can carry hydrophobic drugs with PNIPAM and the hydrogels could be useful as final drug delivery systems having lipoic acid as an antioxidant.

• BMB Reports
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• v.52 no.10
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• pp.613-618
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• 2019

Microglial cells are known as the main immune cells in the central nervous system, both regulating its immune response and maintaining its homeostasis. Furthermore, the antioxidant ${\alpha}-lipoic$ acid (LA) is a recognized therapeutic drug for diabetes because it can easily invade the blood-brain barrier. This study investigated the effect of ${\alpha}-LA$ on the inflammatory response in lipopolysaccharide (LPS)-treated BV-2 microglial cells. Our results revealed that ${\alpha}-LA$ significantly attenuated several inflammatory responses in BV-2 microglial cells, including pro-inflammatory cytokines, such as tumor necrosis $factor-{\alpha}$ and interleukin (IL)-6, and other cytotoxic molecules, such as nitric oxide and reactive oxygen species. In addition, ${\alpha}-LA$ inhibited the LPS-induced phosphorylation of ERK and p38 and its pharmacological properties were facilitated via the inhibition of the nuclear factor kappa B signaling pathway. Moreover, ${\alpha}-LA$ suppressed the activation of NOD-like receptor pyrin domain containing 3 (NLRP3) inflammasomes, multiprotein complexes consisting of NLRP3 and caspase-1, which are involved in the innate immune response. Finally, ${\alpha}-LA$ decreased the genes accountable for the M1 phenotype, $IL-1{\beta}$ and ICAM1, whereas it increased the genes responsible for the M2 phenotype, MRC1 and ARG1. These findings suggest that ${\alpha}-LA$ alleviates the neuroinflammatory response by regulating microglial polarization.

• Journal of Embryo Transfer
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• v.32 no.3
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• pp.123-130
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• 2017

This study was conducted to investigate the effects of alpha-lipoic acid (aLA) as an antioxidant that decrease the reactive oxygen species (ROS) in bovine embryonic development. Slaughterhouse derived bovine immature oocytes were collected and 4 different concentrations (0, 5, 10 and 20 mM) of aLA was supplemented in bovine in vitro maturation (IVM) medium. After 20 hrs of IVM, maturation rates, levels of ROS and glutathione (GSH), and further embryonic development after parthenogenetic activation (PA) and in vitro fertilization (IVF) was investigated according to aLA concentrations. Maturation rate was significantly higher in 10 mM group than other groups (80.5% vs. 62.9, 73.9, 64.2%; P<0.05). In the levels of ROS and GSH in matured oocytes as an indicator of oocyte quality, significantly better results were shown in 5 and 10 mM groups compared with other 2 groups. After IVM, significantly higher rates of blastocyst formation were shown in 10 mM groups in both of PA (27.9% vs. 18.8, 22.3, 14.2%; P<0.05) and IVF (32.6% vs. 23.9, 27.3, 16.2%; P<0.05) embryos. In addition, significantly more cell total cell number and higher inner cell mass ratio in 10 mM PA and IVP blastocysts showed developmental competence in 10 uM groups. Therefore, based on the entire data from this study, using $10{\mu}M$ of aLA confirmed to be the optimal concentration for bovine oocyte maturation and embryonic development.

• Journal of Sensor Science and Technology
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• v.23 no.5
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• pp.295-298
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• 2014

A novel approach to fabricating high-performance glucose sensors is reported, which is based on the process of self-assembled monolayers (SAMs). In this study, we have particularly used ${\alpha}$-lipoic acid (LA) SAMs for the glucose sensors. To our best knowledge, this study is the first one to use LA as SAMs for this purpose. N-hydroxysuccinimide (NHS) and 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC) were deliberately attached at the same time on the LA SAM. Then, glucose oxidase ($GO_X$) and horseradish peroxidase (HRP) were sequentially immobilized. Thus, the HRP/$GO_X$/NHS-EDC/LA-SAM/Au/Cr/glass working electrode was developed. The glucose-sensing capability of the fabricated sensor was systematically measured by the use of cyclic voltammetry in the range of 1-30 mM glucose in phosphate-buffered saline. The result showed a good sensitivity, that is, as high as $27.5{\mu}A/(mM{\cdot}cm^2)$. This result conspicuously demonstrates that LA can be one of promising substances for use as SAMs for accurately monitoring trace levels of glucose concentration in human blood.

• Asian-Australasian Journal of Animal Sciences
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• v.22 no.8
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• pp.1195-1201
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• 2009

An experiment was conducted to evaluate the effects of dietary alpha-lipoic acid (LA) on growth performance, carcass characteristics and meat quality in Arbor Acres broilers. A total of 240 1-d-old male Arbor Acres broilers were randomly allocated to 4 dietary treatments (0, 300 ppm, 600 ppm, and 900 ppm dietary LA supplementation, respectively). Birds were slaughtered at 42 days old. Live body weight (BW), average daily gain (ADG), average feed intake (AFI), feed conversion ratio (FCR), dressing percentage, breast muscle percentage, thigh muscle percentage, abdominal fat percentage, muscle color (L*, a*, b*), pH values at 24 h postmortem, meat shear force value (SFV) and anti-oxidative ability were measured. Results showed that addition of 600 ppm or 900 ppm LA decreased BW (p<0.01), ADG (p<0.01) and AFI (p<0.05) compared with other diets. FCR was not affected by dietary LA content. LA had no marked effect on dressing percentage, breast muscle percentage or thigh muscle percentage. Abdominal fat percentage was lower (p<0.05) in the 900 ppm LA supplementation group than the control group. Dietary 900 ppm LA increased (p<0.05) breast and thigh muscle pH value at 24 h postmortem compared with the control treatment. Dietary LA increased thigh muscle a* value, though no significant difference was found in thigh muscle a* value among the treatments. Dietary LA significantly decreased breast muscle L* value (p<0.05), breast muscle b* value (p<0.01) and thigh muscle b* value (p<0.05). Broilers fed LA had higher breast muscle a* value (p<0.05) and thigh muscle L* value (p<0.05). All test groups had lower (p<0.05) breast muscle SFV than the control group. Dietary 600 ppm or 900 ppm LA both decreased (p<0.01) thigh muscle SFV compared with the control treatment. Dietary 900 ppm LA significantly increased (p<0.05) TAOC, SOD and GSHPx compared with no LA treatment. Broilers fed LA had lower (p<0.01) MDA compared with the control treatment. These results suggested that dietary LA enhanced the anti-oxidative ability and oxidative stability, and contributed to the improvement of meat quality in broilers.