• Bulletin of the Korean Chemical Society
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• 제35권6호
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• pp.1681-1686
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• 2014

A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)) inhibitory activities were evaluated. Even though the parent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) with the exception of compound 14 ($IC_{50}=255.26{\pm}4.41$ against BuChE), all hybrid molecules demonstrated BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE ($IC_{50}=1.75{\pm}0.30{\mu}M$) and BuChE ($IC_{50}=5.61{\pm}1.25{\mu}M$) comparable to galantamine ($IC_{50}=1.7{\pm}0.9{\mu}M$ against AChE and $IC_{50}=9.4{\pm}2.5{\mu}M$ against BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity ($K_i$) values to AChE and BuChE were $3.8{\pm}0.005{\mu}M$ and $7.0{\pm}0.04{\mu}M$, respectively.

• 동의생리병리학회지
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• 제25권1호
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• pp.55-64
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• 2011

The object of this study was to observe the effects of Scutellariae Radix (SR) aqueous extracts on lipopolysaccharide (LPS)-induced rat acute lung injury. Five different dosages of SR extracts were orally administered once a day for 28 days before LPS treatments, and then 5 hours after lipopolysaccharide treatment, all rats were sacrificed. 8 groups, each of 16 rats per group were used in the present study. Changes on the body weights, lung weights, pulmonary transcapillary albumin transit, arterial gas parameters (pH, $PaO_2$ and $PaCO_2$) bronchoalveolar lavage fluid (BALF) protein, lactate dehydrogenase (LDH) and proinflammatory cytokines tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), interleukin-1${\beta}$ (IL-1${\beta}$) contents, total cell numbers, neutrophil and alveolar macrophage ratios, lung malondialdehyde (MDA), myeloperoxidase (MPO), proinflammatory cytokine TNF-${\alpha}$ and IL-1${\beta}$ contents were observed with histopathology of the lung, changes on luminal surface of alveolus (LSA), thickness of alveolar septum, number of polymorphonuclear neutrophils (PMNs). The results were compared with a potent antioxidant ${\alpha}$-lipoic acid, 60 mg/kg, in which the effects on LPS-induced acute lung injury were already confirmed. The results obtained in this study suggest that over 125 mg/kg of SR extracts showed favorable effects on the LPS-induced acute lung injury, and 250 mg/kg of SR extracts resembling acute respiratory distress syndrome mediated by their antioxidant and anti-inflammatory effects and .as similar to ${\alpha}$-lipoic acid in the present study. Therefore, it is expected that SR will be showed favorable effects on the acute respiratory distress syndrome.

• 한국가금학회지
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• 제43권1호
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• pp.21-29
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• 2016

A total of 144 one-day-old male broilers (ROSS ${\times}$ Ross 308) ($42{\pm}0.1g$) were used in a completely randomized design and allotted to one of three dietary treatments to give 6 replicates per treatment (8 birds per cage). The three watery dietary treatments were 1) a corn-soybean meal-based relation [Negative control (NC); no antimicrobial compounds added] with tab water, 2) 8 ppm liquid-alpha-lipoic acid [Positive control (PC)] or 3) 100 ppm liquid-resveratrol. All dietary treatments were continuously provided as a liquid form. Birds were housed in a battery cage (n=48), and were offered liquid dietary treatments at all times. The ambient temperature was maintained at $32{\pm}1^{\circ}C$ for the first 3 weeks and decreased gradually to $28{\pm}1^{\circ}C$ by the end of the experiment (d 35) to induce moderate heat stress. One bird per pen (n=6) was euthanized via cervical dislocation at day 21 to obtain terminal ileum to measure villous height and crypt depth, while another bird per pen (n=6) was similarly euthanized at day 35 and used to harvest breast meat and drumsticks to evaluate meat quality traits. Birds fed liquid-resveratrol did not improve (P>0.05) body weight and average daily gain compared with those fed other dietary treatments from day 1 to day 35. Birds fed liquid-resveratrol had no effect (P>0.05) on villous height compared with birds were in other dietary treatments at day 21. Liquid-resveratrol had no effect (P>0.05) on thiobarbituric acid reactive substance (TBARS) in drumsticks compared with other dietary treatments at day 35. Furthermore, birds fed liquid-resveratrol had no effect (P>0.05) on DPPH radical scavenging activity both in breast meat and drumsticks compared with those fed other dietary treatments at day 35. Morphological changes of ileum were not observed by immunofluorescence, and the level of occludin protein from ileum extracts also did not differ among groups. Our results suggested that liquid form of antioxidant compounds used in the current study such as alpha-lipoic acid (8 ppm) or resveratrol (100 ppm) did not improve growth performance, meat quality traits and histology of terminal ileum compared with those fed negative control in broiler chickens under moderate heat stress for 35 days.

• Asian-Australasian Journal of Animal Sciences
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• 제32권12호
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• pp.1914-1922
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• 2019

Objective: The study was conducted to evaluate the effect of stocking density and alphalipoic acid (ALA) on the growth performance, feed utilization, carcass traits, antioxidative ability and immune response of broilers. Methods: A total of 1,530 22-day-old male broilers (Arbor Acres) with comparable body weights ($731.92{\pm}5.26$) were placed into 18 cages ($2.46{\times}2.02m$) in groups of 75 birds ($15birds/m^2$, $37.5kg/m^2$; low stocking density [LD]), 90 birds ($18birds/m^2$, $45.0kg/m^2$; high stocking density [HD]) and 90 birds with 300 mg/kg ALA added to the basal diet ($18birds/m^2$, $45.0kg/m^2$; HD+ALA, high stocking density+${\alpha}$-lipoic acid); each treatment was represented by 6 replicates. The experimental period was 3 weeks. Results: The results showed that the high stocking density regimen resulted in a decreased growth, feed conversion ratio, carcass weight, thigh yield and bursa weight relative to body weight (p<0.05) on d 42. The abdominal fat yield in the HD+ALA group was lower (p = 0.031) than that of the LD group at 42 d. The superoxide dismutase and glutathione peroxidase activities in serum were increased, and malondialdehyde content decreased after adding ALA product (p<0.05) on d 42. Additionally, the serum concentrations of immunoglobulin A (IgA) and IgG were decreased (p<0.05) and the level of diamine oxidase was higher (p<0.01) in the HD group on d 42. Conclusion: The high stocking density significantly decreased broiler growth performance, feed utilization and carcass traits, increased physiological and oxidative stress and induced intestinal mucosal injury. The supplementation of ALA product in broiler diet at 300 mg/kg may reduce the adverse effects of high stocking density-mediated stress by maintaining the antioxidant system and humoral immune system.

• 한국미생물·생명공학회지
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• 제10권3호
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• pp.177-184
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• 1982

토양에서 분리, 선별한 Streptomyces 속의 한 균주가 생산하는 Penicillinase의 최적생산조건을 조사한 결과를 요약하면 다음과 같다. 탄소원으로서는 glucose, 실소원으로는 L-as-paragine이 가장 우수했으며 금속감중에서 Mn C $l_2$를 첨가했을때 효소생성을 37% 증가시켰다. Amino 산중에서 L-leucine이 본 효소생산을 약간 증가시켰으며 L-histidine L-methionine은 크게 저하시켰다. Riboflavine, i-inositol, hesperidine, niacinamide, biotin, DL-$\alpha$- lipoic acid, folic acid가 효소생산을 증가시켰으며 항생물질중에서 cephradine, cephalexin, ampicillin, cloxacillin의 첨가가 효소생성을 크게 증가시켰다. 본 효소생산의 최고 pH는 7.0이며 최적온도는 28$^{\circ}C$였다. 또 500$m\ell$ Erlenmeyer flask에서 175$m\ell$의 배지를 가하여 3 일간 배양했을 때 효소생성이 최고에 도달했다.

• Journal of Pharmaceutical Investigation
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• 제37권6호
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• pp.349-354
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• 2007

For decades, the various virtues of ${\alpha}-lipoic$ acid (ALA), a natural material synthesized in most cells, have been intensively studied and proved. Recently it was reported that ALA caused significant bodyweight reduction via appetite suppression. Unfortunately, the efficacy requires an administration over 50 mg/kg. The low bioavailability and the short plasma half life of ALA lead us to explore novel pharmaceutical dosage forms using nanoparticles. In this study, the effect of polymeric stabilizers on the bioavailability improvement of ALA nanoparticles was investigated. The reduction of particle size via nano-comminution technology was successful resulting in volume average particle sizes of 320 - 340 nm. The in vitro release rate of ALA did not reflect the decrease of particle size, possibly because of the self polymerization of ALA during nano-comminution. The type of polymeric stabilizers could not affect the release rate either. However, the in vivo food intake results of ALA showed that nano-suspensions were more effective than microparticles or a salt form. The nano-suspension containing polyvinyl pyrrolidone as the primary stabilizer and polyacrylic acid as the secondary stabilizer showed more improved efficacy for 2 hours.

• Asian-Australasian Journal of Animal Sciences
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• 제27권7호
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• pp.996-1002
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• 2014

An experiment was conducted to evaluate the effects of dietary alpha-lipoic acid (LA) and acetyl-L-carnitine (ALC) on growth performance, carcass characteristics and meat quality in Arbor Acres broilers. A total of 486 1-d-old male Arbor Acres broilers were randomly allocated to 9 dietary treatments, 9 treatments were group A (0 mg/kg LA and 0 mg/kg ALC), group B (50 mg/kg LA and 0 mg/kg ALC), group C (100 mg/kg LA and 0 mg/kg ALC), group D (0 mg/kg LA and 50 mg/kg ALC), group E (50 mg/kg LA and 50 mg/kg ALC), group F (100 mg/kg LA and 50 mg/kg ALC), group G (0 mg/kg LA and 100 mg/kg ALC), group H (50 mg/kg LA and 100 mg/kg ALC), group I (100 mg/kg LA and 100 mg/kg ALC). Birds were slaughtered at 42 days old. Average daily gain (ADG), average feed intake (AFI), feed conversion rate (FCR), eviscerated rate, breast muscle percentage, thigh muscle percentage, abdominal fat percentage, liver weight, muscle color ($L^*$ value, $a^*$ value, $b^*$ value), pH values at 45 min and 24 h postmortem were measured. Results showed that there existed an interaction between LA and ALC in growth performance of broilers, carcass traits and meat quality. The overall result is that high level of LA and ALC led to lower AFI, ADG (p<0.01), lower abdominal fat percentage, liver weight (p<0.01), lower $L^*$ value, $a^*$ value, and $b^*$ value of breast muscle, $L^*$ value of thigh muscle (p<0.05), and higher FCR (p<0.01), eviscerated rate (p<0.01), breast muscle percentage, thigh muscle percentage (p<0.05), $a^*$ value, pH 45 min and pH 24 h of thigh muscle (p<0.01). These results suggested that dietary LA and ALC contributed to the improvement of meat quality in broilers.

• Asian-Australasian Journal of Animal Sciences
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• 제28권10호
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• pp.1465-1470
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• 2015

The present study was conducted to determine the effects of L-carnosine (LC) and/or alpha-lipoic acid (ALA) supplementation on growth performance, blood thyroid hormones and lipid profiles in finishing pigs. A total of 40 ($Landrace{\times}Yorkshire$) pigs with an initial body weight of $57.93{\pm}3.14kg$ were randomly allocated to 4 experimental diets using a $2{\times}2$ factorial arrangement with 2 LC supplemental levels (0 or 0.1%) and 2 ALA supplemental levels (0 or 0.03%) in basal diets. The results showed that pigs fed LC-supplemented diets increased final live weight, average daily gain, and average daily feed intake compared to those of pigs fed without LC-supplemented diets (p<0.05). Dietary supplementation with ALA did not affect the growth performance and carcass traits of pigs (p>0.05). Additionally, LC supplementation increased serum triiodothyronine, thyroxine levels, and ALA supplementation increased serum triiodothyronine levels (p<0.05). Serum total cholesterol and triglycerides levels were significantly decreased in LC and ALA supplemented groups, respectively (p<0.05). Moreover, serum low density lipoprotein cholesterol levels were lower in the ALA-supplemented groups than those of pigs fed without ALA-supplemented diets (p<0.05). However, no significant $LC{\times}ALA$ interaction effect on growth performance, blood thyroid hormones and lipid profiles was found. This study suggested that dietary supplementation of LC resulted in better growth performance compared to that of ALA supplementation. L-carnosine and/or ALA supplementation positively modified blood lipid profiles, which may have the potential to prevent cardiovascular diseases.

• Asian-Australasian Journal of Animal Sciences
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• 제22권8호
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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.

• Journal of Dental Anesthesia and Pain Medicine
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• 제22권5호
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• pp.323-338
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• 2022

Burning mouth syndrome (BMS) is a chronic oral disorder of unknown etiology which presents therapeutic challenges. Alpha-lipoic acid (ALA) has been studied as a potential treatment for BMS. The objective of this systematic review and meta-analysis was to evaluate the effectiveness of ALA compared to that of placebo or other interventions in individuals with BMS. Randomized controlled trials (RCT) using ALA to treat BMS were identified from MEDLINE, Cochrane Library, EMBASE, and Web of Science up to February 3, 2021. The assessment of the risk of bias in the included studies was based on the Cochrane guidelines. The primary outcome evaluated was the visual analog scale (VAS) pain intensity. ALA was compared with placebo, clonazepam, gabapentin, pregabalin, ALA plus gabapentin, capsaicin, Biotène^®, and laser therapy. Altogether, 137 records were scanned for inclusion/exclusion, and nine RCTs (two unclear and seven at high risk of bias) were included in the qualitative and quantitative analyses, with a total of 594 patients with BMS included in this review. All studies reported an improvement in VAS pain scores ranging from -0.72 to -2.77. Meta-analysis results showed a non-significant reduction in pain intensity for ALA (P = 0.616) compared to that of placebo on a VAS of 0-10. Patients taking ALA were 1.923 times more likely to show an improvement in self-reported BMS symptoms (P = 0.031) than those in the placebo group. Clonazepam and pregabalin showed a significant VAS pain reduction of 4.08 and 4.68 (P < 0.001), respectively, compared to that with ALA. Although ALA intervention provided a non-significant improvement in the pain score and was more likely to produce a reduction in BMS symptoms, the evidence was of low quality. Further research is needed to establish clear guidelines for the use of ALA for BMS treatment.