• Proceedings of the Korean Society of Applied Pharmacology
• /
• 2003.11a
• /
• pp.3-4
• /
• 2003

Body weight is maintained at a relatively constant level over days and months despite variability in food intake and physical activity. To achieve energy homeostasis, the hypothalamus receives information related to energy surplus or shortage from the periphery and controls food intake and energy expenditure. Leptin, an adipocyte derived hormone, is a principal mediator that signals the brain about the stored energy status. Increased leptin signaling in the brain prevents excess energy stores by suppressing food intake and increasing energy expenditure. In addition, insulin and nutrients themselves, such as glucose and free fatty acids, also regulate food intake.

• 한국생물공학회:학술대회논문집
• /
• 2001.11a
• /
• pp.642-645
• /
• 2001

Enterococcus faecalis was cultivated under oxidative conditions established by adding some oxidants. FAD and lipoic acid either stimulate the biosynthesis of benzoylformate reductase or stabilize the enzyme, while $MV^{2+}$ enhance the biosynthesis of the oxidoreductase but destabilize it. Since $MV^{2+}$ destabilize the benzoylformate reductase, substituting FAD for $MV^{2+}$ as a redox mediator would be desirable. Production of (R)-(-)-mandelic acid by a coupled reaction between the enzymatic reaction using benzoylformate reductase and the electrocatalytic reduction under the conditions of 1.5 U LiDH $ml^{-1}$, 0.2 mM FAD, and 0.3 mM $NAD^+$ is now performing.

• Journal of Chest Surgery
• /
• v.45 no.1
• /
• pp.1-10
• /
• 2012

Background: ${\alpha}$-Lipoic acid (${\alpha}$-LA) has been studied as an anticancer agent as well as a therapeutic agent for diabetes and obesity. We performed this study to evaluate the anticancer effects and mechanisms of ${\alpha}$-LA in a lung cancer cell line, A549. Materials and Methods: ${\alpha}$-LA-induced apoptosis of A549 cells was detected by fluorescence-activated cell sorting analysis and a DNA fragmentation assay. Expression of apoptosis-related genes was analyzed by western blot and reverse transcription.polymerase chain reaction analyses. Results: ${\alpha}$-LA induced apoptosis and DNA fragmentation in A549 cells in a dose- and time-dependent manner. ${\alpha}$-LA increased caspase activity and the degradation of poly (ADP-ribose) polymerase. It induced expression of endoplasmic reticulum (ER) stress-related genes, such as glucose-regulated protein 78, C/EBP-homologous protein, and the short form of X-box binding protein-1, and decreased expression of the anti-apoptotic protein, X-linked inhibitor of apoptosis protein. Reactive oxygen species (ROS) production was induced by ${\alpha}$-LA, and the antioxidant N-acetyl-L-cysteine decreased the ${\alpha}$-LA-induced increase in expression of apoptosis and ER stress-related proteins. Conclusion: ${\alpha}$-LA induced ER stress-mediated apoptosis in A549 cells via ROS. ${\alpha}$-LA may therefore be clinically useful for treating lung cancer.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.25 no.1
• /
• pp.55-64
• /
• 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.

• Journal of Dental Rehabilitation and Applied Science
• /
• v.35 no.3
• /
• pp.123-131
• /
• 2019

Burning mouth syndrome (BMS) is defined as the xerostomia, burning sensation and various discomfort of tongue and oral mucosa. BMS can occur in both men and women, but is more frequent in middle-aged menopausal women. Because exact cause can't be identified clearly and it is hard to make diagnosis in clinic, the purpose of the treatment have been to relieve symptoms. Etiology of BMS is divided into local, systemic, and psychological factors. ${\alpha}$-lipoic acid, clonazepam, supplemental therapy and cognitive behavior therapy can be prescribed for BMS. Nowdays, many experts focus attention on effect of combination therapy. It is necessary to solve the symptoms of the patients by combination of pharmacological approach and psychotherapy with cognitive behavior therapy considering the factors in various aspects.

• Journal of Oral Medicine and Pain
• /
• v.34 no.4
• /
• pp.429-433
• /
• 2009

Burning mouth syndrome (BMS) is defined as burning pain in the tongue or other oral mucous membrane associated with normal sign and laboratory findings at least 4 to 6 months. There are many factors that affect this condition and the pain characters are various among the sufferers, so it is difficult to diagnose exactly and treat properly. The cause of BMS is currently unknown. The etiology is presumed to be that it is related with local, systemic and psychogenic factor. The BMS is related with local factor such as allergic reaction, oral fungal infection(candidiasis), parafunctional oral habits and systemic factors such as diabetes mellitus, hypothyroidism, nutritional deficiencies(vitamin $B_{12}$, folic acid), hyposalivation and psychogenic factor such as depression, anxiety, cancerphobia. So clinicians must be aware of these factors and can give proper treatment options to patients. The management of BMS are pharmacologic management, cognitive behavioral therapy and psychotherapy treatment. Clonazepam, gabapentin, amitriptyline, alpha-lipoic acid and capsaicin are used to manage the BMS. Among these, topical clonazepam is reported that the effect is higher than systemic medication and the complications are rare. This case report is about some cases of the effect of topical clonazepam on BMS.

• Journal of the Korea Academia-Industrial cooperation Society
• /
• v.19 no.12
• /
• pp.62-70
• /
• 2018

In this study, we synthesized Oligo Peptide (Lys-Val-Ala-Arg-Pro: KVARP) and peptide derivatives using Solid Phase Peptide Synthesis(SPPS). KVARP was commonly known to improve whitening of skin. We measured bio-activity of the synthesized compounds. The whitening effect was measured in tyrosinase inhibition and the result showed to be highly effective with 93% inhibition rate at $5000{\mu}g/m{\ell}$ of Geranic-KVARP, on the other hand the IC50 value was $68{\mu}g/m{\ell}$. The wrinkle-reducing effect was measured by elastase inhibition at a concentration of 63% at $400{\mu}g/m{\ell}$ of Salicylic-KVARP, and the IC50 value was $253{\mu}g/m{\ell}$. In the DPPH assay, Caffeic-KVARP showed more than 95% antioxidant activity at $400{\mu}g/m{\ell}$ with high concentration and IC50 value was $31{\mu}g/m{\ell}$. The anti-inflammatory effect of Nitric Oxide inhibition was 67% at $400{\mu}g/m{\ell}$ of Lipoic-KVARP. Therefore, the four types of KVARP derivative that were synthesized from various experiments has shown that it could have potential to be used to develop new medicines, cosmetics as well as in various industries.

• Korean Journal of Clinical Laboratory Science
• /
• v.52 no.3
• /
• pp.253-260
• /
• 2020

Alzheimer's disease (AD) is a chronic and progressive neurodegenerative disease that can be described by the occurrence of dementia due to a decline in cognitive function. The disease is characterized by the formation of extracellular and intracellular amyloid plaques. Amyloid beta (Aβ) is a hallmark of AD, and microglia can be activated in the presence of Aβ. Activated microglia secrete pro-inflammatory cytokines. Furthermore, S100A9 is an important innate immunity pro-inflammatory contributor in inflammation and a potential contributor to AD. This study examined the effects of metformin and α-LA on the inflammatory response and NLRP3 inflammasome activation in Aβ- and S100A9-induced BV-2 microglial cells. Metformin and α-LA attenuated inflammatory cytokines, such as tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). In addition, metformin and α-LA inhibited the phosphorylation of JNK, ERK, and p38. They activated the nuclear factor kappa B (NF-κB) pathway and the NOD-like receptor pyrin domain containing 3 (NLRP3) inflammasome. Moreover, metformin and α-LA reduced the marker levels of the M1 phenotype, ICAM1, whereas the M2 phenotype, ARG1, was increased. These findings suggest that metformin and α-LA are therapeutic agents against the Aβ- and S100A9-induced neuroinflammatory responses.

• Journal of the Korean Chemical Society
• /
• v.60 no.2
• /
• pp.125-130
• /
• 2016

With the goal of developing Alzheimer’s disease therapeutics, we have designed and synthesized new triazole linked decursinol derivatives having potency inhibitory activities against cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)]. Since inhibition of cholinesterase (ChE) is still considered to be one of the most effective targets to treat AD patients, many new classes of ChE inhibitors have been synthesized. In an effort of identifying new type of cholinergic drug, decursinol derivatives 11-17 have been synthesized between decursinol and other biological interesting compounds such as lipoic acid, polyphenols, etc by using the click reaction and then evaluated their biological activities. Compound 12 (IC₅₀ = 5.89 ± 0.31 mM against BuChE) showed more effective inhibitory activity against BuChE than galantamine (IC₅₀ = 9.4 ± 2.5 mM). Decursinol derivatives can be considered a new class inhibitor for BuChE and can be applied to be a novel drug candidate to treat AD patients.

• Korean Journal of Pharmacognosy
• /
• v.16 no.3
• /
• pp.129-135
• /
• 1985

In order to search for potential antidotes for T-2 toxin poisoning, seven Chinese herbal drug extracts and five natural constituents were tested on mice intoxicated with T-2 toxin. When extracts of Panax ginseng and Atractylodes japonica (500 mg/kg) were administered p.o. once 3 hrs before and once 1 hr after T-2 toxin treatment, a 30% complete survival rate was noted. In case of Paeonia albiflora var. typica, a 30% complete survival rate was also produced at a dose of 250 mg/kg. Other extracts, Glycyrrhiza uralensis, Scutellaria baicalensis, Rehmannia glutinosa and Plantago asiatica exhibited no significant protection from the T-2 toxin poisoning. A nucleoside, thymidine showed protective activity against T-2 toxin toxicity and it produced a 40% complete survival rate when administered i.p. once 0.5 hr after T-2 toxin treatment. Other natural constituents, aucubin, vitamin C and E, and lipoic acid did not show any significant protective activities.