• Journal of the Korean Society of Food Science and Nutrition
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• v.39 no.1
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• pp.154-158
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• 2010

The purposes of this work were to study germination conditions on $\gamma$-aminobutyric acid (GABA) contents and to develop a simple and effective technique for the production of germinated brown rice with an enhanced GABA levels. The samples were subjected to heat treatments at 40 and $45^{\circ}C$ before the soaking step. Moreover, four medicinal plant extracts including Schizandra chinensis, Dimocarpus longan Lour, Angelica dahurica, and Gastrodia elata Blume were used as soaking and germinating media. GABA levels were enhanced in the germinated brown rice compared to the non-germinated brown rice and the highest GABA contents were observed in heat treatment at $35^{\circ}C$. The brown rice soaked in Gastrodia elata Blume extract showed the highest GABA contents compared to the control sample. These results demonstrate that the GABA levels during germination could be significantly enhanced by the heat treatment and the treatment of medicinal plant extracts in the soaking step.

• Progress in Medical Physics
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• v.28 no.4
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• pp.135-143
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• 2017

Chemical Exchange Saturation Transfer (CEST) imaging is a method to detect solutes based on the chemical exchange of mobile protons with water. The solute protons exchange with three different patterns, which are fast, slow, and intermediate rates. The CEST contrast can be obtained from the exchangeable protons, which are hydroxyl protons, amine protons, and amide protons. The CEST MR imaging is useful to evaluate tumors, strokes, and other diseases. The purpose of this study is to review the mathematical model for CEST imaging and for measurement of the chemical exchange rate, and to measure the chemical exchange rate using a 3T MRI system on several amino acids. We reviewed the mathematical models for the proton exchange. Several physical models are proposed to demonstrate a two-pool, three-pool, and four-pool models. The CEST signals are also evaluated by taking account of the exchange rate, pH and the saturation efficiency. Although researchers have used most commonly in the calculation of CEST asymmetry, a quantitative analysis is also developed by using Lorentzian fitting. The chemical exchange rate was measured in the phantoms made of asparagine (Asn), glutamate (Glu), ${\gamma}-aminobutyric$ acid (GABA), glycine (Gly), and myoinositol (MI). The experiment was performed at a 3T human MRI system with three different acidity conditions (pH 5.6, 6.2, and 7.4) at a concentration of 50 mM. To identify the chemical exchange rate, the "lsqcurvefit" built-in function in MATLAB was used to fit the pseudo-first exchange rate model. The pseudo-first exchange rate of Asn and Gly was increased with decreasing acidity. In the case of GABA, the largest result was observed at pH 6.2. For Glu, the results at pH 5.6 and 6.2 did not show a significant difference, and the results at pH 7.4 were almost zero. For MI, there was no significant difference at pH 5.6 or 7.4, however, the results at pH 6.2 were smaller than at the other pH values. For the experiment at 3T, we were only able to apply 1 s as the maximum saturation duration due to the limitations of the MRI system. The measurement of the chemical exchange rate was limited in a clinical 3T MRI system because of a hardware limitation.

• Journal of Pharmaceutical Investigation
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• v.35 no.3
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• pp.193-199
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• 2005

Gabapentin is an antiepileptic drug that is structurally similar to ${\gamma}-aminobutyric$ acid (GABA), but does not interact with the GABA receptor. It does not bind significantly to plasma proteins, and is excreted to unchanged form in the urine. The purpose of the present study was to evaluate the bioequivalence of two gabapentin capsules, $Neurontin^{TM}$ capsule 300 mg (Pfizer Pharm. Co., Ltd.) and Kuhnil $Gabapentin^{TM}$ capsule 300 mg (Kuhnil Pharm. Co., Ltd), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of gabapentin from the two gabapentin formulations in vitro was tested using KP VIII Apparatus II method with various dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty six healthy male subjects, $22.46{\pm}1.86$ years in age and $67.64{\pm}7.24$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After a single capsule containing 300 mg as gabapentin was orally administered, blood samples were taken at predetermined time intervals and the concentrations of gabapentin in serum were determined using HPLC with fluorescence detector. The dissolution profiles of two formulations were similar at all dissolution media. In addition, the pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Neurontin^{TM}$ capsule 300 mg, were -2.03, -0.43 and 4.29% for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 $(e.g.,\;log\;0.89{\sim}log\;1.09\;and\;log\;0.91{\sim}log\;1.09$ for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Kuhnil $Gabapentin^{TM}$ capsule 300 mg was bioequivalent to $Neurontin^{TM}$ capsule 300 mg.

• The Korean Journal of Physiology and Pharmacology
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• v.17 no.2
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• pp.127-132
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• 2013

Ginsenosides, one of the active ingredients of Panax ginseng, show various pharmacological and physiological effects, and they are converted into compound K (CK) or protopanaxatriol (M4) by intestinal microorganisms. CK is a metabolite derived from protopanaxadiol (PD) ginsenosides, whereas M4 is a metabolite derived from protopanaxatriol (PT) ginsenosides. The ${\gamma}$-aminobutyric acid $receptor_C$ ($GABA_C$) is primarily expressed in retinal bipolar cells and several regions of the brain. However, little is known of the effects of ginsenoside metabolites on $GABA_C$ receptor channel activity. In the present study, we examined the effects of CK and M4 on the activity of human recombinant $GABA_C$ receptor (${\rho}$ 1) channels expressed in Xenopus oocytes by using a 2-electrode voltage clamp technique. In oocytes expressing $GABA_C$ receptor cRNA, we found that CK or M4 alone had no effect in oocytes. However, co-application of either CK or M4 with GABA inhibited the GABA-induced inward peak current ($I_{GABA}$). Interestingly, pre-application of M4 inhibited $I_{GABA}$ more potently than CK in a dose- dependent and reversible manner. The half-inhibitory concentration ($IC_{50}$) values of CK and M4 were $52.1{\pm}2.3$ and $45.7{\pm}3.9{\mu}M$, respectively. Inhibition of $I_{GABA}$ by CK and M4 was voltage-independent and non-competitive. This study implies that ginsenoside metabolites may regulate $GABA_C$ receptor channel activity in the brain, including in the eyes.

• The Korean Journal of Physiology and Pharmacology
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• v.17 no.2
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• pp.175-180
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• 2013

Resveratrol is a phytoalexin found in grapes, red wine, and berries. Resveratrol has been known to have many beneficial health effects, such as anti-cancer, neuroprotective, anti-inflammatory, and life-prolonging effects. However, relatively little is known about the effects of resveratrol on the regulation of ligand-gated ion channels. We have previously reported that resveratrol regulates subsets of homomeric ligand-gated ion channels such as those of 5-$HT_{3A}$ receptors. The ${\gamma}$-aminobutyric $acid_C$($GABA_C$) receptor is mainly expressed in retinal bipolar cells and plays an important role in visual processing. In the present study, we examined the effects of resveratrol on the channel activity of homomeric $GABA_C$ receptor expressed in Xenopus oocytes injected with cRNA encoding human $GABA_C$ ${\rho}$ subunits. Our data show that the application of GABA elicits an inward peak current ($I_{GABA}$) in oocytes that express the $GABA_C$ receptor. Resveratrol treatment had no effect on oocytes injected with $H_2O$ or with $GABA_C$ receptor cRNA. Co-treatment with resveratrol and GABA inhibited $I_{GABA}$ in oocytes with $GABA_C$ receptors. The inhibition of $I_{GABA}$ by resveratrol was in a reversible and concentration-dependent manner. The $IC_{50}$ of resveratrol was $28.9{\pm}2.8{\mu}M$ in oocytes expressing $GABA_C$ receptor. The inhibition of $I_{GABA}$ by resveratrol was in voltage-independent and non-competitive manner. These results indicate that resveratrol might regulate $GABA_C$ receptor expression and that this regulation might be one of the pharmacological actions of resveratrol on the nervous system.

• Journal of Life Science
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• v.19 no.9
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• pp.1232-1238
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• 2009

Neurotransmitter release is regulated by various proteins of the active zone in the presynaptic nerve terminals. Dopamine (DA) is an essential neurotransmitter associated with the pathophysiology of diverse behavioral and mental illness such as schizophrenia and drug addiction. We measured synaptosomal DA release of knockout (KO) mice which lacked major genes related to neurotransmitter release. Synaptosomal DA uptake and release were performed and measured using [$^3H$]-DA and superfusion experiments. 3 of the 17 KO mice exhibited altered DA release compared to their littermate controls. In $Rim1{\alpha}$ KO, [$^3H$]-DA release evoked by membrane depolarization significantly decreased. Both basal (physiological buffer-evoked) and membrane depolarization-evoked DA release significantly decreased in dopaminergic conditional KO of $Rim1{\alpha}{\beta}$. Dopaminergic conditional KO of neurexin3 demonstrated a significant increase of membrane depolarization-evoked DA release. These data explain the similarities and distinctions between DA and other classical neurotransmitters such as glutamate and GABA ($\gamma$-aminobutyric acid) release. In conclusion, $Rim1{\alpha}$ and neurexin3 may be important regulators of presynaptic DA release and related to disorders of the nervous system.

• The Korean Journal of Food And Nutrition
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• v.27 no.4
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• pp.692-698
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• 2014

In this study, we investigated cancer cell growth inhibitory effects of kimchi extracts obtained from cabbage kimchi. Kimchi extracts (S46h, S47h, S48h) were obtained from the samples fermented at $15^{\circ}C$ for 46 h, 47 h, and 48 h during the first 10 days, which were subsequently stored at $-1.4^{\circ}C$ in kimchi refrigerator (hereinafter DV kimchi extracts). The samples showed a higher anti-proliferative effect against AGS (human, gastric adenocarcinoma) cell lines compared to control kimchi extract (S0h) obtained from sample stored at $-1.4^{\circ}C$ without fermentation. The DV kimchi contained higher levels of ${\gamma}$-aminobutyric acid (GABA) and ornithine compared to the control kimchi extract. Among the DV kimchi extracts, the S46h sample showed a higher anti-proliferative effect against the cancer cell growth and contained higher amount of GABA than the other kimchi samples. These results suggest that the consumption of DV kimchi can be more beneficial, as it is rich in GABA and ornithine. Therefore, it could be helpful in retarding the proliferation of cancer cells compared to the control kimchi.

• Journal of the Korean Society of Food Science and Nutrition
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• v.39 no.8
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• pp.1201-1206
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• 2010

As a means to increase the production and consumption of the brown colored rice with high content of GABA ($\gamma$-aminobutyric acid), this study was conducted to develop brown colored rice tea. After roasting at various temperatures and times, color values and GABA content of the brown colored rice were analyzed. Physicochemical properties such as browning, turbidity, reducing sugar, soluble solid, total polyphenol and pH of brown colored rice tea were determined after the rice powder was put into tea bags and leached in hot water. Sensory characteristics were investigated for three kinds of tea roasted at $170^{\circ}C$ for 10, 20 and 30 min. As the roasting temperature and time increased, L, a and b values decreased as well as GABA content. The brown colored rice roasted at $170^{\circ}C$ for 10 min contained the highest content of GABA. Browning, turbidity, reducing sugar, soluble solid and total polyphenol of the brown colored rice tea increased as the roasting temperature and time increased, on the contrary, pH decreased. The brown colored rice tea roasted for 30 min was preferred the most in color, flavor, taste and overall acceptance. From this result, the brown colored rice tea needs to be manufactured by a combination of the brown colored rice roasted at $170^{\circ}C$ for 10 min and 30 min to satisfy the consumer's preference and high content of GABA.

• Journal of the Korean Society of Food Science and Nutrition
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• v.41 no.7
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• pp.963-969
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• 2012

This study evaluated the physicochemical properties of brown rice (BR) and germinated brown rice (GBR) in Korea. The protein content of BR was significantly higher than that of GBR. The amylose content of BR and GBR ranged from 17.42 to 18.48% and from 17.50 to 19.69%, respectively. The GBR contained higher ${\gamma}$-aminobutyric acid (GABA) content than that of BR. In an RVA examination, pasting temperatures of BR and GBR were $67.97{\sim}68.03^{\circ}C$. Texture analysis test showed that GBR Yeonghojinmi had the lowest hardness and highest stickiness. In conclusion, this study showed that compared to BR, GBR has a much softer texture, improved eating quality and increased GABA content.

• Plant Biotechnology Reports
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• v.5 no.3
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• pp.225-234
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• 2011

Arabidopsis mutants with T-DNA insertion in seven calmodulin genes (CAM) were used to determine the specific role of CAM in the tolerance of plants to oxidative stress induced by paraquat and hydrogen peroxide ($H_2O_2$) treatments. Arabidopsis calmodulin mutants (cam) were screened for seedling growth, seed germination, induced oxidative damage, and levels of ${\gamma}$-aminobutyric acid (GABA) shunt metabolites. Only the cam5-4 and cam6-1 mutants exhibited an increased sensitivity to paraquat and $H_2O_2$ during seed germination and seedling growth. In response to treatments with $3{\mu}M$ paraquat and 1 mM $H_2O_2$, only the cam5-4, cam6-1 mutants showed significant changes in malonaldehyde (MDA) levels in root and shoot tissues, with highly increased levels of MDA. In terms of the GABA shunt metabolites, GABA was significantly elevated in root and shoot tissues in response to the paraquat treatments in comparison to alanine and glutamate, while the levels of all shunt metabolites increased in root tissue but not in the shoot tissue following the $H_2O_2$ treatments. GABA, alanine and glutamate levels were significantly increased in root and shoot of the cam1, cam4, cam5-4, and cam6-1 mutants in response to paraquat (0.5, 1 and $3{\mu}M$), while they were increased only in the root tissue of the cam1, cam4, cam5-4, and cam6-1 mutants in response to $H_2O_2$ (200 and $500{\mu}M$, 1 mM). These data show that the cam5-4 and cam6-1 mutants were sensitive to the induced oxidative stress treatments in terms of seed germination, seedling growth, and oxidative damage. The accumulation of GABA shunt metabolites as a consequence of the induced oxidative stress treatments (paraquat and $H_2O_2$ treatments) suggests that the GABA shunt pathway and the accumulation of GABA metabolites may contribute in antioxidant machinery associated with reactive oxygen species and in the acquisition of tolerance in response to induced oxidative stress in Arabidopsis seedlings.