• KOREAN JOURNAL OF CROP SCIENCE
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• v.53 no.2
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• pp.171-178
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• 2008

In the methanol extract from safflower seeds, two kinds of antioxidant were detected by preparative HPLC [$\mu$-Bondapak $C_{18}$ column ($7.8{\times}300\;mm$)]. Two unknown compounds were defined as CA and CB which had peaks at 22.1 min and 24.5 min, respectively. Antioxidant activity was measured by their scavenging ability on the stable tree radical of 1,1-diphenly-2-picrylhydrazyl (DPPH). For bulk extraction of antioxidants, the methanol extract was fractionated with hexan, chloroform, ethyl acetate and butanol. The ethyl acetate traction showing the highest DPPH radical scavenging activity was further purified by silica gel column chromatography to CA and CB. By NMR analysis, CA and CB were identified as N-(p-Coumaroyl)serotonin and N-feruoylserotonin, respectively. The content of N-(p-Coumaroyl)serotonin and N-feruoylserotonin were analyzed by reverse phase HPLC using a $\mu$-Bondapak $C_{18}$ column ($3.9{\times}300\;mm$) with linear gradient elution from 10% acetonitrile to 50% acetonitrile for 30min on UV detector at 300 nm. The contents of N-(p-Coumaroyl)serotonin and N-feruoylserotonin were 4.11 mg/g DW and 7.29 mg/g DW, respectively, and these two DPPH radical scavengers were detected only in the hull of seeds.

• Applied Chemistry for Engineering
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• v.24 no.6
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• pp.605-610
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• 2013

Gamma-aminobutyric acid (GABA) is a non-protein amino acid widely present in organisms, which has shown several important physiological functions such as neurotransmission, hypotension induction, as well as diuretic and tranquilizer effects. They have also been extensively used in food industry. GABA contents in the grain and brown rice are about 1~4 mg/100 g and 4~8 mg/100 g, respectively but it is difficult to expect physiological activity from such low amounts of natural food intake. We investigate the effects of GABA-coated rice on the secretion of melatonin and serotonin which both have been used as sleep inductive compounds. As a result, the secretion of melatonin and serotonin from mice were found to be $3.578{\pm}0.158pg/mL$, $5.918{\pm}0.169ng/mL$ respectively. The melatonin and serotonin in mice increased significantly up to the 8.7 and 22.8 times respectively, when compared to that of the rice, but there was no cumulative effects. Due to the continuous intake of GABA-coated rice, which was developed as a functional food nutrient, inductive effects of melatonin and serotonin from general rice could be achieved and also the similar effect as taking up directly 25 mg/mL of GABA could be obtained.

• Journal of the Korean Society of Food Science and Nutrition
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• v.32 no.5
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• pp.733-738
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• 2003

Chemical compositions and DPPH radical scavenger activity in different sections of safflower (Carthamus tinctorious L.) were investigated. Protein contained 28.39% in sprout and fat contained 20.47% in seed, respectively. Linoleic acid as predominant unsaturated fatty acid of safflower contained 80.01% in sprout and 78.27% in seed. Glucose contained 1253.6mg% in sprout and fructose contained 970.7mg% in sprout. Sucrose contained 912.0mg% in flower bud. Succinic acid was included 2795.3 mg% in flower, malic acid was included 2054.8mg% in leaf. K as minerals contained 2826.8mg% in leaf and 2613,6 mg% in sprout, Ca contained 1999.8mg% in leaf and 1160.9mg% in sprout. Total phenolics contained 5.8%, 4.7%, 4.4% in flower, sprout and leaf, and total flavonoid contained 6.5%, 2.5%, 2.0% in flower, sprout and leaf, respectively Serotonin-I (Ν- [2- (5-hydroxy - l Η- indol -3- yl)ethyl] ferulamide) as serotonin compounds was determined 147.7mg% in seed, serotonin - II (Ν-［2-(5-hydroxy-lΗ-indo-1-3yl )ethyl]-p-coumaramide) was determined 155.4 mg% in seed. Acacetin as flavonoid compounds was contained 116.5mg% in seed. Luteolin as flavonoid compounds was identified 388.3mg% in sprout, luteolin 7-glucoside was determined 692.3mg% in leaf, respectively. DPPH radical scavenger activity was measured by DPPH method, it was shown higher 114.2% in ethanol extract of flower and 113.6% in ethanol extract of leaf than 88.05% of 100 ppm BHA as chemical antioxidant.

• Preventive Nutrition and Food Science
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• v.4 no.4
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• pp.221-225
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• 1999

Antioxidative compounds contained in roasted safflower seeds were investigated. Six phenolic compounds, N-feruloylserotonin, N-(p-coumaroyl) serotonin, matairesinol, 8'-hydroxyarctigenin, acacetin 7-Ο-β-D-glucoside(tilianine) and acacetin were isolated and identified from the extract of seeds. The inhibitory effects of six phenolic compounds on 1,1-dipheny1-2-picrylhydrazyl(DPPH) radical and lipid peroxidation induced by H₂O₂/FeSO₄in rat liver microsomes were determined. Two serotonins showed more potent DPPH radical scavenging activity, and a stronger inhibitory effect on the lipid peroxidation than that of α-tocopherol. In addition, acacetin and matairesinol also considerably inhibited lipid peroxidation, while 2-hydroxy-arctigenin and tilianine were inactive. These results suggest that phenolic compounds, including serotonins, lignans and flavonoids in the roasted safflower seeds can be used as potential dietary natural antioxidants.

• Journal of the Korean Society of Food Science and Nutrition
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• v.37 no.9
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• pp.1162-1167
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• 2008

This study was to investigate the chemical compositions of germinated (GSS)- and ungerminated (UGSS)-safflower (Carthamus tinctorius) seeds. GSS had higher amount of sugar and crude fiber than UGSS, but less amounts of protein and lipid. Levels of $\alpha$-tocopherol and essential amino acids of GSS were higher than those of UGSS, although there are no difference in fatty acid composition between GSS and UGSS. Among the nine phenolic compounds detected, five phenolic compounds, except for two lignans and two flavonoids, were found in both GSS and UGSS. Four serotonin derivatives accounted for about 80 per cent of total phenolic compounds, and levels of five phenolic compounds decreased slightly with germination. These results suggest that germination may enhance the functionality of safflower seed by increasing nutritional compositions and by decreasing phenolic compounds with bitter taste and cathartic effects.

• Preventive Nutrition and Food Science
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• v.14 no.4
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• pp.373-377
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• 2009

Safflower seed extract was prepared by a high-pressure extraction technology and its quality characteristics were compared to that of other conventional extraction techniques, such ultrasonic and reflux extractions. Safflower seeds were extracted with 80% aqueous ethanol by three above extraction methods, and further fractionated with Diaion HP-20 column chromatography to obtain a partially purified safflower seed extract (PPSSE). Among the three extraction techniques examined, the reflux extraction showed the higher yields of EtOH extract and PPE than the ultrasonic and high-pressure extractions. Levels of most phenolic compounds in the EtOH extract of safflower seed are higher in reflux and ultrasonic extractions than the high pressure extraction, but levels of two serotonin aglycones, N-(p-coumaroyl)serotonin (CS) and N-feruloylserotonin (FS), in PPSSE were higher in the high pressure extraction than the reflux and ultrasonic extractions. In addition, color values (L and a) of the PPSSE were higher in the high-pressure extraction than the reflux and ultrasonic extractions, although there were no significant differences in pH and UV maxima absorption spectra among three extraction techniques. These results indicate that the high-pressure extraction technology is a simple and effective extraction for preparation of a high quality of safflower seed extract containing CS and FS with anti-wrinkle activity.

• Bulletin of the Korean Chemical Society
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• v.28 no.2
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• pp.285-291
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• 2007

The 5-HT6 antagonists are mainly related to the treatment of cognitive dysfunction or impairment associated with Alzheimer's disease and schizophrenia. There have been lots of efforts to develop 5-HT6 antagonists. As in our efforts, arylsulfonylpiperazine derivatives 1-3 were designed, synthesized and biologically evaluated against the human recombinant 5-HT6 serotonin receptor. Total 36 compounds were synthesized and the most active compound among the synthesized compounds is compound 2h with an IC50 value of 1.5 μM. The compound 2h is novel as 5-HT6 receptor ligand and could act as lead for the novel 5-HT6 receptor ligands.

• Proceedings of the Korean Society of Food Science and Nutrition Conference
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• 2001.12a
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• pp.22-37
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• 2001

Melatonin is secreted during the hours of darkness and is thought to influence the circadian and seasonal timing of a variety of physiological processes. Serotonin N-acetyltransferase (AA-NAT) which is found to be expressed in pineal gland, retina, and various tissues, catalyses the conversion of serotonin to N-acetylserotonin and is known as the rate-limiting enzyme in the biosynthetic pathway of melatonin. The compounds that modulate the activity of AA-NAT can be used to treat serotonin-and melatonin-related diseases such as insomnia, depression and seasonal affective disorders (SAD). Several assay methods have been developed by which to measure AA-NAT activity. We have also developed a simple, rapid and sensitive AA-NAT assay method that takes advantage of differences in the organic solubilities between acetyl CoA and N-acetyltryptamine. We screened modulators of AA-NAT activity from the water extracts of the medicinal plants. We found MNP1005 which strongly inhibited the activity of AA-NAT ($IC_{50}$=2.2$\mu$M). Enzyme inhibitory kinetic studies revealed that MNP1005 exhibited a noncompetitive inhibition toward tryptamine. The antidepressant effect of MNP1005 was investigated on behavioral despair test so called forced swimming test (FST). MNP1005 significantly increased swimming behavior by reducing immobility with treatment of 10 mg/kg when compared to the vehicle-treated control group (P < 0.05). This suggests that MNP1005 possesses antidepressant activity. The influence of chronic MNP1005 treatment on the expression of brain-derived neurotrophic factor (BDNF) was examined by in situ hybridization and Northern blot. Chronic treatment of MNP1005 blocked the downregulation of BDNF mRNA in the frontal cortex and other cortex regions in response to restraint stress.

• Applied Biological Chemistry
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• v.19 no.1
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• pp.24-30
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• 1976

Rhizomes of the common reed (Phragmites communis Trin.) were incubated for three days in the dark. Methanol extract of the shoots was thin layer chromatographed with several solvent systems and visualized with five reagents. The results may be summarized as follows: 1. Serotonin, tryptophan, and tryptamine were identified by cochromatography with the respective authentic compounds. Bufotenine, N-methylserotonin, and N,N-dimethyltryptamine were tentatively identified by their Rf values and colour reactions. The presence of skatole and gramine was suggested. 2. It was esteemed that the common reed might have an active methylation/hydroxylation system of indole compounds at least for a period of time. 3. The presently devised 'overlap' thin layer chromatographic technique may be a useful tool for the identification of a compound whose Rf value was diverse from that of the authentic one by the interferance containing in a sample material.

• Bulletin of the Korean Chemical Society
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• v.33 no.8
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• pp.2597-2602
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• 2012

Novel 1,4-substituted piperazine derivatives 5, Series A and B were designed by fragment analysis and molecular modification of 4 selected piperazine-containing compounds which possess antidepressant activity. We synthesized new 39 analogues of Series A and 10 compounds of Series B, respectively. The antidepressant screening against DA, NE, and serotonin neurotransmitter uptake inhibition was carried out using the Neurotransmitter Transporter Uptake Assay Kit. The compounds in Series B showed relatively higher reuptake inhibitory activity for SERT, NET, and DAT than those in Series A. The length of spacer between the central piperazine core and the terminal phenyl ring substituted at the piperazine ring in Series B seems to exert an important role in the activity.