• Journal of the Society of Cosmetic Scientists of Korea
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• v.37 no.2
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• pp.171-176
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• 2011

N-feruloylserotonin (FS) and N-(pcoumaroyl) serotonin (CS), serotonin derivatives, which have been isolated as major and unique phenolics of safflower seed extract (SSE), are member of hydroxycinnamic acid amides and are implicated in the defense against pathogen infection and insect feeding. In this study, we evaluate inhibitory effects of N-(p-Coumaroyl)serotonin and N-Feruloylserotonin on adipogenesis using oil-red O staining, triglyceride and GPDH activity. we found that while serotonin itself did not suppress differentiation of preadipocytes into adipocytes, N-(p-Coumaroyl)serotonin and N-Feruloylserotonin inhibited the differentiation of preadipocytes into adipocytes in a concentration-dependent manner. In addition, they showed antioxidant effects in DPPH assay. Taken together, these results show that N-feruloylserotonin (FS) and N-(pcoumaroyl) serotonin (CS) suppress differentiation of preadipocytes, suggesting the possibility that these serotonin derivatives can be utilized as an anti-obesity agent.

• Food Science and Biotechnology
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• v.16 no.1
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• pp.71-77
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• 2007

The antioxidant properties of twelve phenolic compounds, including matairesinol 4'-O-$\beta$-D-glucoside, 8'-hydroxyarctigenin 4'-O-$\beta$-D-glucoside, matairesinol, 8'-hydroxyarctigenin, N-feruloylserotonin 5-O-$\beta$-D-glucoside, N-(p-coumaroyl)-serotonin-5-O-$\beta$-D-glucoside, N-feruloylserotonin, N-(p-coumaroyl)serotonin, luteolin 7-O-$\beta$-D-glucoside, luteolin, acacetin 7-O-$\beta$-glucuronide, and acacetin, isolated from defatted safflower (Carthamus tinctorius L.) seeds were evaluated with regard to the DPPH, superoxide and hydroxyl radicals. Additionally, levels of phenolic compounds were determined by HPLC in two cultivars of safflower seeds. Among them, four serotonin derivatives showed potent DPPH ($IC_{50}=10.83-21.75\;{\mu}M$) and hydroxyl ($IC_{50}=75.93-374.63\;{\mu}M$) radical scavenging activities, and their activities were significantly stronger than that of ${\alpha}-tocopherol$. Four flavonoids ($IC_{50}=170.65-275.83\;{\mu}M$) and four lignans ($IC_{50}=114.22-406.10\;{\mu}M$) exhibited significant superoxide and hydroxyl radical scavenging activities, respectively, whereas these compounds contained less activity toward the DPPH and hydroxyl radicals than serotonin derivatives. The levels of serotonin derivatives, lignans and flavonoids in safflower seeds of two cultivars ranged from 49.30 to 260.40, 3.72 to 158.90, and 11.72 to 214.97 mg% (dry base), respectively. Of the two cultivars, 'Cheongsu' had somewthat higher concentrations of phenolic compounds than 'Uisan'. These results suggest that phenolic compounds in safflower seeds may playa role as protective phytochemical antioxidants against reactive oxygen-mediated pathological diseases.

• 한국약용작물학회:학술대회논문집
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• 2008.05a
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• pp.57-58
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• 2008

• Journal of Integrative Natural Science
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• v.9 no.2
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• pp.128-135
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• 2016

5-hydroxytryptamine (serotonin) receptor ($5-HT_7R$) 7 is one of G-Protein coupled receptors, which is activated by the neurotransmitter Serotonin. After activation by serotonin, $5-HT_7$ activates the production of the intracellular signaling molecule cyclic AMP. $5-HT_7$ receptor has been found to be involved in the pathophysiology of various disorders. It is reported that $5-HT_7$ receptor antagonists can be used as antidepressant agents. In this study, we report the important structural and chemical parameters for 2-methoxyphenylpiperazinylakanamides as $5-HT_7R$ inhibitors. A 3D QSAR study based on comparative molecular field analysis (CoMFA) was performed. The best predictions were obtained for the best CoMFA model with $q^2$ of 0.594 with 6 components, $r^2$ of 0.986, Fisher value as 60.607, and an estimated standard error of 0.043. The predictive ability of the test set was 0.602. Results obtained the CoMFA models suggest that the data are well fitted and have high predictive ability. The contour maps are generated and studied. The contour analyses may serve as tool in the future for designing of novel and more potent $5-HT_7R$ derivatives.

• Nuclear Medicine and Molecular Imaging
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• v.41 no.2
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• pp.118-131
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• 2007

Neurotransmitter imaging with radiopharmaceuticals plays major role for understanding of neurological and psychiatric disorders such as Parkinson's disease and depression. Radiopharmaceuticals for neurotransmitter imaging can be divided to dopamine transporter imaging radiopharmaceuticals and serotonin trnasporter imaging radiopharmaceuticals. Many kinds of new dopamine transporter imaging radiopharmcaeuticals has a tropane ring and they showed different biological properties according to the substituted functional group on tropane ring. After the first clinical trials with $[^{123}I]{\beta}-CIT$, alkyl chain substituent introduced to tropane ring amine to decrease time for imaging acquisition and to increase selectivity. From these results, $[^{123}I]PE2I$, [18F]FE-CNT, $[^{123}I]FP-CIT$ and $[^{18}F]FP-CIT$ were developed and they showed high uptake on the dopamine transporter rich regions and fast peak uptake equilibrium time within 4 hours after injection. $[^{11}C]McN$ 5652 was developed for serotonin trnasporter imaging but this compound showed slow kinetics and high background radioactivity. To overcome these problems, new diarylsulfide backbone derivatives such as ADAM, ODAM, AFM, and DASB were developed. In these candidates, $[^{11}C]AFM$ and $[^{11}C]DASB$ showed high binding affinity to serotonin transporter and fast in vivo kinetics. This paper gives an overview of current status on dopamine and serotonin transporter imaging radiopharmaceuitcals and the development of new lead compounds as potential radiopharmaceuticals by medicinal chemistry.

• YAKHAK HOEJI
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• v.31 no.3
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• pp.154-163
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• 1987

Daidzein and its methyl derivatives were synthesized and their anti-inflammatory activities were examined. Daidzein suppressed the carrageenin-induced edema, but its methyl derivatives showed decrease or abolition of the anti-inflammatory effect. Daidzein did not significantly suppress the complete Freund's adjuvant-induced arthritis, and the mixed phlogistics (histamine+serotonin)-induced edema. Daidzein inhibited the leukocyte emigration and protein exudation when it was administered into the CMC pouch at low doses (5,25mg/pouch). Daidzein significantly suppressed the cotton-pellet granuloma formation.

• 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.

• 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.

• Journal of Plant Biotechnology
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• v.42 no.4
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• pp.364-369
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• 2015

Safflower (Carthamus tinctorius) seeds are wellknown traditional oriental medicines that have long been used for the remedies of blood stasis and bone formation in east Asia. In this study, ethyl acetate (EtOAc) was used for extraction of the main chemical compounds from C. tinctorius seeds. Four major compounds were identified, acacetin, cosmosiin, N-feruloyl serotonin and N-(p-coumaroyl) serotonin. Each compound was evaluated for its inhibitory activity against the inflammatory process of macrophages. All compounds significantly inhibited production of lipopolysaccharide (LPS)-stimulated nitric oxide (NO) and pro-inflammatory cytokines. The protein levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) were dramatically decreased by serotonins in a dose-dependent manner in LPS-stimulated RAW 264.7 macrophages. These results suggest that serotonin derivatives from safflower seeds may reduce inflammation-related diseases.

• Bulletin of the Korean Chemical Society
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• v.30 no.8
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• pp.1873-1876
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• 2009