• Title/Summary/Keyword: $1-{\alpha}(OH)D_3$

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DPPH Radical Scavenging Effect and in vitro Lipid Peroxidation Inhibition Activity of Portulaca oleracea and Its Active Principles (쇠비름(Portulaca oleracea) 추출물의 DPPH radical 소거능과 in vitro 지질과산화 억제 효과와 활성성분)

  • Lee, Hee-Jung;Lee, Burm-Jong;Lee, Dong-Seok;Seo, Young-Wan
    • 한국생물공학회:학술대회논문집
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    • 2003.04a
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    • pp.668-672
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    • 2003
  • An antioxidative activity of Portulaca oleracea was tested by in vitro experimental models. The antioxidative activities were determined by evaluation the DPPH radical scavenging activity and by measuring lipid peroxide using 2-thiobarbituric acid (TBA). The crude extract was sequentially partitioned with n-hexane, 15% aq. MeOH, EtOAc, n-BuOH, $H_2O$. Among them, a remarkable antioxidative effect was observed in the fractions of EtOAc and n-BuOH. The DPPH radical scavenging effect $(IC_{50}=17.90{\mu}g/ml)$ of the n-BuOH soluble fraction was comparable with that of natural antioxidant, ${\alpha}-tocopherol(IC_{50}=\;6.99{\mu}g/ml)$ and the inhibitory effect of lipid peroxidation in mouse liver homogenate was similar to that of natural antioxidant, L-ascorbic acid at a concentration of 0.1mg/ml to 5mg/ml. From the BuOH soluble fraction yielded two biophenolic glycosides, 3-hydroxy-1-(2-hydroxyethyl)phenyl-4-O-${\beta}$-D-glucopyranoside(1) and 2-(3,4-dihydroxyphenyl)ethyl-O-${\beta}$-D-glucopyranoside(2) using column chromatography and revered-phase HPLC. In particular, the DPPH radical scavenging activity of 2 was comparable to that tocopherol$(IC_{50}=6.59{\mu}g/ml)$.

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Preparation of Natural Compounds-tripeptides Derivatives and Their Melanogensis Inhibitory Activity (천연유래물질 펩타이드 유도체의 제조와 멜라닌 생성 저해 효과 탐색)

  • Shin, Kyong-Hoon;Lee, Jae-Ho;Ryu, Geun-Seok;Jee, Kyung-Yup;Park, Soo-Nam;Kim, Jae-Il;Cho, In-Shik;Kim, Han-Young
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.36 no.3
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    • pp.233-240
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    • 2010
  • Derivatives of a novel natural compunds, melanostatin (PLG-$NH_2$) were prepared by solid phase synthesis[1,2] and assayed to evaluate their melanogensis inhibitory activity. Also, a small library (natural compound-XLG-$NH_2$, natural compound-X LG-OH) was prepared with same method for increasing synthetic yield and cost-reduction. PLG-$NH_2$ (Proline-Leucine-Glycine-$NH_2$) was well-known tripeptide as its $\alpha$-MSH release-inhibiting activity and tyrosinase inhibitory activity[3-5]. In order to choose best candidate for peptide derivatization, various natural compounds were screened by their tyrosinase inhibitory activity. As a result, caffeic acid and coumaric acid were selected. Most of these derivatives showed better activities than the parent natural compound, melanostatin.

Chemical Constituents from the Stems of Lagerstroemia indica and Their Anti-oxidant Effect (배롱나무의 항산화 활성 성분)

  • Woo, Kyeong Wan;Sim, Mi Ok;Park, Eel Jong;Kim, Min Suk;Suh, Won Se;Cho, Hyun Woo;Kwon, Hak Cheol;Park, Jong Cheol;Lee, Kang Ro
    • Korean Journal of Pharmacognosy
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    • v.47 no.3
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    • pp.204-210
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    • 2016
  • Phytochemical investigation of the 80% MeOH extract from the stems of Lagerstroemia indica resulted in the isolation of eighteen compounds; four norsesquiterpenes, fourteen phenolic derivatives. Their chemical structures were characterized by spectroscopic methods to be tachioside (1), isotachioside (2), 2,4,6-trimethoxyphenyl ${\beta}$-D-glucopyranoside (3), gallic acid 4-methyl ether (4), protocatechuic acid (5), gallic acid (6), vanillic acid (7), vanillin (8), 2-methoxy-5-hydroxymethyl-phenyl-1-O-(6"-galloyl)-${\beta}$-D-glucopyranoside (9), 2,4,6-trimethoxyphenol-1-O-${\beta}$-D-(6'-O-galloyl)-glucopyranoside (10), 4-hydroxy-3-methoxyphenyl-1-O-(6'-O-galloyl)-${\beta}$-D-glucopyranoside (11), vomifoliol (12), vomifoliol 9-O-${\beta}$-D-glucopyranoside (13), 6R,9R-3-oxo-${\alpha}$-ionol-9-O-${\beta}$-D-glucopyranoside (14), dihydrophaseic acid 4'-O-${\beta}$-D-glucopyranoside (15), ${\beta}$-hydroxypropiovanillone 3-O-${\beta}$-D-glucopyranoside (16), myrciaphenone A (17), and coumaric acid (18). Compounds 1-5 and 7-18 were isolated for the first time from this plant. Compounds 1-18 were investigated for their antioxidant properties using DPPH and ABTS radical scavenging capacity assay, $Fe^{2+}$ chelating, and FRAP assay. It was found that 4, 6, and 11 possessed the highest antioxidant capacities.

Characterization and Transcriptional Activity of a Vitamin D Receptor Ortholog in the Ascidian Halocynthia roretzi (멍게(Halocynthia roretzi) 비타민 D 수용체 상동체 동정 및 전사활성)

  • Lee, Jung Hwan;Sohn, Young Chang
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.48 no.6
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    • pp.913-919
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    • 2015
  • In vertebrates, the vitamin D receptor (VDR), a member of the nuclear receptor superfamily, binds the biologically active ligand $1{\alpha},25-(OH)_2$-vitamin $D_3$ (1,25 $D_3$). Nearly all vertebrates, including Agnatha, possess a VDR with high ligand selectivity for 1,25 $D_3$ and related metabolites. Although a putative ancestral VDR gene is present in the genome of the chordate invertebrate Ciona intestinalis, the functional characteristics of marine invertebrate VDR are still obscure. To elucidate the ascidian Halocynthia roretzi VDR (HrVDR), we cloned full-length HrVDR cDNA and investigated the transcriptional activity of HrVDR in HEK293 cells. HrVDR consists of 1,680 nucleotides (559 amino acids [aa]), including a short N-terminal region (A/B domain; 26 aa), DNA-binding domain (C domain; 72 aa), hinge region (D domain; 272 aa), and C-terminal ligand-binding domain (E domain; 161 aa). The amino acid sequence identity of HrVDR was greatest to that of C. intestinalis VDR (56%). In the luciferase reporter assays, the transcriptional activity of HrVDR was not significantly increased by 1,25 $D_3$, whereas the farnesoid X receptor agonist GW4064 increased the transactivation of HrVDR. These results suggest the presence of a novel ligand for and a distinct ligand-binding domain in ascidian VDR.

Pathophysiological Regulation of Vascular Smooth Muscle Cells by Prostaglandin F2α-dependent Activation of Phospholipase C-β3 (Prostaglandin F2α 의존적 phospholipase C-β3 활성화에 의한 혈관평활근세포의 병태생리 조절 연구)

  • Kang, Ki Ung;Oh, Jun Young;Lee, Yun Ha;Lee, Hye Sun;Jin, Seo Yeon;Bae, Sun Sik
    • Journal of Life Science
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    • v.28 no.12
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    • pp.1516-1522
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    • 2018
  • Atherosclerosis is an obstructive vessel disease mainly caused by chronic arterial inflammation to which the proliferation and migration of vascular smooth muscle cells (VSMCs) is the main pathological response. In the present study, the primary responsible inflammatory cytokine and its signaling pathway was investigated. The proliferation and migration of VSMCs was significantly enhanced by the prostaglandin $F_{2{\alpha}}$ ($PGF_{2{\alpha}}$), while neither was affected by tumor necrosis factor ${\alpha}$. Prostacyclin $I_2$ was seen to enhance the proliferation of VSMCs while simultaneously suppressing their migration. Both prostaglandin $D_2$ and prostaglandin $E_2$ significantly enhanced the migration of VSMCs, however, proliferation was not affected by either of them. The proliferation and migration of VSMCs stimulated by $PGF_{2{\alpha}}$ progressed in a dose-dependent manner; the $EC_{50}$ value of both proliferation and migration was $0.1{\mu}M$. VSMCs highly expressed the phospholipase isoform $C-{\beta}3$ ($PLC-{\beta}3$) while others such as $PLC-{\beta}1$, $PLC-{\beta}2$, and $PLC-{\beta}4$ were not expressed. Inhibition of the PLCs by U73122 completely blocked the $PGF_{2{\alpha}}$-induced migration of VSMCs, and, in addition, silencing $PLC-{\beta}3$ significantly diminished the $PGF_{2{\alpha}}$-induced proliferation and migration of VSMCs. Given these results, we suggest that $PGF_{2{\alpha}}$ plays a crucial role in the proliferation and migration of VSMCs, and activation of $PLC-{\beta}3$ could be involved in their $PGF_{2{\alpha}}$-dependent migration.

A Monoacyldigalactosyl Glycerol from the Green Alga Enteromorpha prolifera

  • Kim, Ju-Sun;Shim, Sang-Hee;Lee, Sang-Hyun;Chae, Sung-Wook;Han, Sang-Jun;Kang, Sam-Sik;Lee, Yeon-Sil;Jung, Sang-Hoon;Shin, Kuk-Hyun
    • Natural Product Sciences
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    • v.10 no.6
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    • pp.341-343
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    • 2004
  • A monoacyldigalactosyl glycerol was isolated from the $CH_2Cl_2$ soluble fraction of the MeOH extract from the green alga Enteromorpha prolifera. The structure was established as $1-O-palmitoyl-3-O-[{\alpha}-D-galactopyranosyl(1{\rightarrow}6)-{\beta}-D-galactopyranosyl]-sn-glycerol$ (1) by chemical and spectroscopic methods.

Determination of Heterocyclic Amines and Acrylamide in Agricultural Products with Liquid Chromatography-Tandem Mass Spectrometry

  • Lee, Kyung-Jun;Lee, Gae-Ho;Kim, HaeSol;Oh, Min-Seok;Chu, Seok;Hwang, In Ju;Lee, Jee-yeon;Choi, Ari;Kim, Cho-il;Park, Hyun-Mee
    • Toxicological Research
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    • v.31 no.3
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    • pp.255-264
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    • 2015
  • Heterocyclic amines (HCAs) and acrylamide are unintended hazardous substances generated by heating or processing of foods and are known as carcinogenic and mutagenic agents by the animal experiments. A simple method was established for a rapid and accurate determination of 12 types of HCAs (IQ, MeIQ, Glu-P-1, Glu-P-2, MeIQx, Trp-P-1, Trp-P-2, PhIP, $A{\alpha}C$, $MeA{\alpha}C$, Harman and Norharman) and acrylamide in three food matrices (non-fat liquid, non-fat solid and fat solid) by isotope dilution liquid chromatography-tandem mass spectrometry (LC-MS/MS). In every sample, a mixture of internal standards including $IQ-d_3$, $MeIQx-d_3$, $PhIP-d_3$, $Trp-P-2-^{13}C_2-^{15}N$ and $MeA{\alpha}C-d_3$ was spiked for quantification of HCAs and $^{13}C_3$-acrylamide was also spiked for the analysis of acrylamide. HCAs and acrylamide in sample were extracted with acetonitrile and water, respectively, and then two solid-phase extraction cartridges, ChemElut: HLB for HCAs and Accucat: HLB for acrylamide, were used for efficiently removing interferences such as pigment, lipid, polar, nonpolar and ionic compounds. Established method was validated in terms of recovery, accuracy, precision, limit of detection, limit of quantitation, and linearity. This method showed good precision (RSD < 20%), accuracy (71.8~119.1%) and recovery (66.0~118.9%). The detection limits were < 3.1 ng/g for all analytes. The correlation coefficients for all the HCAs and acrylamide were > 0.995, showing excellent linearity. These methods for the detection of HCAs and acrylamide by LC-MS/MS were applied to real samples and were successfully used for quantitative monitoring in the total diet study and this can be applied to risk assessment in various food matrices.

Anti-Inflammatory Activity of Compounds from the Whole Plant of Patrinia saniculaefolia

  • An, Ren-Bo;Na, Min-Kyun;Min, Byung-Sun;Chang, Hyeun-Wook;Bae, Ki-Hwan
    • Natural Product Sciences
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    • v.17 no.2
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    • pp.90-94
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    • 2011
  • An in vitro bioassay-guide revealed that the methanol (MeOH) extract of the whole plant of Patrinia saniculaefolia (Valerianaceae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity by assessing their effects on the production of prostaglandin $D_2$ ($PGD_2$) and leukotriene $C_4$ ($LTC_4$) in mouse bone marrow-derived mast cells (BMMCs). Phytochemical study of the MeOH extract of this plant led to the isolation of twelve compounds; ${\beta}$-farnesene (1), squalene (2), nardostachin (3), patridoid I (4), patridoid II (5), patridoid II-A (6), oleanolic acid (7), oleanonic acid (8), 23-hydroxyursolic acid (9), oleanolic acid 3-O-${\alpha}$-L-arabinopyranoside (10), oleanolic acid 3-O-${\beta}$-D-glucopyranoside (11), oleanolic acid 3-O-[${\beta}$-D-xylopyranosyl-(1${\rightarrow}$3)-${\beta}$-D-(6-O-butyl)glucuronopyranoside] (12). Among the compounds, 4 and 5 strongly inhibited both the COX-2-dependent $PGD_2$ generation with $IC_{50}$ values of 8.7 and 13.6 ${\mu}M$, respectively, and the generation of $LTC_4$ in the 5-LOX dependent phase with $IC_{50}$ values of 41.7 and 46.9 ${\mu}M$, respectively, which suggest that the anti-inflammatory activity of P. saniculaefolia might occur in part via the inhibition of both $PGD_2$ and $LTC_4$ generation by 4 and 5.

Pytochemical Constituents of the Aerial Parts from Solidago virga-aurea var. gigantea

  • Choi, Sang-Zin;Choi, Sang-Un;Lee, Kang-Ro
    • Archives of Pharmacal Research
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    • v.27 no.2
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    • pp.164-168
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    • 2004
  • The chromatographic separation of the MeOH extract of the aerial parts of Solidago virga-aurea var. gigantea $M_{IQ}$ . (Compositae) led to the isolation of six terpenoids and four phenolic compounds, trans-phytol (1), ent-germacra-4(15),5,10(14 )-trien-1$\alpha$-ol (2), $\beta$-amyrin acetate (3), ent-germacra-4(15),5,10(14)-trien-1$\beta$-ol (4), $\beta$-dictyopterol (5), oleanolic acid (6), kaempferol (7), kaempferol-3-O-rutinoside (8), methyl 3,5-di-O-caffeoyl quinate (9), and 3,5-di-O-caffeoyl quinic acid (10). Their structures were established by chemical and spectroscopic methods. Compounds 4, 5, and 10 showed moderate cytotoxicity against five cultured human tumor cell lines in vitro with its E $D_{50}$ values ranging from 1.52∼18.57 $\mu\textrm{g}$/mL.L.

Effects of osteotropic hormones on the nitric oxide production in culture of ROS17/12.8 cells (뼈흡수유도호르몬이 ROS17/2.8세포로부터 Nitric Oxide 형성에 미치는 영향)

  • Ko Seon-Yle;Kim Min-Sung;Han Won-Jeong;Kim Se-Won;Kim Jung-Keun
    • Imaging Science in Dentistry
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    • v.35 no.3
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    • pp.127-131
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    • 2005
  • Purpose : We performed the present study to investigate whether osteotropic hormomes play roles on the nitric oxide (NO) production in culture of ROS 17/12.8 osteoblastic cells. Materials and Methods : The osteoblastic cell line ROS17/2.8 cells were cultured In F12 medium supplemented with $5\%$ fetal bovine serum (FBS) at $37^{\circ}C$ in a humidified atmosphere of $5\%\;CO_2$ in air. ROS17/2.8 cells were plated in 96-well plates at a density of $2-3\times10^3cells/well$ and grown to confluence. Then the cells were pretreated with osteotropic hormones (parathyroid hormone (PTH) 20-500 ng/mL, 1, 25-dihydroxycholecalciferol $(1,\;25[OH]_2D_3)$ 1-100 nM; prostaglandin $E_2 (PGE_2)$ 20-500 ng/mL in the medium supplemented with $0.4\%$ FBS for 72 hours and the cells were treated with cytokines $(TNF{\alpha}\;and\;IFN{\gamma})$ in phenol red-free F12 medium for an additional 48 hours. NO synthesis was assessed by measuring the nitrite anion concentration, the reaction product of NO, in the cell culture medium using Griess reagent. Results : PTH and $1,\;25[OH]_2D_3$ pretreatment induced a significant increase in NO production in the presence of $TNF{\alpha}\;and\;IFN{\gamma}.\;PGE_2$ slightly induced NO production compared to the control group. But, $PGE_2$ pretreatment did not affect in NO production in the presence of $TNF{\alpha}\;and\;IFN{\gamma}$. Conclusions : These results suggest that the actions of osteotropic hormones In bone metabolism may be partially mediated by NO in the presence of cytokines.

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