• 제목/요약/키워드: $1{\alpha}-(OH)D_3$

검색결과 196건 처리시간 0.044초

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

  • 이희정;이범종;이동석;서영완
    • 한국생물공학회:학술대회논문집
    • /
    • 한국생물공학회 2003년도 생물공학의 동향(XII)
    • /
    • pp.668-672
    • /
    • 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$(IC_{50}=6.59{\mu}g/ml)$.

  • PDF

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

  • 신경훈;이재호;류근석;지경엽;박수남;김재일;조인식;김한영
    • 대한화장품학회지
    • /
    • 제36권3호
    • /
    • pp.233-240
    • /
    • 2010
  • 신규 미백 소재 개발을 위하여 tyrosinase의 활성을 억제하는 천연물과, alpha-melanocyte stimulating hormone ($\alpha$-MSH)을 저해하는 펩타이드를 결합한 소재를 고체상 합성법으로 제조하였다[1,2]. Tyrosinase 활성 억제 효능이 있는 천연유래물질을 기존 연구를 바탕으로 선정하였으며, 이중에서 상업화 된 물질 17종에 대해 Mushroom Tyrosinase 활성 억제 효과를 측정하여, 그 중 caffeic acid, coumaric acid를 선별하였다. 펩타이드는 $\alpha$-MSH 분비를 억제하며, tyrosinase활성을 억제하는 것으로 알려진 melanostatin을 선정하였으며[3-5], PLG-$NH_2$ (Proline-Leucine-Glycine-$NH_2$) 중에서 유도체화 수율의 저하 원인으로 예상되는 Proline (Pro)의 서열을 다른 아미노산으로 변경하면서 선별된 천연물인 coumaric acid와 caffeic acid에 도입하였다. 또한 최종물질의 원가를 고려하여 acid-amide 형태를 acid형태로 전환한 유도체를 합성하였다. 이들 펩타이드 유도체들에 대해서 B16F1 melanoma cell에서의 멜라닌 생성 억제 효능을 평가하여 유도체화된 물질이 기존의 천연유래물질이나 펩타이드에 비하여 높은 저해효과를 가지는 것을 확인하였다.

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

  • 우경완;심미옥;박종일;김민석;서원세;조현우;권학철;박종철;이강노
    • 생약학회지
    • /
    • 제47권3호
    • /
    • pp.204-210
    • /
    • 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.

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

  • 이정환;손영창
    • 한국수산과학회지
    • /
    • 제48권6호
    • /
    • pp.913-919
    • /
    • 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.

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

  • 강기웅;오준영;이윤한;이혜선;진서연;배순식
    • 생명과학회지
    • /
    • 제28권12호
    • /
    • pp.1516-1522
    • /
    • 2018
  • 죽상동맥경화는 대동맥의 만성염증에 의해 주로 발병되는 폐쇄동맥질환이다. 혈관평활근세포의 증식 및 이동은 죽상동맥경화 발병의 주된 병리적 반응이다. 본 연구에서는 죽상동맥경화 발병기전을 유도하는 표적 염증반응 물질의 탐색 및 이들에 의한 신호전달 기전을 연구하였다. 혈관평활근세포의 증식 및 이동은 prostaglandin $F_{2{\alpha}}$ ($PGF_{2{\alpha}}$)에 의해 의미 있게 증가하였으나 tumor necrosis factor ${\alpha}$ ($TNF{\alpha}$)에 의해서는 증가하지 않았다. Prostacyclin $I_2$ ($PGI_2$)는 혈관평활근세포의 증식은 촉진시켰으나 이동은 오히려 억제하였다. prostaglandin $D_2$ ($PGD_2$) 및 prostaglandin $E_2$ ($PGE_2$)는 혈관평활근세포의 증식을 촉진시켰으나 이동에는 영향을 미치지 않았다. $PGF_{2{\alpha}}$는 용량 의존적으로 혈관평활근세포의 증식 및 이동을 촉진시켰고 EC50는 약 $0.1{\mu}M$로 관찰되었다. 혈관평활근세포에서 phospholipase $C-{\beta}3$ ($PLC-{\beta}3$) 아형의 발현은 매우 높았으나 $PLC-{\beta}1$, $PLC-{\beta}2$, 및 $PLC-{\beta}4$의 발현은 관찰되지 않았다. U73122 처리를 통해 PLC의 활성을 억제하면 $PGF_{2{\alpha}}$에 의한 혈관평활근세포의 이동이 억제되었다. 또한 $PLC-{\beta}3$의 발현을 억제하면 $PGF_{2{\alpha}}$에 의한 혈관평활근세포의 증식 및 이동이 억제되었다. 이러한 결과들을 바탕으로 $PGF_{2{\alpha}}$ 는 혈관평활근세포의 증식 및 이동에 중요한 역할을 수행하고, 여기에는 $PLC-{\beta}3$가 필수적인 역할을 담당하고 있음을 제안한다.

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
    • /
    • 제10권6호
    • /
    • pp.341-343
    • /
    • 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
    • /
    • 제31권3호
    • /
    • pp.255-264
    • /
    • 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
    • /
    • 제17권2호
    • /
    • pp.90-94
    • /
    • 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
    • /
    • 제27권2호
    • /
    • pp.164-168
    • /
    • 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.

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

  • 고선일;김민성;한원정;김세원;김정근
    • Imaging Science in Dentistry
    • /
    • 제35권3호
    • /
    • pp.127-131
    • /
    • 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.

  • PDF