• Title/Summary/Keyword: Natural ester

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Analgesic, Anti-inflammatory and Antiviral Effects of Melandrin Derivatives (Melandrin유도체의 진통 소염 및 항바이러스 효과)

  • Lim, Jung-Ki;Lee, Eun-Bang;Woo, Won-Sik;Lee, Kang-Ro;Lee, Yeong-Sun;Ma, Eun-Sook
    • YAKHAK HOEJI
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    • v.38 no.3
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    • pp.345-350
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    • 1994
  • Fourteen melandrin derivatives(I-XIV) were investigated on analgesic, anti-inflammatory and antiviral activities . Compound I [N-(p-hydroxybenzoyl)-5-hydroxyanthranilic acid methvl ester], Xll [N-(2-phenoxypropionyl)-5-hydroxy anthranilic acid propyl ester and XIV [N-(2-phenoxypropionyl)-5-hydroxyanthranilic acid exhibited analgesic activity in tail pressure and Randall-Selitto method. But no anti-inflammatory activity was shown. Compound I exhibited weak antiviral activity on Herpes simplex virus type I F strain by virus-induced cytopathic effect(CPE) assay and it's selectivity index(Sl) was 8.17.

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Reduced Anti-inflammatory Activity of Acetylsalicylic Acid Maltol Ester, Aspalatone

  • Han, Byung-Hoon;Suh, Dae-Yeon;Yang, Hyun-Ok;Lee, Song-Jin;Kim, Hyun-Pyo
    • Archives of Pharmacal Research
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    • v.17 no.3
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    • pp.166-169
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    • 1994
  • The anti-inflammatory activity of acetylsalicylic acid maltol ester (aspalatone), a potential anti-thombotic agent, was studied using the several experimental animal models of inflammation. By oral administration, aspalatone was found to possess the weak anti-inflammatory activity in models of an acute inflammation, in which aspalatone showed approximately one-third to one-fourth of the anti-inflammatory activity of aspirin. Aspalatone (200 mg/kg/day) and aspirin (50 mg/kg/day), however, did not show the inhibitory activity against granuloma fomation and adjuvant-induced arthritis.

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Antiinflammatory Constituents from the Roots of Smilax bockii warb.

  • Xu Jing;Li Xian;Zhang Peng;Li Zhan-Lin;Wang Yi
    • Archives of Pharmacal Research
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    • v.28 no.4
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    • pp.395-399
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    • 2005
  • From $70\%$ ethanol extract of the roots of Smilax bockii warb., seven flavonoids, kaempferol (1), $kaempferol-7-O-\beta-D-glucopyranoside$ (2), quercetin (3), isorhamnetin (4), (+)-dihydro­kaempferol (5), engeletin (6), isoengeletin (7), and $n-butyl-\beta-D-fructopyranoside$ (8), caffeic acid n-butyl ester (9) were isolated and identified by means of chemical and spectroscopic. Compounds 2, 4, and 6-9 were isolated for the first time from the roots of S. bockii and compounds 2, 8, and 9 were firstly isolated from the genus Smilax. In addition, using the SEAP (Secreted alkaline phosphatase) assay system, we investigated the in vitro anti-inflammatory activity of the $70\%$ ethanol extract of the roots of S. bockii, which showed moderate activity in inhibiting $TNF-\alpha-induced NF-{\kappa}B$ activation with an $IC_{50}$ value of $166.6 {\mu}g/mL$.

Anti-inflammatory Effect of Achyranthoside E Dimethyl Ester in LPS-stimulated RAW 264.7 Cells (LPS로 인한 RAW 264.7 세포의 염증반응에 미치는 achyranthoside E dimethyl ester의 효과)

  • Bang, Soo Young;Kim, Ji-Hee;Moon, Hyung-In;Kim, Young Hee
    • Journal of Life Science
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    • v.23 no.6
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    • pp.736-742
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    • 2013
  • Achyranthoside E dimethyl ester (AEDE) is an oleanolic acid glycoside from Achyranthes japonica. In this study, we investigated the effects of AEDE on nitric oxide (NO) production and underlying molecular mechanisms in lipopolysaccharide (LPS)-stimulated macrophages. AEDE inhibited LPS-induced NO secretion as well as inducible NO synthase (iNOS) expression, without affecting cell viability. Further study demonstrated that AEDE induced heme oxygenase-1 (HO-1) gene expression. In addition, the inhibitory effects of AEDE on iNOS expression were abrogated by small interfering RNA-mediated knock-down of HO-1. Moreover, AEDE induced nuclear translocation of nuclear factor E2-related factor 2 (Nrf2), a transcription factor that regulates HO-1 expression. AEDE-induced expression of HO-1 was inhibited by inhibitors of phosphatidylinositol 3-kinase (PI-3K) and extracellular signal regulated kinase (ERK1/2). AEDE phosphorylated Akt and ERK1/2 as well. Therefore, these results suggest that AEDE suppresses the production of pro-inflammatory mediator such as NO by inducing HO-1 expression via PI-3K/Akt/ERK-Nrf2 signaling. These findings provide the scientific rationale for anti-inflammatory therapeutic use of AEDE.

Effects of Achyranthoside C Dimethyl Ester on Heme Oxygenase-1 Expression and NO Production (Heme Oxygenase-1 발현과 NO 생성에 미치는 Achyranthoside C Dimethyl Ester의 효과)

  • Bang, Soo Young;Song, Ji Su;Moon, Hyung-In;Kim, YoungHee
    • Journal of Life Science
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    • v.25 no.9
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    • pp.976-983
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    • 2015
  • Achyranthoside C dimethyl ester (ACDE) is an oleanolic acid glycoside from Achyranthes japonica which has been used in traditional medicine for the treatment of edema and arthritis. In this study, we investigated the anti-inflammatory effects of ACDE in RAW264.7 macrophages. ACDE significantly induced heme oxygenase-1 (HO-1) gene expression in RAW264.7 cells, while ACDE improved LPS-induced toxicity of cells. And ACDE induced nuclear translocation of nuclear factor E2-related factor 2 (Nrf2), a transcription factor that regulates HO-1 expression. Further study demonstrated that ACDE-induced expression of HO-1 was inhibited by inhibitors of phosphatidylinositol 3-kinase (PI-3K) (LY294002), c-Jun kinase (JNK) (SP600125), extracellular signal regulated kinase (ERK) (PD98059) and p38 kinase (SB203580). Moreover, ACDE phosphorylated Akt, JNK, ERK, and p38 MAPK. In addition, ACDE inhibited LPS-induced NO secretion as well as inducible NO synthase (iNOS) expression in a dose-dependent manner. The inhibitory effects of ACDE on iNOS expression were abrogated by small interfering RNA (siRNA)-mediated knock-down of HO-1. Therefore, these results suggest that ACDE suppresses the production of pro-inflammatory mediator such as NO by inducing HO-1 expression via PI-3K/Akt/MAPK-Nrf2 signaling pathway. These findings could help us to understand the active principle included in the roots of A. japonica and the molecular mechanisms underlying anti-inflammatory action of ACDE.

A Study on Structural Design of Natural Fiber Composites Automobile Body Panel Considering Impact Load (충돌 하중을 고려한 친환경 자연섬유 복합재 적용 자동차 차체 패널의 구조 설계 연구)

  • Park, Kilsu;Kong, Changduk;Park, Hyunbum
    • Composites Research
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    • v.28 no.5
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    • pp.291-296
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    • 2015
  • In this study, structural design and analysis of the automobile bonnet is performed. The flax/vinly ester composite material is applied for structural design. The Vacuum Assisted Resin Transfer Molding-Light (VARTML) manufacturing method is adopted for manufacturing the flax fiber composite bonnet. The VARTML is a manufacturing process that the resin is injected into the fly layered-up fibers enclosed by a rigid mold tool under vacuum. A series of flax/vinyl ester composite panels are manufactured, and several kinds of specimens cut out from the panels are tested to obtain mechanical performance data. Based on this, structural design of the automobile bonnet is performed.

Screening of Acyl-CoA:Cholesterol Acyltransferase(ACAT) Inhibitors from Natural Sources (천연자원으로부터 아실코에이: 콜레스테롤아실 전달효소 저해제의 탐색)

  • Kim, Mi-Kyung;Kwon, Byoung-Mog;Bae, Ki-Hwan;Choi, Don-Ha;Lee, Hak-Ju;Kim, Hong-Eun;Kim, Young-Kook
    • Korean Journal of Pharmacognosy
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    • v.30 no.4
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    • pp.384-396
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    • 1999
  • Acyl-CoA: Cholesterol Acyltransferase (ACAT) is a key enzyme responsible for cholesteryl ester formation in atherogenesis and in cholesterol absorption from the intestines. In addition under pathological conditions, formation and accumulation of cholesteryl ester as lipid droplets by ACAT within macrophages constitute a characteristic feature of early lesions of atherosclerotic plaques. ACAT inhibitors are expected to be effective for treatment of atherosclerosis and hypercholesterolemia. ACAT inhibitors of natural origin have been rarely reported. In our screening program for ACAT inhibitors, 303 plants were extracted with methanol or ethanol, and screened for the inhibitory activity against ACAT from the rat liver microsome. Extracts of 13 plants including Quercus aliena, Diospyros kaki, Platycarya strobilacea and Hibiscus syriacus inhibited more than 90% of ACAT activity and 43 samples in alcohol extracts such as Magnolia obovata and Panax ginseng also inhibited more than 70% of ACAT activity at a concentration of $100\;{\mu}g/ml$.

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Advances in Biodegradable Polymers for Drug Delivery Systems

  • Yong Kiel sung;Kim, Sung-Wan
    • Macromolecular Research
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    • v.8 no.5
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    • pp.199-208
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    • 2000
  • The recent development of biodegradable polymers for drug delivery system (DDS) has been investigated. The biodegradable polymers for DDS are mainly discussed in two categories: one category is natural biodegradable polymers such as polysaccharides, modified celluloses, poly(${\alpha}$-amino acid)s, modified proteins, and microbial biodegradable polymers; the other is synthetic biodegradable polymers such as poly(ester)s, poly(ortho ester)s, poly(phosphazene)s, poly(anhydride)s, poly(alkyl cyanoacrylate)s, and multiblock copolymers. The bioconjugate polymeric drug delivery systems have been also proposed for the design of biocompatible polymeric controlled drug delivery.

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