• 제목/요약/키워드: sub-compounds

검색결과 990건 처리시간 0.03초

생약의 류코트리엔 $B_4$ 수용체결합 저해작용 검색 (Screening of Leukotriene $B_4$ Receptor Antagonist Activity from the Herbal Drugs)

  • 이화진;류재하
    • 생약학회지
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    • 제31권3호
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    • pp.273-279
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    • 2000
  • Leukotriene $B_4\;(LTB_4)$ is a pro-inflammatory mediator synthesized in myeloid cells from arachidonic acid. Elevated levels of $LTB_4$ have been found in a number of inflammatory diseases and levels are related to disease activity in some of these. Because $LTB_4$ interacts with cells through specific cell surface receptors, $LTB_4$ receptor blockade is the most specific approach to reduce the pathogenic role of $LTB_4$. In order to find $LTB_4$ receptor antagonist from plants, we screened the $LTB_4$ receptor antagonistic activity of the methanol extract and solvent fractions of herbal drugs. The ability of samples to inhibit specific binding of $[^3H]-LTB_4$ to human peripheral neutrophils was used as assay to evaluate the antagonistic activity of plant materials. Among the tested methanol extracts of herbal drugs, Mori Radicis Cortex, Perillae Semen, Armeniacae Semen and Sophorae subprostratae Radix showed potent inhibitory activity above 70% at the concentration of $100\;{mu}g/ml$. The inhibitory activities of $LTB_4$ binding to human neutrophils were evaluated for several solvent fractions at three different concentrations. Especially, hexane soluble fractions of Anemarrhenae Rhizoma and Embeliae Radix, and ethyl acetate soluble fractions of Aristolochiae Fructus, Magnoliae Cortex and Zingiberis Rhizoma crudus showed moderate activity at $25\;{mu}g/ml$. These fractions were promising candidates for the study of the activity-guided chromatographic purification of active compounds. Silica gel column chromatography of hexane soluble fractions of Anemarrhenae Rhizoma and Embeliae Radix gave very active sub-fractions, AA-4 and ES-4, and their inhibition activities of $LTB_4$ binding to human neutrophil at $30\;{mu}g/ml$ were 78% and 62%, respectively. From these results we could anticipate new $LTB_4$ receptor antagonist from herbal drugs, and the block of $LTB_4$ effects may provide beneficial in neutrophil mediated diseases such as inflammation and bronchial asthma.

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Tranquilizer-like Effects of Sanjoinine A: Possible GABA/Benzodiazepine Receptors Complex Involvement

  • Ma, Yu-An;Eun, Jae-Soon;Oh, Ki-Wan
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 2008년도 Proceedings of the Convention
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    • pp.119-142
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    • 2008
  • Zizyphi Spinosi Semen (ZSS) has been widely used for the treatment of anxiety and insomnia in Korea and China. This experiment was performed to know whether sanjoinine A, one of major alkaloid compounds of ZSS has anxiolytic and hypnotic effects through the GABAergic systems. Our results showed that administration of sanjoinine A increased open arm entries and spent time in open arm in the elevated plus-maze and increased head dips in hole board test. Different from traditional anxiolytic, diazepam, sanjoinine A itself did not decrease locomotor activity and strength level in mice. Furthermore, Sanjoinine A (0.5-2.0 mg/kg) prolonged sleeping time and reduced sleeping latency induced by pentobarbital in a dose-dependent manner similar to muscimol, a $GABA_A$ receptor agonist. Sanjoinine A (0.25-1.0 mg/kg) also increased sleeping rate and sleeping time in the combined administration at the sub-hypnotic dose of pentobarbital and showed synergic effects with muscimol in potentiating sleeping onset and enhancing sleeping time induced by pentobarbital. However, sanjoinine A itself did not induce sleeping at the higher dose. In addition, both of sanjoinine A and pentobarbital increased chloride influx in primary cultured cerebellar granule cells. Sanjoinine A decreased the $GABA_A$ receptor ${\alpha}$-subunit expression and increased ${\gamma}$-subunit expression, and had no effects on abundance of ${\beta}$-subunit in primary cultured cerebellar granule cells, showing different expression of subunits from pentobarbital. In conclusion, sanjoinine A shows anxiolytic-like effects and augments pentabarbital-induced sleeping behaviors through the modification of GABAergic systems. [This work was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD) (The Regional Research Universities Program/Center for Healthcare Technology Development)].

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카르노스산에 의한 화이트소시지의 항산화 및 항균 효과 (Antioxidant and Antibacterial Effects of Carnosic Acid on White Sausage)

  • 이조원;최일신;김완섭
    • 한국유기농업학회지
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    • 제21권2호
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    • pp.219-232
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    • 2013
  • 로즈마리의 주요성분으로는 carnosic acid, carnosol, rosmarinic acid, ursolic acid 등의 폴리페놀(polyphenolic)로 구성되어 있다. 식물기원의 페놀혼합물은 항산화 작용과 항균작용을 포함한 유용한 기능과 영양적인 효과에 주목을 끌고 있다. 본 연구는 로즈마리 추출물의 하나인 카르노스산을 화이트소시지 원료에 첨가한 후 실온 저장기간 동안 pH, TBARS, VBN, 전자공여능 및 총균수의 변화를 조사하였다. 카르노스산의 첨가는 무첨가구인 대조구에 비해 낮은 pH, TBARS값, 그리고 VBN값을 보여 주었으며, 높은 항산화 작용과 항균작용을 나타내었다. 이들의 활성은 카르노스산의 농도가 높을수록 증가하였다. 또한 카르노스산의 병원성균에 대한 항균활성을 측정한 결과, 두 병원성균(E. coli KCCM 11234와 S. enteritidis KCCM 12021)에 대하여 강한 항균활성을 보여주었다. 따라서 화이트소시지에 있어서 카르노스산은 천연보존제로서 충분히 이용 가능한 결과를 나타내었다.

대도시 및 주변 교외지역의 대기 중 휘발성 유기화합물 농도 비교에 관한 연구 (A Study on the Comparison of Atmospheric Concentrations of Volatile Organic Compounds in a Large Urban Area and a Sub-Urban Area)

  • 박지혜;서영교;백성옥
    • 한국대기환경학회지
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    • 제22권6호
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    • pp.767-778
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    • 2006
  • This study was carried out to evaluate the temporal variations of VOCs at an urban site, and to compare the concentrations of VOCs at an urban site in Daegu with those at a suburban site in Gyeongsan. Three hourly VOC samples in the ambient air were collected using a sequential tube sampler (STS 25, Perkin Elmer) throughout two weeks during May and July representing spring and summer seasons, respectively. The VOC concentrations were determined by an automatic thermal desorption apparatus with GC/MS analysis. A total of 12 VOCs of environmental concern were determined, which are chloroform, benzene, trichloroethylene, toluene, tetra-chloroethylene, ethylbenzene, m+p-xylenes, o-xylene, styrene, 1,3,5- and 1,2,4-trimethylbenzenes. Among 12 target VOCs, the most abundant compound appeared to be toluene, being followed by xylenes. The mean concentrations at the urbn site were 1.2 pub for benzene and 20.4 ppb for toluene (n=221) while the mean levels at the suburban site were 0.9 ppb and 4.3 ppb for benzene and toluene (n=96), respectively. The urban site concentrations were typically several-fold higher than those measured at the suburban site. It was found that general trends of VOC levels were significantly dependent on traffic conditions at the sampling site since VOC concentrations were at their maximum during rush hours, i.e. $9{\sim}12a.m$ and $6{\sim}9p.m$. Statistical investigations were conducted to investigate any significant relationships between VOC concentrations and affecting factors. Calculated correlation coefficients among VOCs were positively significant at a level of 0.05 in most cases. Increased concentrations of toluene in the urban site were estimated to reflect the effect of large industrial sources, mainly from textile industry.

선복화(旋覆花)의 휘발성(揮發性) 성분(成分)에 관(關)한 연구(硏究) (Studies on the volatile components of Inulae flos(Inula britannica var. chinensis REGEL))

  • 선우선;김형섭;변근수
    • Applied Biological Chemistry
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    • 제34권4호
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    • pp.312-317
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    • 1991
  • 선복화(旋覆花)의 휘발성(揮發性) 성분(成分)을 동정(同定)하기 위하여 국내산(國內産) 및 중국산(中國産)을 시료(試料)로 사용(使用)하였다. 휘발성(揮發性) 성분(成分) 포집(捕集)은 SDE 방법(方法)을 사용(使用)하여 건조(乾燥)된 시료(試料) 100g중 국내산(國內産) 155.3 mg 중국산(中國産) 101.6 mg을 얻었다. 포집(捕集)된 휘발성(揮發性) 성분(成分)을 GC 및 GC/MS를 이용(利用)하여 hydrocarbon 류(類) 10, aldehyde 류(類) 7, alcohol 류(類) 18, ketone 류(類) 3, ester 류(類) 5, acid 류(類) 13 및 miscellaneous compounds 6 성분(成分)으로 모두 62 성분(成分)을 동정(同定)하였다. 또한, 이들 성분(成分)을 좀 더 세밀(細密)히 검토(檢討)코자 silica gel column chromatography에 의해 용출용매(溶出溶媒)의 극성(極性)을 변화(變化)시킴으로 성분조성(成分組成)을 세분(細分)하였다. 그 결과(結果) 국내산(國內産) 선복화(旋覆花)의 휘발성(揮發成) 성분중(成分中) 탄화수소(炭化水素) 화합물(化合物) 분획(分劃)이 16.85% 함산소화합물(含酸素化合物) 분획(分劃)이 83.15%이며, 중국산(中國産) 선복화(旋覆花)는 탄화수소(炭化水素) 화합물(化合物) 분획(分劃)이 23.46% 함산소화합물(含酸素化合物) 분획(分劃)이 76.53%를 함유(含有)하고 있다.

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Halon 1301과 Halon 대체 소화약제를 기포제로 이용한 포 소화약제에 대한 연구 (A Study On The Application Of Foam Extinfuishing Agent By Using Halon 1301 And Halon Alternatives)

  • 정기창;임성묵;이창섭;강영구;김홍
    • 한국화재소방학회논문지
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    • 제10권3호
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    • pp.29-40
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    • 1996
  • 포 소화약제는 물보다 비중이 가벼운 액체 가연물 또는 입체면이 많은 건물에서 포 수용액을 팽창 발포시켜 대상물을 덮어 씌우거나 봉쇄해서 질식소화 시킬 수 있다. 포 소화약제로 소화성능이 탁월한 수성막포(AFFF) 소화약제를 노즐에 의해 공기와의 혼합으로 포를 형성하는 기존의 방법과 다른 방법으로 본 연구에서 는 Halon 1301 및 Halon 대체 소화약제를 기포제로 사용하여 소화성능과 팽창비를 향상시킨 소화약제를 개발하게 되었다. 개발한 Halon 1301과 Halon대체 소화약제를 기포제로 사용한 수성막포 소화약제는 적은 양의 수성막포 수용액으로 많은 양의 포를 형성하므로 휴대용 포 소화기 또는 포 소화설비 등에 유용하게 사용할 수 있다.

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Identification of 3'-Hydroxymelanetin and Liquiritigenin as Akt Protein Kinase Inhibitors

  • Yang Hye-Young;Lee Hong-Sub;Ko Jong-Hee;Yeon Seung-Woo;Kim Tae-Yong;Hwang Bang-Yeon;Kang Sang-Sun;Chun Jae-Sun;Hong Soon-Kwang
    • Journal of Microbiology and Biotechnology
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    • 제16권9호
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    • pp.1384-1391
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    • 2006
  • The signal transduction system is one of the most important devices involved in maintaining life, and many protein kinases are included in the cellular signal transduction system. Finding a protein kinase inhibitor is very valuable, as it can be used to study cell biology and applied to pharmaceuticals. For the efficient and rapid screening of protein kinase inhibitors, two assay systems were combined; the nonradioactive protein kinase assay system that uses an FITC-labeled IRS-2 peptide and the cell-based paper disc assay system that uses Streptomyces griseus as the indicator strain. Among 330 kinds of herb extracts tested, the extract of Dalbergia odorifera exhibited the strongest inhibitory activity in the two assay systems and was selected for further isolation. Based on solvent extraction and many steps of chromatography, seven compounds were finally separated to homogeneity and their structures determined by $^{1}H$ and $^{13}C$ NMR spectroscopies. Four were to be flavonoids and identified as butin ($C_{15}H_{12}O_5$, Mw=272.07), 3'-hydroxymelanetin ($C_{16}H_{12}O_6$, Mw=300.06), liquiritigenin ($C_{15}H_{12}O_4$, Mw=256.07), and 2'-hydroxyformononetin ($C_{16}H_{12}O_{5}$, Mw=284.07). 3'-Hydroxymelanetin inhibited the phosphorylation of the GSK3 protein by Akt to 37% at a concentration of $10{\mu}g/ml$ and showed the strongest cytotoxicity ($ED_{50}<50{\mu}g/ml$) against the human cancer cell line HCT116. Under the same conditions, liquiritigenin also inhibited the phosphorylation of GSK3 by Akt to 26%, and its cytotoxicity against the HCT116 cell line was lower than $100{\mu}g/ml$.

N-[4-Cyano-2-fluoro-5-(substituted)phenyl]-3,4,5,6-tetrahydrophthalimide 유도체의 합성과 제초활성 (Synthesis and herbicidal activities of N-[4-Cyano-2-fluoro-5-(substituted)phenyl]-3,4,5,6-tetrahydrophthalimide)

  • 류재욱;정근회;고영관;우재춘;구동완;김태준;최정섭;박채현;김대황
    • 농약과학회지
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    • 제9권1호
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    • pp.108-111
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    • 2005
  • N-[4-Cyano-2-fluoro-5-(2-pyrimidinyloxy, 2-benzyloxy 혹은 2-pyridinyloxy)phenyl]-3,4,5,6-tetrahyophtha-limide 유도체를 합성하였고, 밭 조건에서 토양 및 경엽처리후의 제초활성을 온실에서 조사하였다. 이 화합물들의 제초효과는 토양처리보다 경엽처리에서 강하였으며, 광엽 잡초에 대한 제초활성이 화본과 잡초에 대한 활성보다 우수하였다. N-[(4-cyano-2-fluoro-5-(2-pyrimidinyloxy)phenyl]-3,4,5,6-tetrahydrophthalimide가 가장 강한 제초활성을 나타내었을 뿐 만아니라 60 g/ha 농도의 토양처리에서 옥수수에 비교적 안전하였다.

Effects of dihydrocubebin, a lignan isolated from Indonesian plant Piper cubeba, on the histamine release from rat mast cells

  • Nugroho, Agung Endro;Wahyono, Wahyono;Wahyuono, Subagus;Maeyama, Kazutaka
    • Advances in Traditional Medicine
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    • 제10권3호
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    • pp.200-207
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    • 2010
  • The fruits of Piper cubeba L. are used traditionally to treat respiratory disorders in Indonesia. In order to determine the compounds responsible for this activity, the fruits were extracted with nhexane followed by ethanol to give n-hexane and ethanol extracts. Based on tracheospasmolytic assay on these two extracts, the n-hexane extract was more active to inhibit trachea contraction than that of ethanol extract. Upon bioassay guided isolation of the n-hexane extract, a tracheospasmolytic active compound was isolated and identified as dihydrocubebin [(3,4),(3',4')-bis-methylenedioxy-9,9'dihydroxylignan] $(\underline{1})$. Compound $\underline{1}$ was tested further for its ability to inhibit histamine released from mast cells, using rat basophilic leukemia (RBL-2H3) cell line and rat peritoneal mast cells RPMCs) as models; and $DNP_{24}$-BSA, thapsigargin, ionomycin, compound 48/80 and PMA were used as inducers for histamine released from mast cell. The test result showed that $\underline{1}$ inhibited histamine release from RBL-2H3 cells induced by $DNP_{24}$-BSA, thapsigargin and ionomycin. In addition, $\underline{1}$ suppressed histamine release from RPMC induced by either thapsigargin or ionomycin. However, $\underline{1}$ did not inhibit histamine release from RPMC induced by either compound 48/80 or combination PMA-sub optimum dose of ionomycin. Therefore, it was concluded that the inhibitory effects of $\underline{1}$ on the histamine released from mast cells may involve mechanisms related to intracellular $Ca^{2+}$ signaling events or downstream processes of intracellular $Ca^{2+}$ signaling in mast cells.

털두꺼비하늘소(Moechotypa diphysis)로에 대한 18종 식물정유와 주요성분의 훈증효과 (Fumigant Toxicity of 18 Essential oils and Their Major Compounds against Adult Oak Longicorn Beetle, Moechotypa diphysis (Coleoptera: Cerambycidae))

  • 김주섭;서동규;장선아;한주환;김영재;김길하
    • 한국응용곤충학회지
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    • 제45권2호
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    • pp.189-194
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    • 2006
  • 털두꺼비하늘소(Moechotypa diphysis) 성충에 대한 18종 식물정유의 훈증독성을 조사하였다. 그들 중 10 $\mu\ell/\ell$ (공기)의 농도에서 eucalyptus oil, rosemary oil, 그리고 pennyroyal oil은 100%, sage oil은 85%의 살충활성을 나타내었다. 4종 정유의 치사속도를 조사한 결과, eucalyptus oil과 rosemary oil이 처리 후 6시간 이내에 100%의 살충률을 나타내었다. 각 정유에 대한 주요 구성성분을 GC와 GC/MS로 분석한 결과, eucalyptus oil, rosemary oil, sage oil의 주성분인 1,8-cineole과 sage oil의 또 다른 주성분인 thujone과 pennyroyal의 주성분인 pulegone 모두 20 $\mu\ell/\ell$(공기)의 농도에서 100%의 살충효과를 나타내었다.