• 제목/요약/키워드: Active compounds

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Recent advances in pharmacologic study of anticancer natural products from medicinal plants in Morocco

  • Bnouham, Mohamed
    • 셀메드
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    • 제2권3호
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    • pp.22.1-22.9
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    • 2012
  • The aim of this study is to collate all available data on experiments reporting the antiproliferative, cytotoxic effects of plants and natural products in Morocco in the last two decades. A bibliographic investigation was carried out by analyzing recognized books and peer-reviewed papers, consulting worldwide accepted scientific databases (Scirus, Embase, HighWire, MEDLINE/PubMed, LILACS, Ovid, ScienceDirect, SciELO, Google Scholar). We used medical subject heading terms and the words 'anticancer', 'antiproliferative', 'antineoplastic', 'antitumoral', 'cytotoxic', 'Morocco', to identify relevant articles. Moroccan plants with attributed anti-cancer properties studied as plant extracts that have been evaluated for cytotoxic effects, antitumoral effects, plants with active compounds tested on cancer cell lines, and plants with active compounds that have been assayed on animal models were chosen for this research. In the present study, interest is focused on experimental research conducted on medicinal plants, particularly those which show antiproliferative or cytotoxic activities alongside bioactive components. A total of 20 plant species belonging to 12 families have been identified as active or promising sources of phytochemicals with antiproliferative properties. The plant families, which cover all the species studied in this field, are Lamiaceae (7 species) and Asteraceae (4 species); the most studied species being Argania spinosa (Sapotaceae) and Arisarum vulgare (Araceae), Thymus Genus (Labiateae) and Peganum harmala (Zygophyllaceae). Based on the search results, it is recommended to increase the number of experimental studies and to begin conducting clinical trials with Moroccan plants and their active compounds selected by in vitro and in vivo activities.

Characterization of the Aroma of Salt-fermented Anchovy Sauce Using Solid Phase Microextraction-Gas Chromatography-Olfactometry Based on Sample Dilution Analysis

  • Kim, Hyung-Joo;Baek, Hyung-Hee
    • Food Science and Biotechnology
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    • 제14권2호
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    • pp.238-241
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    • 2005
  • Aroma-active compounds were evaluated from salt-fermented anchovy sauce by solid phase microextraction-gas chromatography-olfactometry (SPME-GC-O) based on sample dilution analysis (SDA). SPME extract from carboxen/polydimethylsiloxane (CAR/PDMS) fiber was the most similar to the original odor of salt-fermented anchovy sauce used for this experiment, followed by divinylbenzene/CAR/PDMS (DVB/CAR/PDMS) fiber. Because salt-fermented anchovy sauce contains 23% NaCl, NaCl concentration of diluent was considered when salt-fermented anchovy sauce was serially diluted. Linear relationship between GC response and sample concentration was observed when diluted with 23% NaCl solution, whereas not observed when diluted with deodorized distilled water. Eleven and 16 aroma-active compounds were detected by SPME-GC-O based on SDA using CAR/PDMS and DVB/CAR/PDMS fibers, respectively. Butanoic acid and 3-methyl butanoic acid showed the highest ${\log}_2SD$ factors for CAR/PDMS and DVB/CAR/PDMS fibers. Dimethyl trisulfide, methional, trimethyl amine, 1-penten-3-ol, and acetic acid were also detected as potent aroma-active compounds.

Angiotensin 변환 효소 억제제인 Captopril 유도체들의 구조와 활성관계 연구: 수용액상의 분자동력학적 연구의 중요성 (Structure-Activity Relationships Study of Angiotensin Converting Enzyme Inhibitor Captopril Derivatives: Importance of Solution Moleculnr Dynamics Study)

  • 지명환;윤창노;진창배;박종세
    • Biomolecules & Therapeutics
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    • 제2권1호
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    • pp.34-38
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    • 1994
  • In order to investigate the structure-activity relationships of the stereoisomers of angiotensin converting enzyme inhibitors, captopril and its derivatives were selected as model compounds. In vitro enzymatic activities of them depend on the symmetry at the asymmetric carbons. Especially, the alanyl carbon should have the S configuration to be biologically active. But the demethylated captopril having the achiral carbon also shows the activity although it is less active than captopril. Seven stereoisomers of captopril and its derivatives were chosen and their acidic and ionic forms were used for molecular dynamics simulations. Four computer simulations were practiced for each model compound in order to obtain the good condition for simulation to explain the experimental structure-activity relationships. From the computer simulation results, relativistic movements of three well-known pharmacophoric sites, carboxylate carbon, carbonyl oxygen, and sulfur atoms, were analyzed. Good results were obtained from the aqueous solution molecular dynamics simulation with ionic forms of model compounds. Active model compounds have the pharmacophoric areas of 6.08 to 6.38 $\AA$$^2$and the similarity in the geometrical data. But inactive ones have the largely deviated values of 4.51 to 4.87 $\AA$$^2$from those of active ones.

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유근피 추출물의 radical 소거 활성 성분에 대한 LC-MS/MS 스크리닝 분석법 (LC-MS/MS Screening Method for Radical Scavenging Active Compounds in Extracts of Ulmus pumila Cortex)

  • 임도연;이경인
    • 생명과학회지
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    • 제30권11호
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    • pp.956-964
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    • 2020
  • 액체크로마토그래피 (liquid chromatography; LC) 시스템과 연동된 radical 소거 활성 측정 시스템은 식물 추출물과 같이 수많은 성분으로 구성된 시료 중의 radical 소거 활성 성분을 확인하는 유용한 도구이다. 이와 같은 시스템을 사용하여 항산화 활성 성분을 가지고 있는 생약재로 알려진 유근피의 추출물을 대상으로 DPPH와 ABTS radical 소거 활성을 측정한 후 확인된 소거 활성 성분에 대한 질량분석을 실시하여 procyanidin B2, procyanidin B3, catechin-7-O-β-D-apiofuranoside, catechin-5-O-β-D-apiofuranoside로 각각 추정되는 4가지 성분을 확인하였다. 추출물 시료들 간의 상대적인 함량 비교를 위해 4가지 성분에 대한 MRM mode 분석 조건을 설정하여 LC-MS/MS를 활용한 유근피 추출물 중 radical 소거 활성 성분의 함량 비교 가능성을 검토하였다. 95% 에탄올 추출물을 기준으로 산출한 상대적인 함량 비교 결과에서 추출 용매의 에탄올 농도가 높아지면 radical 소거 활성 성분들의 함량이 높아지는 것으로 나타났으며, 각 추출물의 radical 소거 활성 측정 결과와 마찬가지로 에탄올 농도 50% 이상의 추출물들에서 procyanidin B3로 추정된 성분을 제외한 3가지 성분의 함량 차이가 크게 나타나지 않음을 확인할 수 있었다. 이와 같은 결과에 각 추출물의 수율을 추가로 감안하여 50% 수준의 에탄올 농도가 유근피의 radical 소거 활성 성분 추출에 더 효과적임을 알 수 있었다. 이와 같은 활성 측정 및 분석 방법을 활용하게 되면 유근피 자체의 품질관리뿐만이 아니라 추출물을 활용하는 다양한 제품 개발 단계에서 기존의 LC-UV 검출기 profile 비교보다 활용도가 높은 방법이 될 수 있을 것으로 판단된다.

응축수를 이용한 냉각기의 냄새원인물질 평가방법 검토 (Examination about evaluation method of odor active compounds in evaporator by using condensed water)

  • 김선화;김경환;정영림;김만구;김재호;박하영;지용준
    • 분석과학
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    • 제20권5호
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    • pp.361-369
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    • 2007
  • 냉각기에서 방출되는 불쾌한 냄새는 실내 공기질을 저하시키는 주요 원인이다. 냄새문제를 해결하기 위해서는 냄새원인을 규명하여야 한다. 냉각기에서 냄새가 발생될 때 공기시료는 냄새강도는 약하고 순간적이어서 채취하여 분석하는데 많은 어려움이 따른다. 이 연구에서 응축수를 이용하여 냉각기의 냄새원인물질의 평가 가능성을 확인하였다. 응축수는 headspace-solidphase microextraction(HS-SPME) 방법을 이용하여 채취하였다. GC/FID/Olfactometry(GC/FID/O)로 냄새물질을 확인한 후, GC/AED, GC/MS로 정성하였다. 직접관능평가 결과 및 GC/FID/O의 개별냄새물질 분석 결과, 공기시료와 매우 유사하게 나타났다. 냄새원인물질은 주로 산소를 포함하는 alcohols와 acids로 확인되었다. 응축수를 이용한 냄새원인물질 평가 방법은 채취 용이성, 비용, 분석적인 측면에서 효과적인 방법으로 평가 되었다.

Synthesis of C-(2-Furyl)-N-(4-nitrophenyl)methanohydrazonyl Bromide. Reactions with Nucleophiles and Active Methylene Compounds

  • Hassaneen, Hamdi M.;Shawali, Ahmad S.;Elwan, Nehal M.;Ibrahim, Al Hossien A.
    • Archives of Pharmacal Research
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    • 제14권3호
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    • pp.266-270
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    • 1991
  • Synthesis of C-(2-furyl)-N-(4-nitrophenyl)methanohydrazonyl bromide 2 is described. Treatment of 2 with uncleophiles affords the corresponding substitution products 3-7. Also, compound 2 reacts with selenocyanate anion and thiocyanate anion and give the corresponding selenadiazoline and thiadiazoline 8 and 9, respectively. Moreover, reaction of 2 with enolates of various active methylene compounds afforded the pyrazole derivatives 17-20.

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님 또는 고삼추출물을 주원료로 하는 작물병해충 관리용 유기농업자재의 유효성분 열 안정성 (Stability of Representative Active Compounds on Commercial Biopesticides Based on Neem or Sophora flavescens Extract Under Controlled Temperature)

  • 김진효;최근형;강재은;박병준
    • 농약과학회지
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    • 제19권2호
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    • pp.88-92
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    • 2015
  • 님 추출물 또는 고삼 추출물을 주원료로 하는 유기농업자재의 유효성분인 limonoid계 4성분 (azadirachtin A, azadirachtin B, deacetylsalannin, salannin)과 alkaloid계 2성분 (matrine, oxymatrine)을 중심으로 열 안정성을 평가하였다. 시험은 $30^{\circ}C$, $35^{\circ}C$, $40^{\circ}C$, $45^{\circ}C$, $54^{\circ}C$에서 각각 진행하였으며, 님 추출물을 주성분으로 하는 유기농업자재 3종에서 유효성분 반감기는 25.6-220일로 제품에 따라 열 안정성의 차이가 큰 것을 확인하였다. 반면, 고삼 추출물을 주성분으로 하는 유기농업자재의 유효성분 반감기는 231-346일로 님 추출물에 비해 상대적으로 열 안정성이 높은 것으로 나타났다.

Evaluation of Antioxidant Activities and Active Compounds Separated from Water Soluble Extracts of Korean Black Pine Barks

  • Shen, Chang-Zhe;Jun, Hong-Young;Choi, Sung-Ho;Kim, Young-Man;Jung, Eun-Joo;Oh, Gi-Su;Joo, Sung-Jin;Kim, Sung-Hyun;Kim, Il-Kwang
    • Bulletin of the Korean Chemical Society
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    • 제31권12호
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    • pp.3567-3572
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    • 2010
  • Black pine barks from the southern region of Korea were extracted using pressurized hot water and the water soluble extracts were then separated in a stepwise fashion using a variety of solvents, column chromatography (CC), thin layer chromatography (TLC), and high pressure liquid chromatography (HPLC). The antioxidant activities of each fraction and the active compounds were determined based on the radical scavenging activities of 2,2-diphenyl-1-picrylhydrazyl (DPPH), reductive potential of ferric ion, and total phenol contents. A DPPH test showed that the half maximal effective concentration ($EC_{50}$ value : $6.59{\pm}0.31\;{\mu}g/mL$) of the ethyl acetate fraction (ca. 0.67%) was almost the same as that of the control compounds and inversely proportional to the value of the total phenol contents. The cell viability of the water extracts was confirmed by methyl thiazol-2-yl-2,5-diphenyl tetrazolium bromide (MTT) with enzyme linked immune sorbent assay (ELISA). Catechin, epicatechin, quercetin and ferulic acid were isolated from the ethyl acetate fraction as active compounds and identified by nuclear magnetic resonance. The antioxidant activity as value of DPPH of each of the separated compounds was lower than the ethyl acetate fraction, and ferulic acid was the lowest among these compounds.

A network pharmacology approach to explore the potential role of Panax ginseng on exercise performance

  • Kim, Jisu;Lee, Kang Pa;Kim, Myoung-Ryu;Kim, Bom Sahn;Moon, Byung Seok;Shin, Chul Ho;Baek, Suji;Hong, Bok Sil
    • 운동영양학회지
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    • 제25권3호
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    • pp.28-35
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    • 2021
  • [Purpose] As Panax ginseng C. A. Meyer (ginseng) exhibits various physiological activities and is associated with exercise, we investigated the potential active components of ginseng and related target genes through network pharmacological analysis. Additionally, we analyzed the association between ginseng-related genes, such as the G-protein-coupled receptors (GPCRs), and improved exercise capacity. [Methods] Active compounds in ginseng and the related target genes were searched in the Traditional Chinese Medicine Database and Analysis Platform (TCMSP). Gene ontology functional analysis was performed to identify biological processes related to the collected genes, and a compound-target network was visualized using Cytoscape 3.7.2. [Results] A total of 21 ginseng active compounds were detected, and 110 targets regulated by 17 active substances were identified. We found that the active compound protein was involved in the biological process of adrenergic receptor activity in 80%, G-protein-coupled neurotransmitter in 10%, and leucocyte adhesion to arteries in 10%. Additionally, the biological response centered on adrenergic receptor activity showed a close relationship with G protein through the beta-1 adrenergic receptor gene reactivity. [Conclusion] According to bioavailability analysis, ginseng comprises 21 active compounds. Furthermore, we investigated the ginseng-stimulated gene activation using ontology analysis. GPCR, a gene upregulated by ginseng, is positively correlated to exercise. Therefore, if a study on this factor is conducted, it will provide useful basic data for improving exercise performance and health.

화학요법제 합성연구 II N,N'-disubstituted thiourea derivatives의 합성및 그 항균성과 항인결핵성 (Synthetic studies on chemothe-rapeutic agents (II) : synthesis and antibacterial and antitubercular activity of N,N'-disubstituted thiourea derivatives)

  • 조윤성;고광호
    • 약학회지
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    • 제15권3_4호
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    • pp.87-92
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    • 1971
  • Fourteen novel N,N'-disubstitued thiourea derivatives were synthesized by Hugershof reaction. Antitubercular activities of ten compounds against Mycobacterium tuberculosis H$_{37}$ Rv were tested and was found tat 1-cyclohexyl-3-(4-benzenesulfonepiperidide)-2-thiourea was considerably active at 1mg/ml and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea was slightly active at 1mg/ml. Antibacterial activity of the newly synthesized compounds against E. coli, Sta. aureus and Streptococcus hemolyticus were also tested. 1-cyclohexyl-3-(4-benzenesulfonepiperidide)-2-thiourea was makedly active against E. coli, Sta, aureus and Streptococcus hemolyticus; Phenol coefficients against E. coli, Sta, aureus and Streptococcus hemolyticus were 30,17.5 and 21.3, respectively. 1,1'-p-phenylene-3,3'bis[N-(2-thiazolyl)-sulfamylphenyl]-2,2'-dithiourea and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea were considerably active against E. coli: phenol coefficients, 18.8 and 37.5 respectively. 1-(4-ethoxyphenyl)3-(4-sulfamylphenyl)-2-thiourea was active against Streptococcus hemolyticus: phenol coefficients, 22.5. 1-$\alpha$-naphthyl-3-(4-sulfamylphenyl)-2-thiourea, 1-$\betha$-naphthyl-3-[4-N-(2-thiazolyl)-sulfamylphenyl]-2-thiourea and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea were active against Sta. aureus: phenol coefficients, 17.5, 20.0 and 18.8 respectively.

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