• 제목/요약/키워드: in vitro bioassay

검색결과 163건 처리시간 0.022초

Monoamine Oxidase B Inhibitors from the Fruits of Opuntia ficus-indica var. saboten

  • Han, Yong-Nam;Choo, Yeun-Su;Lee, Young-Chul;Moon, Young-In;Kim, Sung-Dae;Choi, Jong-Won
    • Archives of Pharmacal Research
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    • 제24권1호
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    • pp.51-54
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    • 2001
  • Three varieties of methyl citrate and 1 -methyl malate were isolated from the fruits of Opuntia ficus-indica var. saboten Makino through in vitro bioassay-guided isolation for the inhibition on monoamine oxidase(MAO). The $IC_50$ values for MAO-B of 1-monomethyl citrate, 1,3-dimethy citrate, trimethyl citrate and 1-methyl malate were 0.19, 0.23, 0.61 and 0.25 mM, respectively. However, on MAO-A, their inhibitions showed only marginal activity.

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Phytochemical Constituents of Nelumbo nucifera

  • Kim, Ki-Hyun;Chang, Sang-Wook;Ryu, Shi-Yong;Choi, Sang-Un;Lee, Kang-Ro
    • Natural Product Sciences
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    • 제15권2호
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    • pp.90-95
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    • 2009
  • Phytochemical investigation of the MeOH extract of the leaves of Nelumbo nucifera resulted in the isolation of five norsesquiterpenes, four flavonoids, two triterpenes and one alkaloid. Their chemical structures were characterized by spectroscopic methods to be (E)-3-hydroxymegastigm-7-en-9-one (1), (3S,5R,6S,7E)- megastigma-7-ene-3,5,6,9-tetrol (2), dendranthemoside B (3), icariside $B_2$ (4), sedumoside $F_1$ (5), luteolin (6), quercetin 3-0-${\beta}$-D-glucuronide (7), quercetin 3-0-${\beta}$-D-glucoside (8), isorhamnetin 3-0-rutinoside (9), alphitolic acid (10), maslinic acid (11), and N-methylasimilobine (12). Norsesquiterpenoids (1-5) and triterpenes (10-11) were isolated for the first time from this plant. Compounds 6 and 10-12 exhibited considerable cytotoxicity against four human cancer cell lines in vitro using a SRB bioassay.

An Efficient Synthesis of 3,4-Dihydro-3-substituted-2H-naphtho[2,1-e][1,3]oxazine Derivatives Catalyzed by Zirconyl(IV) Chloride and Evaluation of its Biological Activities

  • Kategaonkar, Amol H.;Sonar, Swapnil S.;Pokalwar, Rajkumar U.;Kategaonkar, Atul H.;Shingate, Bapurao B.;Shingare, Murlidhar S.
    • Bulletin of the Korean Chemical Society
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    • 제31권6호
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    • pp.1657-1660
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    • 2010
  • An efficient and novel one-pot synthesis of new 3,4-dihydro-3-substituted-2H-naphtho[2,1-e][1,3]oxazine derivatives from 1-naphthol, various anilines and formalin at room temperature grinding is presented. The six-membered N,O-heterocyclic skeleton was constructed via zirconyl(IV) chloride promoted Mannich type reaction. In vitro antimicrobial activities of synthesized compounds have been investigated against Gram-positive Bacillus subtilis, Gram negative Escherichia coli and two fungi Candida albicans and Aspergillus niger in comparison with standard drugs. The results of preliminary bioassay indicate that some of title compounds possess significant antibacterial and antifungal activity.

Inhibition of Monamine Oxidase by a Flavone and Its Glycoside from Ixeris dentata Nakai

  • Chung, Ha-Sook
    • Preventive Nutrition and Food Science
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    • 제8권2호
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    • pp.141-144
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    • 2003
  • Ixeris dentata Nakai (Compositae) is a perennial herb which has been used as a folk medicine for treating diabetes and gastroenteric troubles in Korea. Active compounds were isolated from the aerial parts of Ixeris dentata through the bioassay-guided fractionation and isolation method evaluated for inhibition of monoamine oxidase (MAO) in vitro. The compounds were identified as 5,7,3',4'-tetrahydroxyflavone (1) and 5,7,3',4'- tetrahydroxyflavone 7-glucoside (2), based on physical and spectroscopic characteristics. Compounds 1 and 2 showed a selective inhibition of type B MAO (MAO-B) activity, with IC/sub 50/ values of 15.3 μM and 36.4 μM, respectively, but did not inhibit type A MAO (MAO-A) activity.

황색계 천연색소 추출물의 항균 특성 (Antibacterial Characteristics of the Extracts of Yellow Natural Dyes)

  • 한신영;최석철
    • 한국염색가공학회지
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    • 제12권5호
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    • pp.315-322
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    • 2000
  • The purpose of this study was to investigate the antibacterial effects of natural colors extracted from yellow natural dyes(Tumeric, Amur Cork Tree and Onion Shell). The water and the methanol extracts of Tumeric and Amur Cork Tree significally decreased the growth of E. coli in vitro and the methanol extract of Tumeric exhibited the strongest inhibitory effect among the samples. Silk and nylon fabrics dyed with water and methanol extracts of the yellow natural dyes showed antimicrobial activities against E. coli and Staph aureus in the Bioassay Test. Nylon fabric dyed with methanol extracts of them showed strong antibacterial effect on E. coli compared with that of water extracts. However, slik fabrics dyed with the extracts could not reduce the growth of E. coli. Silk or nylon fabrics dyed with methanol or water extracts of yellow natural dyes showed antimicrobial activities against Staph aureus. The antimicrobial activity of the fabrics dyed with methanol extracts from Tumeric, Amur Cork Tree and Onion Shell was stronger than that of water extracts, especially, the fabrics dyed with Tumeric extract showed the highest antibacterial property among the dyed fabrics.

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Cytotoxic Constituents from the Roots of Asarum sieboldii in Human Breast Cancer Cells

  • Kim, Eunae;Kim, Hyun Jung;Oh, Ha-Na;Kwak, Ah-Won;Kim, Su-Nam;Kang, Bok Yun;Cho, Seung-Sik;Shim, Jung-Hyun;Yoon, Goo
    • Natural Product Sciences
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    • 제25권1호
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    • pp.72-75
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    • 2019
  • Bioassay-guided fractionation of the roots of Asarum sieboldii led to the isolation of the six compounds methylkakuol (1), sesamin (2), asarinin (3), xanthoxylol (4), and (2E,4E,8Z,10E/Z)-N-(2-methylpropyl) dodeca-2,4,8,10-tetraenamide (5/6). Among the isolates, xanthoxylol (4) exhibited significant cytotoxicity against human breast cancer cells MCF-7 and MDA-MB-231 in vitro with $IC_{50}$ values of 9.15 and $13.95{\mu}M$, respectively.

In Vitro Antitumor Properties of an Isolate from Leaves of Cassia alata L

  • Olarte, Elizabeth Iglesias;Herrera, Annabelle Aliga;Villasenor, Irene Manese;Jacinto, Sonia Donaldo
    • Asian Pacific Journal of Cancer Prevention
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    • 제14권5호
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    • pp.3191-3196
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    • 2013
  • Leaf extracts of Cassia alata L (akapulko), traditionally used for treatment of a variety of diseases, were evaluated for their potential antitumor properties in vitro. MTT assays were used to examine the cytotoxic effects of crude extracts on five human cancer cell lines, namely MCF-7, derived from a breast carcinoma, SK-BR-3, another breast carcinoma, T24 a bladder carcinoma, Col 2, a colorectal carcinoma, and A549, a nonsmall cell lung adenocarcinoma. Hexane extracts showed remarkable cytotoxicity against MCF-7, T24, and Col 2 in a dose-dependent manner. This observation was confirmed by morphological investigation using light microscopy. Further bioassay-directed fractionation of the cytotoxic extract led to the isolation of a TLC-pure isolate labeled as f6l. Isolate f6l was further evaluated using MTT assay and morphological and biochemical investigations, which likewise showed selectivity to MCF-7, T24, and Col 2 cells with $IC_{50}$ values of 16, 17, and 17 ${\mu}g/ml$, respectively. Isolate f6l, however, showed no cytotoxicity towards the non-cancer Chinese hamster ovarian cell line (CHO-AA8). Cytochemical investigation using DAPI staining and biochemical investigation using terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL)-a method used to detect DNA fragmentation-together with caspase assay, demonstrated apoptotic cell death. Spectral characterization of isolate f6l revealed that it contained polyunsaturated fatty acid esters. Considering the cytotoxicity profile and its mode of action, f6l might represent a new promising compound with potential for development as an anticancer drug with low or no toxicity to non-cancer cells used in this study.

국내 자생 식물의 항산화 및 항미생물 활성 탐색 (Screening of Antioxidants and Antimicrobial activity in native plants)

  • 임요섭;박영민;박문수;김길용;김명조;최용화
    • 한국약용작물학회지
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    • 제8권4호
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    • pp.342-350
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    • 2000
  • 천연물유래의 안전하고 효과적인 항산화 화합물을 찾기 위하여 채취한 86종의 다양한 식물체로부터 얻은 MeOH 추출물을 DPPH free radical 소거법을 이용하여 항산화활성을 검정한 결과 밤껍질 $(RC_{50}=5.8{\mu}g)$과 느릅나무 $(RC_{50}=12{\mu}g)$에서 대조구인 ${\alpha}-tocopherol(RC_{50}=12{\mu}g)$ 과 BHA$(RC_{50}=14{\mu}g)$에 비해 강한 활성을 보였고 그외 13종에서 도 비교적 강한 활성을 나타내었다. 또한 대표적인 식물병원균 중 6종의 균주를 사용하여 in vivo 방법으로 항미생물 활성을 검정한 결과 굴피나무, 비목나무, 산국, 소리쟁이, 가막사리, 아왜나무에서 90% 이상의 식물병원균의 생육저해 효과를 보였다.

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Synthesis of Novel Halobenzyloxy and Alkoxy 1,2,4-Triazoles and Evaluation for Their Antifungal and Antibacterial Activities

  • Wan, Kun;Zhou, Cheng-He
    • Bulletin of the Korean Chemical Society
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    • 제31권7호
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    • pp.2003-2010
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    • 2010
  • A new class of halobenzyloxy or alkoxy 1,2,4-triazoles and their hydrochlorides were synthesized through cyclization starting from commercially available phenylhydrazine. The structures were characterized by MS, IR and $^1H$ NMR spectra as well as elemental analyses. All the synthesized compounds were screened for their antibacterial activities in vitro against Staphylococcus aureus (ATCC29213), methicillin-resistant Staphylococcus aureus (N315), Bacillus subtilis, Escherichia coli (ATCC25922), Pseudomonas aeruginosa, Shigella dysenteriae, Eberthella typhosa, and antifungal activities against Candida albicans (ATCC76615), Aspergillus fumigatus by broth microdilution assay method. The results of preliminary bioassay indicated that 3-(2,4-difluorobenzyloxy)-1-phenyl-1H-1,2,4-triazole hydrochloride exhibited the best inhibitory activity with an MIC value of 56.25 ${\mu}M$ against P. aeruginosa superior to Chloramphenicol, and showed comparable activity with Chloramphenicol against E. coli (ATCC25922).

Monoamine Oxidase Inhibitors from Cinnamomi Cortex

  • Huong, Dang Thi Lan;Jo, Young-Su;Lee, Myung-Koo;Bae, Ki-Hwan;Kim, Young-Ho
    • Natural Product Sciences
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    • 제6권1호
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    • pp.16-19
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    • 2000
  • Four compounds were isolated from the dichloromethane fraction of Cinnamomi Cortex through bioassay-guided isolation. Their structures were identified as coumarin (1), 3,3-dimethoxy-1-propenyl benzene (2), cinnamic acid (3) and o-methoxy cinnamaldehyde (4) on the basis of spectroscopic data. All four compounds showed inhibitory activities in vitro against monoamine oxidase (MAO) prepared by mouse brain. The $IC_{50}$ values were $41.4\;{\mu}M\;(1),\;110.6\;{\mu}M\;(2),\;252.5\;{\mu}M\;(3)\;and\;83.1\;{\mu}M$ (4), respectively.

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