• Title/Summary/Keyword: Bioactivity

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Cholinesterase Inhibitors Isolated from the Fruits Extract of Evodia officinalis (오수유의 Cholinesterase 저해활성 성분)

  • Lee, Ji-Young;Cha, Mi-Ran;Choi, Chun-Whan;Kim, Young-Sup;Lee, Bong-Ho;Ryu, Shi-Yong
    • Korean Journal of Pharmacognosy
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    • v.43 no.2
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    • pp.122-126
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    • 2012
  • The MeOH extract of Evodiae Fructus exhibited a significant inhibition on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), in a dose dependent manner, respectively. The extensive bioactivity-guided fractionation process with the MeOH extract finally isolated four compounds, as rutaecarpine (1), evodiamine (2), limonin (3) and dehydroevodiamine (4). Among them, compound 2 exhibited specific inhibitory activity on BChE with the $IC_{50}$ values 1.7 ${\mu}g/ml$, whereas compound 4 showed the potent inhibition upon both AChE and BChE.

Purification and Characterization of Bioactivity Compound Acemannan from Aloe vera (알로에 베라로부터 생리 활성 물질인 아세만난 분리 정제와 특성)

  • Ryu, Il-Whan;Sim, Chang-Sup;Lee, So-Young
    • Korean Journal of Pharmacognosy
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    • v.28 no.2
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    • pp.65-71
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    • 1997
  • This study was carried out to purify and to characterize various bioactive material acemannan from Aloe vera. Purified acemannan was mannose (67%) and acetyl group (23%), and the rest of glucose was galactose that consists of long chain polydispered beta-(1, 4) linked mannan polymers. The sugar and acetyl group in the molecule were linked by molar ratio of 3 : 1. This polysaccharide from Aloe vera may provide functional flood and potential drug source with antiviral and immunomodulating properties.

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The Chemistry and Biological Activity Studies of Morinda Elliptica

  • Nordin Hj. Lajis;Ismail, Nor-Hadiani;Jasril Karim;Latifah S. Yazan;Azimuddin Abdullah;A. Manaf Ali;Raha A. Rahim;Arbakaria Ariff;Marziah Mahmood
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1998.11a
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    • pp.82-87
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    • 1998
  • Brine shrimp lethality test has become one of our routine tools in selecting plant materials for further chemical or bioactivity studies in our laboratory. Usually, once a potentially bioactive sample has been identified, it will then be subjected to more elaborate bioassay procedures. Out of more than 200 plant samples tested we found eight samples to be toxic towards brine shrimp larvae.

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GENOTOXICITY STUDY OF SOPHORICOSIDE IN BACTERIAL AND MAMMALIAN CELL SYSTEM

  • Kim, Youn-Jung;Kim, Yun-Hwa;Park, Hyo-Joung;Gil, Ji-Suk;Kim, Young-Soo;Kim, Mi-Kyung;Lee, Seung-Ho;Jung, Sang-Hun;Park, Jong-Bum;Kim, Tae-Hwam;Ryu, Jae-Chun
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.10a
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    • pp.182-182
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    • 2001
  • Sophoricoside was isolated as the inhibitor of IL-5 bioactivity from Sophora japonica (Leguminosae). It has been reported to have an anti-inflammatory effect on rat paw edema model. To develope as an anti-allergic drug, genotoxicity of sophoricoside was investigated in bacterial and mammalian cell system such as Ames bacterial test, chromosomal aberration assay and single cell gel electrophoresis (Comet) assay.(omitted)

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Preparation and characterization of zirconium nitride and hydroxyapatite layered coatings for biomedical applications

  • Nathanael, A. Joseph;Lee, Jun-Hui;Hong, Sun-Ik
    • Proceedings of the Materials Research Society of Korea Conference
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    • 2012.05a
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    • pp.102.2-102.2
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    • 2012
  • Different layers of zirconium nitride (ZrN) and hydroxyapatite (HA) coatings were prepared on cp Ti substrate for biomedical applications. The main idea is to improve the mechanical strength as well as the biocompatibility of the coating. ZrN is known for its high mechanical strength, corrosion resistance. HA is well known for its biocompatibility properties. Hence, in this study, both materials were coated on a cp Ti substrate with bottom layer with ZrN for good bonding with substrate and the top layer with HA for induce bioactivity. Middle layer was formed by a composite of HA and ZrN. Detail analyses of the layered coatings for its structural, morphological, topographical properties were carried out. Then the mechanical property of the layered coatings was analyzed by nanoindentation. Biomimetic growths of apatite on the functionally graded coatings were determined by simulated body fluid method. This study provides promising results to use this kind of coatings in biomedical field.

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Recent Discovery of Bioactive Natural Products from Taiwanese Marine Invertebrates

  • Shen, Ya-Ching
    • Journal of Marine Bioscience and Biotechnology
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    • v.1 no.4
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    • pp.225-231
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    • 2006
  • The secondary metabolites from Taiwanese marine soft corals and sponges have attracted much attention because they possess considerable potential biological activities. To explore the origin of bioactivity, many cytotoxic natural products were isolated and characterized in the past few years. For examples, The lipophilic extracts from marine sponges Petrosia elastica and Ircinia formosana were found active against several human tumor cells. The investigation of the gorgonian Junceela has also resulted in the discovery of a series of new juncenolides. Bioassay-directed fractionation of Clavularia viridis yielded seven new prostanoids. These compounds have been tested and evaluated as potential antitumor agents. The soft corals of the genus Cespitularia produced novel secondary metabolites with diverse chemical structures and interesting biological activities. Four new norditerpenoids, designated cespitulactones and cespihypotins were isolated from Cespitularia hypotentaculata. Cespitulactones are novel structures having a bond cleavage between C-10 and C-11. In addition, three novel diterpenes were isolated from C. taeniata and designated cespitulactams A, B and C having a phenylethyl amino side chain.

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cis-Annonacin and (2,4)-cis-and trans-Isoannonacins: Cytotoxic Monotetrahydrofuran Annonaceous Acetogenins from the Seeds of Annona cherimolia

  • Woo, Mi-Hee;Chung, Soon-Ok;Kim, Dal-Hwan
    • Archives of Pharmacal Research
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    • v.22 no.5
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    • pp.524-528
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    • 1999
  • cis-Annonacin (1) and the mixture of (2,4)-cis-and trans-isoannonacins (2 and 3), three known mono-tetrahydrofuran annonaceous acetogenins, have been isolated form the seeds of Annona cherimolia by the use of the brine shrimp lethality test (BST) for bioactivity directed fractionation. Their structures were elucidated based on spectroscopic and chemical methods. 1 showed potent cytotoxicities in the brine shrimp lethality test (BST) and among six human solid tumor cell lines with notable selectivity for the pancreatic cell line (PaCa-2) at about 1,000 times the potency of adriamycin. The mixture of 2 and 3 is over 10,000 times cytotoxic as adriamycin in the pancreatic cell line (PaCa-2). All of the compounds are about 10 to 100 times as cytotoxic as adriamycin in the prostate cell line (PC-3).

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HIV Integrase Inhibitory Activity of Agastache regosa

  • Kim, Hye-Kyung;Lee, Hyeong-Kyu;Shin, Cha-Gyun;Huh, Hoon
    • Archives of Pharmacal Research
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    • v.22 no.5
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    • pp.520-523
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    • 1999
  • We have been screening anti-HIV integrase compounds from Korean medicinal plants by using an in vitro assay system which is mainly composed of recombinant human immunodeficency virus type 1 integrase and radiolabeled oligonucleotides. From the above screening, the aqueous methanolic extract of the roots of Agastache rugosa exhibited a significant activity. Bioactivity-guided chromatographic fractionation of the methanolic extract resulted in the isolation of rosmarinic acid. The structure of the compound was determined by spectroscopic data and by the comparison with the reported values. The $IC_{50}$ of the rosmarinic acid was approximately $10{\mu}g/ml$ against HIV integrase.

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Synthesis, Cytotoxicity and Antitumor Activity of 2,3-Diarylcyclopent-2-ene-1-ones

  • Nam, Nguyen-Hai;Kim, Yong;You, Young-Jae;Hong, Dong-Ho;Kim, Hwan-Mook;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.25 no.5
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    • pp.600-607
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    • 2002
  • Two series of 2,3-diarylcyclopent-2-ene-1-ones including 2-aryl-3-(2,5-dihydroxyphenyl)cyclopent-2-ene-1-ones (2a∼2f) and 3-aryl-2-(3',4',5'-trimethoxyphenyl)cyclopent-2-ene-1-one (3a∼3j) were synthesized and evaluated for the cytotoxicity against three tumor cell lines; B16F10, HCT116 and A431. It was found that the 3,4,5-trimethoxy substituent was optimal for the bioactivity of compounds in series 2. Meanwhile, compounds in series 3 exhibited the most potent cytotoxicity with 3-aryl ring being 4-methoxyphenyl (compound 3f), (3-hydroxy-4-methoxy)phenyl (compound 3e), or (3-amino-4-methoxy)phenyl (compound 3j).

Activity Profiles of Linear, Cyclic Monomer and Cyclic Dimer of Enkephalin

  • Kim, Dong-Hee;Hong, Nam-Joo
    • Bulletin of the Korean Chemical Society
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    • v.33 no.1
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    • pp.261-269
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    • 2012
  • The cyclic dimers of enkephalin were isolated as minor components during the solution synthesis of the corresponding cyclic monomers. The ratio of cyclic dimer to monomer was approximately 1:4 from the percent of yields. In the receptor binding assay of two cyclic dimmers, ($Tyr_2-C[D-Glu-Phe-gPhe]_2$ 6, $Tyr_2-C[D-Asp-Phe-gPhe-rLeu]_2$ 8), both analogs exhibited the high preference for ${\delta}$ receptor compared to monocyclic counterparts. In the nociceptive activity, both showed about 5 times less potent than the cyclic monomers. The repeated synthesis of 14-membered cyclic analog, Tyr-C[D-Glu-Phe-gPhe-D-rLeu] 14, which was known as having three distinct cis-trans isomers, gave rise to apparently different conformational analog arousing only trans isomer. In the receptor binding assay, it showed tremendously high selectivity toward ${\mu}$ receptor $({\delta}/{\mu}=160)$.