• Natural Product Sciences
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• v.11 no.3
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• pp.145-149
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• 2005

A methanol soluble extract from the dried hooks and stems of Uncaria rhynchophylla showed a strong inhibitory activity against monoamine oxidase in mouse brain. Using a bioassay-guided purification of this extract, a known ${\beta}-carboline$ type alkaloid, harman (1), was obtained as an active constituent. In addition, five known indole alkaloids, isocorynoxeine (2), isorhynchophylline (3), corynoxeine (4), cadambine (5), and $3{\alpha}-dihydrocadambine$ (6), were isolated and found to be weakly active or inactive.

• Bulletin of the Korean Chemical Society
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• v.26 no.3
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• pp.447-450
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• 2005

The crude methanol extract of the fruits of Amomum tsao-ko (Zingiberaceae) showed cytotoxic activity. Bioactivity-guided separation led to the isolation of a diarylheptanoid, tsaokoarylone [7-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one] (2). 2 showed cytotoxicity at 4.9 and 11.4 $\mu$g/mL ($IC_{50}$) against human nonsmall cell lung cancer A549 and human melanoma SK-Mel-2, respectively, determined by SRB colorimetric method. During purification-(4-hydroxyphenyl)-4-hydroxyhexan-2-one (4) together with three known diarylheptanoids was also isolated. Their structures were determined from interpretation of spectroscopic data (IR, UV, MS, and NMR) and synthesis confirmed the structure of 2.

• Journal of Applied Biological Chemistry
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• v.42 no.4
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• pp.197-201
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• 1999

Antagonistic bacteria active against phytopathogenic fungi, Phytophthora capsici, Pythium ultimum, Rhizoctonia solani, Botrytis cinerea, and Fusarium oxysporum were isolated from greenhouse soils. An antifungal compound was extracted by ethyl acetate from acidified culture filtrate and purified through column chromatography and thin layer chromatography. Activity-guided bioassay was followed throughout the purification steps using Pythium ultimum as a test organism. The purified antifungal compound was identified as phenylacetic acid (PAA) based on the data obtained from IR, EI/MS, $^1H-NMR$, and $^{13}C-NMR$. Two different isolates, which had vast differences in differential characteristics except 16S rDNA sequence homology, produced the same compound, phenylacetic acid. $ED_{50}$ values of the phenylacetic acid against P. ultimum, P. capsici, R. solani, B. cinerea, and F. oxysporum were 45, 21, 318, 360, and 226 ppm, respectively.

• Biomolecules & Therapeutics
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• v.23 no.1
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• pp.26-30
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• 2015

Wnt/${\beta}$-catenin signaling pathway was mutated in about 90% of the sporadic and hereditary colorectal cancers. The abnormally activated ${\beta}$-catenin increases the cancer cell proliferation, differentiation and metastasis through increasing the expression of its oncogenic target genes. In this study, we identified an inhibitor of ${\beta}$-catenin dependent Wnt pathway from rhizomes of Atractylodes macrocephala Koidzumi (Compositae). The active compound was purified by activity-guided purification and the structure was identified as 2,8-dimethyl-6-hydroxy-2-(4-methyl-3-pentenyl)-2H-chromene (atractylochromene, AC). AC suppressed b-catenin/Tcell factor transcriptional activity of HEK-293 reporter cells when they were stimulated by Wnt3a or inhibitor of glycogen synthase kinase-$3{\beta}$. AC down-regulated the nuclear level of ${\beta}$-catenin through the suppression of galectin-3 mediated nuclear translocation of ${\beta}$-catenin in SW-480 colon cancer cells. Furthermore, AC inhibits proliferation of colon cancer cell. Taken together, AC from A. macrocephala might be a potential chemotherapeutic agent for the prevention and treatment of human colon cancer.

• YAKHAK HOEJI
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• v.42 no.2
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• pp.132-139
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• 1998

Currently, cancer is the primary cause of death and 50% of cancer patients are incurable by surgery, radiotherapy and chemotherapy. Therefore, immunotherpy is interested as the fourth remedy. Biological response modifier (BRM), such as organometallic compounds, glycoproteins, polysaccharides and other natural products. Is the one which can enhance the immune response against cancer cell. To develop new BRM from natural sources, we investigated 63 species Korean traditional medicines by observing the mitogenic activity to splenocytes, generation of activated killer cells and activation of macrophages. Finally, we selected 9 species including Angelicae gigantis Radix, Mori Cortex Radicis, Arisaematis Tuber, Salviae Radix, Cnidii Rhizoma, Ligusti Fructus, Pasoraliae Semen, Loranthi Ramulus, Ginseng Radix. Bioassay-guided fractionation and purification is undergoing.

• Korean Journal of Pharmacognosy
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• v.31 no.3
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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.

• Natural Product Sciences
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• v.11 no.1
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• pp.16-21
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• 2005

Nitric Oxide (NO), derived from L-arginine, is produced by two types (constitutive and inducible) of nitric oxide synthase (NOS: cNOS and iNOS). The NO produced in large amounts by the iNOS is known to be responsible for the vasodilation and hypotension observed in septic shock, cancer metastasis and inflammation. The inhibitors of iNOS, thus, may be useful candidates for the treatment of inflammatory diseases accompanied by the overproduction of NO. We prepared alcoholic extracts of herbal drugs which have been used for the treatment of inflammation in oriental medicine. We have screened the inhibitory activity of NO production in lipopolysaccharide (LPS)-activated macrophages after the treatment of these extracts. Among 82 kinds of extracts of herbal drugs, 35 extracts showed the potent inhibitory activity of NO production above 50% at the concentration of $50\;{\mu}g/mL$. The inhibitory activities of NO production were also evaluated for several solvent fractions at two different concentrations. Especially, hexane and EtOAc fractions of Alpinia officinarum, Angelica gigas, Ostericum koreanum, Saussurea lappa, Torilis japonica, and hexane fractions of Agrimonia pilosa, Machilus thunbergii, Hydrangea serrata, Magnolia obovata, Prunella vulgaris, Tussilago farfara, and EtOAC fractions of Perilla frutescence showed a significant activity at 10 and/or $25\;{\mu}g/mL$. In Western blot analysis, the hexane fractions ($5\;{\mu}g/mL$) of Magnolia obovata and Saussurea lappa, and EtOAc fractions ($20\;{\mu}g/mL$) of Hydrangea Serrata, Perilla frutescence and Torilis japonica inhibited the expression of iNOS protein in LPS-activated macrophages. These plants may be promising candidates for the study of the activity-guided purification of active compounds and might be useful for the treatment of inflammatory diseases and endotoxemia accompanying overproduction of NO.

• Fisheries and Aquatic Sciences
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• v.25 no.4
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• pp.189-201
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• 2022

Jellyfish is an emerging aquaculture species, farmed for Oriental cuisines and nutraceutical ingredients. This study aimed to examine antioxidative and antimicrobial potentials of various fractions of the jellyfish, Acromitus hardenbergi. The bell and oral arms of the jellyfish were sequentially extracted with petroleum ether (PE), dichloromethane (DCM), chloroform (CHCl₃), methanol (MeOH), and water (H₂O) to extract its bioactive in an increasing polarity gradient. Test fractions were assayed for antiradical activities using electron spin resonance spectrometry, β-carotene-linoleate model and Folin-Ciocalteu assay; and antimicrobial activity against 2 Gram-negative bacteria, 4 Gram-positive bacteria and 2 fungal species using the disc diffusion assay. All fractions were also subjected to Fourier Transform Infrared (FTIR) analysis to identify types of functional groups present. It was found that the hydrophilic extracts (H₂O fractions) possessed the most effective radical scavenging activity (p < 0.05) while the lipophilic extracts (PE fractions) the most active antimicrobial activity, especially against Gram-positive bacteria (p < 0.05). Total oxidation substrates content was found to be highest in the PE fractions of jellyfish bell and oral arms (p < 0.05). FTIR data showed that the H₂O and MeOH fractions contains similar functional groups including -OH, -C=O, -N-H and -S=O groups, while the PE, DCM, and CHCl₃ fractions, the -CH₃, -COOH groups. This study showed that A. hardenbergi contains antioxidants and antimicrobials, thereby supporting the traditional claim of the jellyfish as an anti-aging and health-promoting functional food. Bioassay-guided fractionation approach serves as a critical milestone for the strategic screening, purification, and elucidation of therapeutically significant actives from jellyfish.

• Korean Journal of Pharmacognosy
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• v.29 no.2
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• pp.79-85
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• 1998

Six antioxidative compounds in the aerial parts of Potentilla fragarioides were isolated by a bioassay guided purification using a DPPH free radical. They were identified as (+)-catechin, isoquercitrin, quercitrin, $quercetin-3-O-{\beta}-D-glucopyranosyl-{\beta}-D-xylopyranoside$, caffeic acid, and 4-O-caffeoyl-L-threonic acid on the basis of $^{1}H$ and $^{13}C-NMR$ and MS data. The DPPH radical scavenging activity of five compounds $(RC_{50}:\;7.5{\sim}10.5\;{\mu}g)$ except for quercitrin $(16\;{\mu}g)$ was more effective than those of ${\alpha}-tocopherol$ $(12\;{\mu}g)$ and BHA $(14\;{\mu}g)$.

• Journal of Microbiology and Biotechnology
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• v.22 no.1
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• pp.69-79
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• 2012

In an ongoing survey of the bioactive potential of microorganisms from Ladakh, India, the culture medium of a bacterial strain of a new Pseudomonas sp., strain ICTB-745, isolated from an alkaline soil sample collected from Leh, Ladakh, India, was found to contain metabolites that exhibited broad-spectrum antimicrobial and biosurfactant activities. Bioactivity-guided purification resulted in the isolation of four bioactive compounds. Their chemical structures were elucidated by $^1H$ and $^{13}C$ NMR, 2D-NMR (HMBC, HSQC, $^1H$,$^1H$-COSY, and DEPT-135), FT-IR, and mass spectroscopic methods, and were identified as 1-hydroxyphenazine, phenazine-1-carboxylic acid (PCA), rhamnolipid-1 (RL-1), and rhamnolipid-2 (RL-2). These metabolites exhibited various biological activities like antimicrobial and efficient cytotoxic potencies against different human tumor cell lines such as HeLa, HepG2, A549, and MDA MB 231. RL-1 and RL-2 exhibited a dose-dependent antifeedant activity against Spodoptera litura, producing about 82.06% and 73.66% antifeedant activity, whereas PCA showed a moderate antifeedant activity (63.67%) at 60 ${\mu}g/cm^2$ area of castor leaf. Furthermore, PCA, RL-1, and RL-2 exhibited about 65%, 52%, and 47% mortality, respectively, against Rhyzopertha dominica at 20 ${\mu}g/ml$. This is the first report of rhamnolipids as antifeedant metabolites against Spodoptera litura and as insecticidal metabolites against Rhyzopertha dominica. The metabolites from Pseudomonas sp. strain ICTB-745 have interesting potential for use as a biopesticide in pest control programs.