• 생약학회지
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• 제21권2호
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• pp.186-192
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• 1990

This study was conducted to further purify and characterize a polysaccharide fraction from whole parts of Duchesnea indica (Andr.) Focke, which was previously reported to show an antitumor activity by us. Mild acid-treatment of the fraction by 5% acetic acid yielded three subtractions (Fr. A,B and C) on a Sephadex G-25. Fr. A was composed of uronic acid, hexose, pentose and phenolic substance, Fr. C mainly phenolic substance, and Fr. B contained hexose. All three fractions exhibited colony stimulating factor activity.

• Bulletin of the Korean Chemical Society
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• 제32권7호
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• pp.2397-2404
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• 2011

Variable selection k nearest neighbor QSAR modeling approach was applied to a data set of 80 3-arylisoquinolines exhibiting cytotoxicity against human lung tumor cell line (A-549). All compounds were characterized with molecular topology descriptors calculated with the MolconnZ program. Seven compounds were randomly selected from the original dataset and used as an external validation set. The remaining subset of 73 compounds was divided into multiple training (56 to 61 compounds) and test (17 to 12 compounds) sets using a chemical diversity sampling method developed in this group. Highly predictive models characterized by the leave-one out cross-validated $R^2$ ($q^2$) values greater than 0.8 for the training sets and $R^2$ values greater than 0.7 for the test sets have been obtained. The robustness of models was confirmed by the Y-randomization test: all models built using training sets with randomly shuffled activities were characterized by low $q^2{\leq}0.26$ and $R^2{\leq}0.22$ for training and test sets, respectively. Twelve best models (with the highest values of both $q^2$ and $R^2$) predicted the activities of the external validation set of seven compounds with $R^2$ ranging from 0.71 to 0.93.

• 약학회지
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• 제42권4호
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• pp.345-352
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• 1998

Praecoxin A, an ellagitannin, purified from Alnus hirsuta var.microphlla was evaluated on the antitumor activity. Praecoxin A had the significant cytotoxicity to s ix tumor cell lines: human chronic myelogenous leukemia K-562, human promyelocytic leukemia HL-60, mouse leukemia P388, mouse lymphocytic leukemia L-1210, sarcoma-l8O, mouse lymphoma L5178Y except L-1210. And the most sensitive cell line was K-562 ($ED_{50}=2.43{\mu}g/ml$). The $ED_{50} of praecoxin A against HL-60, P388, L-1210, sarcoma7l8O and L5178Y were 6.28, 8.66, 10.00, 7.01, $9.32{\mu}g/ml$, respectively. Praecoxin A showed the increasing effect in life span by 36.8% on the 1st day after treatment of 10mg/kg in mice bearing sarcoma-180 tumor cells (ascitic form) via NCI (National Cancer Institute, U.S.A.) protocol in vivo assay. As a result, praecoxin A is considered to show the antitumor activity.

• Natural Product Sciences
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• 제21권4호
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• pp.251-254
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• 2015

Recently, we reported violapyrones B, C, H and I, unusual 3, 4, 6-trisubstituted ${\alpha}-pyrones$ derivatives, from the culture broth of the marine Streptomyces sp. 112CH148. In previous studies, violapyrones have been shown to have antibacterial and antitumor activities. However, the anti-inflammatory effect of violapyrones has not been reported yet. As part of our ongoing study for the discovery of bioactive metabolites from marine microorganisms, we found that violapyrones also have anti-inflammatory activity. In this study, we investigated the effect of violapyrones on LPS-induced inflammatory responses in vitro. Violapyrones B and C did not affect the viability of RAW 264.7 cells at concentrations up to $25{\mu}M$. However, violapyrones B and C inhibited the production of NO compared to the LPS-induced control. In addition, violapyrones B and C down-regulated the expression of iNOS protein in LPS-stimulated RAW 264.7 cells. To the best of our knowledge, this is the first report on the anti-inflammatory activity of violapyrones B and C.

• Toxicological Research
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• 제16권2호
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• pp.101-107
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• 2000

Cannabidiol derivatives (1, 2 and 3), 5-fluorouracil (4, 5-FU) and adriamycin (5, AM) were tested for their growth inhibitory effects against human tumor cell lines using two different 3-{4,5-dimeth-ylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay and sulforhodamine B protein (SRB) assay. The light microscopic study showed morphological changes of the treated cells. Disruptions in cell organelles were determined by colorimetric methods; MTT assay and STB assay. These results suggest that cannabidiol (1, CBD) retains the most growth-inhibitory activity against human tumor cell lines.

• 생약학회지
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• 제19권3호
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• pp.153-169
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• 1988

The combined use of the J-modulated selective INEPT and CSCM 1DNMR techniques is described for the structure elucidation of several new classes of compound including prionitin, the loureirins and larreantin, and for the regiosubstitution of the furanonaphthoquinones. Spectroscopic studies on the conformation of the cytotoxic agent savinin are also described, together with the NMR assignments and preliminary biosynthetic experiments on the antitumor antibiotic staurosporine.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.211.2-211.2
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• 2003

Glycosaminolycans (GAGs). such as heparin and heparan sulfate, are highly charged molecules and are of great biological importance. Protein-GAGs interactions play prominent roles in cell-cell recognition and cell growth. Acharan sulfate (AS), isolated from the giant African snail Achatina fulica, is a novel member of glycosaminoglycan families. It showed antitumor activity by the inhibition of angiogenesis. (omitted)

• Natural Product Sciences
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• 제6권4호
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• pp.183-188
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• 2000

In order to discover novel potent antitumor agents, methanolic extracts of approximately 180 herbal medicines were prepared and primarily evaluated for cytotoxic activity in cultured human lung (A549) and colon (Col 2) cancer cells. As a result, 17 natural product extracts were found to be active in the criteria of $IC_{50}$<$20\;{\mu}g/ml$. Especially, the extracts of Aristolochia debilis, Cynanchum ascyrifolium, Cynanchum paniculatum, Daphne genkwa, Euphorbia lathyris, Ipomoea hederacea, Magnolia officinalis, Melia azedarach var. japonica, Solanum nigrum, Thuja orientalis, and Trichosanthes kirilowii showed a strong cytotoxic potential. The flower extract of Daphne genkwa was more selective cytotoxic activity against lung cancer cells $(IC_{50};\;0.2\;{\mu}g/ml)$ compared to colon cancer cells $(IC_{50}>20\;{\mu}g/ml)$. In addition, based on the cytotoxic potential of the root extract of Cynanchum paniculatum, the further fractionation of methylene chloride partition with silica gel column chromatography was performed. Several subfractions were considered to be active, and thus indicating that further studies for the identification of active principles from these fractions might be warranted.

• Advances in Traditional Medicine
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• 제1권2호
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• pp.45-51
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• 2000

This study was carried out to evaluate cytotoxicity of the methanol extract from Sophora flavescens Ait. against L1210 (lymphocytic leukemia) and $P388D_1$ (lymphoid neoplasma) Cells in vitro. We have determined cytotoxicity by the MTT (3- (4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H- tetrazolium bromide) assay. The order of cytotoxicity of Sophora flavescens Ait. extracts against L1210 and $P388D_1$ cells in vitro is as follows: Fr. 4 > Fr. 3 > Fr. 5 > Fr. 2 > Fr. 1. These results suggest that the fraction 4 of the methanol extracts from Sophora flavescens Ait. may be a valuable choice for the development of antitumor agents. In order to develop an antimicrobial agent, dried Sophora flavescens Ait. was extracted with hot methanol, and then antimicrobial activity (MIC test) was investigated. In this study, the fraction 3 of the methanol extracts from the roots of S. flavescens showed strong growth inhibition activity against gram-positive and gram-negative bacteria (MIC, $3.125\;{\mu}g/ml$) such as S. mutans, S. epidermidis and P. putida. These results indicate that fractions 3 and 4 inhibit tumor cells and bacteria.

• 대한예방한의학회지
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• 제4권2호
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• pp.235-241
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• 2000

This study was carried out to evaluate cytotoxic effects of Poncirus trifoliata Raf. extract on lymphocytic leukemia tumor (L1210) cell lines. Disruptions in cell organelles were determined by 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) assay The comparison of Ic50 Values of Poncirus trifoliata Raf. extract in L1210 cell lines showed that their susceptibility to these fractons decreased in the following order: adriamycin > Fr.4> Fr. 6> Fr. 5> Fr. 3> Fr. 1> Fr. 2 by the MTT assay. In order to develop an antumicrobial agent, Poncirus trifoliata Raf. was extracted wit ethanol, and then it was fractionated with several mobile phase. The antitumor activities of fractions of the ethanol soluble extract was investigated. The minimal inhibitory concentrations (MIC) of fractions of the ethanol soluble extract of Poncirus trifoliata Raf. against microorganisms were also examined. Antimicrobial activities of ampicillin and ketoconazole as references were compared to those of fractions of the ethanol soluble extract of Poncirus trifoliata Raf. The antimicrobial activities of all fractions from the extract had growth inhibition activities against gram-positive bacteria, gram-negative bacteria and fungi $(MIC\;>\;200{\mu}g/ml)$. These results suggest that fraction 4 of the ethanol soluble extract of Poncirus trifoliata Raf. possessed the most antitumorous agent.