• Archives of Pharmacal Research
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• v.26 no.11
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• pp.925-928
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• 2003

Four guaia-12,6-olide type sesquiterpene lactones, aguerin B (1), 8$\alpha$-acetoxyzaluzanin C (2), cynaropicrin (3), and deacylcynaropicrin (4), were isolated from the flowers of Hemisteptia Iyrata Bunge. It is the first report on the isolation of compounds 1-4 from Hemisteptia species. All the isolates (1-4) were examined for their cytotoxic activity against SK-OV-3, LOX-IMVI, A549, MCF-7, PC-3, and HCT-15 human cancer cell lines.

• Food Science and Biotechnology
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• v.15 no.5
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• pp.672-676
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• 2006

The aim of this study is to evaluate the antioxidant, antimicrobial, and antitumor activities of various concentrations of partially purified substance(s) from green tea seed (Camellia sinensis L.). The total polyphenol contents of each fraction (non-adsorption fraction: F-1, fraction eluted with 40% methanol: F-2, and fraction eluted with 100% methanol: F-3) purified by Diaion HP-20 column chromatography were, in the increasing order: F-1 (3.7 mg tannic acid equivalents, TAB/g) < F-3 (23.2 mg TAB/g) < seed extracts (26.2 mg TAB/g) < F-2 (42.7 mg TAB/g). The scavenging activities toward the 1,1-diphenyl-2-picyrylhydrazyl (DPPH) radical were, in decreasing order: F-2 (93.3%) > butylated hydroxytoluene (BHT; 89.8%) > ascorbic acid (89.3%) > leaf extracts (70.3%) > F-3 (15.9%) > seed extracts (15.8%) > F-1 (14.8%) at a 0.1% concentration. In studies on antimicrobial activities, the results indicate that the growth of yeast (Candida albicans KCCM 11282 and Cryptococcus neoformans KCCM 50544) was inhibited more so than that of other fungi (Alternaria alternate KCTC 6005 and Rhizoctonia solani). In addition, it appears that the antitumor activities of the F-1, F-2, and F-3 fractions at a concentration of $50\;{\mu}g/mL$ showed 6, 7, and 23% growth inhibition of the HEC-1B cell line, 14, 11, 82% inhibition of the HEP-2 cell line, and 8, 16, and 81% inhibition of the SK-OV-3 cell line, respectively. Overall these results indicate that the antioxidant activity is greatest in the F-2 fraction, and the antimicrobial and antitumor activities are greatest in the F-3 fraction.

• Journal of Life Science
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• v.14 no.5
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• pp.815-820
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• 2004

A bacterum containing antitumor activity was isolated from traditional korean food, Jeotgal. Through the 16s rRNA sequence analysis, the bacterium was identitied as a strain of Bacillus subtilis SW-l. The best culture condition for antitumor activity of the bacterium is 3% of soluble starch and 1 % of yeast extract as corbon and nitrogen sources, respectively. Cytotoxicitic concentrations of the culture supernatant of B. subtilis SW-1 against cancer cell lines, A549 and SK-OV3 were 30 ul/ml and 40 ul/ml, respectively, as $IC_{50}$/ values. In DNA fragmentation assay, the culture supernatant showed the programmed cell death (apoptosis) to cause degrading the chromosomal DNA like ladder. Taken together, the culture supernatant of the B. subtilis SW-1 has some possibility to be used as an antitumor agent.

• Journal of Haehwa Medicine
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• v.9 no.2
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• pp.97-109
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• 2001

To evaluate the antitumor activity and antimetastatic effects of HDBT, studies were done experimentally. The results were obtained as follows: 1. HDBT extracts didn't show cytotoxicity against BALB/C mouse lung fibroblast cell. 2. In cytotoxicity against A549, SK-OV-3, B16-BL6 and HT1080 concen- tration inhibiting cell growth up to below 30% of control was recognized at $10^{-3}g/ml$ of HDBT. 3. The concentration inhibiting adhesion of A549 and B16-BL6 to complex extracellular matrix up to below 30% of control was recognized at $10^{-3}g/ml$ of HDBT. 4. In Inhibitory effect on activity of DNA topoisomerase I, the $IC_{50}$ was shown $200-300{\mu}g/m{\ell}$ of HDBT. 5. The T/C% was 137.9% in HDBT-treated group in S-180 bearing ICR mice. 6. In CAM assay, HDBT extracts inhibited angiogenesis significantly at $15{\mu}g/egg$ concentration as compared with control. 7. In pumonary colonization assay, a number of colonies in the lungs were decreased but insignificantly in HDBT-treated group as compared with control group. 8. In hematological changes in B16-BL6 injected C57BL/6, numbers of WBC were decreased significantly in HDBT-treated group but numbers PLT were increased insignificantly as compared with control. From above results it was concluded that HDBT could be usefully applied for the prevention and treatment of cancer.

• Journal of Haehwa Medicine
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• v.9 no.1
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• pp.143-153
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• 2000

To evaluate the antitumor activity and antimetastatic effects of Hongsam -daibotang(HDT-C), studies were done experimentally. The results were obtained as follows: 1. In cytotoxicity against A549, SK-OV-3 and B16-BL6 concentration inhibi ting cell growth up to below 30% of control was recognized at $10^{-3}g/ml$ of HDT-C. 2. The T/C% was 145.4% in HDT-C treated group in S-180 bearing ICR mice. 3. In Inhibitory effect on activity of DNA topoisomerase I, the $IC_{50}$ was shown $100-200{\mu}g/ml$ of HDT-C. 4. The expressing $TNF-{\alpha}$ was increased in HDT-C treated group as compared with control. 5. The expressing MMP-9 was decreased in HDT-C treated group as compared with control. 6. HDT-C extracts exhibited efficient adhesive effect of A549, B16-BL6 cell to complex extracellular matrix. 7. In CAM assays, angiogenesis was significantly inhibited in HDT-C treated group than control group. 8. In pumonary colonization assay, a number of colonies in the lungs were decreased significantly in HDT-C treated group as compared with control group. 9. In hematological changes in B16-BL6 injected C57BL/6, numbers of WBC and were decreased insignificantly and also those of platelet were increased insignificantly in HDT-C treated group as compared with control. 10. In the histological changes of lung in B16-BL6 injected mice, infiltration of cancer cells were inhibited effectively in HDT-C treated groups whereas many cancer cells were infiltrated into erivascular and peribronchiol of control group. These results suggested that HDT-C extracts might be usefully applied for prevention and treatment of cancer.

• YAKHAK HOEJI
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• v.49 no.1
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• pp.38-43
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• 2005

The occurrence of resistance to chemotherapeutic drugs is a major problem for successful cancer treatment. This resistant phenotype of cancer cell frequently reveals a broad spectrum to structurally and/or functionally unrelated anticancer drugs, termed multidrug resistance (MDR). Overexpression of P-glycoprotein (P-gp), a transmembrane drug efflux pump, is a major mechanism of MDR. Accordingly, considerable effort has been directed towards to development of compounds that inhibit P-gp, reverse the MDR phenotype and sensitize cancer cells to conventional chemotherapy without undesired toxicological effects. In an effort to search for novel MDR reversal agent, we tested the cytotoxicity of paclitaxel, a well-known substrate of P-gp, against P-gp-expressing HCT15 and HCT15/CL02 human colorectal cancer cells in the presence or absence of benzotriazepin analogues, as well as against P-gp-negative A549 human non-small cell lung and SK-OV-3 human ovarian cancer cells in vitro. Among the compounds tested, the agents that have phenyl amide moiety at 3 position remarkably increased the cytotoxicity of paclitaxel against P-gp-expressing cancer cells, but not against P-gp-negative cancer cells. BTZ-15 and BTZ-16 at $4\;{\mu}M$ revealed similar MDR reversal activity to $10\;{\mu}M$ verapamil, a well-known MDR reversal agent.

• Journal of Dairy Science and Biotechnology
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• v.26 no.1
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• pp.5-10
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• 2008

This study was conducted to isolate protein components from culture supernatant of Lactobacillus casei. and measure anti-cancer activity. The protein components were isolated A and B on Ultrafiltration membrane(3, 10, 30, 100 KDa). And the protein components A and B were isolated fractions(number $3{\sim}9$) on FPLC. Experimental studies were progressed through the cell cytotoxicity and anti-cancer activities. Cell cytotoxicity test using human kidney normal cell(293) showed cytotoxicity of below 20% by the protein components A and B($100{\mu}g/mL$). The anti-cancer activity was increased up to 70% by the protein components A and B($100{\mu}g/mL$) in AGS(stomach cancer), A549(lung cancer), MCF-7 (breast cancer), SK-OV-3(ovary cancer) and LoVo(colon cancer). Cell cytotoxicity test was showed cytotoxicity of about 50% by the fractions(number 3, 8, 9) isolated FPLC. The others have not the cytotoxicity about the human normal cell. The anti-cancer activity was increased up to 70% by the fraction number 7 in cancer cell line. Therefore the components isolated from culture supernatant of Lactobacillus casei were showed anti-cancer activity.

• Bulletin of the Korean Chemical Society
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• v.32 no.6
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• pp.1891-1896
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• 2011

On the basis of potent HDAC-inhibitory activity and anticancer activity of SAHA, novel SAHA derivatives 3a-d and 7 with a bulky cap such as p-dimethylaminophenyl, 4-phenylaminophenyl, 4-phenyloxyphenyl, 9H-fluorenyl or naphthalenyl ring were synthesized starting from the corresponding aryl amines or naphthalenyl acetic acid using an EDC-mediated amide coupling reaction in the presence of HOBt followed by a nucleophilic addition-elimination reaction with hydroxylamine. Compounds 3b, 3c and 3d showed more potent inhibitory activity on total HDACs (14~27-fold), HDAC1 (8~15-fold), HDAC2 (1.3~25-fold) and HDAC7 (1~3-fold) and more potent anticancer activity (2~22-fold) against MCF-7, MDA-MB-231, MCF-7/Dox, MCF-7/Tam, SK-OV-3, LNCaP and PC3 human cancer cell lines than SAHA.

• Korean Journal of Plant Resources
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• v.24 no.1
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• pp.40-47
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• 2011

Sphagnum palustre is a semi aquatic moss. S. palustre has been used as Korean traditional medicine to treat cardiac pain and stroke. This study was carried out to analyze phytochemical constituents of S. palustre and investigate the biological activity for the promotion of human health. At first, we isolated seven compounds from the ethanolic extract of this plant, and their structures were characterized by spectroscopic methods. Their structures were characterized to be Coumarin(1), Caffeic acid(2), Quercetin(3), Astragalin(4), Luteolin(5), Chlorogenic acid(6), Rutin(7) were for the first time reported from this source. The ethanol extract from S. palustre which was tested for its anticancer activity against three human tumor cell line by in vitro assay.

• Natural Product Sciences
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• v.20 no.3
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• pp.160-169
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• 2014

44 compounds and 9 minerals were isolated from and detected in the New Zealand deer velvet antler Cervus elaphus var. scoticus L$\ddot{o}$nnberg. The chemical structures of (1 - 26) were identified on the basis of the spectroscopic methods and comparisons with literature, respectively. The structures were identified as cholesterol (CS, 6), 7-keto-CS (7), $7{\beta}$-hydroxy-CS (8), and $7{\alpha}$-hydroxy-CS (9), and included 12 steroid $3{\beta}$-O-(palmitic/stearic/myristic acid esters; PM/SA/MS) [CS-$3{\beta}$-O-PM (1 - 1), CS-$3{\beta}$-O-SA (1 - 2), CS-$3{\beta}$-O-MR (1 - 3), 7-keto-CS-$3{\beta}$-O-PM (2 - 1), 7-keto-CS-$3{\beta}$-O-SA (2 - 2), 7-keto-CS-$3{\beta}$-O-MR (2 - 3), $7{\beta}$-hydroxy-CS-$3{\beta}$-O-SA (3 -1), $7{\beta}$-hydroxy-CS-$3{\beta}$-O-PM (3 - 2), $7{\beta}$-hydroxy-CS-$3{\beta}$-O-MR (3 - 3), $7{\alpha}$-hydroxy-CS-$3{\beta}$-O-SA (4 - 1), $7{\alpha}$-hydroxy-CS-$3{\beta}$-O-PM (4 - 2), and $7{\alpha}$-hydroxy-CS-$3{\beta}$-O-MR (4 - 3)], dinonyl phthalate (5), 8 nucleic acids analogues [uracil (10), deoxyguanosine (11), deoxyuridine (12), uridine (13), deoxyadenosine (14), adenosine (15), inosine (16), and guanosine (17)], and the 9 free amino acids [L-phenylalanine (18), L-isoleucine (19), L-leucine (20), L-tyrosine (21), L-valine (22), L-proline (23), L-threonine (24), L-alanine (25), and L-hydroxyproline (26)]. Also, there are 8 kinds of amino acids [asparagine, serine, glutamine, glycine, histidine, arginine, methionine, and lysine], 2 sialic acids [N-acetylneuraminic acid (27), ketodeoxynonulosonic acid (28)], and 9 minerals [Na > K > Ca > Mg > Fe > Zn > B > Al > Cu] were detected from the autoaminoacid analyzer and ICP spectrometer, HPAEC-PAD/HPLC-FLD, respectively. 9 kinds of oxycholesterol-$3{\beta}$-O-fatty acid ester (2 - 1, 2 - 2, 2 - 3, 3 - 1, 3 - 2, 3 - 3, 4 - 1, 4 - 2, and 4 - 3) and 3 nucleic acids (12, 14, and 15) were isolated from the velvet antler for the first time. 6 kinds of steroids (7, 8, 9, 2 - 1, 3 - 1, and 4 - 1) were examined for their anti-proliferative effects against L1210, P388D1, K562, MEG-01, KG-1, MOLT-4, A549, HepG2, MCF-7, SK-OV-3, and SW-620 cancer cell lines. They showed anti-proliferative effects with $IC_{50}$ values of 0.06, 2.16, 2.42, > 50.0, 1.66 and $8.31{\mu}M$ against L1210, while the values were 24.05, 9.44, 5.22, 0.25. 9.48 and $49.77{\mu}M$ against P388D1, respectively. The others were inactive.