• Preventive Nutrition and Food Science
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• v.2 no.4
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• pp.348-353
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• 1997

The antimutagenic and cancer cell growth inhibitory effects of methanol extracts from 9 kinds of seaweed were studied in the Ames assay and cell culture systems, respectively. The methanol extracts from the seaweeds of sea lettuce, chlorella, sea tangle, sea mustard, sporophyll of sea mustard, fusiforme, seaweed papulosa, purple laver and ceylon moss showed antimutagenicities against aflatoxin B₁(AFB₁) and N-methyl-N'-nitro-N-nitrosoguanidine(MNNG) in the Salmonella typhimurium TA100. These extracts revealed relatively higher antimutagenicity against AFB₁(indirect mutagen) than MNNG(direct mutagen). Sporophyll of sea mustard and seaweed papulosa exhibited strong antimutagenic activity against AFB₁, and sporophyll of sea mustard, sea tangle and ceylon moss also reduced the mutagenicity induced by MNNG. The sporophyll fo sea mustard exerted the highest antimutagenic activity among the samples treated. The methanol extracts from 9 kinds of seaweed inhibited the growth of two cancer cell lines, AGS human gastric adenocarcinoma cells and HT-29 human colon carcinoma cells. Sea tangle, sea mustard and sporophyll of sea mustard inhibited the growth of cancer cells significantly. These results suggest that various seaweeds show not only antimutagenic activity but also growth inhibitory effect of some cancer cells.

• Journal of Dairy Science and Biotechnology
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• v.16 no.2
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• pp.98-105
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• 1998

Various peptides derived from food are among the most potent physiologically active agents known, and include anticancer peptides, angiotensin converting enzyme(ACE) inhibitor exhibiting antihypertension action, opioid peptides, antithrombotic peptides, hypocholesterolemic peptides, immunomodulators, calcium absorption enhancers, and other peptides. Hydrophobic peptides extracted from a Cheddar-type cheese slurry were fractionated by gel chromatography and repeated HPLC. A peptide fraction from HPLC showed high cytotoxicity on the tumor cell lines such as a human colon carcinoma, and comprised of Tyr, Ser, Leu, Gly, and others. Hypocholesterolemic peptides were isolated from peptic hydrolyzates of casein and soy proteins. Macropeptides of 1,000${\sim}$5,000 dalton were effective on reducing the cholesterol level of mouse serum. Peptides showing high Krigbaum hydrophobicity and ANS surface hydrophobicity resulted in high hypocholesterolemic effect and fecal steroid concentrations. Caseinomacropeptides(CMP) were isolated from whey powder and treated with soluble and immobilized trypsin to obtain antithrombotic peptides. One fraction from the CMP hydrolyzed with immobilized trypsin for 24h exhibited high antithrombotic activity with 52.5% inhibition of platelet aggregation. These result suggested that peptides from various milk products could be utilized as a good bioactive agents for developing health functional foods.

• Journal of the Korean Applied Science and Technology
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• v.24 no.2
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• pp.109-116
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• 2007

2-Chlorobenzoyl hydrazine refluxed with benzoyl isothiocyanate and phenyl isothiocyanate in ethanol for 3 hours to give benzamide derivative (1) and anilinederivative (2) on yield of 71%and 95%, respectively. Benzamide derivative (1) reacted with ethanolic sodium hydroxide on reflux to afford cyclization product (3), followed by general substitution reaction of two steps to give acetamide (5), and derivatived acetamides 7a-7k, while aniline derivative (2) reacted with ethanolic sodium hydroxide on reflux to afford another cyclization product (4). Thiol (4) reacted with N-phenyl chloroacetamide in the presence of potassim carbonate to give acetamide derivative (6). Compounds 1-7kwere evaluated for their growth inhibition against five cancer cell lines, including human lung carcinoma (A-549), human prostate cancer (DU145), human colon adenocarcinoma (HT-29), human malignant melanoma (SK-MEL-2) and human ovary malignant ascites (SK-OV-3) with sulforhodamine B (SRB) assay. All compounds (1-7k) showed low inhibition activities under 50% on 100M concentration.

• Archives of Pharmacal Research
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• v.27 no.8
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• pp.829-833
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• 2004

The bioactivity-guided fractionation of the methylene chloride extract of the sclerotium of Poria cocos led to the isolation of (S)-(＋)-turmerone (1), ergosterol peroxide (2), polyporenic acid C (3), dehydropachymic acid (4), pachymic acid (5), and tumulosic acid (6). Compounds 4-6 exhibited moderate cytotoxicities, with $IC_{50}$ values of 20.5, 29.1, and $10.4{\;}\mu\textrm{m}$, respectively, against a human colon carcinoma cell line. However, 3-6 not only showed inhibitory activities as potent as etoposide used as a positive control on DNA topoisomerase II (36.1, 36.2, 43.9 and 66.7％ inhibition at a concentration of $20{\;}\mu\textrm{m}$, respectively), but also inhibition of DNA topoisomerase I (55.8, 60.7, 43.5, and 83.3％ inhibition at a concentration of $100{\;}\mu\textrm{m}$, respec-tively).

• Korean Journal of Medicinal Crop Science
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• v.15 no.5
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• pp.329-334
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• 2007

The potential antioxidant and anticancer activities of Hexane, EtOAc (Ethyl acetate), BuOH (n-Buthanol) and water fractions from methanolic (MeOH) extract of Picrasma quassioides (D. Don) Benn. were evaluated in vitro. Tested fractions showed strong antioxidant activity, especially EtOAc fraction had the highest activity ($IC_{50}\;=\;114.01\;{\mu}g/mL$), containing high total phenolics and total flavonoids contents, showed $67.59\;Tan\;{\mu}g/mg$ and $64.95\;Que\;{\mu}g/mg$ respectively. Anticancer activity of these fractions was tested by MTT assay on HT-29 (the human colon carcinoma cells) cell line. BuOH fraction not only showed very high anticancer activity, but also had no cytotoxic effect on 293 (the human normal kidney cells) cell line. Considering these results, we used BuOH fraction of MeOH crude extract from P. quassioides (D.Don) Benn. to do assessment of apoptosis by flow cytometry and the mRNA expression levels of widely established apoptotic-related genes on HT-29 cell line. All the experiments showed that BuOH fraction can induce apoptosis on HT-29 cell line strongly. Taken together, methanolic extract of P. quassioides has potential for antioxidant and anticancer activities products.

• Journal of Acupuncture Research
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• v.23 no.6
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• pp.45-60
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• 2006

Objectives : This study was guided to estimate inhibitory effects against hepatic metastasis and activation of immunocytes by Carthami Semen Herbal Acupuncture. Methods : Colon26-L5 carcinoma cells were injected through hepatic portal vein to induce hepatic metastatic cancer. Changes in weight, morphology of the cancer were estimated and cytokine level was analyzed to produce immunological changes. Results: The experimental group was significantly decreased metastatic size and proliferation compared with the control group. Observing immunocytes from the spleen of experimental group T-lymphocytes were significantly increased. As compared with control group, the differentiation of total T cell, helper T cell, cytotoxic T cell, Macrophage and NK cell was increased. Measuring the level of cytokine $IFN-{\gamma}$ which stimulates Th 1 was significantly increased in splenocyte with Con A stimuli. $IFN-{\gamma}$ and IL-12 were significantly increased in peritoneal exudate macrophage with LPS stimuli. Conclusion : These findings strongly indicate Carthami Semen Herbal Acupuncture improves immunity to inhibit the growth of cancer and metastasis.

• 한국유가공학회:학술대회논문집
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• 1998.05a
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• pp.22-29
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• 1998

Various peptides derived from food are among the most potent physiologically active agents known, and include anticancer peptides, angiotensin converting enzyme(ACE) inhibitor exhibiting antihypertension action, opioid peptides, antithrombotic peptides, hypocholesterolemic peptides, immunomodulators, calcium absorption enhancers, and other peptides. Hydrophobic peptides extracted from a Cheddar-type cheese slurry were fractionated by gel chromatography and repeated HPLC. A peptide fraction from HPLC showed high cytotoxicity on the tumor cell lines such as a human colon carcinoma, and comprised of Tyr, Ser, Leu, Gly, and others. Hypocholesterolemic peptides were isolated from peptic hydrolyzates of casein and soy proteins. Macropeptides of 1,000${\sim}$5,000 dalton were effective on reducing the cholesterol level of mouse serum. Peptides showing high Krigbaum hydrophobicity and ANS surface hydrophobicity resulted in high hypocholesterolemic effect and fecal steroid concentrations. Caseinomacropeptides (CMP) were isolated from whey powder and treated with soluble and immobilized trypsin to obtain antithrombotic peptides. One fraction from the CMP hydrolyzed with immobilized trypsin for 24h exhibited high antithrombotic activity with 52.5% inhibition of platelet aggregation. These results suggested that peptides from various milk products could be utilized as a good bioactive agents for developing health functional foods.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.11a
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• pp.147-172
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• 1994

Aziridinylbenzoquinones such as 3, 6-diaziridinyl-1, 4-benzoquinone (DZQ) and its 2, 5-methyl analog (MeDZQ) require bioreductive activation in order to elicit their anticancer activities. To determine the involvement of DTD in the activation of these drugs, we have used a ligation-mediated polymerase chain reaction to map the intracellular alkylation sites in a sing1e copy gene at the nucleotide level. We have performed this analysis in two human colon carcinoma cells, one proficient (HT-29) and one deficient (BE) in DT-diaphorase (DTD) activity. In the DTD proficient HT-29 cell line, DZQ and MeDZQ were found to alkylate both 5'-(A/T)G(C)-3' and 5'-(A/T)A-3' sequences. This is consistent with the nucleotide preferences observed when DZQ and MeDZQ are activated by purified DTD to reactive metabolites capable of alkylating DNA in vitro [Lee, C. -S., Hartley, J. A., Berardini, M. D., Butler, J., Siegel., D., Ross, D., & Gibson, N. W. (1992) Biochemistry, 31: 3019-3025]. Surprisingly in the DTD-deficient BE cell line a pattern of alkylation induced by DZQ and MeDZQ similar to that observed in the DTD-proficient HT-29 cells was observed. This suggests that reductive enzymes other than DTD can be involved in activating DZQ and MeDZQ to DNA reactive species in vivo.

• Journal of Photoscience
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• v.12 no.3
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• pp.123-127
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• 2005

The polyclonal antibody was generated against the peptide fragment of 62 amino acid residues (D 181-T242) near the COOH-terminal region of the extracellular domain of epithelial-cell adhesion molecule (Ep-CAM) and shown to be able to recognize Ep-CAM in competitive ELISA. Then, sulforhodamine 101 acid chloride (so called Texas red), a fluorescence dye, was conjugated to the affinity-purified anti-Ep-CAM antibody utilizing the reaction between the aliphatic amines of antibody and the sulfonyl chloride of Texas red. The molar ratio of Texas red to antibody was estimated to be approximately 1.86 by measuring optical densities at 280 nm and 596 nm, implying that the two molecules of Texas red at most were conjugated to antibody. The anti-Ep-CAM antibody-Texas red conjugate was then used for immunohistochemistry of CT-26 murine colon carcinoma cells. Based upon the fluorescence microscope images, anti-Ep-CAM antibody is able to deliver Texas red specifically to the surface of CT-26 cells on which Ep-CAM was actively expressed. This result indicates that anti-Ep-CAM antibody could be useful for the tissue-specific delivery of photosensitizers via antigen-antibody interaction.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.10
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• pp.5895-5900
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• 2013

Dictamnine (Dic) has the ability to exert cytotoxicity in human cervix, colon, and oral carcinoma cells and dihydroartemisinin (DHA) also has potent anticancer activity on various tumour cell lines. This report explores the molecular mechanisms by which Dic treatment and combination treatment with DHA and Dic cause apoptosis in human lung adenocarcinoma A549 cells. Dic treatment induced concentration- and time-dependent cell death. FCM analysis showed that Dic induced S phase cell cycle arrest at low concentration and cell apoptosis at high concentration in which loss of mitochondrial membrane potential (${\Delta}{\Psi}m$) was not involved. In addition, inhibition of caspase-3 using the specific inhibitor, z-DQMD-fmk, did not attenuate Dic-induced apoptosis, implying that Dic-induced caspase-3-independent apoptosis. Combination treatment with DHA and Dic dramatically increased the apoptotic cell death compared to Dic alone. Interestingly, pretreatment with z-DQMD-fmk significantly attenuated DHA and Dic co-induced apoptosis, implying that caspase-3 plays an important role in Dic and DHA co-induced cell apoptosis. Collectively, we found that Dic induced S phase cell cycle arrest at low concentration and cell apoptosis at high concentration in which mitochondria and caspase were not involved and DHA enhanced Dic induced A549 cell apoptosis via a caspase-dependent pathway.