• Environmental Mutagens and Carcinogens
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• v.18 no.2
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• pp.98-103
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• 1998

Epigallocatechin gallate (EGCG) was reported to exert weak cytotoxicity against normal healthy cells such as C3H10T1/2 cells, but profound inhibitory effects on the initiation or promotion stage of chemical carcinogenesis in mammary gland, blood and mouse skin. This study was carried out to develop antitumor agents with weak side effects and strong antitumor activity. Human skin melanoma cells (HBT 69) and human oral epitheloid carcinoma cells (OCL 17) were cultured in RPMI-1640 media containing 10% fetal bovine serum, antibiotic, and fungizone. After incubation for 24 hrs, the cells were treated with various amounts of (EGCG) for 48 hrs. The growth inhibitory effects of EGCG in human oral epitheloid carcinoma cells were evaluated by the 3- (4,5-djmethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT), neutral red (NR), and sulforhodamine B protein (SRB) assays of colorimetric methods. The light microscopic study was also carried out to observe morphological changes of the treated cells. These results obtained were as follows; 1. Significantly inhibitory effects of EGCG against cultured human oral epithelioid carcinoma cells. 2. Significantly inhibitory effects against cultured human skin melanoma cells treated with 50 $\mu$M EGCG, but decreased inhibitory effects in 100 $\mu$M EGCG. 3. Degenerative changes against cultured human oral epitheloid carcinoma cells. 4. Degenerative changes against human skin melanoma cells treated with 50 UM EGCG, but recovered degenerative changes in 100 $\mu$M EGCG.

• The Journal of Korean Medicine
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• v.20 no.2
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• pp.128-140
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• 1999

To evaluate the antitumor activity, antimetastatic and immunomodulatory effects of samryongbakchulsankamibang(SBSK) studies were done experimentally, In cytotoxicity against P388, A549. SK-OV-3, B16-F10 and SK-MEL-2. concentration inhibiting cell growth up to below 40% of control was recognized at $10^{-3}g/ml$ of SBSK. In Inhibitory effect on activity of DNA topoisomerase I. the $IC_{50}$ was shown $200-400{\mu}g/ml$ of SBSK. The T/C was 154% in SBSK-treated group in S-180 bearing ICR mice, The concentration inhibiting adhesion of A549 and B16-F10 to complex extracellular matrix up to below 30% of control was recognized at $5{\times}10^{-4}$, $1{\times}10^{-3}\;g/ml$ of SBSK. In pumonary colonization assay with B16-BL/6, a number of colonies in the lungs were decreased significantly in SBSK-treated group as compared with control group, In hematological changes in B16-BL/6 injected C57BL/6, numbers of WBC and platelet were not changed significantly in SBSK-treated groups, In CAM and in vitro neovascularization assay, angiogenesis was inhibited significantly in SBSK-treated group as compared with control group. From above results it was concluded that SBSK could be usefully applied for the prevention and treatment of cancer.

• Asian Pacific Journal of Cancer Prevention
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• v.17 no.11
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• pp.4853-4856
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• 2016

Objective: Gimatecan is a new camptothecin (CPT) analogue that inhibits tumor growth by targeting DNA topoisomerase I (TOP I) and introducing strong and persistent DNA cleavage. Anti-tumor activity has been demonstrated with a wide range of solid tumors in previous preclinical and clinical studies. Here, we investigated for the first time the effects of gimatecan on the proliferation of hepatocellular carcinoma (HCC) cells both in vitro and in vivo. Methods: Anticancer efficacy of gimatecan were evaluated in a panel of HCC cell lines and corresponding mouse xenograft models. Inhibition of cell proliferation was measured by CellTiter-Glo cell viability assay. In vivo, gimatecan and control preparations were orally administered every four days, for a total of four times. Tumor volume and body weights of the mice were measured twice weekly. Results: In vitro cytotoxicity evaluation showed that gimatecan inhibited the proliferation of a large panel of HCC cell lines in a dose dependent manner, with IC50 values ranging between 12.1~1085.0 nM. In vivo evaluation in mouse xenograft models showed significant antitumor effects of gimatecan at 0.8mg/kg and 0.4mg/kg as compared to the control group. Conclusion: This study suggested that gimatecan may have the potential to be used as a chemotherapeutic agent for the treatment of HCC.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.3
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• pp.1703-1706
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• 2013

Lung cancer remains a deadly disease with unsatisfactory overall survival. Resveratrol (Res) has the potential to inhibit growth of several types of cancer such as prostate and colorectal examples. In the current study, we evaluated in vitro and in vivo anticancer efficiency of Res in a xenograft model with A549 cells. Cell inhibition effects of Res were measured by MTT assay. Apoptotis of A549 cells was assessed with reference to caspase-3 activity and growth curves of tumor volume and bodyweight of the mice were measured every two days. In vitro cytotoxicity evaluation indicated Res to exert dose-dependent cell inhibition effects against A549 cells with activation of caspase-3. In vivo evaluation showed Res to effectively inhibit the growth of lung cancer in a dose-dependent manner in nude mice. Therefore, we believe that Res might be a promising phytomedicine for cancer therapy and further efforts are needed to explore this potential therapeutic strategy.

• Journal of Haehwa Medicine
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• v.8 no.2
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• pp.93-106
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• 2000

To evaluate the antitumor activity and antimetastatic effects of Kamicheungyeolhaedog tang(KCHT), studies were done experimentally. The results were obtained as follows: 1. KCHT extracts exhibited a significant cytotoxicity against A549, SK-MEL-2, SK-OV-3, and B16-BL6 cell lines. 2. KCHT extracts showed significant inhibitoty effect on DNA topoisomerase I 3. The T/C% was 145.8% in KCHT treated group in S-180 bearing ICR mice. 4. KCHT extracts exhibited efficient affect adhesive effect of A549, B16-BL6 cell to complex extracellular matrix. 5. In vitro neovascularization assays, angiogenesis was insignificantly inhibited in KCHT treated group as compared with control group. These results suggested that KCHT extracts might be usefully applied for prevention and treatement of cancer.

• Bulletin of the Korean Chemical Society
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• v.32 no.7
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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.

• Macromolecular Research
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• v.9 no.5
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• pp.277-284
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• 2001

Poly(exo-3,6-epoxy-1,2,3,6-tetrahydrophthalic anhydride)s [poly(ETA)s] and poly($\alpha$-ethoxy-exo-3,6-epoxy-1,2,3,6-tetrahydrophthaloyl-5-fluorouracil)s [poly(EETFU)s ] with various average molecular weights were prepared by photopolymerizations. The number average molecular weights of the fractionated poly(ETA)s and poly(EETFU)s determined by GPC were in the range of 3,600∼21,000 and 3,600-33,400, respectively. The release rate of 5-FU from poly(EETFU) decreased with increasing average molecular weight. The in vitro cytotoxicity of poly(ETA) against a normal cell line was lower than that of 5-fluorouracil(5-FU), The in vivo antitumor activities of the synthesized samples at dosage of 0.8 mg/kg against mice bearing sarcoma 180 tumor cell line decreased in the following order: poly(EETFU) > poly(ETA) > EETFU > ETA > 5-FU. The antiangiogenic activities of the poly(ETA)s were better than those of 5-FU.

• Korean Journal of Pharmacognosy
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• v.36 no.4 s.143
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• pp.332-337
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• 2005

We here demonstrate the evidence of increased anti-tumor and immunostimulating activities of crude extracts (GAL) from Galium. aparine L. In experimental lung metastasis of colon26-M3.1 carcinoma or B16-BL6 melanoma cells, prophylactically intravenous (i.v) administration of GAL significantly inhibited lung metastasis in a dose-dependant manner. In an in vitro cytotoxicity analysis, GAL at the concentration up to $500\;{\mu}g/ml$ did not affect the growth of B16-BL6 melanoma cells. In contrast, GAL showed the enhancement of splenocyte proliferating activity in a dose-dependent manner. Peritoneal macrophages stimulated with GAL produced various cytokines such as $1L-1{\beta},\;TNF-{\alpha},\;IFN-{\gamma}$ and IL-12. These data suggest that GAL has an antitumor activity to inhibit tumor metastasis, and its antitumor effects is associated with activation of nonspecific immnune related cells.

• Journal of Haehwa Medicine
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• v.10 no.1
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• pp.109-114
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• 2001

To evaluate the antitumor activity of Paridis Rhizoma(PR), studies were done experimentally. The results were obtained as follows: 1. In cytotoxicity against MCF-7, SK-OV-3, HCT15, concentration inhibiting cell growth up to below 50% of control was recognized at $100-200{\mu}g/m{\ell}$ of PR and also against A549, XF498 was recognized at $50-100{\mu}g/m{\ell}$. 2. In Inhibitory effect on activity of DNA topoisomerase I, the $IC_{50}$ was shown $50-100{\mu}g/m{\ell}$ of PR. 3. The concentration inhibiting adhesion of A549 and SK-OV-3 to complex extracellular matrix up to below 50% of control was recognized at $10-100{\mu}g/m{\ell}$ of PR. 4. The T/C% was 137.9 in PR-treated group in S-180 bearing ICR mice. From above results it was concluded that PR could be usefully applied for the prevention and treatment of cancer.

• Journal of Microbiology and Biotechnology
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• v.25 no.4
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• pp.439-447
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• 2015

The objective of this study was to isolate and identify the chemical structure of a biosurfactant produced by Nocardia farcinica strain BN26 isolated from soil, and evaluate its in vitro antitumor activity on a panel of human cancer cell lines. Strain BN26 was found to produce glycolipid biosurfactant on n-hexadecane as the sole carbon source. The biosurfactant was purified using medium-pressure liquid chromatography and characterized as trehalose lipid tetraester (THL) by nuclear magnetic resonance spectroscopy and mass spectrometry. Subsequently, the cytotoxic effects of THL on cancer cell lines BV-173, KE-37 (SKW-3), HL-60, HL-60/DOX, and JMSU-1 were evaluated by MTT assay. It was shown that THL exerted concentration-dependent antiproliferative activity against the human tumor cell lines and mediated cell death by the induction of partial oligonucleosomal DNA fragmentation. These findings suggest that THL could be of potential to apply in biomedicine as a therapeutic agent.