• Journal of Physiology & Pathology in Korean Medicine
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• v.21 no.4
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• pp.973-981
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• 2007

In the present study, we investigated the antiproliferative activity of the water extract of Samgibopae-tang (SGBPT) in NCI-H460 and A549 non-small-cell lung cancer cell lines. We found that exposure of A549 cells to SGBPT resulted in the growth inhibition in a dose-dependent manner as measured by MTT assay, however SGBPT did not affect the growth of NCI-H460 cells. The antiproliferative effect by SGBPT treatment in A549 cells was associated with morphological changes such as membrane shrinking and cell rounding up. SGBPT treatment did not induce the cell cycle arrest in both cell lines, however the frequency of sub-G1 population was concentration-dependently increased by SGBPT treatment in A549 cells. SGBPT treatment partially induced the expression of tumor suppressor p53 in A549 cells and the expression of cyclin-dependent kinase inhibitor p21(WAF1/CIP1) was markedly increased in both transcriptional and translational levels in A549 cells. The up-regulation of p21 by SGBPT occurred in a similar a concentration dependent manner to that observed with the inhibition of cell viability and induction of sub-G1 population of the cell cycle. However SGBPT treatment did not affect other growth regulation-related genes such as early growth response-1 (Egr-1), nonsteroidal anti-inflammatory drug-activated gene-1 (NAG-1), inducible nitric oxide synthease (iNOS), cyclooxygenases (COXs), telomere-regulatory factors in A549 as well as NCI-H460 cells. Taken together, these findings suggested that SGBPT-induced inhibition of human lung carcinoma A549 cell growth was aoosciated with the induction of p21 and the results provided important new insights into the possible molecular mechanisms of the anti-cancer activity of SGBPT.

• Natural Product Sciences
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• v.10 no.3
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• pp.129-133
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• 2004

Quercetin is a dietary anticancer chemical that is capable of inducing apoptosis in tumor cells. However, little is known about its biological effect in nonmalignant hepatic cells. Using embryonic normal hepatic cell line (BNL CL.2) and its SV40-transformed tumorigenic cell line (BNL SV A.8), we evaluated the effects of quercetin on cell proliferation and apoptosis. As the results, our present study demonstrated that quercetin had a selective growth inhibition in normal versus tumorigenic hepatic cells such that BNL SV A.8 cells were very sensitive to the quercetin-mediated cytotoxicity. In particular, as evidenced by the increased number of positively stained cells in the TUNEL assay, the induction of characteristic nuclear DNA ladders, and the migration of many cells to sub-G1 phase in the BNL SV A.8 cells, quercetin treatment more sensitively induced apoptosis in BNL SV A8 cells than in BNL CL.2 cells. Collectively, our findings suggest that quercetin can be approached as a potential agent that is capable of inducing selective growth inhibition and apoptosis of hepatic cancer cells.

• Journal of Nutrition and Health
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• v.36 no.4
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• pp.382-388
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• 2003

(-)-Epigallocatechin-3-gallate (EGCG) is a polyphenolic compound found in peen tea leaves, and has been known to be one of the most potent catechin species which inhibits cell growth most possibly through an apoptotic cell death. We investigated the apoptotic activity of (-)-EGCG on the human myeloid leukemia cell line, HL-60. Our results of MTT test indicated that (-)-EGCG had a significant antiproliferation effect in HL-60 cells with $IC_{50}$/ (50% inhibition concentration) value of 65 $\mu$M. Giemsa statining of HL-60 cells treated with (-)-EGCG (100 $\mu$M) for 6hrs showed a typical apoptosis-specific morphological change including shrinkage of the cytoplasm, membrane blobbing and compaction of the nuclear chromatin. The DNA fragmentation was observed from the agarose gel electrophoresis of cells treated with (-)-EGCG for 3hrs or longer, and was progressed to a greater degree as treatment time increases. Treatment of the cells with (-)-EGCG (100 $\mu$M) resulted in a rapid release of mitochondrial cytochrome c into the cytosol, and a subsequent cleavage of caspase-3 to an active form in a treatment-time dependent manner. (-)-EGCG (100 $\mu$M) also stimulated proteolytic cleavage of poly-(ADP-ribose) polymerase (PARP) to an active form in HL-60 cells. Tlken together, (-)-EGCG appears to induce the apoptosis in human myeloid leukemia cells via a caspase-dependent pathway. These results suggest the possible application of (-)-EGCG, the major active compound in green tea, as an antiproliferative agent for cancer prevention.

• Journal of Microbiology and Biotechnology
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• v.14 no.3
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• pp.628-630
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• 2004

Antitumor activities of a peptide fraction isolated from traditional Korean soy sauce (SSP) were investigated in vitro and in vivo using cancer cell lines and F9 teratocarcinoma-bearing BALB/c mice. SSP exerted a dose-dependent antiproliferative effect on P388D1 mouse lymphoma, F9 mouse teratocarcinoma, and DLD-l human colon cancer cells with $IC_{50}$ values of 11, 50, and $50\mug/ml$, respectively. Tumor growth in F9 teratocarcinoma-bearing BALB/c mice, orally administered with 80 and 200 mg/kg/day of SSPs, was inhibited 10.3% and 52.4%, respectively, and survival days increased by 11.9% and 22.1%, respectively, compared to the control group. The results of antitumor activities exerted by SSP in vitro and in vivo suggest the feasibility of using SSP as an antitumor agent.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.6
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• pp.2753-2758
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• 2012

Rubia cordifolia Linn, which belongs to the Rubiaceae family, is a well-known herb used in Ayurvedic medicine. In the present study, we investigated the influence of a methanolic extract (RC) on the induction of apoptosis in HEp-2 (human laryngeal carcinoma) cell line, as evidenced by cytotoxicity, morphological changes and modification in the levels of pro-oxidants. Inhibition of cell proliferation and lactate dehydrogenase (LDH) release increased in a time and dose-dependent manner. Further, reduced glutathione (GSH), glutathione transferase (GST) and protein levels decreased and lipid peroxidation increased significantly on RC treatment in a dose dependent manner when compared to controls. Based on the results we determined the optimal dose as 30mg/ ml and the apoptotic effect of RC extract (30 mg/ml) on HEp-2 cells was confirmed by fluorescent microscopy and transmission electron microscopy (TEM) based on morphological and ultrastructural changes. RC extract suppressed the proliferation of HEp-2 oral cancer cells inducing apoptotic cell death in vitro. These results point to potential of RC extract as an agent for the treatment of laryngeal squamous cell carcinoma.

• Nutrition Research and Practice
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• v.12 no.5
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• pp.365-370
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• 2018

BACKGROUND/OBJECTIVES Oxidative stress is a major cause of cancer. This study investigated the effects of the ethanol extracts from germinated and non-germinated Keunnunjami rice, a blackish-purple pigmented cultivar with giant embryo, on selected human cancer cell lines and on the antioxidant defense system of mice fed with a high-fat diet. MATERIALS/METHODS: High fat-fed mice were orally administered with either distilled water (HF) or extracts (0.25%, w/w) from brown (B), germinated brown (GB), Keunnunjami (K), and germinated Keunnunjami (GK) rice. RESULTS: In comparison with the brown rice extract, Keunnunjami extract showed higher anticancer effect against cervical and gastric cell lines but lower anticancer activity on liver and colon cancer cells. Mice from the HF group showed significantly higher lipid peroxidation and lower antioxidant enzyme activities than the control group. However, the oxidative stress induced by high-fat diet markedly decreased in B, GB, K, and GK groups as compared with the HF group. CONCLUSIONS: Germination may be an effective method for improving the anticancer and antioxidative properties of Keunnunjami rice and extracts from germinated Keunnunjami rice may serve as a therapeutic agent against cervical and gastric cancers and oxidative damage.

• Microbiology and Biotechnology Letters
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• v.30 no.4
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• pp.420-424
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• 2002

The purpose of this study is to investigate anticariotic activity of the ethyl acetate soluble extract of Sophora flavescens Ait. for the prevention of dental caries and glucosyltransferase activity caused by Streptococcus mutans. The fraction 5-4-3 showed strong growth inhibition activity against Streptococcus mutans (MIC, 3.13 $\mu\textrm{g}$/ml). The glucosyltransferase activity of the active fraction 5-4-3 inhibited the formation of glucan and showed 77% of the antiproliferative effect at 100 $\mu\textrm{g}$/ml (P<0.05). Two flavanones, (2S)-2'-methoxy kurarinone (1) and (+)-kurarinone (2), were isolated from the active fraction 5-4-3 of the ethyl acetate soluble extract of S. flavescens Ait. Their structures were elucidated using spectroscopic methods.

• Bulletin of the Korean Chemical Society
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• v.34 no.3
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• pp.899-906
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• 2013

Using generated conformations from docking analysis by Gold algorithm, some 3D-QSAR models; CoMFA and CoMSIA have been created on 39 N-benzoylated phenoxazines and phenothiazines, including their S-oxidized analogues. These molecules inhibit the polymerization of tubulin into microtubules and thus they have been studied for the development of antitumor drugs. Training set for the CoMFA and CoMSIA models using 30 docked conformations gives $q^2$ Leave one out (LOO) values of 0.756 and 0.617, and $r^2$ ncv values of 0.988 and 0.956, respectively. The ability of prediction and robustness of the models were evaluated by test set, cross validation (leave-one-out and leave-ten-out), bootstrapping, and progressive scrambling approaches. The all-orientation search (AOS) was used to achieve the best orientation to minimize the effect of initial orientation of the structures. The docking results confirmed CoMFA and CoMSIA contour maps. The docking and 3D-QSAR studies were thoroughly interpreted and discussed and confirmed the experimental $pIC_{50}$ values.

• Preventive Nutrition and Food Science
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• v.12 no.2
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• pp.84-88
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• 2007

In this study, we investigated antimutagenic and anticancer activities of leaf mustard (LM, Brassica juncea) and leaf mustard kimchi (LMK) during their fermentation period. Methanol extracts were prepared from raw mustard, brined leaf mustard in 10% Gueun salt solution for 2 hrs, leaf mustard fermented at 15$^{\circ}C$ for 5 days after brined in 10% Guenun salt solution for 2 hrs (Fr-LM), fresh leaf mustard kimchi (Fresh-LMK) and optimally ripened leaf mustard kimchi fermented at 5$^{\circ}C$ for 30 days (OR-LMK). OR-LMK showed the strongest inhibitory activities against the mutagenicities induced by aflatoxin B1 in Salmonella Typhimurium TA100. LMs and LMKs inhibited the survival or growth of AGS human gastric adenocarcinoma cells and HT-29 human colon carcinoma cells in MTT assay and growth inhibition test. Among the extracts, OR-LMK and FR-LM exhibited strong antiproliferative effect against cancer cells, especially HT-29 cells. DAPI staining assay showed that OR-LMK induced apoptosis cell death of HT-29 cells in a dose-dependent manner. These results suggest that leaf mustards and leaf mustard kimchi have chemopreventive activities.

• The Korean Journal of Food And Nutrition
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• v.13 no.6
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• pp.539-546
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• 2000

The purpose of this study is to investigate antibacterial activities of Sophora flavescens Ait. extracts for the prevention of dental caries caused by Streptococcus mutans. The fraction 5-4-3 of the ethyl acetate soluble extract of Sophora flavescens Ait. Showed strong growth inhibition activity against Streptococcus mutans (MIC, 3.13 ${\mu}$g/ml). The glucosyltransferase activity inhibited the formation of glucan by the fraction 5-4-3 and showed 77% of the antiproliferative effect at 100 ${\mu}$g/ml. This showed a significant activity (p<0.05). These results suggest that the fraction 5-4-3 of the ethyl acetate soluble extract of Sophora flavescens Ait. may be a valuable material as the prevention of dental caries.