• Korean Journal of Food Science and Technology
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• v.29 no.2
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• pp.348-354
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• 1997

This study was designed to evaluate the effects of garlic extracts of various concentrations on the growth of various pathogens and human colon cancer cell lines in vitro. For antibacterial effects against microorganisms, minimal inhibition concentrations (MIC) of alliin were from 5,000 to 20,000 ppm. MIC of ethanol extract were from 1,250 to 10,000 ppm. For cytotoxic effect of alliin and ethanol extract against human colon cancer cell lines (HCT-15), the growth rates of the cancer cells in medium containing alliin and ethanol extract were inhibited gradually to a significant degree in proportion to the increase of these concentration. Morphology of HCT-15 cells in medium containing alliin and ethanol extract were seen to be shrinked and fragmented. The results show that the causes of the antibacterial and cytotoxic effect against a wide range are thermostable substances isolated by the ethanol.

• Journal of Life Science
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• v.18 no.4
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• pp.503-508
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• 2008

Deep sea water from the East sea was tested for breast cancer chemoprevention and metastasis by measuring the activities of cytochrome P450 1A1 and aromatase, invasiveness, and activity and expression of matrix metalloproteinase (MMP)-9 in breast MDA-MB-231 cancer cell. The in vitro incubation of rat liver microsome with deep sea water (a hardness range of $100{\sim}1,000$) showed a hardness-dependent inhibition of 7,12-dimethylbenz[a]anthracene (DMBA)-induced cytochrome P450 1A1 activity. Deep sea water showed 27.1, 45.4 and 51.9% inhibition of microsomal aromatase activity at the hardness of 600, 800 and 1,000, respectively. In addition deep sea water inhibited not only the invasiveness of 12-O-tetradecanoylphorbol-13-acetate (TPA)-treated MDA-MB-231 cells through matrigel-coated membrane in a hardness-dependent manner but also the activity and expression of MMP-9 in MDA-MB-231 cell.

• Bulletin of the Korean Chemical Society
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• v.32 no.6
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• pp.2032-2038
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• 2011

Matrix metalloproteinases (MMPs), a family of zinc-containing endopeptidases, participate in many normal processes such as embryonic development and wound repair, and in many pathological situations such as cancer, atherosclerosis, and arthritis. Peptidomimetic MMP inhibitors were designed and synthesized with N-formylhydroxylamine (retrohydroxamate) as a zinc-binding group and various side chains on the ${\alpha}$, P1', and P2' positions. Using in vitro MMP assays with purified MMPs (MMP-1, MMP-2, MMP-3, MMP-9, and MMP-14) and fluorogenic peptide substrates, it was found that compounds 2d and 2g selectively inhibit gelatinases (MMP-2 and MMP-9) and interstitial collagenase (MMP-1). They also inhibited the chemo-invasion of fibrosarcoma HT-1080 cells and tube formation of human umbilical vascular endothelial cells in a dose-dependent manner. Our results suggest that retrohydroxamate-based MMP inhibitors, especially compounds 2d and 2g, have the potential to be used as therapeutic drugs for cancer and other MMP-related diseases.

• Journal of Acupuncture Research
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• v.21 no.2
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• pp.41-55
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• 2004

Objective : To investigate the possible molecular mechanism (s) of melittin as a candidate of anti-cancer drug, we examined the effects of the compound on the growth of human lung carcinoma cell line A549. Methods : Growth inhibitory study, flow cytometry analysis, SDS-polyacrylamide gel electrophoresis and Western blot analysis, RT-PCR and in vitro caspases activity assay were performed. Results : Melittin treatment declined the cell viability of A549 cells in a concentration-dependent manner, which was associated with induction of apoptotic cell death. Melittin treatment down-regulated the levels of Bcl-XS/L mRNA and protein expression of A549 cells, an anti-apoptotic gene, however, the those of Bax, a pro-apoptotic gene, were up-regulated. Melittin induced the proteolytic cleavage and activation of caspase-3 and caspase-9 protease in a dose-dependent manner without alteration of inhibitor of apoptosis proteins family and Akt expression. Western blot analysis and RT-PCR data revealed that the levels of tumor suppressor p53 and cyclin-dependent kinase inhibitor p21 were also remained unchanged. Conclusions : Taken together, these findings suggest that melittin-induced inhibition of human lung cancer cell growth is associated with the induction of apoptotic cell death via regulation of several major growth regulatory gene products, and melittin may have therapeutic potential in human lung cancer.

• Korean Journal of Pharmacognosy
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• v.37 no.2 s.145
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• pp.110-115
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• 2006

Melittia inouei (Yuri Nabang) larvae are used as a crude drug in East Asia for treating stomach cancer and inflammation, and currently reared as a pharmaceutical insect in Jejudo, Korea. This study evaluated the immuno-modulating activity of these extracts, by determining the level of, cytokine production from mouse splenocytes stimulated with the extracts. The Melittia inouei larvae extracts did not induce the splenocyte proliferation. On the other hand, they stimulated the splenocytes to produce cytokines such as $TNF-{\alpha}$, whereas they did not stimulate IL10, IL12 or $IFN-{\gamma}$. The aqueous portion of its plant (Tri-chosanthis kirilowii) extract (sap) was found to be a potent inducer of NO production from the CPAE cells. However, it showed weak inhibitory effects on vascular endothelial growth factor (VEGF) production from splenocytes. These data suggests that a Melittia inouei larvae extract immune modulatory activity in cytokine prodcutions such as $TNF-{\alpha}$ and VEGF which might be related its anticancer effect.

• Environmental Mutagens and Carcinogens
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• v.25 no.3
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• pp.104-109
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• 2005

[ $7{\beta}$ ]-Hydroxycholesterol (cholest-5-ene-3, 7-diol, $7{\beta}$-OHC) showed the cytotoxicity on human cervical carcinoma cells (HeLa), $10{\mu}M$ of 50% inhibitory concentration. We evaluated $7{\beta}$-OHC as the possibility of radiation sensitizer. The combination effect of $7{\beta}-OHC\;and\;{\gamma}$-irradiation was measured using colony forming assay and flow cytometer with propidium iodide and $DiOC_6$ stained cells, respectively. The combined treatment of $7{\beta}-OHC\;and\;{\gamma}$-irradiation did not show significant enhancing effects on HeLa cells.

• Korean Journal of Agricultural Science
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• v.45 no.4
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• pp.761-767
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• 2018

Degenerative diseases are commonly associated with excess free radicals. Acer okamotoanum, a plant endemic to Korea, is reported to have anti-oxidant, anti-cancer, and anti-viral activities. We previously isolated flavonoids from the ethyl acetate fraction of A. okamotoanum such as quercitrin (QU), isoquercitrin (IQ), and afzelin (AF). In the present study, the in vitro antioxidant activity of flavonoids such as QU, IQ, and AF isolated from the ethyl acetate fraction of A. okamotoanum were investigated by measuring the free radical scavenging activity including 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxyl radical ($^{\cdot}OH$), and superoxide anion ($O_2{^-}$). The flavonoids (QU, IQ, and AF) concentration-dependently showed a DPPH radical scavenging activity. In particular, QU and IQ showed a higher DPPH radical scavenging activity than that of AF. In addition, the flavonoids (QU, IQ, and AF) at $10{\mu}g/mL$ showed over an 80% scavenging effect against $^{\cdot}OH$ radical production. Furthermore, the $O_2{^-}$ radical scavenging activity of the flavonoids, QU, IQ, and AF increased in a dose-dependent manner. Particularly, IQ exerted the strongest scavenging activities against $^{\cdot}OH$ and $O_2{^-}$ radicals among the other flavonoids. These results indicate that the flavonoids from A. okamotoanum, in particular IQ, would have a protective activity against oxidative stress induced by free radicals, and potentially be considered as a natural antioxidant agent.

• Natural Product Sciences
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• v.15 no.3
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• pp.151-155
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• 2009

Phytochemical investigation of the MeOH extract of the aerial parts of Geranium eriostemon resulted in the isolation of one triterpene, three furofuran lignans, one syringic acid and four flavonoids. Their chemical structures were characterized by spectroscopic methods to be oleanolic acid (1), (-)-kobusin (2), (-)-eudesmin (3), (+)-magnolin (4), syringic acid (5), quercetin (6), juglanin (7), juglalin (8), and hyperin (9). All compounds (1 - 9) were isolated for the first time from this plant source and the compounds 2 - 4 were reported first from the genus Geranium. Compounds 4 - 6 exhibited moderate cytotoxicity against four human cancer cell lines in vitro using a SRB bioassay.

• Toxicological Research
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• v.19 no.2
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• pp.147-152
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• 2003

We investigated antitumor activities of the ethanol extract from mushroom Phellinus linteus and Phellinus baumii on mulberry, oak and elm. in vitro test, the ethanol extract of mushroom cultivated on oak of Phellinus linteus showed highest activities about SK-OV-3, HCT15, XF498, SK-MEL-2 and A549. SK-OV-3 cell line showed 100% cytotoxicity in 100 $\mu\textrm{g}$/ml and HCT15 (98.39%), XF498 (89.62%), SK-MEL-2 (84.07%) and A549 (79.92%) cytotoxicity respectively. Also $IC_{50}$ showed 3.99 $\mu\textrm{g}$/ml to SK-OV-3 cell line and HCT15 (4.37 $\mu\textrm{g}$/ml), A549 (5.48 $\mu\textrm{g}$/ml), SK-MEL-2 (6.72 $\mu\textrm{g}$/ml), XF 498 (6.88 $\mu\textrm{g}$/ml). As those results, cultivated oak of Phellinus linteus showed a very low $IC_{50}$ value against SK-OV-3, HCT15, XF498, SK-MEL-2 and A549 cancer cell lines.

• Bulletin of Food Technology
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• v.17 no.4
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• pp.117-128
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• 2004

Sulforaphane은 브로컬리나 십자화과 채소중의 glucoraphanin의 가수분해 산물인 isothiocyanate로서 이는 detoxification 효소의 phase II를 일으키는 것으로 나타났고 설치류에서 화학적으로 발생된 유선 종양을 억제하고 최근에는 대장암 세포에서 cell cycle arrest와 apoptosis를 일으킨다고 알려져 왔다. 여기서는 SUL이 Human MammaryMCF-7 adenocarcinoma 세포의 증폭을 억제하는 역할을 제시하였다. MCF-7 cell에 15umol/L SUL을 처리하였을 때 G2/M cell cycle이 arrest를 보였고 cyclin B1 protein이 24시간 이내에 증가하였다. 15umol/L의 SUL은 in vivo 상에서 histon Hl의 인산화를 유도하고, 초기 mitosis에서 cell을block하며 mitotic microtuble의 중합화를 방해하였다. In vitro 상에서 정제된 bovine braintubulin에 대한 SUL을 고농도로 투여했을 때, tubulin의 중합율과 총 tubulin 중합도의 억제를 보였다. 덧붙여서, isothiocyanate를 함유하는 SULanalog로 처리된 정제 tubulin도 비슷하게 저해를 받았다. 본 연구는 SUL이 mitotic cell cyclearrest를 포함한 mammary cancer 억제력을 가진 것과, 이러한 기작으로 정상적인 tubulin 중합화및 microtubule dynamic에 한층 효과적인 영향을 준다는 것을 제시하였다.