• Korean Journal of Food Science and Technology
• /
• v.34 no.4
• /
• pp.688-693
• /
• 2002

The anticarcinogenic effects of various food components have received much attention in recent years. However mechanism of anticarcinogens in food materials on cancer cells have rarely been investigated. This study was performed to investigate the effects on the cytotoxicity and quinone reductase (QR) activity of Allium tuberusum (AT) on the human cancer cells. The six partition layers which are methanol (ATM), hexane (ATMH), ethylether (ATMEE), ethylacetate (ATMEA), butaonl (ATMB) and aqueous (ATMA) of Allium tuberusum were screened for their cytotoxic effects on HepG2, MCF-7, HeLa and SK-N-MC cells by the MTT assay. Among the six partition layers, ATMEE had the strongest cytotoxic effect at concentration of $150\;{\mu}g/mL$ which resulted over 95% on HepG2, HeLa, MCF-7 and SK-N-MC cell lines. The ATMEA also showed significant cytotoxic effect on HepG2 and SK-N-MC cell lines. The ATMB showed the highest induction activity of QR on HepG2 cells among the other partition layers. QR activity of HepG2 cells, grown in the presence of ATMB at the concentration of $50\;{\mu}g/mL$, was increased by 3.9 times, compared to the control value of 1.0. Based on these results, the ATMEE and ATMB may have potentially anticarcinogenic and chemopreventive activities.

• Archives of Pharmacal Research
• /
• v.20 no.6
• /
• pp.579-585
• /
• 1997

To gain further insight into the mechanism of action of antiestrogens, we examined the interaction of antiestrogen with the estrogen receptor system and with estrogen- noncompetable antiestrogen binding sites. In addition to binding directly to the estrogen receptor, antiestrogens can be found associated with binding sites that are distinct from the estrogen receptor. In contrast to the restriction of estrogen receptors to estrogen target cells, such as those of uterus and mammary glands, antiestrogen binding sites are present in equal amounts in estrogen receptor-positive and -negative human breast cancer cell lines, such as MCF-7, T47D, and MDA-MB-231 that differ markedly in their sensitivity to antiestrogens. In order to gain greater insight into the role of these antiestrogen binding sites in the action of antiestrogens, we have examined the biopotency of different antiestrogens for the antiestrogen binding sites and that is CI628 > tamoxifen > trans-hydroxy tamoxifen > CI628M > H1285 > LY117018. This order of affinities does not parallel the affinity of these compounds for the estrogen receptor nor the potency of these compounds as antiestrogens. Indeed, compounds with high affinity for the estrogen receptor and greatest antiestrogenic potency have low affinities for these antiestrogen binding sites. Antiestrogenic potency correlates best with estrogen receptor affinity and not with affinity for antiestrogen binding sites. In summary, our findings suggested that interaction with the estrogen receptor is most likely the mechanism through which antiestrogens evoke their growth inhibitory effects.

• Biomedical Science Letters
• /
• v.11 no.2
• /
• pp.175-183
• /
• 2005

The two major isoflavones in soy, genistein and daidzein, are well known to prevent hormone-dependent cancers by their anti estrogenic activity. The exact molecular mechanisms for the protective action are, however, not provided yet. It has been reported that genistein and daidzein have a potential anticancer activity through their antiproliferative effect in many hormone-dependent cancer cell lines. Transforming growth $factor-\beta1(TGF-\beta1)$ has also been found to have cell growth inhibitory effect, especially in mammary epithelial cells. This knowledge led to a hypothetical mechanism that the soy isoflavones-induced growth inhibitory effect can be derived from the regulation of $TGF-\beta1$ and $TGF-\beta$ receptors. In order to test this hypothesis, the effects of the soy isoflavones at various concentrations and periods on the expression of $TGF-\beta1$and $TGF-\beta$ receptors were investigated by using Northern blot analysis in human breast carcinoma epithelial cell lines, an estrogen receptor positive cell line (MCF-7) and an estrogen receptor negative cell line (MDA-MB-231). As a result, only genistein has shown a profound dose-dependent effect on $TGF-\beta1$ expression in the $ER^+$ cell line within the range of doses tested, and the expression levels are correspondent to their inhibitory activities of cell growth. Moreover, daidzein showed down-regulated $TGF-\beta1$ expression at a low dose, the cell growth proliferation was promoted at the same condition. Therefore, antiproliferative activity of the soy isoflavones can be mediated by $TGF-\beta1$ expression, and the effects are mainly, if not all, occurred by ER dependent pathway. The expression of $TGF-\beta$ receptors was induced at a lower dose than the one for $TGF-{\beta}1$ induction regardless of the presence of ER, and the expression patterns are similar to those of the cell growth inhibition. These results indicated that the regulation of $TGF-\beta$ receptor expression as well, prior to $TGF-\beta1$ expression, may be involved in the antiproliferative activity of soy isoflavones. Little or no expression of $TGF-\beta$ receptors was found in the MCF-7 and MDA-MB-231 cells, suggesting refractory properties of the cells to growth inhibitory effect of the $TGF-\beta$. The soy isoflavones can seemingly restore the sensitivity of growth inhibitory responses to $TGF-\beta1$ by re-inducing $TGF-\beta$ receptors expression. In conclusions, our findings presented in this study show that the antitumorigenic activity of the soy isoflavones could be mediated by not only $TGF-\beta1$induction but $TGF-\beta$ receptor restoration. Thus, soy isoflavones could be good model molecules to develop new nonsteroidal antiestrogenic chemopreventive agents, associated with, regulation of $TGF-\beta$ and its receptors.

• Natural Product Sciences
• /
• v.17 no.2
• /
• pp.80-84
• /
• 2011

Five known compounds, cimigenol (1), 25-O-acetylcimigenol (2), cimigenol 3-O-${\beta}$-D-xylopyranoside (3), ferulic acid methyl ester (4), and visnagin (5), were isolated from Cimicifugae Rhizoma (Ranunculaceae). The chemical structures of these compounds were determined on the basis of spectroscopic analyses including 2D NMR. Compounds 1 - 5 were evaluated for their cytotoxic activity against the HL-60, MCF-7, and A549 cancer cell lines in in vitro. Among them, compounds 4 and 5 showed moderate inhibitory activity against HL-60 cancer cell lines with $IC_{50}$ values of 24.8 and 18.1 ${\mu}M$, respectively.

• Archives of Pharmacal Research
• /
• v.24 no.3
• /
• pp.211-213
• /
• 2001

A coumestan derivative, psoralidin (1) was found to be a cytotoxic principle of the seeds of Psoralea corylifolia L (Leguminosae) with the IC_{50}$ values of 0.3 and 0.4 ug/ml against the HT-29 (colon) and MCF-7 (breast) human cancer cell lines, respectively. A coumarin, angelicin (2) was also isolated as a marginally cytotoxic agent along with an inactive compound, psoralene (3) from the plant. The isolates 1-3 were not active against the A54l(lung) and HepG2 (liver hepatoma) cancer cell lines.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.34 no.9
• /
• pp.1302-1307
• /
• 2005

In this study, we investigated the anticarcinogenic and antioxidative activities of Rhodiola sachalinensis (RS). Hexane (RSMH), ethylether (RSMEE), ethylacetate (RSMEA), butanol (RSMB), aqueous (RSMA) fractions and methanol extract (RSM) were screened for their growth inhibition effects using 3- (4,5-dimethyl-thiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay on HepG2, HeLa, MCF-7 and HT-29 cells. The anticarcinogenic effects of RSMEE was most significant when tested on MCF-7 and HepG2 cell lines at the concentration of $500{\mu}g/mL$ which resulted about $84\%\;and\;90\%$ on MCF-7 and HepG2 cells, respectively. The quinone reductase (QR)-inducing activity of RSMH on HepG2 cells was 3.5 times higher compared with the control at the concentration of $200{\mu}g/mL$. Antioxidative activities of RSM, RSMEE, RSMEA and RSMB showed about $80\%$ of electron donating activity (EDA) which were very similar to that of vitamin C as a control. We observed morphological changes of shrinking and the blebbing of HepG2 cancer cell membranes depending on the concentration of RSMEE.

• Food Science and Biotechnology
• /
• v.18 no.4
• /
• pp.1019-1021
• /
• 2009

Antiproliferative activity of the ethanol extract of Atractylodes japonica rhizomes (AJEX) was investigated using methyl thiazolyl tetrazolium (MTT) assays with various cancer cell lines (HL-60, MCF-7, SK-Br-3, MDA-MB-453, HepG2, Hep3B, PC-3, LNCaP, MKN 28, MKN 45, and HT-29 cells). Gastric carcinoma cell lines were the most responsive in terms of cell proliferation. The $IC_{50}$ of MKN 28 and MKN 45 cells were 35.98 and 27.57 ${\mu}g/mL$, respectively. Moreover, gastric carcinoma cells exposed to AJEX underwent apoptosis, as determined by Annexin V binding assay. Compared to respective control level, exposure to the AJEX at each $IC_{50}$ concentration resulted in a remarkable increase in the shift of cell populations. Present results suggest that AJEX possess potential anticancer properties.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.30 no.1
• /
• pp.86-91
• /
• 2001

The anticarcinogenic effects of various food components on human cancer cells have received much attention in recent years. The precise effect and mechanisms of anticarcinogens in food materials on cancer cells have rarely been investigated. This study was carried out to determine the effects of Daucus carota L. leaf (DCL) extracts on cytotoxic and chemopreventive effect on human cancer cells. The experiment was conducted to determine cytotoxicity of Daucus carota L. leaf extracts on HepG2, Hela and MCF-7 cells by MTT assay. Among various partition layers of Daucus carota L. leaf, the ethylacetate partition layer (DCLMEA) at 500 $\mu\textrm{g}$/mL was shown to be most effective on MCF-7 cell lines. The four partition layers which are DCLM, DCLMH, DCLMB and DCLMH were less effecitve in inducing cytotoxicity than DCLMEA was. We also determined the induction of intracellular quinone reductase (QR) activity by adding DCL extracts on HepG2 cells. Among various partition layers of DCL extracts, DCLMH and DCLM were tested to be most effective with results such as 4.9 and 4.73 with a control value of 1.0.

• Archives of Pharmacal Research
• /
• v.29 no.4
• /
• pp.276-281
• /
• 2006

A series of 8-alkyl-and 8-aryl-8,9-dihydro-7H-isoindolo[5,6-g]quinoxaline-7,9-diones were synthesized using sultine chemistry as a key step in good yield. These compounds were evaluated for their in vitro cytotoxicity against six human cancer cell lines (HCT15, SK-OV-3, A549, SNB19, MCF7 and MCF7/ADR).

• Archives of Pharmacal Research
• /
• v.26 no.8
• /
• pp.620-630
• /
• 2003

The proliferative effects of thirty Oriental medicinal herbs on MCF-7 (estrogen-sensitive breast cancer cell line) and ROS 17/2.8 osteoblast-like cells were determined using the MTT assay. Methanol extracts from several herbs was found to show proliferative activity on the above two cell lines in the range of 5 to 100 $\mu$g/mL. Among these active herbs, the methanol extract from the rhizomes of Drynaria fortunei showed the most potent proliferative activity, and the cell proliferations were significantly increase by 136 and 158% in the MCF-7 and ROS 17/2.8 cells, respectively, when treated with 100 $\mu$ g/mL. Through a bioassay-guided separation, eight flavonoids, including four new flavan-3-ols and two propelargonidins, together with the known (-)-epiafzelechin and naringin, were isolated. Their chemical structures were characterized as (-)-epiafzelechin (1), (-)-epiafzelechin-3-O-$\beta$-D-allopyranoside (2), (-)-epiafzelechin-3-O-(6"-O-acetyl)-$\beta$-D-allopyranoside (3), 4$\beta$-carboxymethyl-(-)-epiafzelechin methyl ester (4), 4$\beta$-car-boxymethyl-(-)-epiafzelechin sodium salt (5), naringin (6), (-)-epiafzelechin-(4$\beta$\rightarrow8)-4$\beta$-car-boxymethylepiafzelechin methyl ester (7) and (-)-epiafzelechin-($4\beta\rightarrow8, 2\beta\rightarrowΟ\rightarrow7)-epiafzelechin-(4\beta\righarrow8)-epiafzelechin (8) by extensive 1D and 2D NMR spectroscopy. Most of these flavonoids, in the range of $10^{-15}∼10^{-6}$ M, accelerated the proliferation of MCF-7 cell, with compounds 7 and 8, in the range of $10^{-15}∼10^{-12}$ M, showing especially potent proliferation effects. Meanwhile, seven flavonoids, with the exception of compound 4, stimulated the proliferation of ROS 17/2.8 cells in the range of $10^{-15}∼10^{-6}$ M, with compounds 5-8 especially accelerating the proliferation, in dose-dependent manners ($10^{-15}∼10^{-9}$ M), and their proliferative effect was much stronger than that of $E_2$ and genistein. These results suggest that propelargonidin dimers and trimers isolated from the rhizomes of Drynaria fortunei may be useful as potential phytoestrogens, which play important physiological roles in the prevention of postmenopausal osteoporosis.