• Journal of the Korean Chemical Society
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• v.63 no.2
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• pp.85-93
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• 2019

A panel of chalcone-sulphonamide hybrids has been designed by tethering appropriate sulphonamide scaffold with substituted chalcones as a multi-target drug for anticancer screening. Chalcones were prepared by Claisen-Schmidt condensation reaction of a substituted aldehyde with para aminoacetophenone. All the synthesized compounds were evaluated against selected five cancer cell lines, MCF-7 (Breast cancer), DU-145 (Human prostate Carcinoma), HCT-15 (Colon cancer), NCIH-522 (stage 2, adenocarcinoma; non-small cell lung cancer) and HT-3 (Human cervical cancer). Most of the synthesized chalcone-sulphonamide hybrids showed amended cytotoxic activity against various cancer cell lines which may be attributed to the linkage of sulphonamide with chalcone skeleton. The synthesized compounds were characterized by FT-IR, $^1H$ NMR, $^{13}C$ NMR and HR-LCMS and spectral study assert the structures of synthesized sulphonamide-chalcone hybrids.

• Preventive Nutrition and Food Science
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• v.1 no.2
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• pp.220-226
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• 1996

To investigate the effect of long chain n-3 polyunsaturated fatty acids on breast cancer cell growth, estrogen-dependent MCF-7 human breast cancer cells were cultured serum-free DMEM media containing 0.5$\mu\textrm{g}$/ml of differnet kinds of fatty acids; linoleic acid(LA), arachidonic acid(AA), eicosapentaenoic acid(EPA) and docosahexaenoic acid acid(DHA) and 1, 0.1, 0.2, 0.5and 1.0ng/ml 17$\beta$-estradiol as well as 10$\mu\textrm{g}$/mi insulin and 1.25 mg/ml delipidized bovine serum albumin for 3 days. Cell growth monitored by MTT assay was lower in DHA and EPA treatments as compared to LA treatment, but not with AA treatment. Estrogen concentrations at which cell growth was initially stimulated were 0.1ng/ml for LA and DHA treatments and 0.2ng/ml for EPA and AA treatments, but the degree of stimulation was 25~30% lower in DHA and EPA treatments than in LA treatment. Fatty acid analysis showed that each fatty acid in culture medium was well incoporated into celluar lipid. Protein kinase C activity of cells was most elevated in LA treatment from 2 to 8 hours of culture followed by DHA, EPA, and AA treatments. It is concluded that inhibitions of n-3 DHA and EPA on breast cancer cell growth as compard with n-6 LA is mediated via changes in membrane fatty acid composition reducing estrogen sensitivity and increasing protein kinase C activity.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.14
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• pp.5727-5731
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• 2015

Background: There is a long standing interest in natural compounds especially those with a high polyphenolic content and high scavenging activity for hazardous free radicals. Cornus mas (CM) fruit is well known for its antioxidant activities; however, its toxicity against human cancers needs to be addressed. Here, we investigated selective anticancer effects of CM on different human cancer cells. Materials and Methods: A hydro-alcoholic extract of CM (HECM) was prepared and total phenolic content (TPC) and total flavonoid content (TFC) were determined by colorimetric assays. Antioxidant activity was assessed with respectto DPPH radical scavenging. MTT assays were used to evaluate the cytotoxicity of different doses of CM (0, 5, 20, 100, 250, 500, $1000{\mu}g/ml$) towards A549 (lung non small cell cancer), MCF-7 (breast adenocarcinoma), SKOV3 (ovarian cancer) and PC-3 (prostate adenocarcinoma) cells. Results: Significant (P<0.05) or very significant (P<0.001) differences were observed in comparison to negative controls at all tested doses ($5-1000{\mu}g/ml$). In all cancer cells, HECM reduced the cell viability to values below 26%, even at the lowest doses. In all cases, $IC_{50}$ was obtained at doses below $5{\mu}g/ml$. The mean growth inhibition was 81.8%, 81.9%, 81.6% and 79.3% in SKOV3, MCF-7, PC-3 and A549 cells, respectively. Conclusions: Altogether, to our best knowledge, this is a first study that evaluated toxicity of a HECM with high antioxidant activity in different human cancer cells in vitro. Our results indicated that a hydro-alcoholic extract of CM possesses high potency to inhibit proliferation of different tumor cells in a dose independent manner, suggesting that an optimal biological dose is more important and relevant than a maximally tolerated one.

• Advances in nano research
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• v.4 no.2
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• pp.129-143
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• 2016

The present work reports a facile, rapid and an eco-friendly method for the synthesis of silver nanoparticles using Luffa acutangula (L. acutangula) leaves extract and their antibacterial and cytotoxic effects. The synthesized silver nanoparticles (AgNPs) were characterized by UV-Visible spectroscopy (UV-Vis), Fourier transform infrared spectroscopy (FT-IR) and X-ray diffraction analysis (XRD). Additionally the topography, morphology and the elemental composition of the particles were determined by Scanning Electron Microscopy (SEM) and Energy dispersive spectrophotometric (EDS) technique and the measured particle sizes from SEM micrographs are in the range of 12.5 to 24.5nm. The in-vitro antimicrobial activity of the synthesized nanoparticles was high against gram positive Staphylococcus aureus and moderate against gram negative Escherichia coli and Pseudomonas aeruginosa strains. Further, the cytotoxic effects of synthesized AgNPs were evaluated against Human Breast Cancer (MCF 7) cell line.

• Microbiology and Biotechnology Letters
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• v.22 no.4
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• pp.368-372
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• 1994

Three more unusual macrolides in addition to concnamycin B were isolated from the mycelium of Streptomyces sp. strain Bal6. These four compounds showed a potent cytotoxity to hunian cancer cell lines, SNU-1 (stomach cancer cell line), SNU-354 (liver cancer cell line), MCF- 7 (breast cancer cell line) and KB-3-1 (oral epidermoid carcinoma cell line). Interestingly, these compounds confered slight differential cytotoxity on RHEK-1, a human epidermal keratinocyte cell line immotalized by AD12-SV40 hybrid virus and RHEK-1/pSV$_{2}$ ras which was resulted from H-ras transfomation of RHEK-1. These compounds were determined to be concanamycin A, conca- namycin E and 0-methyl concanamycin B by NMR and other spectral analysis.

• Journal of Food Hygiene and Safety
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• v.22 no.3
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• pp.209-212
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• 2007

To evaluate the estrogenic activities of di-ethyl hexyl phthalate (DEHP) and di-butyl phthalate (DBP), two phthalates known as endocrine disrupters, we used MCF-7 human breast cancer cell line. As results, DBP and DEHP had estrogenic effects. In brief, the concentration of maximal MCF-7 cell proliferation was $10^{-7}M\;and\;10^{-8}M$ for DEHP and DBP, respectively. The ratio of maximal cell yield of the test compounds to that of $17{\beta}-estradiol$ was 87.5% for DEHP and 73.4% for DBP. In summary, both DEHP and DBP had cell proliferation potencies in the MCF-7 cell. Potencies ranged from approximately 10 to 100 times less than 17beta-estradiol. DBP was stronger than DEHP in the concentration of maximal efficacy. However, DEHP was stronger than DBP in the MCF-7 cell proliferation. Results from this study suggested that DEHP and DBP may play an important role in the estrogenic activity. Therefore, it is suggested that DEHP and DBP are estrogenic.

• Journal of Applied Biological Chemistry
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• v.58 no.3
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• pp.219-226
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• 2015

The anticancer activity of a methanolic extract from lemon leaves (MLL) was assessed in MCF-7-SC human breast cancer stem cells. MLL induced apoptosis in MCF-7-SC, as evidenced by increased apoptotic body formation, sub-G1 cell population, annexin V-positive cells, Bax/Bcl-2 ratio, as well as proteolytic activation of caspase-9 and caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein. Concomitantly, MLL induced the formation of acidic vesicular organelles, increased LC3-II accumulation, and reduced the activation of Akt, mTOR, and p70S6K, suggesting that MLL initiates an autophagic progression in MCF-7-SC via the Akt/mTOR pathway. Epithelial-mesenchymal transition (EMT), a critical step in the acquisition of the metastatic state, is an attractive target for therapeutic interventions directed against tumor metastasis. At low concentrations, MLL induced anti-metastatic effects on MCF-7-SC by inhibiting the EMT process. Exposure to MLL also led to an increase in the epithelial marker E-cadherin, but decreased protein levels of the mesenchymal markers Snail and Slug. Collectively, this study provides evidence that lemon leaves possess cytotoxicity and anti-metastatic properties. Therefore, MLL may prove to be beneficial as a medicinal plant for alternative novel anticancer drugs and nutraceutical products.

• Proceedings of the Korea Environmental Mutagen Society Conference
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• 2004.05a
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• pp.117-117
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• 2004

• Journal of Pharmaceutical Investigation
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• v.41 no.6
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• pp.381-386
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• 2011

Multi-drug resistance (MDR) has been known as a major hurdle in cancer chemotherapy. One of the most clinically significant causes of MDR was the efflux of anticancer agents mediated by p-glycoprotein (p-gp) over-expressed in MDR cancer cells. To overcome MDR, there have been several strategies such as co-administration with p-gp inhibitors and encapsulation of anticancer drugs into drug delivery systems. In the present study, curcumin was evaluated for its potential as p-gp inhibitor and MDR reversal activity when combined with paclitaxel incorporated into lipid nanoparticles (PTX/LN). Western blot assay showed curcumin did not modulate the level of p-gp expression in MCF-7/ADR which is a MDR variant of human breast cancer cell line, MCF-7, and over-expresses p-gp. However, curcumin inhibited p-gp-mediated efflux of calcein in a dose-dependent manner even though it showed lower activity compared to verapamil, a well-known p-gp inhibitor. Incorporation of paclitaxel into lipid nanoparticles partially recovered the anticancer activity of paclitaxel in MCF-7/ADR. The combined use of curcumin and PTX/LN exhibited further full reversal of MDR, suggesting susceptibility of PTX/LN to the efflux system. In conclusion, combined approach of using p-gp inhibitors and incorporation of the anticancer agents into nano-delivery systems would be an efficient strategy to overcome MDR.

• Proceedings of the Korea Environmental Mutagen Society Conference
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• 2002.11a
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• pp.134-134
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• 2002