• The Korean Journal of Food And Nutrition
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• v.35 no.6
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• pp.464-472
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• 2022

The present study was designed to investigate the antiproliferative activity and molecular mechanisms of Bibimbap in HT-29 human colorectal adenocarcinoma cells. Bibimbap extract inhibited the proliferation of HT-29 cells by 50% at a concentration of 10.1±0.17 mg/mL for 48 h. The population of live cells decreased slightly, and the morphology changed with a reduction in cell volume (pyknosis) with Bibimbap. Treatment with 5 mg/mL of Bibimbap resulted in slight cell shrinkage. Furthermore, as the Bibimbap dose increased to 10 mg/mL, these characteristics were more evident, and HT-29 cells exhibited partial detachment by staining with the DNA-binding dye Hoechst 33342. Flow cytometric analysis by Annexin V and PI double staining showed that Bibimbap increased the levels of apoptosis. Analysis of the mechanism of these events showed that Bibimbap-treated cells exhibited a mitochondria-dependent apoptotic pathway through the modulation of caspase-3, caspase-8, caspase-9, and poly-ADP ribose polymerase, as well as Bax and Bcl-2 expression in dose- and time-dependent manners. Consequently, Bibimbap exerts a significant antiproliferative effect on HT-29 human colorectal adenocarcinoma cells.

• Bulletin of the Korean Chemical Society
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• v.34 no.8
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• pp.2311-2316
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• 2013

A series of new diarylamide and diarylurea derivatives possessing pyrimidinylaminobenzene scaffold was synthesized. Their in vitro antiproliferative activities were tested against A375P human melanoma cell line. Among them, compounds 1a-c, k and 2b-d, f, g, j, l showed superior potencies against A375P human melanoma cell line to Sorafenib. In particular, compound 2f possessing 3-fluoro-5-trifluoromethyl moiety exhibited the highest potency with $IC_{50}$ value in nanomolar scale.

• Journal of dental hygiene science
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• v.7 no.1
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• pp.31-35
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• 2007

Caesalpinia sappan L. (Leguminosae) is an oriental medicinal herb distributed in China and Taiwan, and its heartwood has been traditionally used as an analgesic, a therapy for thrombosis or tumor. This study was to investigate the proliferation and inhibition effects of Caesalpinia sappan extracts against human epithelial cell and cancer cell lines. The methanol extract of dried C. sappan heartwood was evaporated (KS-6), and then sequentially extracted by hexane (KS-01), chloroform (KS-02), ethyl acetate (KS-03), n-butanol (KS-04), and water (KS-05). After 48 hr of exposure, these fractions at a concentration of $50{\mu}g/ml$ significantly increased, and reduced cell proliferation in both human normal epithelial and cancer cell lines. The ethyl acetate fraction (KS-03) among organic solvent fractions was 120.2% of the most proliferation activity ($50{\mu}g/ml$) against HaCaT human epithelial cell. However, fractions from chloroform, butanolic and methanolic extract had 7.2, 28.7 and 20.8% of antiproliferative effect on HaCaT cell, respectively. In cell proliferation effects of C. sappan extract on HeLa, SiHa and C33A human cervical cancer cells, chloroform fraction (KS-2) was the most antiproliferative activity, its antiproliferative rate (dosage, $50{\mu}g/ml$) relative to control was 25.8, 12.2 and 17.4% for SiHa, HeLa and C33A, respectively. The results indicated that the six extract fractions could induce cell cycle stimulate or arrest in some way. Finally, further investigation is needed to assess the molecular mechanisms mediated anticancer activities of this plant.

• Journal of Microbiology and Biotechnology
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• v.19 no.11
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• pp.1348-1354
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• 2009

Bioconversion of the isoflavonoid genistein to 2'-hydroxygenistein (2'-HG) was performed using isoflavone 2'-hydroxylase (CYP81E1) heterologously expressed in yeast. A monohydroxylated product was analyzed by liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS) and NMR spectrometry and was identified as 2'-HG. An initial bioconversion rate of 6% was increased up to 14% under optimized conditions. After recovery, the biological activity of 2'-HG was evaluated. Bioconverted 2'-HG showed higher antioxidant activity against 1,1-diphenyl-2-picryl hydrazine (DPPH) and 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radicals than did genistein. Furthermore, 2'-HG exhibited greater antiproliferative effects in MCF-7 human breast cancer cells than did genistein. These results suggest that 2'-hydroxylation of genistein enhanced its antioxidant activity and cell cytotoxicity in MCF-7 human breast cancer cells.

• Journal of Marine Bioscience and Biotechnology
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• v.10 no.2
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• pp.53-61
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• 2018

Sargassum fulvellum (gulfweed) is a widespread seaweed in the coastal areas of northeast Asia. In the present study, we identified the phenolic compounds present in aqueous and ethanolic extracts of S. fulvellum and evaluated their antioxidative properties and their abilities to block cell proliferation using in vitro assays: antioxidant activity was assessed by using a DPPH assay and superoxide anion scavenging activity, anti-tyrosinase activity, and anti-proliferative activity were assessed using MTT and lactate dehydrogenase [LDH] assays in vascular smooth muscle cells. The hot-water ($65^{\circ}C$) extract had a higher phenol content than the ethanolic extract. The hot-water extract showed a statistically significant increase in free radical scavenging activity and a greater ability to reduce proliferation of vascular smooth muscle cells stimulated with platelet-derived growth factor-BB. Taken together, hot-water extracts of S. fulvellum may be an important source of antioxidative and antiproliferative agents.

• Journal of the Korean Applied Science and Technology
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• v.26 no.2
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• pp.161-170
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• 2009

In this work, a novel series of aminoisoquinolinylamide derivatives 1a-c and 2a-f were synthesized via several reaction steps, starting from 2-methyl-4-nitrobenzonitrile (3) and 1-chloro-5-nitroquinoline (8). And their antiproliferative activities were screened against A375 human melanoma cell line compared to Sorafenib as a reference compound. Among them, compound 1b and 1c exhibited meaningful inhibitory activities. These results demonstrated that aminoisoquinolinylamide scaffold possesses the possibility as the treatment for melanoma.

• Bulletin of the Korean Chemical Society
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• v.33 no.11
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• pp.3635-3639
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• 2012

A series of new diarylureas possessing aminoisoquinoline scaffold was synthesized, and their in vitro antiproliferative activity against A375P human melanoma cell line was tested. Compounds 1d, 1l, 1n, 1p, 1q, and 1t showed superior potency against A375P to Sorafenib. The highest potency was shown by compound 1p possessing 3,5-bis(trifluoromethyl)phenyl terminal ring with $IC_{50}$ value of $0.41{\mu}M$.

• Journal of the Korean Society of Food Science and Nutrition
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• v.39 no.5
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• pp.731-736
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• 2010

The purpose of this study was to evaluate selected functional compounds and biological activities of 11 different pepper cultivars grown in rain-shelter and field. The selected compounds were capsaicinoids, polyphenolic and vitamin C. Antioxidant activities were measured by ABTS radical scavenging activity, reducing power and metal chelating effect. Antiproliferative activity was assessed by the measurement of the inhibition of HCT116, MCF 7 and NCI-H460 cancer cell proliferation. The contents of capsaicin, dihydrocapsaicin, polyphenolics and vitamin C from 11 cultivars grown in field were 0.0~268.3 mg/100 g, 0~55.1 mg/100 g, 635~878 mg/100 g and 4.1~8.2 mg/g, respectively. There were significant differences in the content of selected compounds among the cultivars, although no significant difference in rain-shelter and field was detected. Similar to the results from the selected compounds, there was no difference in antioxidant and antiproliferative activities between rain-shelter and field. This research provides basic information on functional compounds and biological activity of cultivation methods and pepper cultivars.

• Food Science and Biotechnology
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• v.15 no.6
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• pp.914-919
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• 2006

We investigated the catechin content in green tea leaf (GTL) and green tea seed (GTS), the antiproliferative and detoxifying phase II enzyme-inducing activities of the methanolic (80%, v/v) extracts from GTL and GTS. GTL and GTS contained $8,685{\pm}1,061$ and $108{\pm}32\;{\mu}g/g$ epigallocatechin gallate (EGCG), $11,486{\pm}506$ and $116{\pm}72\;{\mu}g/g$ epigallocatechin (EGC), $3,535{\pm}308$ and $821{\pm}95\;{\mu}g/g$ epicatechin gallate (ECG), and $1,429{\pm}177$ and $37{\pm}44\;{\mu}g/g$ epicatechin (EC), respectively. The methanolic extract of GTS showed a greater increase in quinone reductase activity and antiproliferation potential against mouse hepatoma cells than GTL extract did. GTS treatment resulted in the accumulation at sub-G1 phase of mouse hepatoma hepa1c1c7 cells as assessed by flow cytometry. Enhancement of phase II enzyme activity by GTS extract was shown to be mediated, directly or indirectly, via interaction with the antioxidant response element (ARE) sequence in the genes encoding the phase enzymes. As the catechin content in GTS was significantly lower than that in GTL, components other than catechins appear to be responsible for the anticarcinogenic activity of the seed. In summary, these results suggest that the 80% methanolic extract of GTS deserves further study to evaluate its potential as an anticarcinogenic agent and to investigate its mechanism of action.

• Preventive Nutrition and Food Science
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• v.8 no.4
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• pp.356-364
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• 2003

A methanol extract from seeds of Paeonia lactiflora (Paeoniaceae, peony) was found to possess different antiproliferative activities against four different human cancer cell lines: Hela, MCF-7, HepG2 and HT-29. Furthermore, five different methanol (20, 40, 60, 80 and 100 % MeOH) fractions obtained by fractionation of the methanol extract of the seeds on a Diaion HP-20 column exhibited differential antiproliferative effects against the above four cancer cell lines. Among five fractions, the 60 % MeOH fraction showed relatively lower antiproliferative activity on MCF-7 estrogen-sensitive breast cancer cell than the other cancer cell lines. Systematic separation of 60% the MeOH fraction by silica gel and Sephadex LH-20 columns led to the isolation of four known stilbenes, trans-resveratrol (1), trans-(+)- $\varepsilon$ -viniferin (2), gnetin H (3) and suffruticosol B (4). The four stilbenes (1∼4) exerted differential biphasic effects on cell proliferation of MCF-7 cells in a similar manner as genistein, a soybean isoflavone used as a positive reference, in the concentration range from 1.0 to 200 $\mu$M. Three stilbenes (1 ∼ 3) weakly stimulated the proliferation of MCF -7 cells at doses below 10 JIM. However, strong antiproliferative effects on MCF-7 cell were exerted by extract 1 at a dose of 200 JIM, and by 2 and 3 at doses above 25 $\mu$M. In contrast, 4 inhibited the proliferation of MCF-7 cell at a dose below 25 $\mu$M, but stimulated cell proliferation at concentrations of 50 and 100 $\mu$M. All four stilbenes (1∼4) stimulated the proliferation of ROS 17/2.8 osteoblast-like cells in the range of 10$^{-10}$ ∼10$^{-1}$ $\mu$M. Compound 1 exhibited especially potent proliferative activity, although its activity was weaker than that of genistein. Additionally, three resveratrol oligomers (2∼4) also exhibited concentration-dependently moderate proliferative activity, but less than that of 1. These results suggest that resveratrol, and its dimer and trimers from the seeds of Paeonia lactiflora may act as a phytoestrogen, but in a somewhat different manner from that of genistein.