• Archives of Pharmacal Research
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• v.29 no.1
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• pp.16-25
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• 2006

A novel series of 1-(1-benzofuran-2-yl-ethylidene)-4-substituted thiosemicarbazides (2a-d) along with some derived ring systems: substituted-2,3-dihydro-thiazoles(3a-c, 4a-f) and thiazolidin-4-ones(5a-d and 6a-d), were synthesized. In addition, cyanoacetic acid-(1-benzofuran-2-yl-ethylidene) hydrazide(7) was used to prepare another new series of compounds consisting of substituted pyridin-2(1H)-ones(8a-c); 2-thioxo-2,3-dihydro-thiazoles(9a-d) and 2-thioxo-2,3-dihydro-6H-thiazolo[4,5-d]pyrimidin-7-ones (10a-c, 11a-c). The absolute configuration of compound 5c was determined by X-ray crystallography. The compounds prepared were evaluated for their in vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds 5c and 9a produced a significant reduction ㅐ ㄹ the viral cytopathic effect (93.19% and 59.55%) at concentrations $>2.0{\times}10^{-4}\;M\;and\;2.5{\times}10^{-5}\;M$respectively. Compound 9a was confirmed to have moderate anti-HIV activity. Compounds 2a, 2d, and 5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.

• Journal of the Korean Society of Food Science and Nutrition
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• v.28 no.6
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• pp.1321-1325
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• 1999

The inhibitory effect of Ramaria botrytis on the mutagenicity in Salmonella assay and cytotoxicity on cancer cell were studied. Ramaria botrytis methanol extracts showed antimutagenic effects of 60~90% on B(a)P and AFB1 in S. typhimurium TA98 and TA100. These extracts showed 73~85% antimutagenicity on TA100 against MNNG. The methanol extracts with strong antimutagenic activities were further fractionated by ethylacetate and water, the ethylacetate fraction were found to be stronger antimutagen icity against MNNG than water fraction. Ramaria botrytis methanol extracts and ethylacetate fraction revealed the highest cytoxicity against HT 29 human colon adenocarcinoma cells in which cell growth was inhibited by 57~88% and 69~94% at 0.25~1.0mg/ml, respectively. These methanol extract and ethyl acetate fraction exhibited 53~79% and 66~87% inhibition against HepG2 human hepatocarcinoma cells, respectively. But water fraction showed only 10~24% inhibition. However, these extract and fractions did not show cytotoxic effect against human chang liver cells. From these results, it is considered that Ramaria botrytis has stronger antimutagenic and anticancer effects in vitro.

• Journal of Nutrition and Health
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• v.31 no.4
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• pp.739-746
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• 1998

This study was designed to investigated the antitumor effect and change chemosensitivity of chitosan in 2 kinds of humen lung cancer cell lines(NCI-H522, NCI-H596). To evaluate the antitumor effect and synergistic effectof chomosensitivity, MTT assay was used in vitro. then anticancer drugs used were 챤-platin , ectoposide, and adrimycin. The results of this study were as follows; Chitosan shwoed in antitumor effect on both NCI-H522 and NCI-H596. The lung cancer viability percent for NCI-H522 and NCL-H596 showed at the lowest levels of 5.31 and 5.33% when the concentration of chitosan was 25mg/$m\ell$ media and the exposure time of chitosan was 72 hours. ID50 value of chitosan on both NCI-H522 and NCI-H596 showed at the lowest levels of 14.07, 11.68 mg/$m\ell$ media when the exposure time of chitosan was 72 hours. the synergistic effect of chomosensitivity was better in NCI-H596 than in NCI0H522 . When the synergistic effect of chomosensitivity was shown according to the kind of the anticancer drugs, in case of NCI-H522 , in the concentration of 100$\mu\textrm{g}$/$m\ell$, ectoposide showed the highest synergistic effect of chomosensitivity and then was adrimycin In case of NCI-H596, in the concentration of 100$\mu\textrm{g}$/$m\ell$,, the order of the synergistic effect of chomosensitivity was ectoposide>adrimycin>cis-platin and in the concentration of 10$\mu\textrm{g}$/$m\ell$, ectoposide>cis-platin >adrimycin. It is concluded that chitosan is an active antitumor agent and is increased chomosensitivity though there is difference according to the kind and the concentration of anticancer drugs. But to be sued to lung cancer theraphy, further studies on toxicity, the mechanism of action, animal experiment are wanted.

• Journal of Ginseng Research
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• v.40 no.1
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• pp.62-67
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• 2016

Background: Ginseng, which is widely used in functional foods and as an herbal medicine, has been reported to reduce the proliferation of prostate cancer cells by mechanisms that are not yet fully understood. Methods: This study was designed to investigate the changes in ginsenoside content in ginseng after treatment with a microwave-irradiation thermal process and to verify the anticancer effects of the extracts. To confirm the anticancer effect of microwave-irradiated processed ginseng (MG), it was tested in three human prostate cancer cell lines (DU145, LNCaP, and PC-3 cells). Involvements of apoptosis and autophagy were assessed using Western blotting. Results: After microwave treatment, the content of ginsenosides Rg1, Re, Rb1, Rc, Rb2, and Rd in the extracts decreased, whereas the content of ginsenosides 20(S)-Rg3, 20(R)-Rg3, Rk1, and Rg5 increased. Antiproliferation results for the human cancer cell lines treated with ginseng extracts indicate that PC-3 cells treated with MG showed the highest activity with an half maximal inhibitory concentration of $48{\mu}g/mL$. We also showed that MG suppresses the growth of human prostate cancer cell xenografts in athymic nude mice as an in vivo model. This growth suppression by MG is associated with the inductions of cell death and autophagy. Conclusion: Therefore, heat processing by microwave irradiation is a useful method to enhance the anticancer effect of ginseng by increasing the content of ginsenosides Rg3, Rg5, and Rk1.

• Journal of the Korean Society of Food Science and Nutrition
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• v.41 no.9
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• pp.1248-1252
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• 2012

Potassium added with bamboo salt showed better antioxidative effects than bamboo salt, solar salt, or purified salt. It also showed inhibitory effects on the mutagenicity of MNNG (N-methyl-N-nitro-N-nitrosoguanidine) in a Salmonella Typhimurium TA100 tester strain. At concentrations of 1.25 and 2.5 mg/plate, potassium bamboo salt and bamboo salt showed weaker co-mutagenicity effects than either purified salt or solar salt, respectively. Anticancer effects of salts were evaluated using MTT assay in HCT-116 human colon carcinoma cells. At a 1% salt concentration, the growth inhibitory rate of potassium bamboo salt was 54%, higher than that of 1 time baked bamboo salt (36%). However, purified salt and solar salt showed relatively lower inhibitory effects of 19% and 23%, respectively. To determine the inhibitory mechanisms of potassium bamboo salt, the expression levels of Bax and Bcl-2 genes in HCT-116 cells were determined by RT-PCR. Potassium bamboo salt significantly increased Bax and decreased Bcl-2 expression levels unlike bamboo salt, purified salt, and solar salt (p<0.05). Therefore, addition of potassium to salt decreased co-mutagenicity and increased in vitro antioxidative and anticancer effects.

• Journal of the Korean Society of Food Science and Nutrition
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• v.30 no.4
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• pp.732-738
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• 2001

This study was attempted to isolate and identify the anticancer compounds from Eucommia ulmoides leaves using a human colon cancer cell line HCT-116. The petroleum ether extracts with anticancer activity was chromatographed on silica gel TLC and finally anticancer compounds was purified by HPLC. Their chemical structures were roughly elucidate by UV-VIS absorption spectral data HPLC elution pattern and FAM/MS spectroscopy. From this study these compounds were suspected to be pheophytin a formed by the removal of $Mg^{2+}$ from chlorophyll a and pyropheophytina formed by the removal of acetate group from pheophytin a respectively. To confirm the anticancer effects against HCT-116 cancer cell petroleum ether extract fractions of column chromatography and fractions separated on TLC were tested. All samples tested including the extract of petroleum ether fractions of column chromatograph and three bands (0.13,0.19,0.25) of TLC appeared to inhibit the growth of HCT-116 cancer cell however especially 0.19 and 0.25 fractions separated on TLC plate revealed the strongest effect. These results suggest that chlorophyll derivatives in Eucommia ulmoides may be potential anticancer agents against a human colon cancer cell HCT-116.

• Journal of the Korean Society of Food Science and Nutrition
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• v.42 no.5
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• pp.655-662
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• 2013

The antioxidant and anticancer effects of the edible mushrooms Lentinus edodes (LE, Pyogo mushroom) and Agaricus blazei (AB, Agaricus mushroom), and the medicinal mushrooms Cordyceps militaris (CM, Dong chunghacho), Ganoderma lucidum (GL, Youngji mushroom), Inonotus obliquus (IO, Chaga mushroom), and Phellinus linteus (PL, Sangwhang mushroom) were studied in vitro. The bioactive components were extracted by methanol. The antioxidant effects were evaluated using the DPPH and hydroxyl radical scavenging assays. The antioxidant activities of medicinal mushrooms (35~90%) were higher than edible mushrooms (4~23%). The in vitro anticancer effects of the mushrooms were evaluated using the MTT assay in AGS gastric adenocarcinoma cells, HCT-116 colon carcinoma cells, and HepG2 hepatoma cells. The medicinal mushrooms CM, GL, IO, and PL showed 28~91% inhibition, while the edible mushrooms LE and AB exhibited 5~40% inhibition. The medicinal mushrooms, compared to edible mushrooms, effectively down-regulated the gene expression of the anti-apoptosis related gene Bcl-2 and inflammation-related genes iNOS and COX-2, and up-regulated the pro-apoptosis gene Bax (p<0.05). Total polyphenol and flavonoids contents of the medicinal mushrooms were 9.1~35.7 mg/g, while the edible mushrooms showed 0~13.3 mg/g. This study showed that antioxidant activities and anticancer activities in vitro increased in the order LE, AB, GL, CM, IO and PL. LE and AB showed the lowest effects among the samples, GL and CM had medium effects, and IO and PL exhibited the highest effects in the antioxidant and anticancer effect for three different human cancer cells. Taken together, PL resulted in the highest and LE the lowest effects in this study.

• Journal of the Korean Society of Food Science and Nutrition
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• v.44 no.9
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• pp.1270-1278
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• 2015

In vitro anticancer effects of black soybean doenjang on HT-29 human colon cancer cells were studied. SD (soybean doenjang prepared with nine-time baked bamboo salt) and BD (black soybean doenjang prepared with nine-time baked bamboo salt) were compared with CD (commercial doenjang). There were no significant differences between experimental groups in terms of pH, amino-type nitrogen, and ammonia-type nitrogen levels of the doenjang samples. BD showed the highest antioxidative effect, followed by SD and CD in that order. BD also showed the highest total polyphenol concentration of all samples. CD, SD, and BD extracts showed no toxic effects on normal RAW 264.7 cells at a concentration ranging from 0.1 to 0.5 mg/mL. BD exhibited anticancer effect on HT-29 cells by MTT assay. Also, BD manipulated mRNA expressions in certain factors; it suppressed pro-inflammatory cytokines such as $TNF-{\alpha}$, IL-6, and COX-2, promoted cell-cycle-related genes of p21, and p53, suppressed expression of cyclin D1, and suppressed anti-apoptotic Bcl-2; such manipulation by BD was the strongest, followed by SD and CD in order. From the results above, BD exhibited the highest anticancer effects by inhibiting growth of HT-29 cells, probably by regulating pro-inflammatory cytokines, cell cycling related genes, etc. These results might be due to using black soybeans containing high levels of polyphenol, including anthocyanins.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.18
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• pp.7527-7532
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• 2014

Saussurea involucrata is a Mongolian medicinal plant well known for its effects in promoting blood circulation, and anti-inflammation and analgesic functions. Earlier studies reported that Saussurea involucrata has anticancer activity. The purpose of this study was to confirm the anticancer activity of an ethanol extract of Saussurea involucrata against hepatic cancer and elucidate its mechanisms of action. Hepatocellular carcinoma cells were tested in vitro for cytotoxicity, AO/EB staining for apoptotic cells, apoptotic DNA fragmentation and cell cycle distribution in response to Saussurea involucrata extract (SIE). The mRNA expression of caspase-3,-9 and Cdk2 and protein expression of caspase-3,-9, PARP, XIAP, Cdk2 and p21 were analyzed through real time PCR and Western blotting. Treatment with SIE inhibited HepG2 cell proliferation dose- and time-dependently, but SIE only exerted a modest cytotoxic effect on a viability of Chang human liver cells. Cells exposed to SIE showed typical hallmarks of apoptotic cell death. Cell cycle analysis revealed that SIE caused G1-phase arrest in HepG2 cells. In conclusion, Saussurea involucrata ethanol extract has potential cytotoxic and apoptotic effects on human hepatocellular carcinoma cells. Its mechanism of action might be associated with the inhibition of DNA synthesis, cell cycle (G1) arrest and apoptosis induction through up-regulation of the protein expressions of caspase-3,-9 a nd p21, degradation of PARP and down-regulation of the protein expression of Cdk2 and XIAP.

• Nutrition Research and Practice
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• v.18 no.1
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• pp.62-77
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• 2024

BACKGROUND/OBJECTIVES: Colorectal cancer (CRC) is the third most common cancer worldwide with a high recurrence rate. Oxaliplatin (OXA) resistance is one of the major reasons hindering CRC therapy. β-Carotene (BC) is a provitamin A and is known to have antioxidant and anticancer effects. However, the combined effect of OXA and BC has not been investigated. Therefore, this study investigated the anticancer effects and mechanism of the combination of OXA and BC on CRC. MATERIALS/METHODS: In the present study, the effects of the combination of OXA and BC on cell viability, cell cycle arrest, and cancer stemness were investigated using HCT116, HT29, OXA-resistant cells, and human CRC organoids. RESULTS: The combination of OXA and BC enhanced apoptosis, G₂/M phase cell cycle arrest, and inhibited cancer cell survival in human CRC resistant cells and CRC organoids without toxicity in normal organoids. Cancer stem cell marker expression and self-replicating capacity were suppressed by combined treatment with OXA and BC. Moreover, this combined treatment upregulated apoptosis and the stem cell-related JAK/STAT signaling pathway. CONCLUSIONS: Our results suggest a novel potential role of BC in reducing resistance to OXA, thereby enhances the anticancer effects of OXA. This enhancement is achieved through the regulation of cell cycle, apoptosis, and stemness in CRC.