• Journal of Ginseng Research
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• v.46 no.3
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• pp.396-407
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• 2022

Background: Colorectal cancer (CRC) has a high morbidity and mortality worldwide. 20 (S)-ginsenoside Rh2 (G-Rh2) is a natural compound extracted from ginseng, which exhibits anticancer effects in many cancer types. In this study, we demonstrated the effect and underlying molecular mechanism of G-Rh2 in CRC cells in vitro and in vivo. Methods: Cell proliferation, migration, invasion, apoptosis, cell cycle, and western blot assays were performed to evaluate the effect of G-Rh2 on CRC cells. In vitro pull-down assay was used to verify the interaction between G-Rh2 and Axl. Transfection and infection experiments were used to explore the function of Axl in CRC cells. CRC xenograft models were used to further investigate the effect of Axl knockdown and G-Rh2 on tumor growth in vivo. Results: G-Rh2 significantly inhibited proliferation, migration, and invasion, and induced apoptosis and G₀/G₁ phase cell cycle arrest in CRC cell lines. G-Rh2 directly binds to Axl and inhibits the Axl signaling pathway in CRC cells. Knockdown of Axl suppressed the growth, migration and invasion ability of CRC cells in vitro and xenograft tumor growth in vivo, whereas overexpression of Axl promoted the growth, migration, and invasion ability of CRC cells. Moreover, G-Rh2 significantly suppressed CRC xenograft tumor growth by inhibiting Axl signaling with no obvious toxicity to nude mice. Conclusion: Our results indicate that G-Rh2 exerts anticancer activity in vitro and in vivo by suppressing the Axl signaling pathway. G-Rh2 is a promising candidate for CRC prevention and treatment.

• Journal of Physiology & Pathology in Korean Medicine
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• v.23 no.2
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• pp.473-479
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• 2009

The purpose of this study was evaluated physiological activity effect of organic germanium in culture broth of germanium-fortified Tricholoma matsutake mycelium and germanium-fortified yeast. Proliferation Tricholoma matsutake mycelium and yeast was inhibited by addition of germanium. Contents of organic germanium in Tricholoma matsutake mycelium and yeast was increased in dose-dependent manner. And low concentration(1,000 ppm) of germanium in mycelium was almost changed organic germanium. In the result of antioxidant activity as SOD-like activity, contents of total polyphenol compound and electron donating ability, activity of germanium-fortified Tricholoma matsutake mycelium was higher than that of germanium-fortified yeast. To evaluate of antitumor effects in vitro, we examined nitric oxide production of Raw 264,7 cell and cytotoxicity of HT1080 cell by MTT assay. Nitric oxide production of germanium-fortified Tricholoma matsutake mycelium was shown low level in low concentration(1,000 ppm) than other groups. The anticancer effect of germanium-fortified Tricholoma matsutake mycelium on HT 1080 cell was indicated a strong inhibitory effect in low concentration(1,000 ppm). These results suggest that organic germanium in culture broth of germanium-fortified Tricholoma matsutake mycelium has valuable physiological activities as antioxidant and anticancer effect, and it was higher than that of germanium-fortified yeast.

• Natural Product Sciences
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• v.20 no.3
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• pp.146-151
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• 2014

The purification of the MeOH extracts from the aerial parts of Aceriphyllum rossii Engler (Saxifragaceae) using column chromatography furnished fourteen compounds (1 - 14). The chemical structures of the isolated compounds were determined using mainly nuclear magnetic resonance spectra and mass spectrometry. All the isolated compounds were tested for their cytotoxic activity against LH-60, MCF-7 and HeLa cancer cells in vitro using a MTT assay method. Compounds possessing an olean-triterpenoid skeleton entirely exhibit dose dependent cytotoxic activity. These findings partially confirmed the anticancer effect of this medicinal plant, suggesting a further study on the anticancer potential of the triterpenoid structure in compounds from this plant.

• Proceedings of the Korean Nuclear Society Conference
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• 2004.10a
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• pp.1245-1246
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• 2004

• Archives of Pharmacal Research
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• v.27 no.4
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• pp.436-441
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• 2004

SJ compounds (SJ8002 and related compounds) are a group of novel anticancer agents (Cho, Chung, Lee, Kwon, Kang, Joo, and Oh. PCT/KR02/00392). To explore the anticancer mechanism of these compounds, we examined the effect of SJ8002 on microtubules of six human cell lines. At a high concentration ($2\;{\mu}g/mL$), SJ8002 effectively disrupted microtubules of the six cell lines within 1 h. At lower concentrations ($0.05\~1.0\;{\mu}g/mL$), the antimicrotubule activity of SJ8002 varied defending on cell lines. The inhibition of in vitro polymerization of pure tubulin by SJ8002 suggested that SJ8002 acts on free tubulin, inhibits the polymerization of tubulin dimer into microtubules, and hence induces the depolymerization of microtubules.

• Preventive Nutrition and Food Science
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• v.4 no.1
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• pp.33-37
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• 1999

The antimutagenic effects of buchu kimchi and Chinese cabbage kimchi and theri cytotoxic effects against human cancer cell line were investigated in the Salmonella typhimurium system and MTT assay, respectively. Leek and Chinese cabbage were aslo evaluated in the same system. Buchu kimchi was fermented at 15 $^{\circ}C$ for 4 days . Buchu kimchi samples showed somewhat higher antimutagenic effects against aflatoxin B1(AFB1) than CHinese cabbage kimchi in Salmonella typhimurium TA100 strain. There was no difference onthe antimutagenic activity according to the length of fermentation . Leek exerted stronger antimutagenicity against AFB1 than Chinese cabbage in the Ames assay. In MTT assay, 6-day fermented buchu kimchin revealed the highest cytotoxicity against AGS human gastric adenocarcinoma cells in which 62% and 82% of the inhibition were observed wiht the addition of 100ug, 400ug/well, respectively. Buchu kimchi samples caused 60~70% inhibition on the proliferation of HT-29 at 400ug/well. Leek exhibited higher antiproliferative effect against both AGS cells and HT-29 cells than Chinese cabbage in MTT assay. From these results, it is considered that buchu kimchi has stronger antimutagenic and in vitro anticancer effects than Chinese cabbage kimchi and the high inhibition rate of buchu kimchi probably results from leek, the major ingredient of buchu kimchi .

• The Korean Journal of Physiology and Pharmacology
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• v.25 no.5
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• pp.479-488
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• 2021

This study aimed to develop docetaxel (DTX) loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (DTX-NPs) and to evaluate the different pharmacological sensitivity of NPs to MCF-7 and MDA-MB-231 breast cancer cells. NPs containing DTX or coumarin-6 were prepared by the nanoprecipitation method using PLGA as a polymer and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) as a surfactant. The physicochemical properties of NPs were characterized. In vitro anticancer effect and cellular uptake were evaluated in breast cancer cells. The particle size and zeta potential of the DTX-NPs were 160.5 ± 3.0 nm and -26.7 ± 0.46 mV, respectively. The encapsulation efficiency and drug loading were 81.3 ± 1.85% and 10.6 ± 0.24%, respectively. The in vitro release of DTX from the DTX-NPs was sustained at pH 7.4 containing 0.5% Tween 80. The viability of MDA-MB-231 and MCF-7 cells with DTX-NPs was 37.5 ± 0.5% and 30.3 ± 1.13%, respectively. The IC₅₀ values of DTX-NPs were 3.92- and 6.75-fold lower than that of DTX for MDA-MB-231 cells and MCF-7 cells, respectively. The cellular uptake of coumarin-6-loaded PLGA-NPs in MCF-7 cells was significantly higher than that in MDA-MB-231 cells. The pharmacological sensitivity in breast cancer cells was higher on MCF-7 cells than on MDA-MB-231 cells. In conclusion, we successfully developed DTX-NPs that showed a great potential for the controlled release of DTX. DTX-NPs are an effective formulation for improving anticancer effect in breast cancer cells.

• Korean Journal of Medicinal Crop Science
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• v.10 no.4
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• pp.269-272
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• 2002

Ethanol and butanol fractionation of E. senticosus showed strong anti-oxidant activity, and methanol and water extracts also had high anti-oxidant activity. The anti-oxidant activities in ethanol and butanol fractionation were higher than or similar to those of ${\alpha}-tocopherol$. The cytotoxic effect of root extract of E. senticosus was evaluated on seven different human cancer cell lines, The extracts of leaf and stem of E. senticosus also had strong antioxidant activity, but the antioxidant activity in root extract was higher than those in leaf and stem extracts. Methanol, hexane, and aqueous fraction layer had much higher inhibitory activities on lipid peroxidation in rat liver microsomes compared with ${\alpha}-tocopherol$. The effect of root extract of E. senticosus was evaluated on six human cancer cell lines. The values of 50% growth inhibition $(GI_{50})$ for the extracts were mostly below $30{\mu}g/ml$, and the extracts are considered as active inhibitory compounds on cancer cells.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.1
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• pp.199-203
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• 2014

Background: Rosuvastatine, doxazosin, repaglinide and oxcarbazepin are therapeutic drugs available in the market for the treatment of different diseases. Potential to display antitumor activities has also been suggested. The aim of the current study was to evaluate their in vitro effects on some human transformed cell lines. Materials and Methods: Cytotoxicity of the four drugs was tested in MCF-7, HeLa and HepG2 cells by the neutral red assay method and also the effect of rosuvastatine and doxazosin against Ehrlich Ascities Carcinoma Cells (EACC) by trypan blue assay. Results: Rosuvastatine exerted the greatest cytotoxic effect against HepG2 cells with an $IC_{50}$ value of $58.7{\pm}69.3$; in contrast doxazosin showed least activity with $IC_{50}=104.4{\pm}115.7$. Repaglinide inhibited the growth of both HepG2 and HeLa cells with $IC_{50}$ values of $87.6{\pm}117.5$ and $89.3{\pm}119.5$, respectively. Oxcarbazepine showed a potent cytotoxicity against both HeLa ($IC_{50}=19.4{\pm}43.9$) and MCF7 cancer cells (($IC_{50}=22{\pm}35.7$).On the other hand the growth of EACC was completely inhibited by doxazosine (100% inhibition) while rosuvastatine had weak inhibitory activity (11.6%). Conclusions: The four tested drugs may have cytotoxic effects against hepatic, breast and cervical carcinoma cells; also doxazosine may inhibit the growth of endometrial cancer cells. Further investigations in animals are needed to confirm these results.

• Korean Journal of Environmental Biology
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• v.26 no.2
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• pp.115-120
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• 2008

Earlier we have described new water-soluble Ag- and Zn-derivatives of tetrachloride meso-tetra (4-N-oxiethylpyridyl) porphyrin (TOEtPyP) as potential anticancer drugs. In this work the effect of one of these metal porphyrins, TOEtPyP Ag, on the cell population kinetics was studied in vitro using morphological and biochemical techniques. The results suggested that TOEtPyP Ag action consisted in the simultaneous suppression of the cell growth and activation of the cell death. About 40% of the cells were shown to die via apoptotic pathway. So, the porphyrin studied may be attributed to inducers of both necrotic and apoptotic processes. The results obtained support our previous assertion that TOEtPyP Ag may be considered as a potential chemotherapeutic agent.