• Asian Pacific Journal of Cancer Prevention
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• 제17권sup3호
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• pp.125-130
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• 2016

Nepeta cataria L. has been used in traditional medicine of some countries. Here the cytotoxic and apoptogenic activity of methanol extracts, n-hexane, dichloromethane, ethyl acetate, n-butanol, and acqueous extracts and the essential oil obtained from the aerial parts of the plant were evaluated with PC3, DU-145 and MCF-7 cell lines. Cell viability, histograms of PI stained fragmented DNA in apoptotic cells and Western blot analysis of proteins involved in the cascade of apoptosis were compared in all samples. Thirty components were identified as volatile, representing 99.7% of essential oil composition after GC-MS analysis of the oil obtained from aerial parts of the N. cataria by hydro-distillation. The major oil components of the essential oil were nepetalactone stereoisomers. Comparing IC50 values showed estrogen receptor positive PC3 cells were more sensitive to the cytotoxic effects of N. cataria in comparison with low hormone-receptor presenting DU-145 cells. Among multiple extracts and essential oils of the plant, only the ethyl acetate extract could significantly decrease cell viability in PC3 cells, in a concentration dependent manner. Ethyl acetate extract of N. cataria treated cells showed a sub-G1 peak in PC3 cells in a concentration dependent manner that indicates the involvement of an apoptotic process in ethyl acetate extract-induced cell death. Western blotting analysis showed that in PC3 cells treated with ethyl acetate (48 h) caspase 3 and PARP were cleaved to active forms. Overall, the results suggest that further analytical elucidation of N. cataria in respect to finding new cytotoxic chemicals with anti-tumor activity is warranted.

• 동아시아식생활학회지
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• 제15권5
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• pp.542-548
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• 2005

In recent years, propolis has attracted much attention as an useful substance in medicine and functional food, even if it is known as a natural remedy in folk medicine since ancient times. propolis was registered as natural food since 1995 on Korean Food Act by Korean Food and Drug Administration(KFDA). The present study demonstrated the optimization of isolation of crude propolis by ethanol, and tumoricidal effect of pro polis. The optimal concentration of ethanol to separate a high quantity of propolis was $60\%$. The cytotoxic effect of ethanol extracted propolis against various cancer cell lines including murine lymphoma (Sarcoma-180), murine T-lymphoma (YAC-1), human breast carcinoma (MCF-7), human gastric carcinoma (KATOIII) and human hepatocellular carcinoma (Hep3B) and human lung adenocarcinoma (A-549) was observed using SRB and MIT assay. In order to investigate the curative activity by oral administration of propolis on tumor, ICR mice was subcutaneously implanted Sarcoma 180. In 300mg/kg and 600mg/kg propolis administered group, development of implanted tumors was inhibited by $40.9\%\;and\;67.9\%$ at 16th day, respectively. In the same dose of propolis administered group, development of implanted tumors was inhibited more strongly with dose dependent manner. Therefore, these data suggested propolis may show tumoricidal effects. In conclusion, these results indicate that propolis, one of the few natural remedies, can be used as functional food with tumoricidal effects.

• 약학회지
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• 제41권6호
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• pp.718-723
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• 1997

In the course of developing novel antitumor intercalating agents, we synthesized 3- carbamoyloxymethyl-azaanthraquinones 6-12, incorporating the latent alkylating functionality. These compounds were designed to explore the effect of heteroatom incorporation into anthraquinone chromophore and the effect of the incorporation of the latent alkylating functionality. The derivatives were prepared by hetero Diels-Alder reaction as a key step followed by functionality of allylic methyl to the desired substituents. Growth inhibitory studies of the azaanthraquinones were conducted in vitro against human cancer cell lines (SNU-354: liver and MCF7: breast) and human epidermoid carcinoma cells that are sensitive (KB-3-1) and multidrug-resistant (KB-V-1). The derivatives were 10 to 100-fold less potent than doxorubicin against sensitive cell lines. However, they were marginally cross-resistant with doxorubicin against KB-V-1.

• 한국약용작물학회지
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• 제12권4호
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• pp.309-314
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• 2004

Echinacea의 추출물 및 분획물들의 정상세포에 대한 세포독성을 측정한 결과, 0.5 mg/ml이상의 농도에서 정상세포의 생육이 20% 가까이 저해되었으며, 비교적 높은 농도인 1.0 mg/ml의 농도에서도 70%이상의 세포 생존을 나타내었다. 유방암 세포주인 MCF7에 대한 생육억제 활성은 0.5 mg/ml의 농도에서 물 추출물의 butanol 획분과 ethanol 추출물의 ethyl acetate 획분에서 각각 87%와 81%로 가장 높은 억제활성을 나타내었으며, 인간 간암세포주인 Hep3B에 대한 생육억제능은, 물과 ethanol 추출물의 butanol 획분에서 0.5 mg/ml의 농도에서 81%와 63%의 생육 억제능을 나타내었으며, 1.0 mg/ml의 농도에서는 수층획분을 제외하고는 대부분 70% 이상의 높은 생육억제능을 나타내었다. 위암세포인 AGS의 경우 물 추출물의 butanol 획분에서 0.5 mg/ml의 농도에서 80%의 높은 억제율을 나타내었으며, 1.0 mg/ml의 농도에서는 각 추출물의 수층 획분과 ethanol 추출물의 ethyl acetate 획분을 제외하고는 80% 이상의 높은 생육억제 활성을 나타내었다. 폐암세포인 A549에 대한 생육억제능은 물과 ethaonl 추출물의 butanol 획분에서 1.0 mg/ml의 농도에서 92%와 87%로 높게 나타났다. 이전까지 Echinacea에 관해서 보고된 것은 그리 많지 않으며, 본 논문에서 Echinacea의 추출물 및 분획물들에 관해 실험한 내용에 관한 것은 전무한 것으로 사료되어져, 이용에 있어서 본 논문에서 실험한 결과를 바탕으로 Echinacea의 항암활성 효과를 통하여 앞으로의 이용에 다양하게 이용될 수 있음을 알린 것이며, 아울러 Echinacea의 추출물들을 이용시 본 눈문에서 실험한 결과물인 물과 ethanol 추출물 모두 butanol 분획에서 그 효과가 가장 높았으므로 이를 사용한 다양한 암세포 사멸효과뿐만이 아니라 면역 활성 증진 및 여러 생리활성의 이용에 사용되도록 하여야 할 것이다.

• Archives of Pharmacal Research
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• 제29권5호
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• pp.354-362
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• 2006

Dietary flavonoids have attracted a great deal of attention as agents for preventing estrogen-related diseases, such as postmenopausal symptoms, and for reducing the risk of estrogen-dependent cancer. Kaempferol is one of the most commonly found dietary phytoestrogen. The aim of this study was to investigate the estrogenic and/or antiestrogenic effect of kaempferol, which can confirm its potency as a preventive agent against estrogen-related diseases. Kaempferol has both estrogenic and antiestrogenic activity, which are biphasic response on estrogen receptor. The estrogenic activity of kaempferol induced via ER-mediated pathway depending on $E_2$ concentration $(\leq\;10^{-12}M)$. Kaempferol $(10^{-5}\;M)$ also caused antiproliferative effect on MCF-7 cell in the presence of $E_2\;(10^{-11}\;M)$ and restored to the addition of excess $E_2\;(10^{-7}\;M)$, which confirms that antiproliferation of kaempferol was induced via ER-dependent pathway. However, at $10^{-4}\;M$, concentration higher than the concentrations at which the estrogenic effects of kaempferol are detected $(10^{-5}\;M)$, kaempferol induced strong antiproliferative effect, but were unaffected by the addition of excess $E_2\;(10^{-7}\;M)$ indicating that kaempferol exerts antiproliferation via ER-independent pathway. In particular, kaempferol blocked the focus formation induced by $E_2$, which confirms that kaempferol might inhibit the malignant transformation caused by estrogens. Therefore, we suggested that kaempferol might regulate a suitable level of estrogenic activity in the body and is expected to have potential beneficial effects in preventing estrogen imbalance diseases (breast cancer, osteoporosis, cardiovascular disease and etc.).

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2018년도 춘계학술발표회
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• pp.94-94
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• 2018

The gold (LC-AuNPs) and silver (LC-AgNPs) nanoparticles were rapidly synthesized by fruit extract of Lycium chinense within 1.15 and 25 min respectively in an eco-friendly way. The synthesized nanoparticles confirmed by relevant surface plasmon resonance peaks for gold and silver nanoparticles at 536 and 480 nm, respectively. FE-TEM results revealed that LC-AuNPs were 20-50 nm and LC-AgNPs were 50-100 nm. The maximum distribution of gold, silver elements and the crystallographic nature of synthesized were confirmed using EDX, elemental mapping and XRD. LC-AgNPs showed inhibitory activity against pathogenic microorganisms such as E. coli and S. aureus, whereas LC-AuNPs did not show inhibitory activity. The LC-AgNps nanoparticles exhibited significant cytotoxicity to human breast cancer MCF7 cell line and less cytotoxicity to non-diseased RAW264.7 (murine macrophage) cells whereas LC-AuNps showed minimal toxicity to both cell lines. In-depth research on this rapid, facile and greenery nanoparticles may play a potential role in biomedical applications.

• 대한한방부인과학회지
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• 제37권1호
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• pp.1-22
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• 2024

목 적: 본 연구의 목적은 유방암 세포(MCF-7) 이식 누드 마우스 모델을 이용하여 육종용 열수 추출물의 면역활성 효과를 통한 항암 활성을 체계적으로 평가하는 것이다. 육종용 열수 추출물은 유방암 치료제로 자주 사용되는 대표적인 경구용 항암제인 tamoxifen 경구 투여군과 비교하여 분석 연구하였다. 방 법: 총 110마리의 6주령 암컷 누드 마우스를 준비하여, 7일간 적응 후 체중이 일정한 마우스를 선정하여 우측 둔부 피하부위에 MCF-7 세포를 이식하였다. 종양세포 이식을 한 지 20일 후, 종양 크기 및 체중을 기준으로 그룹 당 8마리씩 본 실험에 사용하였다. MCF-7 이종 이식 21일 후부터 매일 1회씩 35일간 육종용 열수 추출물을 10 ml/kg의 용량(400, 200 및 100 mg/kg)으로 경구 투여하였으며, tamoxifen 역시 10 ml/kg의 용량(20 mg/kg)으로 경구 투여하였고, 정상 및 종양 이식 매체 대조군에서는 멸균증류수만 종양 이식 21일 후부터 동일한 방법으로 35일간 경구 투여 하였다. 결 과: 본 실험의 결과, MCF-7 세포 이식을 함으로써 현저한 비장 및 하악하 림프절 무게, 혈중 IFN-γ의 함량, IL-1β 및 IL-10의 함량, 비장내 TNF-α, 비장세포 및 복강 대식구의 활성의 감소가 관찰되었고, 비장 및 하악하 림프절의 림프구 감소에 의한 조직병리학적 위축 또한 관찰되었다. 그리고 체중 및 증체량의 감소 역시 관찰되었으며, 혈중 IL-6 함량의 증가, 난소 주위의 지방 무게의 감소 및 조직병리학적으로 난소 주위의 축적 지방 조직 위축 현상이 인정되어, 종양 이식 후에 전형적인 종양과 관련된 면역억제와 악액질 현상이 유발된 것으로 판단되었다. 한편 육종용 열수 추출물 400, 200 및 100 mg/kg 경구 투여군에서는 종양 이식 대조군에 비해 유의성 있는 현저한 항암활성이 투여 용량 의존적으로 관찰되었다. 또한 tamoxifen 20 mg/kg 경구 투여군에서는 종양 관련 악액질 소견이 오히려 악화되는 반면, 육종용 열수 추출물 경구 투여군에서는 면역활성 및 악액질 억제 효과가 관찰되었다. 결 론: 본 연구 결과, 육종용 열수 추출물의 적절한 경구 투여는 심각한 부작용 없이, 종양 관련 악액질 소견을 포함하여, 효과적인 유방암 치료 수단을 제공할 수 있을 것으로 기대된다.

• The Korean Journal of Physiology and Pharmacology
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• 제18권2호
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• pp.109-120
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• 2014

The epothilones are a class of microtubule inhibitors that exhibit a strong antitumor activity. UTD2 is a novel epothilone analog generated by genetic manipulation of the polyketide biosynthetic gene cluster. This study investigated the effects of UTD2 on the actin cytoskeleton and its critical regulators, and the signaling pathways which are essential for cell motility, growth and survival in MCF-7 breast cancer cells. Results showed that UTD2 inhibited the cellular functions of actin cytoskeleton, such as wound-closure, migration and invasion, as well as adhesion. Our study further demonstrated that UTD2 suppressed Rac1 GTPase activation and reduced the activity of PAK1, which is a downstream effector of Rac1, while the activity of Cdc42 was not affected. Additionally, the phosphorylation of p38 and ERK were significantly inhibited, but the phosphorylation of JNK remained the same after UTD2 treatment. Moreover, UTD2 inhibited the activity and mRNA expression of MMP-2, which plays a key role in cell motility. UTD2 also reduced the phosphorylation of Akt, which is an important signaling kinase regulating the cell survival through Rac1. Furthermore, UTD2 interrupted the synergy between Rac1 and Raf in focus formation assays. Taken together, these results indicated that UTD2 exerted multiple effects on the actin cytoskeleton and signaling pathways associated with Rac1. This study provided novel insights into the molecular mechanism of the antineoplastic and antimetastatic activities of epothilones. Our findings also suggest that the signaling pathways regulated by Rac1 may be evaluated as biomarkers for the response to therapy in clinical trials of epothilones.

• 한국환경성돌연변이발암원학회지
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• 제24권4호
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• pp.163-170
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• 2004

CYP1B1 enzyme metabolize PAHs and estradiol. CYP1B1 metabolize estradiol to 4-hydroxyestradiol that is considered as carcinogenic metabolite. Luciferase activity was induced about 20 folds over that control by 1 nM TCDD (2,3,7,8-tetrchlorodibenzo-p-dioxin) and these inductions were dose-dependent. Recent industrialized society, human hasbeen widely been exposed to widespread environmental contaminants such as PAHs (polycyclic aromatic hydrocarbon) that are originated from the incomplete combustion of hydrocarbons. PAHs are known to be ligands of the AhR (aryl hydrocarbon receptor). Induction of cytochrome P4501B1(CYP1B1) in cell culture is widely used as a biomarket for PAHs. Therefore we have studied the effect of PAHs in the human breast cancer cells MCF-7 to evaluate bioactivity of PAHs. Cytochrome P4501B1(CYP1B1) is known to be inducible by xenobiotic compounda such as policyclic aromatic hydrocarbon (PAH) and dioxins such as 2,3,7,8-tetrachloro-dibenzo-p-dioxin(TCDD). And these induction of CYP1B1 is also regulated by many categories of chemicals. In order to investigate the effects of several chemicals on CYP1B1 gene expression in luciferase gene, and then transfected into these cells. After treatment of chemicals, the luciferase activity was measured. We examined effects of PAHs on the CYP1B1-lucifrease reporter gene and CYP1B1 mRNA level. Benzo(k)fluoranthene showed strong response to CYP1B1 promoter activity stimulation, and also CYP1B1 mRNAs increase in MCF-7 cells in a concentration-dependent manner. flvonoids such as genistein decreased B(k)F induced luciferase activity at low concentration. it exhibited stimulatory effect at high concentration.

• 한국약용작물학회지
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• 제12권1호
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• pp.36-42
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• 2004

사철쑥 추출물은 정상폐세포인 HEL299 세포주에 $0.5\;g/{\ell}$ 이하의 농도로 투여시는 정상세포 생존율을 80% 이상으로 유지시켜 정상세포에 대한 안정성이 유지되었으며, 암세포 생육억제활성은 증류수 및 에탄올 추출물 모두 $0.5\;mg/m{\ell}$ 이상의 농도에서 유방암세포주인 MCF7에 대하여 88%이상, 폐암세포주인 A549에 대하여서는 모든 추출물에서 $0.5\;mg/m{\ell}$의 농도 이상에서 65%이상의 저해를 나타내었다. 또한 간암세포주인 Hep3B에 대하여는, 에탄올 추출물이 87% 이상, 위암세포주인 AGS에 대하여 증류수 추출물이 약 85% 이상의 높은 암세포 생육억제활성을 나타내었다. 또한 정상세포독성에 대한 암세포의 억제율을 나타내는 selectivity에 있어서 각 추출물이 $0.1\;mg/m{\ell}$에서 $1.0\;mg/m{\ell}$의 농도에서 1.5 이상의 수치를 나타내었다. B와 T 세포주의 생육촉진 실험 결과 배양 기간이 증가함에 따라 세포의 생육이 촉진되었으며, 배양 5일째 $0.5\;mg/m{\ell}$의 농도에서 B세포의 생장을 최고 1.2배 이상 증가, T-cell을 $1.2{\sim}1.5$배 이상 생장을 증가시켰으며, 배양 6일째 에탄올 추출물이 IL-6를 $67\;pg/m{\ell},\;TNF-{\alpha}$를 물 추출물이 $68\;pg/m{\ell}$의 분비 하였다.