• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.202.2-202.2
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• 2003

A bioassay-guided fractionation of the whole extract of Viscum album (a parasitic plant : Loranthaceae) led to the isolation of two triterpenoidal components, oleanolic acid (1), ${\beta}$-amyrin acetate (2), homoflavoyadorinin B (3) as well as large quantity of free fatty acid mixtures as active ingredients of the extract responsible for the antitumoral property. The EtOAc soluble part and BuOH soluble part of the extract demonstrated a significant inhibition on the proliferation of cultured human tumor cells such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCT-15 (colon) in vitro, whereas the remaining water soluble part exhibited a poor inhibition. (omitted)

• 혜화의학회지
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• 제10권2호
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• pp.21-29
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• 2002

To evaluate the antitumor activity and antimetastatic effects of Polygoni Orientalis Fructus(POF), studies were done experimentally. The results were obtained as follows : 1. In cytotoxicity against A549, and XF498 cell concentration inhibiting cell growth up to below 30% of control was recognized at $200{\mu}g/m{\ell}$ of POF. Also POF inhibited cell growth up to below 30% of control against SK-OV-3, SK-MEL-2, HCT15 and MCF-7 cell at $100{\mu}g/m{\ell}$. 2. The concentration inhibiting adhesion of A549 and SK-OV-3 to complex extracellular matrix up to below 70% of control was recognized at $100{\mu}g/m{\ell}$ of POF. 3. In pumonary colonization assay, a number of colonies in the lungs were decreased significantly in POF treated group as compared with control group. These results suggested that POF extracts might be usefully applied for prevention and treatment of cancer.

• 생약학회지
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• 제37권3호
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• pp.206-211
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• 2006

The methanol extract from seed of Myristica fragrans (Myristicaceae) demonstrated a potent inhibition on the pro-liferation of cultured human tumor cells such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCT-15 (colon) in vitro. By the continuous effort to purify the active components responsible far the anti-proliferative effect on tumor cell lines, we have isolated eleven kinds of lignan components, i. e., safrole (1), machilin A (2), licarin B (3), macelignan (4), mere-dihydroguaiaretic acid (5), mγnstargenol A (6), methoxyeugenol (7), machilin F (8), licarin A (9), nectandrin B (10), and 2-(4-allyl-2,6-dimethoxyphenoxy)-1-(4-hydroxy-3-methoxyphenyl)propan-1-ol (11) together with a novel furan fatty acid, (E)-3-(3-methyl-5-pentylfuran-2-yl) acrylic acid (12) from seed extract of M. fragrans. Chemical structures of the isolated components (1-12) were established bγ the aid of NMR spectroscopic analyses, i. e., COSY HMQC and HMBC. Each of the Isolates demonstrated a potent inhibition on the proliferation of cultured human tumor cells such as A549 (non small cell lung), SK-OY-3 (ovary), SK-MEL-2 (melanoma) and HCT-15 (colon) in vitro.

• 약학회지
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• 제46권5호
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• pp.301-306
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• 2002

To increase the water solubility, sixteen lupane derivatives bearing aminoacetyl moiety at C3 were synthesized. Their cytotoxic activities against three cancer cell lines, SK-MEL-2, A549, and B16, were tested. Among them, six derivatives showed significant cytotoxic activity.

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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• pp.192.3-193
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• 2000

• Archives of Pharmacal Research
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• 제20권5호
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• pp.491-495
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• 1997

All fifteen flavonoids (1-15) have been isolated from the roots of Sophora flavescens (Leguminosae) as active principles of the cytotoxic property toward human tumor cell lines such as A549, SK-OV-3, SK-Mel-2, XF498 and HCT15, in vitro. By means of spectral analyses, particularlyby the aid of various two dimensional NMR experiments, all $^1H-NMR$ ad $^{13}C$ -NMR signals of 1-15 were completely assigned, and thus the structures of 1-15 were established unambiguously.

• Natural Product Sciences
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• 제17권1호
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• pp.10-13
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• 2011

As parts of our continuing search for biologically active compounds from medicinal plants, we investigated the constituents of the seeds of Amomum xanthioides and isolated a sesquiterpenoid, a nerolidol derivative from its MeOH extract. The chemical structure was determined by spectroscopic methods, including 1D and 2D NMR to be ($2S^*$,$2'R^*$,$5'S^*$)-2-(5'-ethenyltetrahydro-5'-methylfuran-2'-yl)-6-methylhept-5en-2-ol (1). Compound 1 was isolated for the first time from nature source. Compound 1 exhibited a good cytotoxicity against SK-OV-3 and SK-MEL-2 cells ($IC_{50}$: 16.7 and $8.6\;{\mu}M$, respectively) using a SRB bioassay. In this study, we also determined the absolute configuration of 2 reported in previous paper.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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• pp.212-212
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• 1994

본 연구소에서 분리하여 항암활성을 측정한바 있는 Sesquiterpene lactone계열의 KR-53170이 in vitro에 비해 in vivo에서 상대적으로 낮은 효력을 보이는데 착안 그 유도체들을 합성함으로써 in vivo stability 및 efficacy를 개선하고자 하였다. 합성된 물질의 in vivo activity는 human tumor cell중에서 A549(폐암), SK-OV-3(난소암1, SK-MEL-2(피부암), XF-498(중추신경계암), HCT-15(직장암)의 5개 암세포를 이용하여 ED$_{50}$($\mu\textrm{g}$/ml )를 측정하였으며 대조물질로는 KR-53170과 Cisplatin이 사용되었다. 그 결과 HR-53170의 terminal methyl ketone이 carboxylic acid로 변환된 CW-251001과 이것의 methyl ester인 CW-251002, ethyl ester인 CW-251003, 그리고 morpheline과 수용성으로 N-methylpiperazine, N-methyl-N'-aminopiperazine, 4-Piperidinopiperidine을 결합시켜서 합성한 CW-251011, CW-251012, CW-251013, CW-251014가 in vitro에서 어느 정도 활성을 유지하였다. 특히 이들중 CW-251001, CW-251012, CW-251013, CW-2s1014는 물에 대한 용해도가 상당히 개선되어 in vivo 활성검색을 위한 후보물질로 고려되었다. 하지만 이들중 CW-251001은 in vivo에서 낮은 농도에서는 활성이 거의 없었으며 놓은 농도에서는 독성을 나타내었다.

• Archives of Pharmacal Research
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• 제20권1호
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• pp.85-87
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• 1997

The activity-guided fractionation upon the MeOH extract of the aerial parts of Sorbaria sorbifolia var. stellipila led to the isolation of two cucurbitacin-compounds, cucurbitacin D and cucurbitacin F, as active principles. Two compounds were shown to exhibit significant cytotoxicity against cultured human tumor cell lines, A-549, SK-OV-3, SK-MEL-2, XF-498, and HCT 15.

• Biomolecules & Therapeutics
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• 제8권1호
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• pp.22-26
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• 2000

In order to study the cytotoxic properties of sesquitepenes, dehydrocostus lactone (DL) and costunolide from Saussurea lappa, cytotoxicity was measured by SRB method using various human cancer cell lines. Dehydrocostus lactone(DL) and costunolide exhibited significant cytotoxicity against A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT 15 cells. The U937 human leukemia cells treated with DL showed several apoptotic evidences like chromosome condensation and formation of apoptotic bodies. From the results of FACS analysis, early apoptosis was observed by phosphatidylserine externalization detected by annexin V-FITC. Furethermore, these studies determined hypodiploid contents and effects on the cell phase distribution of DL-treated U937 cells. After exposure of U937 cells to $30\mu\textrm{M}$ DL effectively led to G2/M modified cell cycle distribution within 24hr. These observations suggest that DL can be used efficiently for the cancer treatment.